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Planta Medica
Journal Prestige (SJR): 0.581

Citation Impact (citeScore): 2
Number of Followers: 4

Hybrid journal (It can contain Open Access articles)
ISSN (Print) 0032-0943 - ISSN (Online) 1439-0221
Published by Thieme Publishing Group

[233 journals]

Binary Synergistic Combinations of Lavender and Fennel Essential Oils with
Amoxicillin
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  Authors: Karadağ; Ayşe Esra, Çaşkurlu, Ayşegül, Demirci, Betül, Demirci, Fatih
  Abstract: Microbial resistance is an important problem in modern healthcare systems. In addition to drug resistance, the side effects of current antibiotic applications are also known issues. In this present study, binary combinations of amoxicillin with European Pharmacopoeia quality lavender (Lavandula angustifolia) and fennel (Foeniculum vulgare) essential oils were evaluated against human pathogenic microbial strains. The checkerboard method was used to quantify the efficacy of essential oils in combination with amoxicillin. As an initial result, remarkable in vitro antimicrobial activity was observed at relatively low amoxicillin concentrations using different oil combinations against Staphylococcus aureus ATCC 6538, Enterococcus faecalis ATCC 29212, Bacillus cereus ATCC 14579, and Escherichia coli NRRL B-3008, Salmonella typhi (Clinical isolate), respectively. Fractional inhibitory concentrations (FIC) were calculated and interpreted in terms of addition, synergy, antagonism, or indifferent, respectively. A synergistic interaction was shown for E. faecalis and E. coli with the combination F. vulgare essential oil and amoxicillin (FICI= 8.05 x 10-4). Both essential oils together, and in combination with amoxicillin showed a synergistic effect as well.
  Citation: Planta Med ; : -
  PubDate: 2022-09-28T16:24:42+01:00
  DOI: 10.1055/a-1891-1119
In Vitro and In Silico Evaluation of ACE2 and LOX Inhibitory Activity of
Origanum Essential Oils and Carvacrol
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  Authors: Demirci; Fatih, Terali, Kerem, Karadağ, Ayşe Esra, Biltekin, Sevde Nur, Ak Sakallı, Ezgi, Koşar, Müberra, Demirci, Betül, Baser, Kemal Husnu Can
  Abstract: Origanum spp. are used both for culinary purposes and for their biological activities. In this study, commercially Origanum majorana, O. minutiflorum, O. vulgare, and O. onites essential oils, and their prominent constituent carvacrol was evaluated for their in vitro and in silico angiotensin-converting enzyme 2 (ACE2) and lipoxygenase (LOX) enzyme inhibitory potentials. The essential oils were analysed by GC-FID and GC/MS, where carvacrol was identified as the major component (62–81%), confirming the quality. In vitro enzyme inhibition assays were conducted both with the essential oils (20 µg/mL) and with carvacrol (5 µg/mL). The comparative values of ACE2 percent inhibition for O. majorana, O. minutiflorum, O. vulgare and O. onites essential oils were determined as 85.5%, 79.1%, 74.3% and 42.8%, respectively. As a result of the enzyme assays, carvacrol showed 90.7% in vitro ACE2 inhibitory activity. The in vitro LOX inhibition of the essential oils (in the same order) was 89.4%, 78.9%, 81.1%, and 73.5%, respectively, where carvacrol showed 74.8% inhibition. In addition, protein–ligand docking, and interaction profiling was used to gain structural and mechanistic insights into the ACE2 and LOX inhibitory potentials of major Origanum essential oil constituents. The in silico findings agreed with the significant enzyme inhibition activity observed in vitro. Further in vivo studies are suggested to confirm the safety and efficacy of the oils.
  Citation: Planta Med ; : -
  PubDate: 2022-09-28T16:16:42+01:00
  DOI: 10.1055/a-1828-2479
Oligomeric Proanthocyanidin Complex from Avocado Seed as A Promising
α-glucosidase Inhibitor: Characteristics and Mechanisms
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  Authors: Nguyen; Thien Huu, Amen, Yhiya, Othman, Ahmed, Wang, Dongmei, Masako, Matsumoto, Maki, Nagata, Shimizu, Kuniyoshi
  Abstract: Although considered as an abundant source of agricultural by-products, avocado (Persea americana Mill.) seed, with several biological activities and bioactive components, might become a promising resource for phytopharmaceutical development. In this study, through bioassay-guided isolation of the main α-glucosidase inhibitors in avocado seed, we discovered the major α-glucosidase inhibitor to be avocado seed oligomeric proanthocyanidin complex (ASOPC). Thiolysis and UPLC-DAD-HRESIMS showed the presence of A- and B-type procyanidins, and B-type propelargonidin with (epi)afzelechin as extension unit. Mean degree of polymerization (mDP) of ASOPC was calculated as 7.3±1. Furthermore, ASOPC appeared to be a strong, reversible, competitive inhibitor of α-glucosidase, with IC50 value of 0.1 µg/mL, which was significantly lower than Acarbose (IC50 = 75.6 µg/mL), indicated that ASOPC is a potential natural α-glucosidase inhibitor. These findings would contribute to the direction of utilizing avocado seed bioactive components with the possibility to be used as natural anti-diabetic agents.
  Citation: Planta Med ; : -
  PubDate: 2022-09-28T15:41:35+01:00
  DOI: 10.1055/a-1878-3916
Extraction, Purification, Quantification, and Stability of Bioactive
Spilanthol from Acmella oleracea
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  Authors: Grymel; Mirosława, Mazurkiewicz, Roman, Bajkacz, Sylwia, Bilik, Janusz, Kowalczyk, Sławomir
  Abstract: Acmella oleracea is an ethnobotanically significant plant with a relatiwely high content of spilanthol. Due to its broad spectrum of activity, including anti-inflammatory, antioxidant, analgesic, antifungal, and bacteriostatic properties, it is considered a valuable bioactive natural product. In addition, spilanthol as its main bioactive component inhibits facial muscle contractions, making it an attractive ingredient in anti-wrinkle and anti-aging cosmetics. Due to its muscle paralyzing effects, it is called herbal botox. The commercial interest in spilanthol encourages the development of effective methods of isolating it from plant material. The methodology used in this paper allows for the obtaining of extracts from Acmella oleracea with a relatively high content of spilanthol. An effective method of spilanthol extraction from all aerial parts of Acmella oleracea as well as methods of enriching spilanthol concentration in extracts achieved by removing polar and acidic substances from crude extracts was developed. To quantify the concentration of spilanthol, a simple, fast and economically feasible quantification protocol that uses nuclear magnetic resonance (HNMR) was developed. In addition, it has been proven, that oxidation of spilanthol by air gives (2E,7Z)-6,9-endoperoxy-N-(2-methylpropyl)-2,7-decadienamide. The studies on spilanthol solutions stability were carried out and the conditions for the long-time storage of spilanthol solutions have also been developed. Additionally, for confirmation of obtained results a sensitive (LOQ=1 ng/mL), precise (RSD lower than 7%) and accurate (RE lower than 7.5%), new HPLC-MS/MS method was applied.
  Citation: Planta Med ; : -
  PubDate: 2022-08-31T15:25:38+01:00
  DOI: 10.1055/a-1903-2226
Natural Dibenzo[b,f]oxepines, Pacharin and Bauhiniastatin-1, Isolated from
Bauhinia acuruana Induce Apoptosis on Breast Cancer Cells via MCL-1
Protein Reduction
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  Authors: Souza; Silvia de Maria, Souza, Luciano Santos de, Silva, Valdenizia Rodrigues, Soares, Milena Botelho Pereira, Bezerra, Daniel Pereira, Gois, Roberto Wagner da Silva, Silva, Horlando Carlota da, Santiago, Gilvandete Maria Pinheiro, Militao, Gardenia Carmen Gadelha
  Abstract: Herein, we describe the antiproliferative effects of two natural dibenzo [b,f]oxepines, pacharin and bauhiniastatin-1, isolated from Bauhinia acuruana on a breast cancer cell line and the mode of action underlying the cytotoxicity. Both compounds were cytotoxic in a panel of six tumor lines analyzed by the MTT assay, and IC50 values ranged from 7.8 to 45.1 µM, including human breast adenocarcinoma (MCF-7) cells. In contrast, none of the compounds were cytotoxic on normal human peripheral blood mononuclear cells (IC50 > 100 µM). Human breast adenocarcinoma (MCF-7) cells treated with pacharin or bauhiniastatin-1 20 µM for 24 h presented a reduction in cell volume and intensification of chromatin condensation, DNA fragmentation, and apoptotic cells. These findings became more evident after 48 h of exposure. Antiapoptotic B-cell lymphoma-2 family members, such as myeloid cell leukemia-1 and B-cell lymphoma-extra large, are important targets in cancer cells since their overexpression confers resistance to cancer treatments. A significant reduction of the myeloid cell leukemia-1 protein levels in human breast adenocarcinoma (MCF-7) cells after 24 h of treatment with pacharin or bauhiniastatin-1 at 20 µM was observed, while the B-cell lymphoma-extra large protein content was reduced in bauhiniastatin-1-treated cells at 40 µM only. The cytotoxic effects of pacharin and bauhiniastatin-1 are likely linked to myeloid cell leukemia-1 inhibition, which leads to the apoptosis of breast adenocarcinoma cells.
  Citation: Planta Med ; : -
  PubDate: 2022-08-23T13:26:26+01:00
  DOI: 10.1055/a-1910-5776
Comparative Morpho-micrometric Investigations in Six Indigenous Ocimum
Species of India with DOE Based HPTLC Method for Multi-class Component
Analysis
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  Authors: Mirgal; Amit, Ghoshal, Sautik, Ghule, Chetana, Bhatt, Krishna, Patel, Kalpana, Girme, Aboli, Hingorani, Lal
  Abstract: The Ocimum genus is one of Indiaʼs prominent botanical classes of traditional medicinal culture comprising medicinally and agronomically important plants. Morphological resemblances, overlapping geographical distribution, and history of traditional nomenclature have necessitated a comprehensive qualitative report for effective quality control and removing the species ambiguity pertaining to this genus. This paper provides detailed morpho-micrometric characteristics used to differentiate between six indigenous Ocimum species of India. Among them, O. gratissimum was distinguished as the only shrub with a fleshy petiole. In green and purple forms, O. tenuiflorum leaves had serrate margins and showed no particular anatomical differences except for the anthocyanins containing epidermal cells of the latter. O. basilicum had glabrous leaves except for the veins, which were puberulous. O. filamentosum had tenuous anther filaments and was the least aromatic while O. africanum had a citrusy odour, which along with the number of xylary rows, size of mesophyll cells, and epidermal cell wall architecture, distinguished it from O. americanum. An HPTLC method was developed using experimental design and validated for quantification of multi-class compounds from terpenoic, phenolic acids, and flavonoids in Ocimum leaves. It was found linear (r 2 > 0.99) with recoveries between 95 – 100% for all compounds. The eluted bands of marker compounds were subjected to HPTLC-MS analysis as a confirmative tool. This is the first anatomical and analytical report of O. filamentosum Forssk. The obtained results could be effectively used for species identification using vegetative characters alone with the anatomical-HPTLC data backing up the former as a rapid and economical tool.
  Citation: Planta Med ; : -
  PubDate: 2022-08-22T13:24:31+01:00
  DOI: 10.1055/a-1876-3009
Placental Passage of Protopine in an Ex Vivo Human Perfusion System
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  Authors: Spiess; Deborah, Abegg, Vanessa Fabienne, Chauveau, Antoine, Treyer, Andrea, Reinehr, Michael, Oufir, Mouhssin, Duong, Elisa, Potterat, Olivier, Hamburger, Matthias, Simões-Wüst, Ana Paula
  Abstract: The placental passage of protopine was investigated with a human ex vivo placental perfusion model. The model was first validated with diazepam and citalopram, 2 compounds known to cross the placental barrier, and antipyrine as a positive control. All compounds were quantified by partially validated U(H)PLC-MS/MS bioanalytical methods. Protopine was transferred from the maternal to the fetal circuit, with a steady-state reached after 90 min. The study compound did not affect placental viability or functionality, as glucose consumption, lactate production, and beta-human chorionic gonadotropin, and leptin release remained constant. Histopathological evaluation of all placental specimens showed unremarkable, age-appropriate parenchymal maturation with no pathologic findings.
  Citation: Planta Med ; : -
  PubDate: 2022-08-22T13:19:39+01:00
  DOI: 10.1055/a-1829-9546
Icariin Improves Glucocorticoid Resistance in a Murine Model of Asthma
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  Authors: Jin; Hualiang, Zhou, Yan, Ye, Jian, Qiu, Chenhui, Jin, Weizhong, Wang, Limin
