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  Subjects -> CHEMISTRY (Total: 858 journals)
    - ANALYTICAL CHEMISTRY (53 journals)
    - CHEMISTRY (601 journals)
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CHEMISTRY (601 journals)                  1 2 3 4 | Last

Showing 1 - 200 of 735 Journals sorted alphabetically
2D Materials     Hybrid Journal   (Followers: 11)
Accreditation and Quality Assurance: Journal for Quality, Comparability and Reliability in Chemical Measurement     Hybrid Journal   (Followers: 26)
ACS Catalysis     Full-text available via subscription   (Followers: 39)
ACS Chemical Neuroscience     Full-text available via subscription   (Followers: 19)
ACS Combinatorial Science     Full-text available via subscription   (Followers: 23)
ACS Macro Letters     Full-text available via subscription   (Followers: 24)
ACS Medicinal Chemistry Letters     Full-text available via subscription   (Followers: 40)
ACS Nano     Full-text available via subscription   (Followers: 255)
ACS Photonics     Full-text available via subscription   (Followers: 12)
ACS Synthetic Biology     Full-text available via subscription   (Followers: 24)
Acta Chemica Iasi     Open Access   (Followers: 2)
Acta Chimica Sinica     Full-text available via subscription   (Followers: 1)
Acta Chimica Slovaca     Open Access   (Followers: 1)
Acta Chimica Slovenica     Open Access  
Acta Chromatographica     Full-text available via subscription   (Followers: 9)
Acta Facultatis Medicae Naissensis     Open Access  
Acta Metallurgica Sinica (English Letters)     Hybrid Journal   (Followers: 5)
Acta Scientifica Naturalis     Open Access   (Followers: 2)
adhäsion KLEBEN & DICHTEN     Hybrid Journal   (Followers: 5)
Adhesion Adhesives & Sealants     Hybrid Journal   (Followers: 8)
Adsorption Science & Technology     Full-text available via subscription   (Followers: 5)
Advanced Functional Materials     Hybrid Journal   (Followers: 51)
Advanced Science Focus     Free   (Followers: 3)
Advances in Chemical Engineering and Science     Open Access   (Followers: 58)
Advances in Chemical Science     Open Access   (Followers: 13)
Advances in Chemistry     Open Access   (Followers: 15)
Advances in Colloid and Interface Science     Full-text available via subscription   (Followers: 18)
Advances in Drug Research     Full-text available via subscription   (Followers: 23)
Advances in Enzyme Research     Open Access   (Followers: 9)
Advances in Fuel Cells     Full-text available via subscription   (Followers: 16)
Advances in Heterocyclic Chemistry     Full-text available via subscription   (Followers: 9)
Advances in Materials Physics and Chemistry     Open Access   (Followers: 23)
Advances in Nanoparticles     Open Access   (Followers: 14)
Advances in Organometallic Chemistry     Full-text available via subscription   (Followers: 15)
Advances in Polymer Science     Hybrid Journal   (Followers: 41)
Advances in Protein Chemistry     Full-text available via subscription   (Followers: 18)
Advances in Protein Chemistry and Structural Biology     Full-text available via subscription   (Followers: 20)
Advances in Quantum Chemistry     Full-text available via subscription   (Followers: 6)
Advances in Science and Technology     Full-text available via subscription   (Followers: 12)
African Journal of Bacteriology Research     Open Access  
African Journal of Chemical Education     Open Access   (Followers: 2)
African Journal of Pure and Applied Chemistry     Open Access   (Followers: 7)
Agrokémia és Talajtan     Full-text available via subscription   (Followers: 2)
Al-Kimia : Jurnal Penelitian Sains Kimia     Open Access  
Alkaloids: Chemical and Biological Perspectives     Full-text available via subscription   (Followers: 3)
AMB Express     Open Access   (Followers: 1)
Ambix     Hybrid Journal   (Followers: 3)
American Journal of Biochemistry and Biotechnology     Open Access   (Followers: 67)
American Journal of Biochemistry and Molecular Biology     Open Access   (Followers: 15)
American Journal of Chemistry     Open Access   (Followers: 28)
American Journal of Plant Physiology     Open Access   (Followers: 14)
American Mineralogist     Hybrid Journal   (Followers: 15)
Analyst     Full-text available via subscription   (Followers: 39)
Angewandte Chemie     Hybrid Journal   (Followers: 166)
Angewandte Chemie International Edition     Hybrid Journal   (Followers: 235)
Annales UMCS, Chemia     Open Access   (Followers: 1)
Annals of Clinical Chemistry and Laboratory Medicine     Open Access   (Followers: 4)
Annual Reports in Computational Chemistry     Full-text available via subscription   (Followers: 3)
Annual Reports Section A (Inorganic Chemistry)     Full-text available via subscription   (Followers: 4)
Annual Reports Section B (Organic Chemistry)     Full-text available via subscription   (Followers: 9)
Annual Review of Chemical and Biomolecular Engineering     Full-text available via subscription   (Followers: 12)
Annual Review of Food Science and Technology     Full-text available via subscription   (Followers: 16)
Anti-Infective Agents     Hybrid Journal   (Followers: 3)
Antiviral Chemistry and Chemotherapy     Hybrid Journal   (Followers: 1)
Applied Organometallic Chemistry     Hybrid Journal   (Followers: 7)
Applied Spectroscopy     Full-text available via subscription   (Followers: 22)
Applied Surface Science     Hybrid Journal   (Followers: 28)
Arabian Journal of Chemistry     Open Access   (Followers: 6)
ARKIVOC     Open Access   (Followers: 2)
Asian Journal of Biochemistry     Open Access   (Followers: 1)
Atomization and Sprays     Full-text available via subscription   (Followers: 4)
Australian Journal of Chemistry     Hybrid Journal   (Followers: 7)
Autophagy     Hybrid Journal   (Followers: 2)
Avances en Quimica     Open Access   (Followers: 1)
Biochemical Pharmacology     Hybrid Journal   (Followers: 10)
Biochemistry     Full-text available via subscription   (Followers: 338)
Biochemistry Insights     Open Access   (Followers: 6)
Biochemistry Research International     Open Access   (Followers: 6)
BioChip Journal     Hybrid Journal  
Bioinorganic Chemistry and Applications     Open Access   (Followers: 9)
Bioinspired Materials     Open Access   (Followers: 5)
Biointerface Research in Applied Chemistry     Open Access   (Followers: 2)
Biointerphases     Open Access   (Followers: 1)
Biology, Medicine, & Natural Product Chemistry     Open Access   (Followers: 1)
Biomacromolecules     Full-text available via subscription   (Followers: 19)
Biomass Conversion and Biorefinery     Partially Free   (Followers: 10)
Biomedical Chromatography     Hybrid Journal   (Followers: 6)
Biomolecular NMR Assignments     Hybrid Journal   (Followers: 3)
BioNanoScience     Partially Free   (Followers: 5)
Bioorganic & Medicinal Chemistry     Hybrid Journal   (Followers: 121)
Bioorganic & Medicinal Chemistry Letters     Hybrid Journal   (Followers: 85)
Bioorganic Chemistry     Hybrid Journal   (Followers: 10)
Biopolymers     Hybrid Journal   (Followers: 18)
Biosensors     Open Access   (Followers: 2)
Biotechnic and Histochemistry     Hybrid Journal   (Followers: 1)
Bitácora Digital     Open Access  
Boletin de la Sociedad Chilena de Quimica     Open Access  
Bulletin of the Chemical Society of Ethiopia     Open Access   (Followers: 2)
Bulletin of the Chemical Society of Japan     Full-text available via subscription   (Followers: 24)
Bulletin of the Korean Chemical Society     Hybrid Journal   (Followers: 1)
C - Journal of Carbon Research     Open Access   (Followers: 3)
Cakra Kimia (Indonesian E-Journal of Applied Chemistry)     Open Access  
Canadian Association of Radiologists Journal     Full-text available via subscription   (Followers: 2)
Canadian Journal of Chemistry     Hybrid Journal   (Followers: 10)
Canadian Mineralogist     Full-text available via subscription   (Followers: 6)
Carbohydrate Research     Hybrid Journal   (Followers: 26)
Carbon     Hybrid Journal   (Followers: 68)
Catalysis for Sustainable Energy     Open Access   (Followers: 7)
Catalysis Reviews: Science and Engineering     Hybrid Journal   (Followers: 8)
Catalysis Science and Technology     Free   (Followers: 8)
Catalysis Surveys from Asia     Hybrid Journal   (Followers: 3)
Catalysts     Open Access   (Followers: 8)
Cellulose     Hybrid Journal   (Followers: 7)
Cereal Chemistry     Full-text available via subscription   (Followers: 5)
ChemBioEng Reviews     Full-text available via subscription   (Followers: 1)
ChemCatChem     Hybrid Journal   (Followers: 8)
Chemical and Engineering News     Free   (Followers: 16)
Chemical Bulletin of Kazakh National University     Open Access  
Chemical Communications     Full-text available via subscription   (Followers: 71)
Chemical Engineering Research and Design     Hybrid Journal   (Followers: 25)
Chemical Research in Chinese Universities     Hybrid Journal   (Followers: 3)
Chemical Research in Toxicology     Full-text available via subscription   (Followers: 22)
Chemical Reviews     Full-text available via subscription   (Followers: 184)
Chemical Science     Open Access   (Followers: 23)
Chemical Technology     Open Access   (Followers: 16)
Chemical Vapor Deposition     Hybrid Journal   (Followers: 5)
Chemical Week     Full-text available via subscription   (Followers: 8)
Chemie in Unserer Zeit     Hybrid Journal   (Followers: 56)
Chemie-Ingenieur-Technik (Cit)     Hybrid Journal   (Followers: 24)
ChemInform     Hybrid Journal   (Followers: 8)
Chemistry & Biodiversity     Hybrid Journal   (Followers: 7)
Chemistry & Biology     Full-text available via subscription   (Followers: 31)
Chemistry & Industry     Hybrid Journal   (Followers: 5)
Chemistry - A European Journal     Hybrid Journal   (Followers: 149)
Chemistry - An Asian Journal     Hybrid Journal   (Followers: 16)
Chemistry and Materials Research     Open Access   (Followers: 20)
Chemistry Central Journal     Open Access   (Followers: 4)
Chemistry Education Research and Practice     Free   (Followers: 5)
Chemistry in Education     Open Access   (Followers: 9)
Chemistry International     Hybrid Journal   (Followers: 2)
Chemistry Letters     Full-text available via subscription   (Followers: 42)
Chemistry of Materials     Full-text available via subscription   (Followers: 241)
Chemistry of Natural Compounds     Hybrid Journal   (Followers: 9)
Chemistry World     Full-text available via subscription   (Followers: 22)
Chemistry-Didactics-Ecology-Metrology     Open Access   (Followers: 1)
ChemistryOpen     Open Access   (Followers: 2)
Chemkon - Chemie Konkret, Forum Fuer Unterricht Und Didaktik     Hybrid Journal  
Chemoecology     Hybrid Journal   (Followers: 4)
Chemometrics and Intelligent Laboratory Systems     Hybrid Journal   (Followers: 14)
Chemosensors     Open Access  
ChemPhysChem     Hybrid Journal   (Followers: 11)
ChemPlusChem     Hybrid Journal   (Followers: 2)
ChemTexts     Hybrid Journal  
CHIMIA International Journal for Chemistry     Full-text available via subscription   (Followers: 2)
Chinese Journal of Chemistry     Hybrid Journal   (Followers: 6)
Chinese Journal of Polymer Science     Hybrid Journal   (Followers: 10)
Chromatographia     Hybrid Journal   (Followers: 24)
Chromatography     Open Access   (Followers: 2)
Clay Minerals     Full-text available via subscription   (Followers: 10)
Cogent Chemistry     Open Access  
Colloid and Interface Science Communications     Open Access  
Colloid and Polymer Science     Hybrid Journal   (Followers: 10)
Colloids and Interfaces     Open Access  
Colloids and Surfaces B: Biointerfaces     Hybrid Journal   (Followers: 6)
Combinatorial Chemistry & High Throughput Screening     Hybrid Journal   (Followers: 4)
Combustion Science and Technology     Hybrid Journal   (Followers: 22)
Comments on Inorganic Chemistry: A Journal of Critical Discussion of the Current Literature     Hybrid Journal   (Followers: 2)
Composite Interfaces     Hybrid Journal   (Followers: 6)
Comprehensive Chemical Kinetics     Full-text available via subscription   (Followers: 2)
Comptes Rendus Chimie     Full-text available via subscription  
Comptes Rendus Physique     Full-text available via subscription   (Followers: 1)
Computational and Theoretical Chemistry     Hybrid Journal   (Followers: 9)
Computational Biology and Chemistry     Hybrid Journal   (Followers: 11)
Computational Chemistry     Open Access   (Followers: 2)
Computers & Chemical Engineering     Hybrid Journal   (Followers: 9)
Coordination Chemistry Reviews     Full-text available via subscription   (Followers: 3)
Copernican Letters     Open Access   (Followers: 1)
Corrosion Series     Full-text available via subscription   (Followers: 6)
Critical Reviews in Biochemistry and Molecular Biology     Hybrid Journal   (Followers: 5)
Croatica Chemica Acta     Open Access  
Crystal Structure Theory and Applications     Open Access   (Followers: 4)
CrystEngComm     Full-text available via subscription   (Followers: 13)
Current Catalysis     Hybrid Journal   (Followers: 2)
Current Chromatography     Hybrid Journal  
Current Green Chemistry     Hybrid Journal  
Current Metabolomics     Hybrid Journal   (Followers: 5)
Current Microwave Chemistry     Hybrid Journal  
Current Opinion in Colloid & Interface Science     Hybrid Journal   (Followers: 9)
Current Opinion in Molecular Therapeutics     Full-text available via subscription   (Followers: 18)
Current Research in Chemistry     Open Access   (Followers: 8)
Current Science     Open Access   (Followers: 64)
Dalton Transactions     Full-text available via subscription   (Followers: 23)
Detection     Open Access   (Followers: 2)
Developments in Geochemistry     Full-text available via subscription   (Followers: 2)
Diamond and Related Materials     Hybrid Journal   (Followers: 12)
Dislocations in Solids     Full-text available via subscription  
Doklady Chemistry     Hybrid Journal  
Drying Technology: An International Journal     Hybrid Journal   (Followers: 4)
Eclética Química     Open Access   (Followers: 1)
Ecological Chemistry and Engineering S     Open Access   (Followers: 3)