  Abstract: Icariin, a flavonoid glycoside isolated from Epimedium brevicornum, exerts a variety of biological activities. However, its effects on depression-induced glucocorticoid resistance in asthma and the underlying mechanisms have not been elucidated. In this study, a murine model of asthma with depression was established by exposure to ovalbumin combined with chronic unpredictable mild stress, and icariin was given orally during ovalbumin challenge and chronic unpredictable mild stress exposure. Depression-like behaviors were assessed by the open field test, forced swim test, and tail suspension test. The characteristic features of allergic asthma, including airway hyperreactivity, histopathology, inflammatory cytokine levels in bronchoalveolar lavage fluid, and immunoglobulin E and corticosterone levels in serum, were examined. Following splenocyte isolation in vitro, the inhibitory effects of corticosterone on the proliferation and cytokine secretion of splenocytes, glucocorticoid receptor DNA-binding activity, and expression of p-glucocorticoid receptor s226, glucocorticoid receptor α, and p-p38 mitogen-activated protein kinase in splenocytes were determined. We found that icariin had limited effects on depression-like behaviors, however, it markedly suppressed airway hyperresponsiveness, inflammatory infiltration in lung tissues, levels of interleukin-4, interleukin-5, and interleukin-6 in bronchoalveolar lavage fluid, and immunoglobulin E in serum. Furthermore, icariin improved the inhibitory effects of corticosterone on lipopolysaccharide-stimulated splenocytes, increased the glucocorticoid receptor expression and glucocorticoid receptor DNA-binding activity, and inhibited the phosphorylation of glucocorticoid receptors S226 and p38 mitogen-activated protein kinase. Taken together, icariin improved glucocorticoid resistance in a murine model of asthma with depression associated with enhancement of glucocorticoid receptor function and glucocorticoid receptor expression, and its effects on the glucocorticoid receptor function were related to decreased phosphorylation of glucocorticoid receptors S226 and p38 mitogen-activated protein kinase.
  Citation: Planta Med ; : -
  PubDate: 2022-08-22T13:08:37+01:00
  DOI: 10.1055/a-1902-4244
Herbal Products and Their Active Constituents Used Alone and in
Combination with Antibiotics against Multidrug-Resistant Bacteria
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  Authors: Herman; Anna, Herman, Andrzej P.
  Abstract: The purpose of this review is to summarize the current knowledge acquired on herbal products and their active constituents with antimicrobial activity used alone and in combination with antibiotics against multidrug-resistant bacteria. The most promising herbal products and active constituents used alone against multidrug-resistant bacteria are Piper betle (methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus, extended-spectrum beta-lactamase, Acinetobacter baumannii, Pseudomonas aeruginosa), Glycyrrhiza glabra (methicillin-resistant S. aureus, vancomycin-resistant Enterococcus, P. aeruginosa), and berberine (methicillin-resistant S. aureus, A. baumannii, P. aeruginosa), respectively. The synergistic effect of the combination of herbal products and their active constituents with antibiotics against multidrug-resistant bacteria are also described. These natural antibacterial agents can be promising sources of inhibitors, which can modulate antibiotic activity against multidrug-resistant bacteria, especially as efflux pump inhibitors. Other possible mechanisms of action of herbal therapy against multidrug-resistant bacteria including modification of the bacterial cell wall and/or membrane, inhibition of the cell division protein filamenting temperature sensitive Z-ring, and inhibition of protein synthesis and gene expression, all of which will also be discussed. Our review suggests that combination herbal therapy and antibiotics can be effectively used to expand the spectrum of their antimicrobial action. Therefore, combination therapy against multidrug-resistant bacteria may enable new choices for the treatment of infectious diseases and represents a potential area for future research.
  Citation: Planta Med ; : -
  PubDate: 2022-08-22T13:05:19+01:00
  DOI: 10.1055/a-1890-5559
Cytotoxic Polyprenylated Benzoylphloroglucinol Derivatives from the
Branches of Garcinia schomburgkiana
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  Authors: Kaennakam; Sutin, Sukandar, Edwin Risky, Rassamee, Kitiya, Siripong, Pongpun
  Abstract: Five undescribed polyprenylated benzoylphloroglucinol derivatives (1 – 5), named garschomcinols A – E, and five known analogues (6 – 10) were isolated from the branches of Garcinia schomburgkiana. Their structures were determined on the basis of 1D and 2D NMR and HRESIMS analyses. The absolute configuration of the bicyclo [3.3.1]nonane core structure of the polyprenylated benzoylphloroglucinols was assigned by comparison of its experimental electronic circular dichroism data with that of related compounds. All isolated compounds were evaluated for their cytotoxicity in vitro against five cancer cell lines. Compound 6 showed potent cytotoxicity against five cancer cell lines including KB, HeLa S3, HT-29, MCF-7, and Hep G2 with IC50 values in the range of 5.05 – 7.03 µM.
  Citation: Planta Med ; : -
  PubDate: 2022-07-28T16:40:12+01:00
  DOI: 10.1055/a-1841-0745
Potent anti-amoebic effects of Ibogaine, Voacangine and the root bark
alkaloid fraction of Tabernaemontana arborea.
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  Authors: Carrero; Julio César, Curay-Herrera, Violeta, Chacón-Niño, Lysette, Krengel, Felix, Guzmán-Gutiérrez, Silvia Laura, Silva-Miranda, Mayra, González-Ramírez, Luisa-Carolina, Bobes-Ruíz, Raúl, Espitia, Clara I., Reyes-Chilpa, Ricardo, Laclette, Juan Pedro
  Abstract: Plants of Tabernaemontana species have several pharmacological activities including antimicrobial effects. Amoebiasis continues to be a public health problem with increasing evidence of resistance to metronidazole. In this study we assessed the effect of the alkaloid fraction of T. arborea root bark and its alkaloids ibogaine and voacangine on the viability and infectivity of Entamoeba histolytica trophozoites. Cultures were exposed to 0.1-10 µg/mL for 24, 48 and 72 h, and then viability was determined using a tetrazolium dye reduction assay and type of cellular death analysed by flow cytometry. Results showed that the alkaloid fraction, but mainly ibogaine and voacangine alkaloids, exhibited potent dose-dependent anti-amoebic activity at 24h post-exposure (IC50 4.5 and 8.1 μM, respectively), comparable to metronidazole (IC50 6.8 μM). However, the effect decreased after 48 and 72 h of exposure to concentrations below 10 μg/mL, suggesting that the alkaloids probably were catabolized to less active derivatives by the trophozoites. The treatment of trophozoites with the IC50s for 24 h induced significant morphological changes in the trophozoites, slight increase in granularity, and death by apoptonecrosis. The capacity of T. arborea alkaloids to inhibit the development of amoebic liver abscesses in hamsters was evaluated. Results showed that even when the treatments reduced the number of amoebic trophozoites in tissue sections of livers, they were unable to limit the formation of abscesses, suggesting their rapid processing to inactive metabolites. This work leaves open the possibility of using Tabernaemontana alkaloids as a new alternative for amoebiasis control.
  Citation: Planta Med ; : -
  PubDate: 2022-07-22T15:38:33+01:00
  DOI: 10.1055/a-1809-1157
Discrimination of Zicao Samples Based on DNA Barcoding and HPTLC
Fingerprints, and Identification of
(22E)-Ergosta-4,6,8(14),22-tetraen-3-one As a Marker Compound
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  Authors: Kretschmer; Nadine, Durchschein, Christin, Heubl, Guenther, Pferschy-Wenzig, Eva-Maria, Kunert, Olaf, Bauer, Rudolf
  Abstract: The unambiguous identification of plant material is a prerequisite of rational phytotherapy. Misidentification can even cause serious health problems, as in the case of the Chinese medicinal herb Zicao. Commercial material labelled “Zicao” may be derived from the roots of Arnebia euchroma (ruan zicao), Lithospermum erythrorhizon (ying zicao), or Onosma paniculata (dian zicao). All of these roots contain shikonin derivatives as main bioactive constituents, but ying zicao and dian zicao contain also hepatotoxic pyrrolizidine alkaloids in high amounts. Therefore, the use of A. euchroma with a very low pyrrolizidine alkaloid content is desirable. Confusions of the species occur quite often, indicating an urgent need for an unambiguous identification method. Discrimination of 23 zicao samples has been achieved by analyses of the nuclear internal transcribed spacer ITS2 and trnL-F intergenic spacer of the chloroplast DNA. Data were analyzed using Bioedit, ClustalX, Mega 11 and BLAST. Results indicate that ITS2 barcoding can accurately distinguish Arnebia euchroma from their adulterants. Subsequently, an HPTLC method has been developed allowing a chemical discrimination of the most widely used species. (22E)-Ergosta-4,6,8(14),22-tetraen-3-one has been identified as characteristic marker compound, allowing an unambiguous discrimination of A. euchroma and L. erythrorhizon.
  Citation: Planta Med ; : -
  PubDate: 2022-07-22T15:33:15+01:00
  DOI: 10.1055/a-1855-1778
A New Triterpenoid Saponin from Albizia zygia Induced Apoptosis by
Reduction of Mitochondrial Potential Status in Malignant Melanoma Cells
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  Authors: Simo; Line Made, Messi, Lin Marcellin, Mbing, Joséphine Ngo, Muller, Christian D., Boyom, Fabrice Fekam, Begoudé, Aime-Didier Boyogueno, Pegnyemb, Dieudonné Emmanuel, Haddad, Mohamed, Noté, Olivier Placide
  Abstract: In our ongoing research program on the proapoptotic function of saponins, two previously undescribed saponins, named zygiaosides E (1) and F (2), were isolated from the leaves of Albizia zygia. Their structures were established based on extensive analysis of 1D and 2D NMR data, HR-ESI-MS analysis, and by chemical degradation. The proapoptotic effect of zygiaoside E (1) was evaluated on human malignant melanoma (A375), human epidermoid cancer (A431), and normal Homo sapiens skin tissue (TE 353.SK.) cell lines by cytometric analysis. Zygiaoside E (1) induced apoptosis of the two human cancer cell lines (A375 and A431) in a dose-dependent manner at 1 µM but did not induce apoptosis in noncancerous skin cells (TE 353.Sk), even when treated with concentrations up to 15 µM. The underlying mechanism of the apoptosis induction activity of zygiaoside E (1) on the mitochondrial membrane potential status in A375 cells was further assessed by monitoring the uptake rate of DiOC6, a mitochondrial specific and voltage-dependent fluorescent dye. The number of malignant melanoma cells emitting high fluorescence levels was decreased when cells were treated with 3 or 5 µM of zygiaoside E (1) during either 12 or 24 h, thereby revealing a drop of mitochondrial membrane potential in A375 cells upon treatment, which indicated mitochondrial perturbation.
  Citation: Planta Med ; : -
  PubDate: 2022-07-22T15:28:28+01:00
  DOI: 10.1055/a-1806-2692
Food Interactions Observed in a Pharmacokinetic Investigation Comparing
Two Marketed Cold Preparations (BNO1016 and ELOM-080) after Administration
to Beagle Dogs – A Pilot Study
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  Authors: Seibel; Jan, Neumann, Astrid, Müller, Anne, Wonnemann, Meinolf
  Abstract: Sinupret extract (BNO 1016) and Gelomyrtol forte (ELOM-080) represent the two top-selling cold remedies in Germany nowadays. Whereas BNO 1016 is a typical immediate release coated tablet, ELOM-080 is an enteric-coated soft gelatin capsule. The latter formulation, however, is at risk of pharmacokinetic interactions affecting absorption, especially in cases of concomitant food intake. In the present pilot study, we investigated the risk of a possible food effect in three male beagle dogs. Single doses of BNO 1016 and ELOM-80 were administered under fasting and fed conditions. Blood was sampled up to 30 h post-administration and plasma concentrations of the characteristic ingredients of BNO 1016 as well as ELOM-080 analytes were determined. Pharmacokinetic parameters focusing on the rate and extent of absorption were derived. BNO 1016 analytes demonstrated a similar course in both the fasted and fed states. ELOM-080 analytes also showed a similar picture in the fasted state. However, lag times (time from administration to first quantifiable time point in plasma) of up to 2 h post-administration with corresponding time to reach maximum concentration (obtained directly from the measured concentration) values of 3 to 4 h were observed, reflecting a longer gastric residence time. In the fed state, ELOM-080 showed significant pharmacokinetic characteristics, suggesting a clear food effect. A major observation was a double peak phenomenon that could be observed in two of three dogs. Furthermore, lag times of some analytes, up to 3 – 4 h, and corresponding time to reach maximum concentration values, up to 6 – 8 h, occurred. In contrast to BNO 1016, these findings suggest that, as with other enteric-coated formulations, there may also be a significant risk for food effects with ELOM-080 in humans.