        1 2 3 4 | Last

Journal Cover Chemistry & Biodiversity
  [SJR: 0.542]   [H-I: 49]   [7 followers]  Follow
    
   Hybrid Journal Hybrid journal (It can contain Open Access articles)
   ISSN (Print) 1612-1872 - ISSN (Online) 1612-1880
   Published by John Wiley and Sons Homepage  [1592 journals]
  • Salvisertin A, a New Hexacyclic Triterpenoid, and Other Bioactive Terpenes
           from Salvia deserta Root
    • Authors: Yin-Ru Wang; Yun Yu, Shu-Ming Li, Wei Liu, Wei Li, Susan L. Morris-Natschke, Masuo Goto, Kuo-Hsiung Lee, Xue-Feng Huang
      Abstract: Using various chromatographic methods, a new hexacyclic triterpenoid, 2β, 3β, 24β-trihydroxy-12, 13-cyclo-taraxer-l4-en-28oic acid (1), together with ten known compounds, 2α, 3α, 23- trihydroxyurs-12, 20(30)-dien-28oic acid (2), 6, 7-dehydroroyleanone (3), horminone (4), 7-O-methylhorminone (5), sugiol (6), demethylcryptojaponol (7), 14-deoxycoleon U (8), 5, 6-didehydro-7-hydroxy-taxodone (9), ferruginol (10) and dichroanone (11), were isolated from the roots of Salvia deserta. Their structures were identified on the basis of spectroscopic analysis and comparison with the reported data. The individual compounds (1, 3—8) were screened for cytotoxic activity, using the sulforhodamine B bioassay (SRB) method. As the results, Compounds 3, 5 and 8 showed cytotoxic potency against A549, MDA-MB-231, KB, KB-VIN, and MCF7 cell lines with IC50 values ranging from 6.5 to 10.2 μM.This article is protected by copyright. All rights reserved.
      PubDate: 2018-02-16T09:55:28.449386-05:
      DOI: 10.1002/cbdv.201800019
       
  • Simultaneous preparation and comparison of the osteogenic effects of
           epimedin A, B and C and icariin from E. brevicornu
    • Authors: Yani Guo; Xiufeng Wang, Jing Gao
      Abstract: In this study, epimedin A-, B- and C- and icariin-rich extracts were simultaneously prepared from Epimedium brevicornu Maxim (E. brevicornu) through a convenient four-stage process consisting of solvent extraction, macroporous resin column pre-concentration, extraction fractionation and reversed-phase (RP)-silica gel column chromatography. Single factor experiments and response surface methodology (RSM) were used to optimize the preparation conditions. In the final products, the purity of epimedin A, B and C and icariin were 23.04%, 64.50%, 54.92% and 77.54%, respectively, which will lay a foundation for the further purification of epimedin monomers and full utilization of Epimedium resources. Meanwhile, the osteogenic effects of epimedin A, B and C were investigated for the first time and compared with that of icariin, which will provide guidance for the clinical applications of Epimedium in the treatment of osteoporosis.This article is protected by copyright. All rights reserved.
      PubDate: 2018-02-16T09:40:45.366431-05:
      DOI: 10.1002/cbdv.201700578
       
  • Chemical composition of cacti wood and comparison with the wood of other
           taxonomic groups
    • Authors: Agustín Maceda; Marcos Soto-Hernández, Cecilia B. Peña-Valdivia, Teresa Terrazas
      Abstract: The aims of this study were to determine the wood chemical composition of 25 species of Cactaceae and to relate the composition to their anatomical diversity. The hypothesis was that wood chemical components differ in relationship to their wood features. The results showed significant differences in wood chemical compounds across species and genera (p < 0.05). Pereskia had the highest percentage of lignin, whereas species of Coryphantha had the lowest; extractive compounds in water were highest for Echinocereus, Mammillaria and Opuntia. Principal component analysis showed that lignin proportion separated the fibrous, dimorphic and non-fibrous groups; additionally, the differences within each type of wood occurred because of the lignification of the vascular tissue and the type of wall thickening. Compared with other groups of species, the Cactaceae species with fibrous and dimorphic wood had a higher lignin percentage than did gymnosperms and Acer species. Lignin may confer special rigidity to tracheary elements to withstand desiccation without damage during adverse climatic conditions.This article is protected by copyright. All rights reserved.
      PubDate: 2018-02-14T13:50:27.719062-05:
      DOI: 10.1002/cbdv.201700574
       
  • Cover Picture
    • Abstract: Back Cover. Bcr-Abl is an oncogenic fusion protein which expression enhances tumorigenesis, and has been highly associated with chronic myeloid leukemia (CML). Moreover, acquired drug resistance have been reported with the use of single therapy agents such as Nilotinib. Allosteric targeting has been identified to consequentially inhibit Bcr-Abl activity, which led to the recent development of ABL001 (asciminib) that selectively binds the myristoyl pocket. Experimental studies reported that combination of both inhibitors induces a bent conformation in the C-terminal helix, a characteristic feature associated with inhibited Bcr-Abl. Accordingly, molecular dynamics simulation reveals that dual targeting involving the combination of both inhibitors induces a bent conformation in the C-terminal helix as reported by El Rashedy et al. in their full paper at https://doi.org/10.1002/cbdv.201700533.
      PubDate: 2018-02-13T03:26:35.954287-05:
      DOI: 10.1002/cbdv.201870033
       
  • Cover Picture
    • Abstract: Inside Cover. Ventilago denticulata is a Thai traditional plant, and its crude extract was previously found to exhibit various biological activities. Compounds responsible for cytotoxic, antibacterial, phosphodiesterase inhibitory, nitric oxide radical scavenging, and antioxidant activities in V. denticulata were identified for the first time, as reported by Molee et al. in their full paper at https://doi.org/10.1002/cbdv.201700537.
      PubDate: 2018-02-13T03:25:50.021122-05:
      DOI: 10.1002/cbdv.201870032
       
  • Chemical composition and antimicrobial activity of Ageratina deltoidea
    • Authors: Amira Arciniegas; Ana-L. Pérez-Castorena, Mariana Meléndez-Aguirre, José Guillermo Ávila, Ana María García-Bores, José Luis Villaseñor, Alfonso Romo de Vivar
      Abstract: The chemical study of Ageratina deltoidea afforded grandiflorenic acid (1), kaurenoic acid (2) and eight benzylbenzoates (3 – 10), two of them, 3′,5′-dimethoxybenzyl 2,3,6-trimethoxybenzoate (5) and 4′-O-β-ᴅ-glucopyranosyloxy-3′-hydroxybenzyl 2,6-dimethoxybenzoate (9), described for the first time. In addition, the new sesquiterpene lactone deltoidin C (13), together with the known 11, and 12, the phenolic compounds: ayanin, 2,6-dimethoxybenzoic acid, methyl 3,4-dihydroxycinnamate, chlorogenic acid, and 3,5-dicaffeoylquinic acid were also isolated. The structures of these compounds were determined by spectroscopic methods and chemical reactions. The antibacterial and antifungal activities of compounds 1 – 12 were evaluated on Staphylococcus aureus, Escherichia coli and Candida albicans. Deltoidin A (11) was the most active antibacterial agent (MIC 16.0 μg ml−1) against E.coli, and the ent-kaurenoid derivatives (1 – 2) showed activity (MIC 31.0 μg ml−1) against S. aureus.This article is protected by copyright. All rights reserved.
      PubDate: 2018-02-10T06:00:29.781372-05:
      DOI: 10.1002/cbdv.201700529
       
  • Isolation, Synthesis and AChE Inhibitory Potential of Some Novel Cinnamyl
           Esters of Taraxerol, the Major Metabolite of the Mangrove Bruguiera
           cylindrica
    • Authors: K. V. Nithyamol; Dwaipayan Bhattacharya, Sumana Chakravarty, U.V. Mallavadhani
      Abstract: Systematic chemical screening of the leaves ofBruguiera cylindrica, the tree mangrove of Rhizophoraceae family, afforded five single and purecompounds. Thestructures of the isolated compounds were established by their spectroscopic data astaraxerol (1), 3β-(E)-coumaroyltaraxerol (2), 3β-(Z)-coumaroyltaraxerol (3),β-sitosterol (4) and eicosanol (5).In view of significant accumulation and interesting biological activities, taraxerol (1) was chemically transformed to synthesize a series of ten cinnamyl esters in very good to excellent yields. The synthesized analogues along with the parent compound were evaluated for their AChE inhibitory potential, BBB permeability and cytotoxicity against Neuro 2A cell line. Among the tested samples, compound 9 showed promising AChE inhibition with significantly low IC50 values, low cytotoxicity and high BBB permeability. Hence, compound 9 can be considered as a lead molecule for further development as potent AChE inhibitor.This article is protected by copyright. All rights reserved.
      PubDate: 2018-02-08T05:50:31.588581-05:
      DOI: 10.1002/cbdv.201800008
       
  • New Methoxyflavone from Casmiora sapota and the Biological Activities of
           Its Leaves Extract against Lead Acetate Induced Hepatotoxicity in Rats
    • Authors: Nada M. Mostafa; Eman A. Abd El-Ghffar, Hoda G. Hegazy, Omayma A. Eldahshan
      Abstract: Flavonoids are agents with strong antioxidant properties and ameliorate many diseases associated with oxidative stress. Leaves of Casimiroa sapota (CS) was investigated for components and anti-inflammatory activities against lead acetate (PbAc) induced hepatotoxicity in rats. Two groups of male albino rats were administrated orally CS (100 and 200 mg/kg b.w/day) for 28 days; other group was injected with sub-acute dose (100 mg/kg b.w/day) of PbAc. Three protective groups were injected with PbAc (100 mg/kg b.w/day) for 7 days at day 22 after treatment with either CS (100 or 200 mg/kg b.w/day) or silymarin (SILY) for 28 days. We isolated and identified, from CS, a new compound for the 1st time in nature; 5, 6, 2′, 3′- tetramethoxy flavone in addition to the rare compound 5, 6, 3′- trimethoxyflavone (second report of isolation from nature) and the known compound 5, 6, 2′, 3′, 4′- pentamethoxy flavone. There is an improvement in all hemato-biochemical parameters, antioxidant defense system and anti-inflammatory cytokines of protective groups, which received CS in dose dependent manner. The percentage of changes of all parameters measured in Pb groups that received vehicle, 100 CS, 200 CS or SILY were109.2, 37.3, 12.5% and 1.2% compared with the healthy control group. The former groups confer a better antioxidant activity on CS extract for preventing oxidative stress and inflammation in PbAc fed rats. The compounds isolated are responsible at least in part for the observed protective effects.This article is protected by copyright. All rights reserved.
      PubDate: 2018-02-06T20:10:25.349037-05:
      DOI: 10.1002/cbdv.201700528
       