  Citation: Planta Med ; : -
  PubDate: 2022-05-06T00:00:00+01:00
  DOI: 10.1055/a-1821-8690
In Vitro Investigation on the Effect of Dendrobine on the Activity of
Cytochrome P450 Enzymes
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  Authors: Wang; Zhiheng, Zhou, Kuilong, Liang, Zhijie, Zhang, Huiting, Song, Yangjie, Yang, Xiaomin, Xiang, Dongguo, Xie, Qingfan
  Abstract: Dendrobine is the major active ingredient of Dendrobium nobile, Dendrobium chrysotoxum, and Dendrobium fimbriatum, all of which are used in traditional Chinese medicine owing to their antitumor and anti-inflammation activities. Hence, investigation on the interaction of dendrobine with cytochrome P450 enzymes could provide a reference for the clinical application of Dendrobium. The effects of dendrobine on cytochrome P450 enzymes activities were investigated in the presence of 0, 2.5, 5, 10, 25, 50, and 100 µM dendrobine in pooled human liver microsomes. The specific inhibitors were employed as the positive control and the blank groups were set as the negative control. The Lineweaver-Burk plots were plotted to characterize the specific inhibition model and obtain the kinetic parameters. The study reveals that dendrobine significantly inhibited the activity of CYP3A4, 2C19, and 2D6 with IC50 values of 12.72, 10.84, and 15.47 µM, respectively. Moreover, the inhibition of CYP3A4 was found to be noncompetitive (Ki = 6.41 µM) and time dependent (KI = 2.541 µM−1, Kinact = 0.0452 min−1), while the inhibition of CYP2C19 and 2D6 was found to be competitive with the Ki values of 5.22 and 7.78 µM, respectively, and showed no time-dependent trends. The in vitro inhibitory effect of dendrobine implies the potential drug-drug interaction between dendrobine and CYP3A4-, 2C9-, and 2D6-metabolized drugs. Nonetheless, these findings need further in vivo validation.
  Citation: Planta Med ; : -
  PubDate: 2022-05-06T00:00:00+01:00
  DOI: 10.1055/a-1806-2935
The Role of Herbal Medicine in Cholangiocarcinoma Control: A Systematic
Review
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  Authors: Na-Bangchang; Kesara, Plengsuriyakarn, Tullayakorn, Karbwang, Juntra
  Abstract: The growing incidence of cholangiocarcinoma (bile duct cancer) and limited treatment options stimulate a pressing demand for research and the development of new chemotherapeutics against cholangiocarcinoma. This study aimed to systematically review herbs and herb-derived compounds or herbal formulations that have been investigated for their anti-cholangiocarcinoma potential. Systematic literature searches were conducted in three electronic databases: PubMed, ScienceDirect, and Scopus. One hundred and twenty-three research articles fulfilled the eligibility critera and were included in the analysis (68 herbs, isolated compounds and/or synthetic analogs, 9 herbal formulations, and 119 compounds that are commonly found in several plant species). The most investigated herbs were Atractylodes lancea (Thunb.) DC. (Compositae) and Curcuma longa L. (Zingiberaceae). Only A. lancea (Thunb.) DC. (Compositae) has undergone the full process of nonclinical and clinical development to deliver the final product for clinical use. The extracts of A. lancea (Thunb.) DC. (Compositae), Garcinia hanburyi Hook.f. (Clusiaceae), and Piper nigrum L. (Piperaceae) exhibit antiproliferative activities against human cholangiocarcinoma cells (IC50
  Citation: Planta Med ; : -
  PubDate: 2022-04-25T00:00:00+01:00
  DOI: 10.1055/a-1676-9678
Quality Requirements for Medicinal Cannabis and Respective Products in the
European Union – Status Quo
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  Authors: Veit; Markus
  Abstract: Medicinal cannabis and respective products have been available in EU member states as single-patient prescriptions without regular marketing authorizations for a couple of years. The Netherlands was the first member state to realize this; in the meantime other member states have followed. Today, aside from the Netherlands, Germany is the most important market for such products. The regulatory framework for the approval of medicinal cannabis and its distribution to patients in the EU member states is, however, not harmonized at all, and there are distinct national regulations. Regarding the quality of such products, the general requirements for herbal medicinal products as defined in the European Pharmacopoeia, national pharmacopoeias, and the EMA guidance documents in place beside GMP requirements in the EU are applicable. However, for a couple of aspects, every EU member state follows its own interpretation of these requirements. To facilitate free distribution of such products between EU member states in future and to harmonize requirements for quality and GMP, an EU-wide approach is needed. As a first step, this should be realized by implementing monographs for cannabis medicinal products in the European Pharmacopoeia.
  Citation: Planta Med ; : -
  PubDate: 2022-03-25T00:00:00+0100
  DOI: 10.1055/a-1808-9708
Morphinan Alkaloids from the Leaves of Alphonsea cylindrica and Their
Antibacterial Properties
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  Authors: Cho; Kin-Hau, Tan, Siow-Ping, Tan, Hui-Yin, Liew, Sook Yee, Nafiah, Mohd Azlan
  Abstract: A phytochemical study has been carried out on CH2Cl2 extract of Alphonsea cylindrica leaves, resulting in the isolation of three new morphinan alkaloids. They are kinomenine (1), N-methylkinomenine (2), and hydroxymethylkinomenine (3). The structures of these compounds were elucidated by extensive spectroscopic analysis (1D and 2D NMR, IR, UV, HRESIMS) and comparison with the data reported in literature for similar alkaloids. Kinomenine (1) and N-methylkinomenine (2) showed weak inhibition against S. aureus (MIC values of 1 and 2 = 500 µg/mL; pIC50 values in 95% C. I. of: 1 = 2.9 to 3.0; 2 = 2.9 to 3.1), while kinomenine (1) also showed weak inhibition against E. coli (MIC values of 1 = 500 µg/mL; pIC50 value in 95% C. I. of: 1 = 2.9) by broth microdilution method. The results obtained can be used as future referencefor the discovery of morphinans and the potential of A. cylindrica as an antibacterial source.
  Citation: Planta Med ; : -
  PubDate: 2022-03-14T00:00:00+0100
  DOI: 10.1055/a-1797-0548
Development and evaluation of khellin-loaded microemulgel for
dermatological applications
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  Authors: Grifoni; Lucia, Vanti, Giulia, vannucchi, Maria Giuliana, Bergonzi, Maria Camilla, BILIA, Anna Rita
  Abstract: Microemulsions are optically nanosized emulsions, isotropic and thermodynamically stable. They represent versatile drug delivery systems with high potential because can be administered through all routes. In the present study, we report on the formulation of a microemulsion made with glycerol (2.25%), Labrasol (20.25%) vitamin E acetate (2.50%), and water (75.00%), which was developed using the pseudo-ternary phase diagram. Globules of the microemulsion had PdI less than 0.25 and size of about 17 nm, evaluated by DLS analysis. These values did not change after loading khellin, a natural lipophilic molecules with interesting biological activities, used as a model of lipophilic drug. Carboxymethyl cellulose was selected as gelling polymer to obtain a microemulgel. Viscosity was 22,100.0±1555.6 mPas·s at 21±2°C, while it was 8,916.5±118.1 mPas·s at 35±2°C, remaining stable over time. Khellin recovery was 93.16±4.39% and it was unchanged after 4 weeks of storage (93.23±2.14%). The pH was 6.59±0.19 and it was found 6.42±0.34 at the end of the storage lifetime. The diffusion of khellin from the developed formulation was prolonged over an extended period. Based on overall results and due to the dermatological properties of the ingredients of the formulation, the developed microemulgel loaded with khellin is very promising and suitable for skin care applications.
  Citation: Planta Med ; : -
  PubDate: 2022-03-04T00:00:00+0100
  DOI: 10.1055/a-1789-3112
NO Release Inhibitory Activity of Flavonoids from Aesculus wilsonii Seeds
through MAPK (p38), NF-κB and STAT3 Cross-talk Signaling Pathways
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  Authors: Cao; Huina, Ruan, Jingya, Han, Yu, Zhao, Wei, Zhang, Ying, Gao, Chang, Wu, Honghua, Ma, Lin, Gao, Xiumei, Zhang, Yi, Wang, Tao
  Abstract: The flavonoid constituents of Aesculus wilsonii, a source of the Chinese medicinal drug Suo Luo Zi, and their in vitro anti-inflammatory effects were investigated. Fifteen flavonoids, including aeswilflavonosides IA–IC (1–3) and aeswilflavonosides IIA–IIE (4–8), along with seven known derivatives were isolated from a seed extract. Their structures were elucidated by extensive spectroscopic methods, acid and alkaline hydrolysis, and calculated electronic circular dichroism (ECD) spectra. Among them, compounds 3 and 7 possess a 5-[2-(carboxymethyl)-5-oxocyclopent-yl]pent-3-enylate or oleuropeoylate substituent, respectively, which are rarely reported in flavonoids. Compounds 2, 3, 7, and 1215 were found to inhibit lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cell lines. In a mechanistic assay, the flavonoid glycosides 2, 3, and 7 reduced the expressions of interleukin-6 (IL-6) and tumor necrosis factor (TNF-α) induced by LPS. Further investigations suggest that 2 and 3 down-regulate the protein expression of TNF-α and IL-6 by inhibiting the phosphorylation of p38. Compound 7 was found to reduce the production of inducible nitric oxide synthase (iNOS), and the secrection of TNF-α and IL-6 through inhibiting nuclear factor kappa-light-chain-enhancer of activated B (NF-κB) signaling pathway. Compounds 2, 3 and 7 possessed moderate inhibitory activity on the expression of signal transducer and activator of transcription 3 (STAT3). Taken together, the data indicate that the flavonoid glycosides of A. wilsonii seeds exhibit NO release inhibitory activity through mitogen-activated protein kinase (p38) [MAPK (p38)], NF-κB and STAT3 cross-talk signaling pathways.
  Citation: Planta Med ; : -
  PubDate: 2022-03-04T00:00:00+0100
  DOI: 10.1055/a-1789-2983
Berberine Regulates GPX4 to Inhibit Ferroptosis of Islet β Cells
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  Authors: Bao; Lei, Jin, Yixuan, Han, Jiani, Wang, Wanqiu, Qian, Lingling, Wu, Weiming
  Abstract: Ferroptosis, as a kind of non-apoptotic cell death, is involved in the pathogenesis of type 1 diabetes mellitus (T1DM). Islet B cells mainly produce insulin that is used to treat diabetes. Berberine (BBR) can ameliorate type 2 diabetes and insulin resistance in many ways. However, a few clues concerning the mechanism of BBR regulating ferroptosis of islet β cells in T1DM have been detected so far. We measured the effects of BBR and GPX4 on islet β cell viability and proliferation by MTT and colony formation assays. Western blot and qRT-PCR were utilized to examine GPX4 expression in islet β cells with distinct treatments. The influence of BBR and GPX4 on ferroptosis of islet β cells was investigated by evaluating the content of Fe2+ and reactive oxygen species (ROS) in cells. The mechanism of BBR targeting GPX4 to inhibit ferroptosis of islet β cells was further revealed by the rescue experiment. Our results showed that BBR and overexpression of GPX4 could notably accelerate cell viability and the proliferative abilities of islet β cells. Moreover, BBR stimulated GPX4 expression to reduce the content of Fe2+ and ROS, thereby repressing the ferroptosis of islet β cells, which functioned similarly as ferroptosis inhibitor Fer-1. In conclusion, BBR suppressed ferroptosis of islet β cells via promoting GPX4 expression, providing new insights into the mechanism of BBR for islet β cells.
  Citation: Planta Med 2022; :
  PubDate: 2022-11-09T11:44:31+0100
  DOI: 10.1055/a-1939-7417
  Issue No: Vol. Planta Me, No. Planta Medica Women (2022)
The therapeutic potential of salidroside for Parkinson’s disease
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  Authors: Li; Li, yao, wenlong
  Abstract: Parkinson’s disease (PD), a neurological disorder, is characterized by the progressive loss of dopaminergic (DA) neurons in the substantia nigra. Its incidence increases with age. Salidroside, a phenolic compound extracted from Sedum roseum, reportedly has multiple biological and pharmacological activities in the nervous system. However, its effects on PD remain unclear. In this review, we summarize the effects of salidroside on PD with regard to DA metabolism, neuronal protection, and glial activation. In addition, we summarize the susceptibility genes and their underlying mechanisms related to antioxidation, inflammation, and autophagy by regulating mitochondrial function, ubiquitin, and multiple signaling pathways involving NF-κB, mTOR, and PI3K/Akt. Although recent studies were based on animal and cellular experiments, this review provides evidence for further clinical utilization of salidroside for PD.
  Citation: Planta Med ; : -
  PubDate: 2022-11-21T11:16:15+0100
  DOI: 10.1055/a-1948-3179
  Issue No: Vol. eFirst