  • Design, Synthesis and Anti-HIV-1 Evaluation of a Novel Series of
           1,2,3,4-Tetrahydropyrimidine-5-carboxylic acid Derivatives
    • Authors: Saghi Sepehri; Sepehr Soleymani, Rezvan Zabihollahi, Mohammad R. Aghasadeghi, Mehdi Sadat, Lotfollah Saghaie, Hamid R. Memarian, Afshin Fassihi
      Abstract: A series of tetrahydropyrimidine derivatives (2a-l) were designed, synthesized and screened for anti-HIV-1 properties based on the structures of HIV-1 gp41 binding site inhibitors, NB-2 and NB-64. A computational study was performed to predict the pharmacodynamics, pharmacokinetics and drug-likeness features of the studied molecules. Docking studies revealed that the carboxylic acid group in the molecules forms salt bridges with either Lys574 or Arg579. Physiochemical properties (e.g. molecular weight, number of hydrogen bond donors, number of hydrogen bond acceptors and number of rotatable bonds) of the synthesized compounds confirmed and exhibited that these compounds were within the range set by Lipinski's rule of five. Compounds 2e and 2k with 4-chlorophenyl substituent and 4-methylphenyl group at C4 position of the tetrahydropyrimidine ring was the most potent one among the tested compounds. This suggests that these compounds may serve as leads for development of novel small-molecule HIV-1 inhibitors.This article is protected by copyright. All rights reserved.
      PubDate: 2018-02-06T20:05:25.239214-05:
      DOI: 10.1002/cbdv.201700502
       
  • Response of biomass development, essential oil and composition of
           Plectranthus amboinicus (Lour.) Spreng to irrigation frequency and harvest
           time
    • Authors: Ali S. Sabra; Tessema Astatkie, Abed Alataway, Abeer A. Mahmoud, Ahmed S.H. Gendy, Hussein A.H. Said-Al Ahl, Kirill G. Tkachenk
      Abstract: A greenhouse experiment was conducted to study the effects of four irrigation intervals (4, 8, 12 and 16 days) and six harvests (2, 4, 6, 8, 10 and 12 months after transplanting) on biomass, essential oil content and composition of Plectranthus amboinicus (Lour.) Spreng. Fresh weight and essential oil yield decreased with increasing irrigation interval; whereas, essential oil content was stimulated by water stress and increased as the irrigation interval increased. Fresh weight of Plectranthus amboinicus irrigated every 4 days peaked when harvested at 6 months, but essential oil content peaked when irrigated every 16 days and harvested at 2 months after transplantation. On the other hand, essential oil yield peaked when irrigated every 8 days and harvested at 6 months. Thymol, p-cymene, γ-terpinene and β-caryophyllene were the major compounds, and they peaked at different irrigation intervals and harvest times. This study showed biomass, essential oil content and yield as well as the major and minor constituents of Plectranthus amboinicus are influenced by irrigation interval and the timing of harvest.This article is protected by copyright. All rights reserved.
      PubDate: 2018-02-02T07:55:25.626697-05:
      DOI: 10.1002/cbdv.201800005
       
  • Cover Picture
    • Abstract: Natural metal complexes of naamidines and naamidine-type alkaloids are a group of sponge-derived natural products with unique scaffold. Biogenetically, these complexes are postulated to be charged by numerous metalloenzymes that require metal ions for catalytic activity. Some of them exerted antimicrobial activity against pathogen bacteria. Chemical examination of the bright yellow sponge Leucetta chagosensis resulted in the isolation of three new homodimer metal complexes, namely chagosendines A – C. Bioassay results indicated that the copper complexes chagosendines B and C showed significant inhibition against the human tumor cell lines K562, HepG2, and HeLa, possessing more effects than the corresponding alkaloid ligands. The preliminary structure–activity relationship of the natural complexes and the synthesized analogues with different metal ions was discussed, as reported by Lin et al. in their full paper https://doi.org/10.1002/cbdv.201700481.
      PubDate: 2018-01-30T23:35:25.683486-05:
      DOI: 10.1002/cbdv.201870021
       
  • Volatiles and nonvolatiles in Flourensia campestris Griseb. (Asteraceae),
           how much do capitate glandular trichomes matter'
    • Authors: Leonardo A. Piazza; Daniela López, Mariana P. Silva, Marisa J. López Rivilli, Mónica G. Tourn, Juan J. Cantero, Ana L. Scopel
      Abstract: The distribution and ultrastructure of capitate glandular trichomes (GTs) in Flourensia species (Asteraceae) have been recently elucidated, but their metabolic activity and potential biological function remain unexplored. Selective nonvolatile metabolites from isolated GTs were strikingly similar to those found on leaf surfaces. The phytotoxic allelochemical sesquiterpene (-)-hamanasic acid A ((-)HAA) was the major constituent (ca. 40%) in GTs. Although GTs are quaternary ammonium compounds (QACs)-accumulating species, glycine betaine was not found in GTs; it was only present in the leaf mesophyll. Two (-)HAA accompanying surface secreted products: compounds (1) 4-hydroxyacetophenone (piceol) and (2) 2-hydroxy-5-methoxyacetophenone, which were isolated and fully characterized (GC-MS, NMR), were present in the volatiles found in GTs. The essential oils of fresh leaves revealed ca. 33% monoterpenes, 26% hydrocarbon- and 30% oxygenated sesquiterpenes, most of them related to cadinene and bisabolene derivatives. Present results suggest a main role of GTs in determining the volatile and nonvolatile composition of F. campestris leaves. Based on the known activities of the compounds identified, it can be suggested that GTs in F. campestris would play key ecological functions in plant-pathogen and plant-plant interactions. In addition, the strikingly high contribution of compounds derived from cadinene and bisabolene pathways, highlights the potential of this species as a source of high-valued bioproducts.This article is protected by copyright. All rights reserved.
      PubDate: 2018-01-30T09:36:02.470569-05:
      DOI: 10.1002/cbdv.201700511
       
  • Isocyanides Derived from α,α-Disubstituted Amino Acids: Synthesis and
           Antifouling Activity Assessment
    • Authors: Yuki Inoue; Shuhei Takashima, Yasuyuki Nogata, Erina Yoshimura, Kazuhiro Chiba, Yoshikazu Kitano
      Abstract: Herein, we contribute to the development of environmentally friendly antifoulants by synthesizing eighteen isocyanides derived from α,α-disubstituted amino acids and evaluating their antifouling activity/toxicity against the cypris larvae of the Balanus amphitrite barnacle. Almost all isocyanides showed good antifouling activity without significant toxicity and exhibited EC50 values of 0.07–7.30 μg/mL after 120-h exposure. The lowest EC50 values were observed for valine-, methionine-, and phenylalanine-derived isocyanides, which achieved >95% cypris larvae settlement inhibition at concentrations of less than 30 μg/mL without exhibiting significant toxicity. Thus, the prepared isocyanides should be useful for further research focused on the development of environmentally friendly antifouling agents.This article is protected by copyright. All rights reserved.
      PubDate: 2018-01-30T09:35:40.279477-05:
      DOI: 10.1002/cbdv.201700571
       
  • Two new dolabrane diterpenes from the Chinese mangrove Ceriops tagal
    • Authors: Shu-Jun Ni; Jun Li, Min-Yi Li
      Abstract: Two new dolabrane diterpenes, tagalenes J and K (1-2), together with eleven known analogues (3-13), were isolated from the ethanolic extract of the Chinese mangrove Ceriops tagal. The structures of these compounds were determined by extensive spectroscopic analysis, including 1D and 2D NMR and HR-ESI-MS, as well as the comparison with data in the literatures. Cytotoxicities of isolated compounds against MCF-7, SW480, HepG2, HeLa, PANC-1, and A2058 cancer cell lines were also evaluated. Compound 4 exhibited weak cytotoxic activity against SW480, HeLa and PANC-1 cell lines with IC50 values of 27.7, 22.2, and 17.6 μM, respectively.This article is protected by copyright. All rights reserved.
      PubDate: 2018-01-29T06:00:27.424474-05:
      DOI: 10.1002/cbdv.201700563
       
  • Instructions for Authors (2018)
    • PubDate: 2018-01-27T10:07:49.636472-05:
      DOI: 10.1002/cbdv.201870012
       
  • Eudesmanolides and Other Constituents from the Flowers of Wedelia
           trilobata
    • Authors: Yang Hui; Jian Cao, Jing Lin, Jian-Ni Yang, Ya-Jun Liu, Chang-Ri Han, Xiao-Ping Song, Chun-Yan Dai, Xiao-Peng Zhang, Wen-Hao Chen, Guang-Ying Chen
      Abstract: Two eudesmane sesquiterpene lactones, wedetrilides B (1) and C (2), along with five known analogues (3–8), an ent-kaurane diterpenoid (9), a steroid (10) as well as cinnamic acid derivatives (11–13) were isolated from the flowers of Wedelia trilobata. Their structures were elucidated on the basis of extensive spectroscopic analyses and by comparison of their NMR data with those of related compounds. Furthermore, the structures of 1, and 3–5 were confirmed by X-ray single-crystal diffraction analyses. Compounds 4, and 5 exhibited weak cytotoxic activities against the MCF-7, Hela, and A549 cell lines. Compounds 3–5 were also evaluated for their inhibitory effects against HIV lytic replication.This article is protected by copyright. All rights reserved.
      PubDate: 2018-01-25T04:30:29.806931-05:
      DOI: 10.1002/cbdv.201700411
       
  • Five new alkaloids from the roots of Sophora flavescens
    • Authors: Sheng-Yuan Zhang; Wen Li, Hua Nie, Mei Liao, Bo Qiu, Ya-Li Yang, Yan-Fen Chen
      Abstract: Five new quinolizidine alkaloids, including three sparteine-type alkaloids (1-3) and two cytisine-type alkaloids (4-5), along with four known ones, were isolated from the roots of Sophora flavescens. Their structures were determined by extensive spectroscopic techniques including IR, UV, NMR and HR-ESI-MS. All the compounds were evaluated for their antibacterial activities against Staphylococcus aureus and Escherichia coli.This article is protected by copyright. All rights reserved.
      PubDate: 2018-01-22T03:03:50.996689-05:
      DOI: 10.1002/cbdv.201700577
       
  • Six New Polyhydroxysteroidal Glycosides, Anthenosides S1-S6, from the
           Starfish Anthenea sibogae
    • Authors: Alla A. Kicha; Dinh T. Ha, Natalia V. Ivanchina, Timofey V. Malyarenko, Anatoly I. Kalinovsky, Pavel S. Dmitrenok, Svetlana P. Ermakova, Olesya S. Malyarenko, Nguyen A. Hung, Tran T. T. Thuy, Pham Q. Long
      Abstract: Six new polyhydroxysteroidal glycosides, anthenosides S1-S6 (1–6), along with a mixture of two previously known related glycosides, 7 and 8, were isolated from the methanolic extract of the starfish Anthenea sibogae. The structures of 1–6 were established by NMR and HR-ESI-MS techniques as well as by chemical transformations. All new compounds have a 5α-cholest-8(14)-ene-3α,6β,7β,16α-tetrahydroxysteroidal nucleus and differ from majority of starfish glycosides in positions of carbohydrate moieties at C(7) and C(16) (1–4, 6) or only at C(16) (5). The 4-O-methyl-β-D-glucopyranose residue (2) and Δ24-cholestane side chain (3) have not been found earlier in the starfish steroidal glycosides. The mixture of 7 and 8 slightly inhibited the proliferation of human breast cancer T-47D cells and decreased the colony size in the colony formation assay.This article is protected by copyright. All rights reserved.
      PubDate: 2018-01-22T02:58:24.668897-05:
      DOI: 10.1002/cbdv.201700553
       
  • Genetic and chemical diversity in Perovskia abrotanoides Karel.
           