Unravelling the Chemotaxonomic Identity of “White” and “Black”
Oregano (Origanum vulgare) in Northern Greece

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Authors: Mertzanidis; Dimitrios, Nakas, Alexandros, Assimopoulou, Andreana N., Kokkini, Stella
Abstract: The two types of oregano used by the inhabitants of the villages of Μount Belles (GR1260001), the “white” oregano with white flowers and “black” oregano with purple flowers, were studied. The two oregano types were collected from five localities along an altitudinal gradient from 217 m up to 1299 m. “White” oregano, was found in the three lowland regions (up to 752 m) where the Pannonian-Balkanic turkey oak-sessile oak forest habitat (code 91M0) dominates. The “black” oregano was collected from the two higher altitudes, at 1177 m and 1299 m, where the Asperulo-Fagetum beech forest habitat (9130) occurs. Measurements of the density and size of peltate glandular hairs (sessile glands) on calyces, bracts, and leaves suggest that “white” oregano is distinguished by its conspicuous – apparently larger – glands. These differences were reflected in the total essential oil content, with the “white” oregano being much richer (up to 4.3 mL/100 g dry weight) than the “black” (up to 0.6%). Striking differences have also been found in the volatile fraction of their essential oil composition. The “white” oregano oils were characterized by the high content of carvacrol (up to 92.6% of identified peaks, by Headspace GC-MS). On the other hand, the two “black” oregano oils have a different aromatic profile, first reported from Greece, with main components including the sesquiterpenes β-caryophyllene, D-germacrene, δ-cadinene and β-bisabolene. The results so far indicate that “white” and “black” oregano, Origanum vulgare subsp. hirtum and subsp. vulgare respectively, can be clearly distinguished either by their morphological (glandular) differences or by chemical (essential oil) composition.
Citation: Planta Med ; : -
PubDate: 2022-11-20T16:55:11+0100
DOI: 10.1055/a-1949-8895
Issue No: Vol. eFirst