    • Authors: Seyyed Hossein Pourhosseini; Javad Hadian, Ali Sonboli, Samad Nejad Ebrahimi, Mohammad Hossein Mirjalili
      Abstract: Genetic and the essential oil composition variability among twelve Perovskia abrotanoides populations (PAbPs) growing wild in Iran were assessed by ISSR markers, GC–FID and GC–MS, respectively. Nine selected ISSR primers produced 119 discernible bands, of them 96 (80.7%) being polymorphic. Genetic similarity values among populations ranged between 0.07 and 0.79 which indicated a high level of genetic variation. Polymorphic information content, resolving power and marker index generated by ISSR primers were, 0.31, 6.14 and 3.32, respectively. UPGMA grouped PAbPs into four main clusters. Altogether, 38 chemical compounds were identified in the oils, and a relatively high variation in their contents was found. Camphor (11.9-27.5%), 1,8-cineole (11.3-21.3%), α-bisabolol (0.0-13.1%), α-pinene (5.9-10.8%) and δ-3-carene (0.1-10.5%) were the major compounds. Oxygenated monoterpenes (32.1-35.8%) and monoterpene hydrocarbons (25.7-30.4%) were the main groups of compounds in the oils studied. Cluster analysis and principal-component analysis were used to characterize the samples according to oil components. Four main chemotypes were found to be Chemotype I (camphor/1,8-cineol), Chemotype II (1,8-cineole/camphor), Chemotype III (camphor/1,8-cineol/α-bisabolol), and Chemotype IV (camphor/δ-3-carene/α-bisabolol). The information provided here, on P. abrotanoides populations will be useful to introduce this plant into agricultural systems.This article is protected by copyright. All rights reserved.
      PubDate: 2018-01-19T11:05:27.476922-05:
      DOI: 10.1002/cbdv.201700508
       
  • Synthesis, cytotoxic and antibacterial evaluation of quinazolinone
           derivatives with substituted amino moiety
    • Authors: Xiaoping Zhan; Yun Xu, Qi Qi, Yaolin Wang, Huiying Shi, Zhenmin Mao
      Abstract: A series of novel quinazolinone derivatives containing a substituted amino moiety were synthesized, evaluated for their cytotoxic and antibacterial activities. The results of MTT assay showed that all synthesized target compounds 5A~O showed potent cytotoxicity against SGC-7901 (IC50, 0.72~1.41μM). Moreover, the compounds 5D, 5I and 5K showed better selectivity as compared with positive controls pemetrexed and MTX due to weak cytotoxicity against normal tissue cell line HUVSMC. Among synthesized compounds, the compounds 5E, 5J, 5L and 5N showed broad-spectrum cytotoxic activities against at least four cancer cell lines at a micromolar level. The results of antibacteria evaluation revealed that all synthesized compounds showed good to moderate antibacterial activities against Gram-negative bacteria Escherichia coli. Among them, the MIC values of the compounds 5C, 5F and 5M were 0.31μg/mL.This article is protected by copyright. All rights reserved.
      PubDate: 2018-01-14T23:45:24.794031-05:
      DOI: 10.1002/cbdv.201700513
       
  • Dual drug targeting of mutant Bcr-Abl induces inactive conformation: New
           strategy for the treatment of chronic myeloid leukemia and overcoming
           monotherapy resistance
    • Authors: Ahmed A El Rashedy; Fisayo A. Olotu, Mahmoud E. S. Soliman
      Abstract: Bcr-Abl is an oncogenic fusion protein which expression enhances tumorigenesis, and has been highly associated with chronic myeloid leukemia (CML). Acquired drug resistance in mutant Bcr-Abl has enhanced pathogenesis with the use of single therapy agents such as Nilotinib. Moreover, allosteric targeting has been identified to consequentially inhibit Bcr-Abl activity, which led to the recent development of ABL-001 (asciminib) that selectively binds the myristoyl pocket. Experimental studies have revealed that the combination of Nilotinib and ABL-001 induced a “bent” conformation in the C-terminal helix of Bcr-Abl; a benchmark of inhibition, thereby exhibiting a greater potency in the treatment of CML, surmounting the setbacks of drug resistance, disease regression and relapse. Therefore, we report the first account of the dynamics and conformational analysis of oncogenic T334I Bcr-Abl by dual targeting. Our findings revealed that unlike in the Bcr-Abl-Nilotinib complex, dual targeting by both inhibitors induced the bent conformation in the C-terminal helix that varied with time. This was coupled with significant alteration in Bcr-Abl stability, flexibility and compactness and an overall structural re-orientation inwards towards the hydrophobic core, which reduced the solvent-exposed residues indicative of protein folding. This study = will facilitate allosteric targeting and the design of more potent allosteric inhibitors for resistive target proteins in cancer.This article is protected by copyright. All rights reserved.
      PubDate: 2018-01-11T19:20:27.74904-05:0
      DOI: 10.1002/cbdv.201700533
       
  • Naphthalene Derivatives and Quinones from Ventilago denticulata and Their
           Nitric Oxide Radical Scavenging, Antioxidant, Cytotoxic, Antibacterial,
           and Phosphodiesterase Inhibitory Activities
    • Authors: Wannapha Molee; Anuchit Phanumartwiwath, Chatchai Kesornpun, Sanya Sureram, Nattaya Ngamrojanavanich, Kornkanok Ingkaninan, Chulabhorn Mahidol, Somsak Ruchirawat, Prasat Kittakoop
      Abstract: New naphthalene derivatives (1 and 2) and a new isomer (3) of ventilagolin, together with known anthraquinones, chrysophanol (4), physcion or emodin 3-methyl ether (5), and emodin (6), were isolated from vines of Ventilago denticulata. The isolated compounds exhibited cytotoxic activity with IC50 values of 1.15-40.54 μg/mL. Compounds 1-3 selectively exhibited weak antibacterial activity (MIC values of 200.0-400.0 μg/mL), while emodin (6) displayed moderate antibacterial activity with MIC values of 25.0 μg/mL. The isolated compounds showed nitric oxide and DPPH radical scavenging activities. Compounds 1-3 and 6 exhibited weak xanthine oxidase inhibitory activity, while emodin (6) acted as an aromatase inhibitor with the IC50 value of 10.1 μM. Compounds 1 and 2 exhibited phosphodiesterase 5 inhibitory activity with IC50 values of 8.28 μM and 6.48 μM, respectively.This article is protected by copyright. All rights reserved.
      PubDate: 2018-01-11T19:20:25.997615-05:
      DOI: 10.1002/cbdv.201700537
       
  • Oplopane Sesquiterpenes from Ligularia knorringiana and their
           anti-complementary activity
    • Authors: Wei Dai; Chuang-Qi Lu, Yan Wang, Yan Lu, Dao-Feng Chen, Qi Wang
      Abstract: Three new oplopane sesquiterpenes, knorringianalarins D – F (1 – 3, resp.), and five known analogues (4 – 8, resp.) were isolated from the roots and rhizomes of Ligularia knorringiana. The structures of three new compounds were identified as 4-acetoxy-2β-hydroxy-3β-(2-methylbutyryloxy)-9α-(4-methylsenecioyloxy)-11α,12-epoxyoplop-10(14)-ene (1), 3β,4-diacetoxy-8α-(2-methylbutyryloxy)-9α-(4-acetoxy-4-methylsenecioyloxy)-11α,12-epoxyoplop-10(14)-ene (2), and (1R,5R,6R,7R,9R)-5,9,11-trihydroxy-4,15-dinor-10(14)-oplopen-3-one (3) based on spectroscopic methods including 1D, 2D NMR, mass spectrometry, and CD spectroscopy techniques. All compounds were evaluated for their anti-complementary activity on the classical pathway of the complement system in vitro. Among which, three oplopane sesquiterpenes (3, 7 and 8) exhibited better anti-complementary effects with CH50 values ranging from 0.33 to 0.89 mM, which are plausible candidates for developing potent anti-complementary agents.This article is protected by copyright. All rights reserved.
      PubDate: 2018-01-11T19:20:23.914627-05:
      DOI: 10.1002/cbdv.201700515
       
  • Cover Picture
    • Abstract: The halotolerant fungus Aspergillus variecolor produced diverse natural products with various scaffolds. The fungal strains from different environmental locations usually generated distinct secondary metabolites, suggesting that ecological impacts may lead to the structural modifications. A marine coral-associated fungus A. versicolor LZD-44-03 has been examined chemically to afford two new thiol-bearing compounds with trivial names of varicuothiols A and B. Both compounds exhibited significant inhibition against LPS-induced RAW24.7 cell proliferation caused by the down regulation of nitrite production and cytokines (MCP-1, IL-6, and TNF-α), as reported by Lin et al. in their full paper https://doi.org/10.1002/cbdv.201700445.
      PubDate: 2018-01-08T02:55:27.652205-05:
      DOI: 10.1002/cbdv.201870011
       
  • Hybrid Pharmacophore Design, Molecular Docking, Synthesis, and Biological
           Evaluation of Novel Aldimine-Type Schiff Base Derivatives as Tubulin
           Polymerization Inhibitor
    • Authors: Alieh Ameri; Ghadamali Khodarahmi, Hamid Forootanfar, Farshid Hassanzadeh, Gholam-Hosein Hakimelahi
      Abstract: A series of hybrid Aldimine-type Schiff base derivatives including trimethoxyphenyl ring and 1,2,4-triazle-3-thiol/thione were designed as tubulin inhibitors. The molecular docking simulations on tubulin complex (PDB: 1SA0) revealed that derivatives with nitro and /or chloro or dimethylamine substitutes (4-Nitro, 2-Nitro, 3-Nitro, 4-Cl-3-nitro, and 4-N(CH3)2) on the aldehyde ring were the best compounds with remarkable binding energies (-9.09, -9.07, -8.63, -8.11, and -8.07 kcalmol−1, respectively) compared to Colchicine (-8.12 kcalmol−1). These compounds were also showed remarkable binding energies from -10.66 to -9.79 and -10.12 to -8.95 kcalmol−1 on human (PDB: 1PD8) and Candida albicans (PDB: 3QLS) DHFR, respectively. The obtained results of cytotoxic activities against HT1080, HepG2, HT29, MCF-7, and A549 cancer cell lines indicated that 4-Nitro and 2-Nitro substituted compounds were the most effective agents by mean IC50 values of 11.84±1.01 and 19.92±1.36 μM, respectively. 4-Nitro substituted compound (5 μM) and 2-Nitro substituted compound (30 μM) were able to strongly inhibit the tubulin polymerization compared to Colchicine (5 μM) and 4-Nitro substituted compound displayed IC50 values of 0.16±0.01 μM compared to that of colchicine (0.19±0.01 μM). This compound also showed the lowest MIC values on all tested microbial strains including three Gram-positive, four Gram-negative, and three yeast pathogens.This article is protected by copyright. All rights reserved.
      PubDate: 2018-01-01T23:10:49.9172-05:00
      DOI: 10.1002/cbdv.201700518
       
  • Chemical composition, antioxidant and anti-melanogenic activities of
           essential oils from Chrysanthemum boreale Makino at different harvesting
           stages
    • Authors: Do-Yoon Kim; Kyung-Jong Won, Dae Il Hwang, Soo Min Park, Bokyung Kim, Hwan Myung Lee
      Abstract: In the present study, the chemical compositions and skin whitening-related anti-oxidant and anti-melanogenic effect of essential oils (EOs) extracted from Chrysanthemum boreale MAKINO (CBM) (CBMEOs) at vegetative, pre-flowering and full-flowering are investigated and contrasted among the three stages. The yields and components of the CBMEOs were different at each stage. The CBMEOs increased DPPH and ABTs scavenging activities and attenuated the α-melanocyte stimulating hormone (α-MSH)-induced tyrosinase activity and melanin synthesis in B16BL6 cells. Among CBMEO components, eugenol had the highest DPPH and ABTs scavenging activities and cuminaldehyde was the strongest inhibitor of α-MSH-induced tyrosinase activity and melanin synthesis. The CBMEOs in each stage showed the different levels of phosphorylation of extracellular signal-regulated kinase1/2 and p38 MAPK. These findings demonstrate that the CBMEOs have anti-oxidative and anti-melanogenic activities in all the CBM harvesting stages, resulting in skin-whitening biological activities and that the levels of their component contents and bioactivities differ among the CBM harvesting stages. The CBMEOs may have the potential for use in cosmetics and alternative medicine.This article is protected by copyright. All rights reserved.
      PubDate: 2018-01-01T23:05:32.910429-05:
      DOI: 10.1002/cbdv.201700506
       
  • Chemical composition of essential oils from Thymus vulgaris, Cymbopogon
           citratus and Rosmarinus officinalis and their effects on the HIV-1 Tat
           protein function
    • Authors: Feriotto Giordana; Marchetti Nicola, Costa Valentina, Beninati Simone, Tagliati Federico, Mischiati Carlo
      Abstract: New drugs would be beneficial to fight resistant HIV strains, in particular those capable of interfering with essential viral functions other than those targeted by highly active antiretroviral therapy drugs. Despite the central role played by Tat protein in HIV transcription, a search for vegetable extracts able to hamper this important viral function was never carried out. In this work, we evaluated the chemical composition and possible interference of essential oil from Thymus vulgaris, Cananga odorata, Cymbopogon citratus and Rosmarinus officinalis with the Tat/TAR-RNA interaction and with Tat-induced HIV-1 LTR transcription. GC/MS analysis demonstrated that biodiversity of herbal species translated into essential oils composed of different blends of terpenes. In all of them, 4-6 constituents represent from 81,63 to 95,19% of the total terpenes. Essential oils of Thymus vulgaris, Cymbopogon citratus and Rosmarinus officinalis were active in interfering with Tat functions, encouraging further studies to identify single terpenes responsible for the antiviral activity. In view of the quite different composition of these essential oils, we concluded that their interference on Tat function depends on specific terpene or a characteristic blend.This article is protected by copyright. All rights reserved.
      PubDate: 2017-12-28T02:00:13.89475-05:0
      DOI: 10.1002/cbdv.201700436
       