Metabolite Profiling of Swertia cincta Extract in Rats and
Pharmacokinetics Study of Three Bioactive Compounds Using UHPLC-MS/MS

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Authors: Ye; Xiaoyin, Zhang, Tong, Han, Han
Abstract: Swertia cincta, a plant of the genus Swertia in Gentianceae, has “heat-clearing” and detoxifying effects that normalize the gallbladder function in the treatment of jaundice. Although numerous studies on Swertia cincta have been performed, the absorption and pharmacokinetic behaviors remain unclear. In this study, the compounds of Swertia cincta in serum, bile, feces, and urine of rats were analyzed using a ultra-high-performance liquid chromatography-tandem mass spectrometry. A total of 9 prototype components and 48 metabolites were detected in biological samples. Furthermore, we determined the main components absorbed in the blood of Swertia cincta and established a method for simultaneously determining these components (sweroside, swertiamarin, and gentiopicroside) in positive ionization mode within 6 min. The quantitative method was successfully applied for the multiple-component pharmacokinetic study of Swertia cincta.
Citation: Planta Med ; : -
PubDate: 2022-11-20T16:55:07+0100
DOI: 10.1055/a-1942-5504
Issue No: Vol. eFirst

The Use of Herbal Medicine in the Treatment of Vitiligo: An Updated Review

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Authors: Castillo; Encarna, González-Rosende, María Eugenia, Martínez-Solís, Isabel
Abstract: Vitiligo is a chronic disease of unknown etiology that causes progressive cutaneous depigmentation. Current pharmacological treatments have limited success and present significant risks. Many efforts have been made in recent years to explore new anti-vitiligo therapeutic strategies, including herbal-based therapies. The objective of the present review is to provide an updated overview on the most frequently used medicinal plants in the treatment of vitiligo. A bibliographical search was carried out in scientific databases Pubmed, Scifinder, Scopus, Google Scholar, and Medline up to October 2021 using the descriptors vitiligo, herbal, medicinal plants, and alternative therapies. In our search, the highest number of published studies comprise plants commonly used in traditional herbal medicine, highlighting the usefulness of ethnopharmacology in the discovery of new therapeutic agents. The review outlines current understanding and provides an insight into the role of psoralens and khellin (photosensitizing agents obtained from plants such as Cullen corylifolium or Ammi visnaga). The paper also describes other traditional herbs such as Ginkgo biloba, Phlebodium aureum, Piper nigrum, Picrorhiza kurroa, and Baccharoides anthelmintica that can likewise act as potential therapeutical agents. Based on our findings, photosensitizing agents in combination with phototherapy, the association of oral Phebodium aureum with phototherapies as well as oral G. biloba in monotherapy showed greater scientific evidence as therapeutic options. The research results emphasize that further investigation in this area is merited. More long-term follow up clinical trials and higher quality randomized trials are needed.
Citation: Planta Med ; : -
PubDate: 2022-11-15T09:40:19+0100
DOI: 10.1055/a-1855-1839
Issue No: Vol. eFirst

Identification of Nrf2 Activators from the Roots of Valeriana officinalis

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Authors: Afzal; Sualiha, Zhou, Xian, Or, King, Raju, Ritesh, Münch, Gerald
Abstract: Various age-related chronic diseases have been linked to oxidative stress. The cellular antioxidant response pathway is regulated by the transcription factor nuclear erythroid factor 2. Therefore, plant-derived nuclear erythroid factor 2 activators might be useful therapeutics to stimulate the bodyʼs defense mechanisms. Our study focused on the discovery of potent nuclear erythroid factor 2 activators from medicinal plants. Initially, a variety of medicinal plant extracts were screened for nuclear erythroid factor 2 activity using a nuclear erythroid factor 2 luciferase reporter cell line. Among these, Valerian (Valeriana officinalis) root was identified as a potent candidate. Sequential extraction and bioassay-guided fractionation led to the isolation of four nuclear erythroid factor 2-active compounds, which were structurally identified by NMR and LC/HRMS as the known compounds isovaltrate, valtrate, jatamanvaltrate-P, and valerenic acid. These four compounds were then tested in relevant biological assays. Firstly, their effects on the expression of glutathione S-transferase, glutamate–cysteine ligase catalytic subunit, glutathione peroxidase, and heme oxygenase 1 were determined in HepG2 cells. Glutathione S-transferase P1 and glutamate–cysteine ligase catalytic subunit were upregulated by isovaltrate, valtrate, and jatamanvaltrate-P, while heme oxygenase 1 was upregulated by isovaltrate, jatamanvaltrate-P, and valerenic acid. The four compounds also increased the levels of glutathione and its metabolite, CysGly. As glutathione aids in the detoxification of hydrogen peroxide, cytoprotective effects of these four nuclear erythroid factor 2 activators against hydrogen peroxide toxicity were investigated, and indeed, the compounds significantly improved cell survival. This study provides evidence that four valepotriates from the roots of V. officinalis are activators of nuclear erythroid factor 2-mediated antioxidant and detoxification pathways. Our data might expand the medical use of this plant beyond its current application as a sleep aid.
Citation: Planta Med ; : -
PubDate: 2022-11-15T09:35:22+0100
DOI: 10.1055/a-1887-2016
Issue No: Vol. eFirst

Scutellaria baicalensis Pith-decayed Root Inhibits Macrophage-related
Inflammation Through the NF-κB/NLRP3 Pathway to Alleviate LPS-induced
Acute Lung Injury

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Authors: Zhang; Fanglei, Ke, Chang, Zhou, Zhongshi, Xu, Kang, Wang, Yan, Liu, Yanju, Tu, Jiyuan
Abstract: Acute lung injury (ALI) is one of the representative “lung heat syndromes” in traditional Chinese medicine (TCM). Scutellaria baicalensis is an herbal medicine used in TCM for treating lung diseases, due to its remarkable anti-inflammatory and antiviral effects. When used in TCM, S. baicalensis root is divided into two categories: S. baicalensis pith-not-decayed root (SN) and S. baicalensis pith-decayed root (SD). Compared to SN, SD has a better effect on lung diseases. We constructed a lipopolysaccharide (LPS)-induced acute lung injury (ALI) mouse model to study the pharmacodynamic mechanism of SD. The ethanolic extract of Scutellaria baicalensis pith-decayed root (EESD) significantly affected LPS-induced ALI by reducing alveolar interstitial thickening, pulmonary edema, and other pathological symptoms, decreasing the infiltration of inflammatory cells, especially macrophages, and inhibiting IL-1β, TNF-α, and IL-6 transcription and translation. Furthermore, in the THP-1 macrophage model induced by LPS, EESD inhibited the expression of phosphorylated nuclear factor inhibitory protein alpha (p-IκBα), phosphorylated nuclear factor-κB P65 (p-p65), cleaved-caspase-1, cleaved-IL-1β protein, and the release of inflammatory factors in the NF-κB/NLRP3 pathway, inhibiting macrophage function. In vivo experiments yielded similar results. Therefore, the present study clarified the potential of EESD in the treatment of ALI and revealed its potential pharmacodynamic mechanism by inhibiting the NF-κB/NLRP3 inflammasome pathway and suppressing the pro-inflammatory phenotype activation of lung tissue macrophages.
Citation: Planta Med ; : -
PubDate: 2022-11-07T13:18:30+0100
DOI: 10.1055/a-1878-5704
Issue No: Vol. eFirst

Prevention of Dental Biofilm Formation with Polyphenols: A Systematic
Review

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Authors: Schestakow; Anton, Meyer-Probst, Clara Theres, Hannig, Christian, Hannig, Matthias
Abstract: Polyphenols are plant secondary products with health-promoting properties against various degenerative or infectious diseases, and thus may help in the prevention of oral diseases. The aim of the present systematic review was to investigate polyphenols as a possible adjuvant in inhibiting dental biofilm formation, which is an important precondition for the most prevalent oral disease – caries and periodontitis. A literature search was conducted using the databases PubMed, CENTRAL and Scopus. Only studies with oral healthy participants and plaque level as outcome were included. Data search and extraction was conducted by two authors independently. Of the 211 initially identified studies, only six met all inclusion criteria. Meta-analysis was performed with five studies using the random effect model. Treatment with polyphenols reduced the plaque level in comparison to a negative control, but not significantly. Strong evidence of heterogeneity was observed. The diversity and complexity of polyphenols and their preparation need to be considered. There is no clear evidence that clinical use of polyphenols can prevent dental biofilm formation. Additional research with more and larger randomized controlled trials are required.
Citation: Planta Med ; : -
PubDate: 2022-11-07T13:14:08+0100
DOI: 10.1055/a-1939-7615
Issue No: Vol. eFirst

Green Tea Catechol (−)-Epigallocatechin Gallate (EGCG) Conjugated with
Phenylalanine Shows Enhanced Autophagy Stimulating Activity in Human
Aortic Endothelial Cells

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Authors: Lee; Taegum, Oh, Yeonji, Kim, Mi Kyoung, Chong, Youhoon
Abstract: (−)-Epigallocatechin gallate (EGCG) is one of the autophagy stimulators that have been reported to protect vascular endothelial cells from oxidative stress-induced damage. In this study, we attempted potentiation of the autophagy-stimulating activity of EGCG in human aortic epithelial cells (HAECs) by using the EGCG-phenylalanine conjugate, E10. Autophagy-stimulating activity of E10 was evaluated by LC3-II measurement in the absence and presence of the lysosomal blocker chloroquine, CTYO-ID staining, and reporter assay using tandem fluorescence-tagged LC3. These experiments revealed significantly enhanced autophagic flux stimulation in HAECs by E10 compared with EGCG. Further elaboration of E10 showed that activation of AMPK through phosphorylation as the major mechanism of its autophagy stimulation. Like other autophagy stimulators, E10 protected HAECs from lipotoxicity as well as accompanying endothelial senescence. Finally, stimulation of autophagy by E10 was shown to protect HAECs from oxidative stress-induced apoptosis. These findings collectively suggest potential clinical implications of E10 for various cardiovascular complications through stimulation of autophagy.
Citation: Planta Med ; : -
PubDate: 2022-11-07T13:11:14+0100
DOI: 10.1055/a-1948-4290
Issue No: Vol. eFirst

Acrotrione B, a Prenylated and Highly Oxidized Xanthenoid with
Antibacterial and Anti-proliferative Activities from the Roots of
Acronychia pedunculata

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Authors: Wisetsai; Awat, Lekphrom, Ratsami, Suebrasri, Thanapat, Tontapha, Sarawut, Senawong, Thanaset, Pudhom, Khanitha, Choodej, Siwattra, Schevenels, Florian T.
Abstract: A new prenylated xanthenoid with a highly oxidized core, acrotrione B (1), together with six previously reported acetophenones (2 – 7), were isolated from the roots of Acronychia pedunculata. The structures of the isolated compounds were elucidated by thorough analysis of their 1D and 2D NMR spectroscopic data. The relative and absolute configurations of acrotrione B were determined by electronic circular dichroism (ECD) calculations. Acrotrione B is an unusual, oxidized xanthenoid with a cyclohexadienone core that has not been previously reported. It thus represents a new skeletal type within the xanthenoid class. Acrotrione B (1) exhibited anti-proliferative activity against Hela (IC50 = 16.0 µM) and A549 (IC50 = 16.3 µM) cell lines. 5′-Prenylacrovestone (4) and acrovestone (5) were even more potent with IC50 values of 5.1 µM and 0.77 µM, respectively, against Hela cells and 11.8 µM and 1.13 µM, respectively, against A549 cells. Moreover, acrotrione B (1) displayed moderate antibacterial activities against Staphylococcus aureus, Bacillus cereus, and Bacillus subtilis, with MIC values in the range of 16 – 64 µg/mL. Finally, acropyrone (6) showed a significant suppression of lipopolysaccharide (LPS) induced NO production in murine macrophage J774.A1 cells (IC50 = 8.9 µM).
Citation: Planta Med ; : -
PubDate: 2022-10-27T09:02:22+01:00
DOI: 10.1055/a-1953-0479
Issue No: Vol. eFirst