  • Antiviral activity of Faramea hyacinthina and Faramea truncata leaves on
           dengue virus type-2 and their major compounds
    • Authors: Rodolfo S. Barboza; Ligia M. M. Valente, Thiago Wolff, Iranaia Assunção-Miranda, Rômulo S. L. Neris, Iris P. Guimarães-Andrade, Mário Gomes
      Abstract: The defatted fractions of the Faramea hyacinthina and F. truncata (Rubiaceae) leaf MeOH extracts showed in vitro non-cytotoxic and anti-dengue virus serotype 2 (DENV2) activity in human hepatocarcinoma cell lineage (HepG2). Submitting these fractions to the developed RP-SPE method allowed isolating the antiviral flavanone (2S)-isosakuranetin-7-O-β-D-apiofuranosyl(16)-β-D-glucopyranoside (1) from both species and yielded less active sub-fractions. The new diasteroisomeric epimer pair 2S + 2R of 5,3′,5′-trihydroxy-flavanone-7-O-β-D-apiofuranosyl(16)-β-D-glucopyranoside (2a/2b) from F. hyacinthina; the known narigenin-7-O-β-D-apiofuranosyl(16)-β-D-glucopyranoside (3) from both species; rutin (4) and quercetin-4′-β-D-O-glucopyranosyl-3-O-rutinoside (5) from F. hyacinthina, and kaempferol-3-O-rutinoside (6), erythroxyloside A (7) and asperuloside (8) from F. truncata have been isolated from these sub-fractions. Compounds 4 - 8 are reported for the first time in Faramea spp.This article is protected by copyright. All rights reserved.
      PubDate: 2017-12-26T09:30:25.671589-05:
      DOI: 10.1002/cbdv.201700393
       
  • Reaction product variability and biological activity of the
           lactoperoxidase system depending on medium ionic strength and pH, and on
           substrate relative concentration
    • Authors: Françoise Bafort; Christian Damblon, Nicolas Smargiasso, Edwin De Pauw, Jean-Paul Perraudin, M. Haïssam Jijakli
      Abstract: The potential of ions produced in water by the lactoperoxidase system against plant pests has shown promising results. We tested the bioactivity of ions produced by the lactoperoxidase oxidation of I- and SCN- in several buffers or in tap water and characterized the ions produced. In vitro biological activity was tested against Penicillium expansum, the causal agent of mold in fruits, and the major cause of patulin contamination of fruit juices and compotes. In buffers, the ionic concentration was increased 3-fold, and pathogen inhibition was obtained down to the 1/15 dilution. In tap water, the ionic concentration was weaker, and pathogen inhibition was obtained only down to the 1/3 dilution. Acidic buffer increased ion concentrations as compared to less acidic (pH 5.6 or 6.2) or neutral buffers, as do increased ionic strength. 13C-labelled SCN- and MS showed that different ions were produced in water and in buffers. In specific conditions the ion solution turned yellow and a product was formed, probably diiodothiocyanate (I2SCN-), giving an intense signal at 49.7 ppm in 13C NMR. The formation of the signal was unambiguously favored in acidic media and disadvantaged or inhibited in neutral or basic conditions. It was enhanced at a specific SCN-: I- ratio of 1:4.5, but decreased when the ratio was 1:2, and was inhibited at ratio SCN->I-. We demonstrated that the formation of the signal required the interaction between I2 and SCN-, and MS showed the presence of I2SCN-.This article is protected by copyright. All rights reserved.
      PubDate: 2017-12-20T00:15:49.388529-05:
      DOI: 10.1002/cbdv.201700497
       
  • Effects of biorelevant media components on dissolution behaviour of
           1,2,4-thiadiazole derivative designed for Alzheimer's disease prevention
    • Authors: Maria Promzeleva; Mikhail Chislov, Tatyana Volkova, Alexey Proshin, Roman Kumeev, Irina Terekhova
      Abstract: In this study, dissolution behaviour of 1,2,4-thiadiazole derivative (1-[5-(3-chloro-phenylamino)-1,2,4-thiadiazol-3-yl]-propan-2-ol) displaying an anti-Alzheimer activity was examined in biorelevant media such as Simulated Gastric Fluid (SGF, pH 1.2), Fasted State Simulated Gastric Fluid (FaSSGF, pH 1.6) and Fasted State Simulated Intestinal Fluid (FaSSIF, pH 6.5). It was found that solubility and dissolution rate of 1,2,4-thiadiazole derivative under consideration are not strongly dependent on pH, whereas these parameters are significantly affected by the buffer composition. Dissolution was found to be more effective in buffers composed of the surfactant micelles. It was demonstrated that considerable increase in solubility and dissolution rate in SGF is achieved through the interaction of 1,2,4-thiadiazole derivative with the micelles of sodium dodecyl sulfate. On the contrary, CMC of sodium taurochalate was shifted in the presence of 1,2,4-thiadiazole derivative, therefore, dissolution process is not so efficient in FaSSIF. Interactions occurring between 1,2,4-thiadiazole derivative and the components of biorelevant media were investigated in detail by means of UV-vis spectroscopy, 1H NMR and phase solubility methods.This article is protected by copyright. All rights reserved.
      PubDate: 2017-12-16T03:21:21.945208-05:
      DOI: 10.1002/cbdv.201700459
       
  • Optimizing Water Exchange Rates and Rotational Mobility for
           High-Relaxivity of a Novel Gd-DO3A Derivative Complex Conjugated to Inulin
           as Macromolecular Contrast Agents for MRI
    • Authors: Luigi Granato; Luce Vander Elst, Celine Henoumont, Robert N. Muller, Sophie Laurent
      Abstract: Thanks to the understanding of the relationships between the residence lifetime τM of the coordinated water molecules to macrocyclic Gd-complexes and the rotational mobility τR of these structures, and according to the theory for paramagnetic relaxation, it is now possible to design macromolecular contrast agents with enhanced relaxivities by optimizing these two parameters through ligand structural modification. We succeeded in accelerating the water exchange rate by inducing steric compression around the water binding site, and by removing the amide function from the DOTA-AA ligand [1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid mono(p-aminoanilide)] (L) previously designed. This new ligand 10[2(1-oxo-1-p-propylthioureidophenyl-propyl]-1,4,7,10-tetraazacyclodecane-1,4,7-tetraacetic acid (L1) was then covalently conjugated to API [O-(aminopropyl)inulin] to get the complex API-(GdL1)x with intent to slow down the rotational correlation time (τR) of the macromolecular complex. The evaluation of the longitudinal relaxivity at different magnetic fields and the study of the 17O NMR at variable temperature of the low-molecular-weight compound (GdL1) showed a slight decrease of the τM value (τM310=331ns vs τM310=450ns for the GdL complex). Consequently to the increase of the size of the API-(GdL1)x complex, the rotational correlation time becomes about 360 times longer compared to the monomeric GdL1 complex (τR = 33700ps), which results in an enhanced proton relaxivity.This article is protected by copyright. All rights reserved.
      PubDate: 2017-12-16T03:20:49.734509-05:
      DOI: 10.1002/cbdv.201700487
       
  • Iridoides of chemotaxonomy relevance, a new antirrhinoside ester and other
           constituents from Kickxia spuria subsp. integrifolia (Brot.) R. Fern
    • Authors: Alessandro Venditti; Claudio Frezza, Ilaria Serafini, Alessandro Ciccòla, Fabio Sciubba, Mauro Serafini, Armandodoriano Bianco
      Abstract: In this work, the secondary metabolite content of the ethanolic extract of Kickxia spuria subsp. integrifolia (Brot.) R. Fern. is reported. Fourteen compounds were isolated and identified by means of Column Chromatography and NMR and MS spectrometric techniques, respectively. Among these compounds, the chemotaxonomic markers of the species were evidenced whereas others were reported for the first time in the genus. Among these a new antirrhinoside derivative (12) was recognized. The iridoid content show a molecular pattern very similar to those reported for other taxa comprised in the Antirrhinae tribe of Plantaginaceae, thus providing an additional evidence to support the current botanical classification of the Kickxia genus. Anyway, most of the recognized components are able to exert important pharmacological properties which might suggest the possible employment of also this species in traditional medicine just like already happens for some other species of the Kickxia genus.This article is protected by copyright. All rights reserved.
      PubDate: 2017-12-14T05:27:52.58241-05:0
      DOI: 10.1002/cbdv.201700473
       
  • New Metabolites Produced by Cylindrocarpon sp. SY-39 from a Driftwood
    • Authors: Takuma Suzuki; Seiya Yoshida, Takuya Koseki, Takako Aboshi, Tetsuya Murayama, Unang Supratman, Yoshihito Shiono
      Abstract: Four novel cylindropyrone A (1), 10′-hydroxyilicicolinic acid D (3), cylindrolactones A (4) and B (5), together with known dihydroinfectopyrone (2) were isolated from the culture of Cylindrocarpon sp. SY-39 from a driftwood. Their structures were elucidated using 1D- and 2D-NMR spectroscopy. Compound 3 showed antimicrobial activity against Staphylococcus aureus with MIC value of 5.0 μg/ml.This article is protected by copyright. All rights reserved.
      PubDate: 2017-12-13T09:31:28.733744-05:
      DOI: 10.1002/cbdv.201700493
       
  • Phytochemical Composition and Biological Activities of Dyssodia
           tagetiflora Lag
    • Authors: Ana María García-Bores; Amira Arciniegas-Arciniegas, Alma Reyna Campos, Carlos Céspedes-Acuña, Betsaida Avila-Suárez, Julio Alarcón-Enos, Saul Flores-Maya, Adriana Montserrat Espinosa-González, Alfonso Romo de Vivar-Romo, Carlos Pérez Plasencia, José Guillermo Avila-Acevedo
      Abstract: While plants of the genus Dyssodia are used by man to a certain extent, few phytochemical and pharmacological studies have been performed with species of this genus. D. tagetiflora is an endemic plant of Mexico and has been used as fodder. The aim of this research was to isolate and identify the main bioactive components and evaluate the insecticidal, antioxidant, genotoxic and cytoprotective activities of D. tagetiflora. The isolated substances included an essential oil composed of six monoterpenes, and extracts containing two flavonols, three flavonol-glycosides and four thiophenes. The compounds were characterised using spectroscopic and spectrometric methods, including GC/MS, MS and NMR. The essential oil showed insecticidal activity against Drosophila melanogaster larvae. The methanolic extract of D. tagetiflora (DTME) had strong antioxidant activity against DPPH and ABTS radicals; DTME showed no evidence of genotoxic or cytotoxic effects. In contrast, DTME showed a cytoprotective effect attenuating the formation of H2O2-induced micronuclei in Vicia faba roots. This report is the first to describe the phytochemical and biological activity of D. tagetiflora.This article is protected by copyright. All rights reserved.
      PubDate: 2017-12-10T02:40:41.972296-05:
      DOI: 10.1002/cbdv.201700415
       
  • Chagosendines A-C, New Metal Complexes of Imidazole Alkaloids from the
           Calcareous Sponge Leucetta chagosensis
    • Authors: Bang An; Fuling Yin, Nicole J. de Voogd, Xiaoguang Chen, Wei Cheng, Wenhan Lin
      Abstract: Chemical examination of the bright yellow sponge Leucetta chagosensis resulted in the isolation of three new imidazole-based alkaloid complexes namely chagosendines A-C (1-3), together with known analogues pyronaamidine, naamidine J, and naamine C. Their structures were determined on the basis of extensive spectroscopic (IR, MS, NMR and single-crystal X-ray diffraction) analysis in association with the chemical conversion. The isolated alkaloids together with three synthesized new homodimer complexes were evaluated for the antitumor activities. The copper complexes of imidazole alkaloids 2 and 3, as found from nature for the first time, exerted selective and remarkable activities against the tumor cell lines K562, HepG2 and Hela.This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-30T08:00:39.438421-05:
      DOI: 10.1002/cbdv.201700481
       
  • Chemical composition and in vitro anthelmintic activity of extracts of
           Tagetes patula against a multidrug-resistant isolate of Haemonchus
           contortus
    • Authors: Flávio Augusto Sanches Politi; Amauri Alves Souza, Rafaela Regina Fantatto, Rosemeire Cristina Linhari Rodrigues Pietro, Waldomiro Barioni, Márcio Dias Rabelo, Humberto Ribeiro Bizzo, Ana Carolina de Souza Chagas, Maysa Furlan
      Abstract: Sheep breeding has suffered economic losses due to parasitism by gastrointestinal nematodes, particularly Haemonchus contortus. The use of natural products, specifically Tagetes patula, has been suggested as an alternative method of combatting this issue. Chemical analyses of the extracts of this species described in the literature report the presence of important classes of secondary metabolites such as thiophenes, flavonoids, alkaloids and benzofurans, some of which were identified and isolated in this study. The aim of this work was to test the effect of the essential oil (EO) and the ethanolic extract of the aerial parts (TpEtOH) of T. patula on eggs and larvae of H. contortus, through an egg hatch test (EHT) and a larval development test (LDT). In the EHT, the EO showed 100% inhibition at 0.75 mg.mL−1 (LC50 = 0.0780 mg.mL−1), and the TpEtOH showed 100% inhibition at 100 mg.mL−1 (LC50 = 12.8 mg.mL−1). In the LDT, the EO showed 100% inhibition at 0.375 mg.mL−1 (LC50 = 0.0400 mg.mL−1), and the TpEtOH showed 100% inhibition at 1.56 mg mL−1 (LC50 = 0.340 mg.mL−1). Compared to available literature data, the results presented here suggest that the crude extracts of T. patula have substantial potential for controlling this nematode by interrupting its life cycle and/or preventing it from reaching the infective stage.This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-27T03:10:47.080352-05:
      DOI: 10.1002/cbdv.201700507
       
  • Bioactive Pimarane Diterpenes from the Arctic Fungus Eutypella sp. D-1
    • Authors: Xiaoli Wang; Kunlai Sun, Bin Wang
      Abstract: Two new pimarane diterpenes, libertellenone M (1) and libertellenone N (2), together with five known compounds were isolated from the culture extract of Eutypella sp. D-1 derived from high-latitude soil of the Arctic. The structures of these compounds were determined by spectroscopic data as well as experimental and calculated electronic circular dichroism (ECD) analysis. Antimicrobial and cytotoxic activities of the isolated compounds were evaluated. Compound 3 exhibited weak antibacterial activity against Escherichia coli, Bacillus subtilis, and Vibrio vulnificus, each with MIC values of 16 μg/mL. Compounds 2 and 3 showed moderate cytotoxic activity against K562 and MCF-7 cell lines with IC50 values of 7.67 and 9.57 μM, respectively.This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-23T02:11:07.68289-05:0
      DOI: 10.1002/cbdv.201700501
       
  • Cytotoxic Triterpenoids from Roots of Actinidia chinensis
    • Authors: Liu-Bin Wei; Si-Yuan Ma, Hong-xing Liu, Chu-Sheng Huang, Na Liao
      Abstract: Phytochmical investigation of roots of Actinidia chinensis PLANCH led to the isolation triterpenoids 1 - 16, including a new compound 2α,3α,23,24-tetrahydroxyurs-12,20(30)-dien-28-oic acid (1). Their structures were identified on the basis of spectroscopic analysis, including 1D- and 2D-NMR, HR-ESI mass spectrometry, and by comparison with the literatures. The cytotoxicities of triterpenoids 1 - 16 against a panel of cultured human cancer cell lines (HepG2, A549, MCF-7, SK-OV-3, and HeLa) were evaluated. The new compound 1 exhibited moderate antitumor activities with IC50 values of 19.62 ± 0.81, 18.86 ± 1.56, 45.94 ± 3.62, 62.41 ± 2.29, and 28.74 ± 1.07 μM, respectively. The experiment data might be available to explain the use of roots of A. chinensis to treat various cancers in traditional Chinese medicine.This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-21T22:36:34.71745-05:0
      DOI: 10.1002/cbdv.201700454
       
  • Chemical Polymorphism of Essential Oils of Artemisia vulgaris Growing Wild
           in Lithuania
    • Authors: Asta Judzentiene; Jurga Budiene
      Abstract: Compositional variability of mugwort (Artemisia vulgaris L.) essential oils has been investigated in the study. Plant material (over ground parts at full flowering stage) was collected from forty-four wild populations in Lithuania. The oils from aerial parts were obtained by hydrodistillation and analyzed by GC(FID) and GC/MS. In total, up to 111 components were determined in the oils. As the major constituents were found: sabinene, 1,8-cineole, artemisia ketone, both thujone isomers, camphor, cis-chrysanthenyl acetate, davanone and davanone B.The compositional data were subjected to statistical analysis. The application of PCA (Principal Component Analysis) and AHC (Agglomerative Hierarchical Clustering) allowed grouping the oils into six clusters. AHC permitted to distinguish an artemisia ketone chemotype, which, to the best of our knowledge, is very scarce. Additionally, two rare cis-chrysanthenyl acetate and sabinene oil types were determined for the plants growing in Lithuania. Besides, davanone was found for the first time as a principal component in mugwort oils.The performed study revealed significant chemical polymorphism of essential oils in mugwort plants native to Lithuania; it has expanded our chemotaxonomic knowledge both of A. vulgaris species and Artemisia genus.This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-21T22:36:23.617937-05:
      DOI: 10.1002/cbdv.201700257
       
  • Four New Acylated Iridoid Glycosides from the Aerial Part of Veronicastrum
           sibiricum and Their Antioxidant Response Element-Inducing Activity
    • Authors: Myeong Il Kim; Chul Young Kim
      Abstract: Four new (1 − 4) and one known (5) acylated iridoid glycosides were isolated from aerial parts of Veronicastrum sibiricum (L.) Pennell. The chemical structures of isolated compounds were determined to be 3′′,4′′-dicinnamoyl-6-O-rhamnopyranosyl-10-O-bergaptol-5,7-bisdeoxycynanchoside (1), 3′′,4′′-dicinnamoyl-6-O-rhamnopyranosylpaulownioside (2), 2′′,4′′-dicinnamoyl-6-O-rhamnopyranosylcatalpol (3), 3′′,4′′-dicinnamoyl-6-O-rhamnopyranosylaucubin (4), and 3′′,4′′-dicinnamoyl-6-O-rhamnopyranosylcatalpol (5) using spectroscopic techniques. Among these compounds, compound 5 increased antioxidant response element (ARE) luciferase activity.This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-21T22:30:45.606524-05:
      DOI: 10.1002/cbdv.201700447
       
  • Inter- and intraspecific variability of nitrogenated compounds in
           gorgonian corals via application of a fast one-step analytical protocol
    • Authors: Chiara Samorì; Federica Costantini, Paola Galletti, Emilio Tagliavini, Marco Abbiati
      Abstract: Gorgonian corals play a structural role in temperate and tropical biogenic reefs, forming animal forests and creating biodiversity hot spots. In the Mediterranean Sea, slow-growing and long-lived gorgonian species are threatened by human disturbances and global environmental changes and concern about their conservation is rising. Alkaloid metabolites have proven to be essential in protecting these species from environmental stressors.. Traditional profiling methodologies to detect these metabolites require a large quantity of living tissue. Here, the chemodiversity of gorgonian alkaloids was investigated by applying a fast and effective protocol combining extraction and derivatization using small-scale tissue samples and GC-MS analysis. The method was effective in identifying and quantifying alkaloids and guanine-based compounds. Eight N-heterocyclic compounds were found in six Mediterranean gorgonians differing for types and quantity. The metabolomic profile was conservative in species of the Eunicella genus, with three species sharing the same pattern. Conversely, Paramuricea clavata displayed a noticeable spatial pattern of variation among colonies collected in different locations. The analytical approach presented here proved to be effective, allowing rare, endangered, and small-sized species to be screened rapidly for detection of new compounds in order to explore their biological and ecological functions.This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-21T22:30:27.482279-05:
      DOI: 10.1002/cbdv.201700449
       
  • Comparative Study of Fatty Acids Profile in Eleven Wild Mushrooms of
           Boletacea and Russulaceae Families
    • Authors: Marija V. Dimitrijevic; Violeta D. Mitic, Olga P. Jovanovic, Vesna P. Stankov Jovanovic, Jelena S. Nikolic, Goran M. Petrovic, Gordana S. Stojanovic
      Abstract: Eleven species of wild mushrooms which belong to Boletaceae and Russulaceae families were examined by gas chromatography (GC) and gas chromatography–mass spectrometry (GC-MS) analysis for the presence of fatty acids. As far as we know, the fatty acid profiles of B. purpureus and B. rhodoxanthus were described for the first time. Twenty-six fatty acids were determined. Linoleic (19.5 – 72%), oleic (0.11 – 64%), palmitic (5.9 – 22%) and stearic acids (0.81 – 57%) were present in the highest contents. In all samples, unsaturated fatty acids dominate. Agglomerative hierarchical clustering was used to display the correlation between the fatty acids and their relationships with the mushroom species. Based on the fatty acids profile in the samples, the mushrooms can be divided into two families: Boletaceae and Russulaceae families, using cluster analysis.This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-21T22:25:25.854904-05:
      DOI: 10.1002/cbdv.201700434
       
  • The relationship between endogenous β-glucuronidase activity and
           biologically active flavones-aglycone contents in hairy roots of Baikal
           skullcap
    • Authors: V.S Dikaya; A.I Solovyeva, R. A Sidorov, P. A Solovyev, A.Yu Stepanova
      Abstract: Here we examine the relationship between contents of principal flavones in hairy roots of Scutellaria baicalensis with the activity of the β-glucuronidase (sGUS) enzyme during a culturing cycle. Using RP-HPLC, we show that the highest contents of aglycones, baicalin and wogonin is observed at the growth days 8, 14 and 71 and reach 45, 41 and 62% (based on the total weight of hairy roots of the Baikal skullcap), correspondingly. Their accumulation is accompanied by increase of the sGUS activity, which we determined fluorometrically. Moreover, the enzyme activity is characterized by significant and reasonable correlation only with the wogonin contents. Our results confirm a significant role of sGUS at the final steps of the metabolism in root-specific flavones of Baikal skullcap and suggest how one can optimize the conditions of culturing the hairy roots for biotechnological production of individual flavonoids. For example, at the culturing day 71 wogonin constituted over 80% of all flavones extracted from cells.This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-21T12:00:24.582865-05:
      DOI: 10.1002/cbdv.201700409
       
  • Cross-Reactivity of Polyclonal Antibodies against Canavalia Ensiformis
           (Jack Bean) Urease and H. Pylori Urease Subunit A Fragments
    • Authors: Zbigniew Jerzy Kaminski; Inga Relich, Iwona Konieczna, Wieslaw Kaca, Beata Kolesinska
      Abstract: Overlapping decapeptide fragments of H. pylori urease subunit A (UreA) were synthesized and tested with polyclonal antibodies against Canavalia ensiformis (Jack bean) urease. The linear epitopes of UreA identified using the dot blot method were then examined using epitope mapping. For this purpose, series of overlapping fragments of UreA, frameshifted +/- 4 amino acid residues were synthesized. Most of the UreA epitopes which reacted with the Jack bean urease polyclonal antibodies had been recognized in previous studies by monoclonal antibodies against H. pylori urease. Fragments 11-24, 21-33, and 31-42 were able to interact with the Jack bean urease antibodies, giving stable immunological complexes. However, the lack of recognition by these antibodies of all the components in the peptide map strongly suggests that a non-continuous (nonlinear) epitope is located on the N-terminal domain of UreA.This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-20T18:45:50.073336-05:
      DOI: 10.1002/cbdv.201700444
       
  • Melanogenesis-inhibitory and cytotoxic activities of chemical constituents
           from the leaves of Sauropus androgynus L. Merr. (Euphorbiaceae)
    • Authors: Jie Zhang; Wan-Fang Zhu, Wei-Yuan Zhu, Pan Pan Yang, Jian Xu, Jiradej Manosroi, Takashi Kikuchi, Masahiko Abe, Toshihiro Akihisa, Feng Feng
      Abstract: A new steroid, 20-hydroxyisofucosterol (stigmasta-5,24(28)-diene-3β,20β-diol) (7), along with six known compounds 1 – 6 were isolated from the MeOH extract of the leaves of Sauropus androgynus L. Merr. (Euphorbiaceae). The structure of new steroid was determined by HR-APCI-MS and various NMR techniques in combination with literature data. Subsequently, their anti-inflammatory, cytotoxic activities against five human cell lines, as well as inhibitory activities against the α-MSH induced melanogenesis on the B16 cell line were evaluated. As the results, steroid compounds, 6 and 7 exhibited moderate cytotoxic to HL60, AZ521, SKBR3, and A549 tumor cell lines (IC50 26.9 – 45.1 μM) with high tumor selectivity for A549 relative to WI38 cell lines (SI 2.6 and 3.0, resp.). And, flavonoid compounds, 4 and 5 exhibited superior inhibitory activities against melanogenesis (67.0 – 94.7% melanin content), even with no or low toxicity to the cells (90.1 – 99.6% cell viability) at the concentrations from 10 to 100 μM. Furthermore, western blot analysis suggested that the compound 5 could inhibit melanogenesis by suppressing the protein expressions of MITF, TRP-1, TRP-2, and tyrosinase.This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-16T11:00:59.654183-05:
      DOI: 10.1002/cbdv.201700486
       
  • Varicuothiols A and B, New Fungal Metabolites from Aspergillus versicolor
           with Anti-inflammatory Activities
    • Authors: Ran Chen; Dong Liu, Peng Guo, Wenhan Lin
      Abstract: Chemical examination of a coral-associated fungus Aspergillus versicolor LZD-44-03 resulted in the isolation of two new compounds with the trivial names of varicuothiols A (1) and B (2) as a unique scaffold. Their structures were determined through extensive spectroscopic analyses in association with the modified Mosher's method and chemical conversion. Both 1 and 2 exhibited significant inhibition against LPS-induced RAW24.7 cell proliferation, in association with the down regulation of nitrite production and cytokines (MCP-1, IL-6, and TNF-α).This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-16T10:57:02.835772-05:
      DOI: 10.1002/cbdv.201700445
       