A flavonoid-rich Zuccagnia punctata extract prevents high fat diet-induced
normal weight obesity in a rabbit model

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Authors: Valoy; Agostina, Alarcon, Gabriela, Roco, Julieta, Zampini, Catiana, Isla, Maria Ines, Jerez, Susana Josefina
Abstract: Oral administration of rich in flavonoids hydroalcoholic extract from Zuccagnia punctata (ZpE) improves lipid profile and prevents vascular dysfunction in hypercholesterolemic rabbits. This study aimed to evaluate the ability of ZpE to prevent metabolic and vascular alterations induced by high fat diet (HFD) on a metabolically obese and normal weight rabbit model. The major components of ZpE were analyzed by HPLC method. Rabbits were separated into six groups: 1-fed on standard chow (CD); 2-fed on HFD; 3, 4, 5- fed on HFD and orally administrated 2.5 mg, 5 mg or 10 mg GAE/day of ZpE, respectively (ZpE- HFD); 6- fed on HFD and orally administrated administered 30 mg orlistat/day (Or-HFD). All diets were administrated by 6 weeks. The major compounds of ZpE identified were chalcones: 2′,4′-dihydroxy-3′-methoxychalcone and 2′,4′-dihydroxychalcone. Oral treatment with ZpE 5 mg GAE/day as well as orlistat prevented the HFD-induced increase of triglycerides, fasting glucose, intraperitoneal glucose test, white cells, and TyG index. Acetylcholine relaxation was reduced in arteries from HFD group and oral administration of ZpE reached this response to CD values. Contractile response to angiotensin II was lower in arteries from rabbits fed on HFD treated with ZpE 5 and 10 mg GAE/day than those of untreated rabbits. Moreover, ZpE could inhibit the activity of pancreatic lipase in vitro and in vivo. In conclusion the ZpE may prevent normal weight obesity by inhibiting the pancreatic lipase. Thus, the use of ZpE as a natural product in the prevention of metabolic syndrome and endothelial dysfunction is very promising
Citation: Planta Med ; : -
PubDate: 2022-10-27T08:57:42+01:00
DOI: 10.1055/a-1891-3588
Issue No: Vol. eFirst

PET Imaging and Neurohistochemistry Reveal that Curcumin Attenuates Brain
Hypometabolism and Hippocampal Damage Induced by Status Epilepticus in
Rats

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Authors: Slowing; Karla, Gomez, Francisca, Delgado, Mercedes, Fernández de la Rosa, Rubén, Hernández-Martín, Nira, Pozo, Miguel Ángel, García-García, Luis
Abstract: Numerous preclinical studies provide evidence that curcumin, a polyphenolic phytochemical extracted from Curcuma longa (turmeric) has neuroprotective, anti-inflammatory and antioxidant properties against various neurological disorders. Curcumin neuroprotective effects have been reported in different animal models of epilepsy, but its potential effect attenuating brain glucose hypometabolism, considered as an early marker of epileptogenesis that occurs during the silent period following status epilepticus (SE), still has not been addressed. To this end, we used the lithium-pilocarpine rat model to induce SE. Curcumin was administered orally (300 mg/kg/day, for 17 days). Brain glucose metabolism was evaluated in vivo by 2-deoxy-2-[18F]Fluoro-D-Glucose ([18F]FDG) positron emission tomography (PET). In addition, hippocampal integrity, neurodegeneration, microglia-mediated neuroinflammation, and reactive astrogliosis were evaluated as markers of brain damage. SE resulted in brain glucose hypometabolism accompanied by body weight (BW) loss, hippocampal neuronal damage, and neuroinflammation. Curcumin did not reduce the latency time to the SE onset, nor the mortality rate associated with SE. Nevertheless, it reduced the number of seizures, and in the surviving rats, curcumin protected BW and attenuated the short-term glucose brain hypometabolism as well as the signs of neuronal damage and neuroinflammation induced by the SE. Overall, our results support the potential adaptogen-like effects of curcumin attenuating key features of SE-induced brain damage.
Citation: Planta Med ; : -
PubDate: 2022-10-27T08:52:49+01:00
DOI: 10.1055/a-1948-4378
Issue No: Vol. eFirst

Anti-adipogenic effects of sulforaphane-rich ingredient with broccoli
sprout and mustard seed in 3T3-L1 preadipocytes

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Authors: Men; Xiao, Han, Xionggao, Lee, Se-Jeong, Park, Keun-Tae, Han, Jong-Kwon, Choi, Sun-Il, Lee, Ok-Hwan
Abstract: Glucoraphanin (GRA) is a precursor of sulforaphane (SFN), which can be synthesized by the enzyme myrosinase. In this study, we developed and validated HPLC analytical methods for the determination of GRA and SFN in mustard seed powder (MSP), broccoli sprout powder (BSP), and the MSP-BSP mixture powder (MBP) and evaluated their anti- adipogenic effects in 3T3-L1 adipocytes. We found that the analysis methods were suitable for the determination of GRA and SFN in MSP, BSP, and MBP. The content of GRA in BSP was 131.11±1.84 μmol/g, and the content of SFN in MBP was 162.29±1.24 μmol/g. In addition, BSP and MBP effectively decreased lipid accumulation content without any cytotoxicity. Both BSP and MBP can significantly inhibited the expression of adipogenic proteins and increased the expression of proteins related to lipolysis and lipid metabolism. BSP and MBP inhibited the expression of adipocyte protein 2 (aP2), CCAAT/enhancer-binding protein-α (C/EBP-α), and peroxisome proliferator-activated receptor-γ (PPAR-γ) in 3T3-L1 adipocytes and inhibited the expression of fatty acid synthase (FAS) through AMP-activated protein kinase (AMPK). Meanwhile, BSP and MBP also increased the expression of the lipolysis-related proteins uncoupling protein-1 (UCP-1) and carnitine palmitoyltransferase-1 (CPT-1). Moreover, MBP exert anti-adipogenic to a greater extent than BSP in 3T3-L1 preadipocytes.
Citation: Planta Med ; : -
PubDate: 2022-10-11T14:15:47+01:00
DOI: 10.1055/a-1853-7101
Issue No: Vol. eFirst

Neuroprotective Properties of Chlorogenic Acid and 4,5-Caffeoylquinic Acid
from Brazilian arnica (Lychnophora ericoides) after Acute Retinal Ischemia

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Authors: Liberato; José Luiz, Rosa, Marcela Nunes, Miranda, Matheus C. Romeiro, Lopes, João Luís Callegari, Lopes, Norberto Peporine, Gobbo-Neto, Leonardo, Fontana, Andreia C. K., dos Santos, Wagner Ferreira
Abstract: Lychnophora is a genus of South American flowering plants in the daisy family, popularly known as “Brazilian arnica”. It is used in traditional medicine as an anti-inflammatory and analgesic agent, whose active components are derived from chlorogenic acid (CGA) and C-flavonoids. Since the drugs currently used are ineffective to treat glaucoma, agents with antioxidant and anti-inflammatory properties may represent new alternatives in preventing cellular lesions in retinal ischemia. In this study, we report the neuroprotective effects of CGA and 4,5-di-O-[E]-caffeoylquinic (CQA) acid, isolated from Lychnophora plants, in a rodent glaucoma model. Wistar rats were administered intravitreally with 10 µg CGA or CGA, and then subjected to acute retinal ischemia (ISC) by increasing intraocular pressure (IPO) for 45 minutes followed (or not) by 15 minutes of reperfusion (I/R). Qualitative and quantitative analyses of neurodegeneration were performed using hematoxylin-eosin or Fluoro-Jade C staining protocols. All retinas submitted to ISC or I/R exhibited matrix disorganization, pyknotic nuclei, and pronounced vacuolization of the cytoplasm in the ganglion cell layer (GCL) and inner nuclear layer (INL). Pretreatment with CGA or CQA resulted in the protection of the retinal layers against matrix disorganization and a reduction in the number of vacuolized cells and pyknotic nuclei. Also, pretreatment with CGA or CQA resulted in a significant reduction in neuronal death in the GCL, the INL, and the outer nuclear layer (ONL) after ischemic insult. Our study demonstrated that CGA and CQA exhibit neuroprotective activities in retinas subjected to ISC and I/R induced by IPO in Wistar rats.
Citation: Planta Med ; : -
PubDate: 2022-10-11T14:11:07+01:00
DOI: 10.1055/a-1903-2387
Issue No: Vol. eFirst