  • Total synthesis and antibacterial study of cyclohexapeptides Desotamide B,
           Wollamide B and their analogs
    • Authors: Yixing Chen; Chao Liu, Nan Liu, Ye Wu, Qingjie Zhao, Honggang Hu, Xiang Li, Yan Zou
      Abstract: As natural-product-derived antibiotics, Desotamides A-D and wollamides exhibit growth inhibitory activity against Gram-posivite bacteria (IC50 0.6-7 μM) and are noncytotoxic to mammalian cells (IC50>30 μM). Herein we firstly report the total synthesis of above two cyclohexapeptides as well as a series of structural variants through solid phase peptide synthesis (SPPS), of which DE-3 displayed a 2-fold increase of anti-bacterial activity when compared with the original peptide DE-1. This strategy may offer good improvements for the synthesis of other cyclic peptides.This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-10T06:55:24.706517-05:
      DOI: 10.1002/cbdv.201700414
       
  • Costus spiralis (Jacq.) Roscoe: a novel source of flavones with
           α-glycosidase inhibitory activity
    • Authors: Ana P. de Oliveira; Juliana S. Coppede, Bianca W. Bertoni, Antônio E. M. Crotti, Suzelei C. França, Ana Maria S. Pereira, Silvia H. Taleb-Contini
      Abstract: Costus spiralis, a plant used in traditional Brazilian medicine for the treatment of complications in diabetes, was investigated. Assay of hexane, ethyl acetate, methanol and aqueous fractions obtained by partition of a crude methanol extract of dried leaves of C. spiralis revealed that AGI activity was confined to the ethyl acetate fraction. Purification of this fraction yielded schaftoside and isoschaftoside. The AGI activities of the two flavones were lower than, but comparable with, that of the anti-diabetic drug acarbose. In contrast, the IC50 value of the ethyl acetate fraction was 1.95-, 2.34- and 2.22-fold higher than those of acarbose, schaftoside and isoschaftoside, respectively. The results demonstrate for the first time that schaftoside and isoschaftoside are responsible, in part, for the AGI activity of C. spiralis. Our study suggests that further investigations into C. spiralis may lead to the discovery of additional compounds with antihyperglycemic activity.This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-10T04:06:14.364943-05:
      DOI: 10.1002/cbdv.201700421
       
  • In-vitro, in silico elucidation of antiurease activity, kinetic mechanism
           and COX-2 inhibitory efficacy of Coagulansin-A of Withania coagulans
    • Authors: Abdul Rehman Phull; Mubshir Hassan, Qamar Abbas, Hussain Raza, Ihsan ul Haq, Sung Yum Seo, Song Ja kim
      Abstract: Urease enzyme plays a crucial role in the survival of Helicobacter pylori that contributes to different diseases, including peptic ulcer. Coagulansin-A is the steroidal lactone found in plants of solanaceae family such Withania coagulans. The current study was carried out to examine the in vitro urease, COX-2 inhibitory activity and effect on type II collagen expression of coagulansin-A. Moreover, we investigated cytotoxic effects on rabbit articular chondrocytes through MTT assay. COX-2 and type II collagen expressions were determined through a western blotting. Molecular docking and simulation studies of urease and COX-2 proteins were also performed as an in silico approach. Results showed that COX-2 expression was decreased dose dependably, significantly higher expression of type II collagen was observed at higher doses. In the current study coagulansin-A was found as non-toxic, and showed notable urease inhibitory activity in non-competitive manner with IC50 23.14 μM in comparison to reference drug thiourea 17.81 μM. Significant decrease in COX-2 and increase in type II collagen were observed as compared to control. In silico results unveiled the strong binding affinities of cagulansin-A with both of these urease and COX-2 proteins. Therefore, herein we proposed the significant antiurease potential of this compound that could be used in treating different diseases such as ulcers. Moreover, detailed in vivo studies and molecular mechanism based studies are suggested.This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-09T14:15:19.685364-05:
      DOI: 10.1002/cbdv.201700427
       
  • Tricalycoside, a New Cerebroside from Tricalysia coriacea (Rubiaceae)
    • Authors: Maurice D. Awouafack; Pierre Tane, Hiroyuki Morita
      Abstract: A new cerebroside, named as tricalycoside (1), was isolated from the CH2Cl2 / MeOH (1:1) extract of twigs and leaves of Tricalysia coriacea using repeated silica gel open column chromatography followed by Prep. TLC and Sephadex LH-20, together with six known compounds (2 - 7). The structure of the new compound was determined by analysis of 1D and 2D NMR, MS data, chemical conversion, and by comparison of these data with those from the literature. Tricalycoside (1) possessed a weak antibacterial activity against Klebsiella pneumoniae (MIC = 75 μg/mL).This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-08T20:15:31.701596-05:
      DOI: 10.1002/cbdv.201700472
       
  • Neuroprotective effects of butanol fraction of Cordyceps cicadae on
           glutamate-induced damage in PC12 cells involving oxidative toxicity
    • Authors: Dan Wang; Jibiao Wang, Dujun Wang, Xiaofeng Yu, Opeyemi Joshua Olatunji, Zhen Ouyang, Yuan Wei
      Abstract: The current study was aimed at investigating the neuroprotective effects of the butanol fraction from C. cicadae (CBU), which was responsible for the anti-aging effect of this medicine. Glutamate-induced PC12 cells were used as a model to determine the neuroprotective effect against oxidative cell death. Cell viability, cytotoxicity, flow cytometry, mitochondrial transmembrane potential (MMP), reactive oxygen species (ROS), glutathione peroxidase (GSH-Px) and superoxide dismutase (SOD) levels were analyzed to assess neuronal cell survival or death. The results obtained from the above evaluations showed that CBU was the most effective fraction and even better than pure compounds present in C. cicadae. in terms of suppressing glutamate-induced damage in PC12 cells, increasing cell viability, decreasing lactase dehydrogenase (LDH) release, and reduction of apoptosis induced by exposure to glutamate. Furthermore, CBU protected cells against mitochondrial dysfunction and oxidative stress as indicated by the suppression of ROS accumulation and up regulation of the levels of GSH-Px and SOD. In summary, the above results showed that CBU exerted neuroprotective effect against oxidative damage, and this activity could be partly due to the action of nucleosides present in the CBU.This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-07T18:55:31.423197-05:
      DOI: 10.1002/cbdv.201700385
       
  • Athenolide A, a New Steroidal Lactone from the Leaves of Athenaea martiana
           (Solanacea) Determined by means of HPLC-HRMS-SPE-NMR Analysis
    • Authors: Eder L. Silva; Rita C. Almeida-Lafetá, Ricardo M. Borges, Dan Staerk
      Abstract: Athenaea (Solanaceae) is an endemic genus belonging to the Brazilian Atlantic Rainforest. Recently, botanical investigations suggested the re-evaluation of the generic status of the genus Athenaea as a synonym of Aureliana. In this study, the first investigation of the Athenaea genus performed on Athenaea martiana by means of HPLC-HRMS-SPE-NMR combined with high-resolution radical scavenging profile led to identification of several phenolic acids as radical scavengers: protocatechuic acid (1), 4-hydroxybenzoic acid (2), caffeic acid (3), vanillic acid (4) and ferulic acid (6). Additional analysis revealed a new steroidal lactone, named athenolide A (9). Their structures were elucidated by extensive use of NMR spectroscopy as well as HRMS. Chemotaxonomic considerations based on these results supported the chemical relationships between the Athenaea and Aureliana genus, in agreement with the recent botanical findings.This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-01T21:21:10.841611-05:
      DOI: 10.1002/cbdv.201700455
       
  • Isolation and Antifouling activity of Azulene Derivatives from the
           Antarctic Gorgonian Acanthogorgia laxa
    • Authors: Laura P. Patiño C; Rodrigo Quintana Manfredi, Miriam Pérez, Mónica García, Guillermo Blustein, Ralf Cordeiro, Carlos D. Pérez, Laura Schejter, Jorge A. Palermo
      Abstract: Three azulenoid sesquiterpenes (1- 3) were isolated from the Antarctic gorgonian Acanthogorgia laxa collected by bottom trawls at –343 m. Besides linderazulene (1), and the known ketolactone 2, a new brominated C-16 linderazulene derivative (3) was also identified. This compound has an extra carbon atom at C-7 of the linderazulene framework. The antifouling activity of compounds 1 and 2 was assayed in the laboratory with Artemia salina larvae, and also in field tests, by incorporation in soluble-matrix experimental antifouling paints. The results obtained after a 45 days field trial of the paints, showed that compounds 1 and 2 displayed good antifouling potencies against a wide array of organisms. Compound 3, a benzylic bromide, was unstable and for this reason was not submitted to bioassays. Two known cembranolides: pukalide and epoxypukalide, were also identified as minor components of the extract.This article is protected by copyright. All rights reserved.
      PubDate: 2017-11-01T11:25:24.911784-05:
      DOI: 10.1002/cbdv.201700425
       
  • Phytochemical Investigation of Male and Female Hedyosmum scabrum (Ruiz &
           Pav.) Solms leaves from Ecuador
    • Authors: Claudia Herrera; Vladimir Morocho, Giovanni Vidari, Carlo Bicchi, Gianluca Gilardoni
      Abstract: This paper reports the chemical composition of the essential oils obtained by hydrodistillation of male and female H. scabrum fresh leaves. The essential oils, HSMO and HSFO, respectively, were analyzed by GC-MS and GC-FID. A total of 93 components were detected, accounting for 94.8% and 95.3% of HSMO and HSFO, respectively. The prevalent constituents of HSMO were pinocarvone (13.1%), D-germacren-4-ol (12.6%), 1,8-cineole (10.8%), α-pinene (6.4%), and β-pinene (4.8%), whereas the major components of HSFO were 1,8-cineole (20.5%), linalool (16.5%), α-pinene (15.0%), β-pinene (6.4%), and sabinene (6.3%). The different enantiomeric distribution of β-pinene, sabinene, limonene, linalool in the two oils, was determined. The non-volatile esters of p-coumaric and ferulic acids with borneol (1 and 4), cis-chrysanthenol (2 and 5), and cis-pinocarveol (3 and 6) were identified in the leaves after basic hydrolysis and analysis of the NMR spectra of the free acids, and GC-MS spectra of the monoterpene alcohols, respectively. Compounds 2, 3, 5, 6 have been found in nature for the first time. These findings demonstrated that, from a chemical point of view, male and female individuals of H. scabrum collected in Ecuador seem quite differentiated between each other and from samples of the same species growing in Bolivia and in Peru.This article is protected by copyright. All rights reserved.
      PubDate: 2017-10-31T07:05:24.301055-05:
      DOI: 10.1002/cbdv.201700423
       
  • Chemical Composition and Biological Investigations of Eryngium triquetrum
           Essential Oil from Algeria
    • Authors: Ali Medbouhi; Nadjiya Merad, Abdelmounaim Khadir, Mourad Bendahou, Nassim Djabou, Jean Costa, Alain Muselli
      Abstract: The chemical composition, antibacterial and antioxidant activities of the essential oil obtained from Eryngium triquetrum from Algeria were studied. The chemical composition of sample oils from 25 locations was investigated using GC-FID and GC/MS. Twenty-four components representing always more than 87% were identified in essential oils from total aerial parts of plants, stems, flowers and roots. Falcarinol is highly dominant in the essential oil from the roots (95.5%). The relative abundance of falcarinol in the aerial parts correlates with the phenological stages of the plant. Aerial parts of E. triquetrum produce an essential oil dominated by falcarinol during the early flowering stage, and then there is a decrease in falcarinol and rebalancing of octanal during the flowering stage. To our knowledge, the present study is the first report of the chemical composition of E. triquetrum essential oil. Evaluation of the antibacterial activity by means of the paper disc diffusion method and minimum inhibitory concentration (MIC) assays, showed a moderate efficiency of E. triquetrum essential oil. Using the DPPH method, the interesting antioxidant activity of E. triquetrum essential oil was established. These activities could be attributed to the dominance of falcarinol. The outcome of our literature search on the occurrence of falcarinol in essential oils suggests that E. triquetrum from Algeria could be considered as a possible source of natural falcarinol.This article is protected by copyright. All rights reserved.
      PubDate: 2017-10-30T09:30:24.140455-05:
      DOI: 10.1002/cbdv.201700343
       
  • Allelopathic activity and chemical composition of Rhynchosia minima (L.)
           DC. essential oil from Egypt
    • Authors: Ahmed M. Abd El-Gawad; Yasser A. El-Amier, Giuliano Bonanomi
      Abstract: Aromatic plants attract the attention of many researchers worldwide due to their worthy applications in agriculture, human prosperity, and the environment. Essential oil (EO) could be exploited as effective alternatives to synthetic compounds as it has several biological activities including allelopathy. The EO from the aerial parts of Rhynchosia minima was extracted by hydro-distillation and investigated by gas chromatography/mass spectrometry (GC-MS). Different concentrations (50, 100, 150 and 200 μL L−1) of the EO were prepared for investigation of their allelopathic potential on two weeds; Dactyloctenium aegyptium and Rumex dentatus. Twenty-eight compounds, mainly sesquiterpenes (69.13%) were determined. The major compounds are α-eudesmol, 2-allyl-5-t-butylhydroquinone, caryophyllene oxide, trans-caryophyllene, and .tau.-cadinol. The VOCs from the R. minima showed a significant inhibition of D. aegyptium and R. dentatus germination, while the seedling growth was stimulated. Therefore, it is not recommended to treat these noxious weeds with the EO of R. minima before the germination. In contrast, the apparent stimulatory effect on the seedling growth offers further studies to use the EO of R. minima to enhance the fitness of different economic crops. However, characterization of green bio-herbicides such as EO (allelochemicals) from wild plants raises a new opportunity for the incorporation of new technology of bio-control against the noxious weeds.This article is protected by copyright. All rights reserved.
      PubDate: 2017-10-24T08:50:27.141031-05:
      DOI: 10.1002/cbdv.201700438
       
  • Synthesis and characterization of the hemi-salen ligands and their
           
    • Authors: Ahmet Kilic; Ismail Koyuncu, Mustafa Durgun, Ismail Ozaslan, İbrahim Halil Kaya, Ataman Gönel
      Abstract: The synthesis, spectroscopic properties and in vitro cytotoxicity activity of a series of various salen-based triboron complexes have been designed and prepared from hemi-salen (L1H3-L4H3) ligands and BF3.Et2O or BPh3 under simple reaction conditions. The hemi-salen (L1H3-L4H3) ligands and their BF2 or BPh2 chelating triboron complexes were characterized by means of NMR (1H, 13C, 19F and 11B) spectra, FT-IR spectra, UV-Vis spectra, fluorescence spectra, mass spectra, melting point as well as elemental analysis. The triboron [L(1-4)(BF2)3] and [L(1-4)(BPh2)3] complexes were investigated for their absorption and emission properties and these complexes are also good chelates towards boron(III) fragments such as BF2 or BPh2 quantum yield in solution reaching up to 38%. The hemi-salen (L1H3-L4H3) ligands and their BF2 or BPh2 chelating triboron complexes were tested for the in vitro anticancer activity against various the cancer and normal cells (HeLa, DLD-1, ECC-1, PC-3, PNT-1A, and CRL-401O) and it was found that the cell viability of cancer cells was decreased while most of the healthy cells could still be viable. Also, the cytotoxicity studies showed that anti-cancer activity of hemi-salen (L1H3-L4H3) ligands is higher than that of triboron [L(1-4)(BF2)3] and [L(1-4)(BPh2)3] complexes. The hemi-salen (L1H3-L4H3) ligands showing the strongest cytotoxic effect in PC-3 cells were found to exhibit anticancer activity with apoptosis by increasing the level of ROS in the PC-3 cells.This article is protected by copyright. All rights reserved.
      PubDate: 2017-10-15T03:40:22.91368-05:0
      DOI: 10.1002/cbdv.201700428
       
  • Hispanane-type Diterpenoid and Secoiridoid Glucosides from Viburnum
           cylindricum
    • Authors: Li-Xia Wang; Yin-Dong Fang, Rui-Han Zhang, Fu-Cai Ren, Xing-Jie Zhang, Fei Wang, Wei-Lie Xiao
      Abstract: Three hitherto unknown compounds, including one new hispanane-type diterpenoid glucoside, namely viburnumoside (1), two new secoiridoid glucosides, 7α-galloyloxysweroside (2), and 7β-galloyloxysweroside (3), together with ten known compounds (4 – 13) were isolated from the ethanol extract of twigs and leaves of Viburnum cylindricum. Their structures were elucidated on the basis of extensive spectroscopic studies, and the absolute configuration of compound 1 was confirmed by the experimental and calculated electronic circular dichroism (ECD) data.This article is protected by copyright. All rights reserved.
      PubDate: 2017-10-15T03:35:23.679766-05:
      DOI: 10.1002/cbdv.201700418
       
  • Larvicidal activity of essential oils of five Apiaceae taxa and some of
           their main constituents against Culex quinquefasciatus
    • Authors: Roman Pavela; Filippo Maggi, Kevin Cianfaglione, Maurizio Bruno, Giovanni Benelli
      Abstract: Apiaceae are aromatic herbs producing essential oils which are used on an industrial scale for various purposes. Notably, Apiaceae essential oils may replace synthetic insecticides keeping most of their efficacy and avoiding environmental pollution and human poisoning. In the present work, we explored the insecticidal potential of the essential oils from five Apiaceae taxa, namely Sison amomum, Echinophora spinosa, Heracleum sphondylium subsp. sphondylium, Heracleum sphondylium subsp. ternatum and Trachyspemum ammi, as well as their major constituents (sabinene, p-cymene, terpinolene, myristicin and thymol), against the filariasis vector Culex quinquefasciatus. For the purpose, the essential oils were obtained by hydrodistillation and their composition was achieved by gas chromatography-mass spectrometry (GC-MS). Their acute toxicity on third instar larvae of Cx. quinquefasciatus was determined. The two most active essential oils were those from T. ammi fruits and E. spinosa roots, showing LC50 below 20 μl/l and LD90 below 50 μl/l. These oils were dominated by the monoterpene phenol thymol and the phenylpropanoid myristicin, respectively, which showed the strongest larvicidal activity (LC50 OF 15.1 and 16.3 μl/l, respectively) among the pure compounds tested. These results showed that Apiaceae may be useful as source of larvicidal compounds to be used for the development of cheap, effective and eco-friendly insecticidal formulations.
      PubDate: 2017-10-09T03:34:40.061731-05:
      DOI: 10.1002/cbdv.201700382
       
  • Is the profile of fatty acids, tocopherols and amino acids suitable to
           differentiate Pinus armandii suspicious to be responsible for the Pine Nut
           syndrome (PNS) from other Pinus species'
    • Authors: Bertrand Matthäus; Peiwu Li, Fei Ma, Haiyan Zhou, Jun Jiang, Mehmet Musa Özcan
      Abstract: Pinus armandii is suspicious to be responsible for the Pine Nut Syndrome, a long lasting bitter and metallic taste after the consumption of pine nuts. To find chemical characteristic features for the differentiation of P. armandii from other Pinus species 41 seed samples of the genus Pinus from 22 plant species were investigated regarding the content and the composition of fatty acids, tocopherols and amino acids. The predominant fatty acids in the seed oils were linoleic acid (35.2 – 58.2 g/100 g), oleic acid (14.6 – 48.5 g/100 g) and pinolenic acid (0.2 – 22.4 g/100 g, while the vitamin-E-active compounds were dominated by γ-tocopherol. The amino acid composition was mainly characterized by arginine and glutamic acid with amounts between 0.9 and 8.9 g/100 g as well as 2.1 g/100 g and 8.3 g/100 mg.On basis of this investigation a Principle Component Analysis has been used to identify most important components for the differentiation of P. armandii from other Pinus species. Using the data for glutamic acid, 20:2Δ5,11, 18:3Δ5,9,12, 18:1Δ9, and oil content a classification of the 41 samples into four different groups by cluster analysis was possible, but the characteristic features of P. armandii were too close to some other members of the genus Pinus making a clear differentiation of this species difficult. Nevertheless the investigation showed the similarities of different members of the genus Pinus with regard to fatty acids, vitamin-E-acitve compounds and amino acids.This article is protected by copyright. All rights reserved.
      PubDate: 2017-10-04T13:40:22.613569-05:
      DOI: 10.1002/cbdv.201700323
       
  • Synthesis of 8-Substituted 2′-Deoxyisoguanosines, via Unprotected
           8-Brominated 2-Amino-2′-deoxyadenosine
    • Authors: Wen Zhang; Qian Gao, Shuxian Wei, Bicheng Fu, Qian Yang, Xin Ming
      Abstract: A variety of applications of 8-alkynylated nucleosides has prompted the synthesis of new purine analogues. Bromination of unprotected 2-amino-2′-deoxyadenosine with Br2/AcOH/NaOAc gives 8-bromo-2-amino-2′-deoxyadenosine (87%). Brominated derivative is converted to 8-alkynylated 2-amino-2′-deoxyadenosines by palladium-catalyzed Sonogashira cross-coupling reaction via microwave assistance (81-95%). The resulting compounds are further transformed to 8-alkynylated 2′-deoxyisoguanosines (52-70%). The physical properties of new compounds are investigated.This article is protected by copyright. All rights reserved.
      PubDate: 2017-08-29T19:20:30.47873-05:0
      DOI: 10.1002/cbdv.201700335
       
  • The Cytochrome P450 Enzyme Responsible For The Production of
           Z-Norendoxifen In Vitro
    • Authors: Dabei Tang; Zhong Chu, Jessica Bo Li Lu, Jinzhong Liu, Qingyuan Zhang
      Abstract: BackgroundNorendoxifen, an active metabolite of tamoxifen, is a potent aromatase inhibitor. Little information is available regarding production of norendoxifen in vitro. Here, we conducted a series of kinetic and inhibition studies in human liver microsomes (HLMs) and expressed P450s to study the metabolic disposition of norendoxifen.MethodsTo validate that norendoxifen was the metabolite of endoxifen, metabolites in HLMs incubates of endoxifen were measured using a HPLC/MS/MS method. To further probe the specific isoforms involved in the metabolic route, endoxifen was incubated with recombinant P450s (CYP 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4, 3A5 and CYP4A11). Formation rates of norendoxifen were evaluated in the absence and presence of P450 isoform specific inhibitors using HLMs.ResultsThe peak of norendoxifen was found in the incubations consisting of endoxifen, HLMs and cofactors. The retention times of norendoxifen, Endoxifen and the internal standard (diphenhydramine) were 7.81, 7.97 and 5.86 min, respectively. The Km (app) and Vmax (app) values of norendoxifen formation from endoxifen in HLM was 47.8 μM and 35.39 pmol/min/mg. The apparent hepatic intrinsic clearances [Clint app] of norendoxifen formation were 0.74 μl/ mg × min. CYP3A5 and CYP2D6 were the major enzymes capable of norendoxifen formation from endoxifen with rates of 0.26 and 0.86 pmol/pmol P450×min. CYP1A2, 3A2, 2C9 and 2C19 also contributed to norendoxifen formation, but the contributions were at least 6-fold lower.1μM ketoconazole (CYP3A inhibitor) showed an inhibitory effect on rates of norendoxifen formation by 45%, but 1μM quinidine (CYP2D6 inhibitor) does not show an inhibitory effect.ConclusionNorendoxifen, metabolism from endoxifen by multiple P450s that including CYP3A5.This article is protected by copyright. All rights reserved.
      PubDate: 2017-08-17T11:10:21.360533-05:
      DOI: 10.1002/cbdv.201700287
       
  • Biocidal potential and chemical composition of industrial essential oils
           from Hyssopus officinalis, Lavandula x intermedia var. super and Santolina
           chamaecyparissus
    • Authors: Gonzalo Ortiz de Elguea-Culebras; Raúl Sánchez-Vioque, María Isabel Berruga, David Herraiz-Peñalver, Azucena González-Coloma, María Fé Andrés, Omar Santana-Méridas
      Abstract: This work presents the biocidal (insecticidal, ixodicidal, nematicidal and phytotoxic) effects and chemical compositions of three essential oils obtained from the industrial steam distillation (IEOs) of hyssop (Hyssopus officinalis L.), lavandin (Lavandula x intermedia or L. x hybrida var. Super) and cotton lavender (Santolina chamaecyparissus L.). Their chemical composition analyzed by gas chromatography coupled to mass spectrometry showed 1,8-cineole (53%) and β-pinene (16%) as the major components of H. officinalis, linalyl acetate (38%) and linalool (29%) of L. x intermedia; and 1,8-cineole (10%) and 8-methylene-3-oxatricyclo[5.2.0.0(2.4)]nonane (8%) in S. chamaecyparissus. The biocidal tests showed that L. x intermedia IEO was the most active against the insect Spodoptera littoralis and toxic to the tick Hyalomma lusitanicum, IEO of H. officinalis was strongly active against S. littoralis, and finally, S. chamaecyparissus IEO was a strong antifeedant against the aphid Rhopalosiphum padi, toxic to H. lusitanicum and with moderate effects against Leptinotarsa decemlineata, S. littoralis and Lolium perenne.This article is protected by copyright. All rights reserved.
      PubDate: 2017-08-12T03:05:21.380337-05:
      DOI: 10.1002/cbdv.201700313
       
  • Bioactive Pimarane-type Diterpenes from Marine Organisms
    • Authors: Xiaoli Wang; Haobing Yu, Yixin Zhang, Xiaoling Lu, Bin Wang, Xiaoyu Liu
      Abstract: Marine organisms represent an abundant sources of bioactive natural products with unique chemical structure. Pimarane diterpenes are a structurally diverse family of natural products with various biological activities and pharmacological properties. A prolific source of new marine-derived pimarane diterpenes have attracted considerable interest because of their unique structural diversity and varied biological activities, including antimicrobial, antitumor, and antiproliferative activities. This review provides a comprehensive overview of the structures, names, bioactivities, and references of 80 marine-derived pimarane-type natural products for the first time.This article is protected by copyright. All rights reserved.
      PubDate: 2017-07-24T03:00:22.261443-05:
      DOI: 10.1002/cbdv.201700276
       
 
 
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