Microstructured Polymer System Containing Proanthocyanidin-Enriched
Extract from Limonium brasiliense as a Prophylaxis Strategy to Prevent
Recurrence of Porphyromonas gingivalis

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Authors: Pilatti; Fernanda, Isolani, Raquel, Valone, Larissa, de Paula, Mariana Nascimento, Caleare, Angelo de Oliveira, Ferreira, Sabrina Barbosa de Souza, Bruschi, Marcos Luciano, de Medeiros Araújo, Daniela Cristina, Guedes, Terezinha Aparecida, Hensel, Andreas, de Mello, João Carlos Palazzo
Abstract: Periodontal diseases are a global oral health problem affecting almost 10% of the global population. Porphyromonas gingivalis is one of the main bacteria involved in the initiation and progression of inflammatory processes as a result of the action of the cysteine proteases lysin- and arginine-gingipain. Surelease/polycarbophil microparticles containing a lyophilized proanthocyanidin-enriched fraction from the rhizomes of Limonium brasiliense, traditionally named “baicuru” (ethyl acetate fraction), were manufactured. The ethyl acetate fraction was characterized by UHPLC by the presence of samarangenins A and B (12.10 ± 0.07 and 21.05 ± 0.44%, respectively) and epigallocatechin-3-O-gallate (13.44 ± 0.27%). Physiochemical aspects of Surelease/polycarbophil microparticles were characterized concerning particle size, zeta potential, entrapment efficiency, ethyl acetate fraction release, and mucoadhesion. Additionally, the presence of the ethyl acetate fraction-loaded microparticles was performed concerning potential influence on viability of human buccal KB cells, P. gingivalis adhesion to KB cells, gingipain activity, and P. gingivalis biofilm formation. In general, all Surelease/polycarbophil microparticles tested showed strong adhesion to porcine cheek mucosa (93.1 ± 4.2% in a 30-min test), associated with a prolonged release of the ethyl acetate fraction (up to 16.5 ± 0.8% in 24 h). Preincubation of KB cells with Surelease/polycarbophil microparticles (25 µg/mL) resulted in an up to 93 ± 2% reduced infection rate by P. gingivalis. Decreased activity of the P. gingivalis-specific virulence factors lysin- and arginine-gingipain proteases by Surelease/polycarbophil microparticles was confirmed. Surelease/polycarbophil microparticles decreased biofilm formation of P. gingivalis (97 ± 2% at 60 µg/mL). Results from this study prove the promising activity of Surelease/polycarbophil microparticles containing ethyl acetate fraction microparticles as a prophylaxis strategy to prevent the recurrence of P. gingivalis.
Citation: Planta Med ; : -
PubDate: 2022-09-28T16:20:08+01:00
DOI: 10.1055/a-1858-6898
Issue No: Vol. eFirst

A Systematic Review of the Potential Effects of Propolis Extracts on
Experimentally-induced Diabetes

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Authors: Cunha; Gustavo Aparecido da, Carlstrom, Paulo Fernando, Franchin, Marcelo, Alencar, Severino Matias, Ikegaki, Masaharu, Rosalen, Pedro Luiz
Abstract: Oxidative stress (OS) is involved in the development of diabetes mellitus (DM) and its complications. Thus, OS reduction may be an important strategy for DM therapy. Propolis is bee resins with high antioxidant activity and is used in the treatment of different diseases, including DM. Therefore, in this systematic review, we evaluated the impact of propolis administration in diabetic animals. We used the PRISMA strategy to collect preclinical studies published in English up to November 2021 in three databases (PubMed/Medline, Scopus, and Web of Science). We used the SYRCLE tool to analyze the risk of methodological bias. Our primary search returned 198 studies, of which 14 were considered eligible to be included in this review. The administration of propolis induced a hypoglycemic effect in the treated animals, which is probably due to the reduction of OS. The animals showed restoration of endogenous antioxidant defenses and reduced levels of markers for OS. The administration of propolis resulted in improvement in the lipid profile of treated animals. Our risk of bias assessment showed a methodological quality score of less than 30% due to a lack of randomization, blinding, and proper allocation of animals. Heterogeneity in treatments, lack of results, and use of non-standard extracts are limitations in our data analysis. Despite these limitations, propolis induced a significant hypoglycemic effect in diabetic animals when compared to untreated controls. This effect was associated with a reduction in OS, a process mediated by ROS neutralization and restoration of endogenous antioxidant defenses.
Citation: Planta Med ; : -
PubDate: 2022-09-28T16:08:12+01:00
DOI: 10.1055/a-1910-3505
Issue No: Vol. eFirst

Steroidal Saponins from the Rhizomes of Smilax china and Their Inhibitory
Effects on Lipopolysaccharide-Induced Proinflammatory Cytokines Expression

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Authors: Li; Yu-Ting, Feng, Xiao, Feng, Yunjiang, Cheng, Yuanyuan, Tian, Li-Wen
Abstract: Four new furostanol saponins (1 – 4) and a new pregane-type saponin (5) along with six known steroidal saponins (6 – 11) were isolated from the rhizomes of Smilax china. The structures of 1 – 5 were elucidated by extensive analysis of NMR and HR-ESI-MS data in addition to enzymatic hydrolysis and other chemical methods. Compounds 1, 4, and 11 showed inhibitory activity against the expression of proinflammatory mediators, inducible nitric oxide synthase, interleukin-1β, interleukin-6, and tumor necrosis factor-α in lipopolysaccharide-induced RAW264.7 cells. Compound 1, at a concentration of 20 µM, decreased the production of inducible nitric oxide synthase, interleukin-1β, interleukin-6, and tumor necrosis factor-α by 36, 62, 72, and 67%, respectively, which is comparable to that of the positive control dexamethasone.
Citation: Planta Med ; : -
PubDate: 2022-09-28T15:48:19+01:00
DOI: 10.1055/a-1896-1098
Issue No: Vol. eFirst

Guttiferone E Displays Antineoplastic Activity Against Melanoma Cells

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Authors: Ribeiro; Arthur Barcelos, Nicolella, Heloiza Diniz, da Silva, Lucas Henrique Domingos, Mejía, Jennyfer Andrea Aldana, Tanimoto, Matheus Hikaru, Ambrósio, Sérgio Ricardo, Bastos, Jairo Kenupp, Orenha, Renato Pereira, Parreira, Renato Luis Tame, Tavares, Denise Crispim
Abstract: Guttiferone E (GE) is a benzophenone found in Brazilian red propolis. In the present study, the effect of GE on human (A-375) and murine (B16-F10) melanoma cells was investigated. GE significantly reduced the cellular viability of melanoma cells in a time-dependent manner. In addition, GE demonstrated antiproliferative effect, with IC50 values equivalent to 9.0 and 6.6 µM for A-375 and B16-F10 cells, respectively. The treatment of A-375 cells with GE significantly increased cell populations in G0/G1 phase and decreased those in G2/M phase. Conversely, on B16-F10 cells, GE led to a significant decrease in the populations of cells in G0/G1 phase and concomitantly an increase in the population of cells in phase S. A significantly higher percentage of apoptotic cells was observed in A-375 (43.5%) and B16-F10 (49.9%) cultures after treatment with GE. Treatments with GE caused morphological changes and significant decrease to the melanoma cellsʼ density. GE (10 µM) inhibited the migration of melanoma cells, with a higher rate of inhibition in B16-F10 cells (73.4%) observed. In addition, GE significantly reduced the adhesion of A375 cells, but showed no effect on B16-F10. Treatment with GE did not induce changes in P53 levels in A375 cultures. Molecular docking calculations showed that GE is stable in the active sites of the tubulin dimer with a similar energy to taxol chemotherapy. Taken together, the data suggest that GE has promising antineoplastic potential against melanoma.
Citation: Planta Med ; : -
PubDate: 2022-09-28T15:05:39+01:00
DOI: 10.1055/a-1890-5446
Issue No: Vol. eFirst

Comparative Pharmacokinetic Study of Two Pyrrolizidine Alkaloids
Lasiocarpine and Heliotrine in Rats

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Authors: Lin; Feifei, Zhao, Lijuan, Wang, Yingying, Ye, Yang, Liu, Jia
Abstract: Lasiocarpine (LAS) and heliotrine (HEL) are two different ester types of toxic pyrrolizidine alkaloids (PAs): open-chain diester and monoester. However, the pharmacokinetics of these two types of PAs in rats have not been reported. In the present study, two LC-MS/MS methods for determining LAS and HEL were established and validated. The methods exhibited good linearity, accuracy, and precision and were then applied to a comparative pharmacokinetic study. After intravenous administration to male rats at 1 mg/kg, the AUC0-t values of LAS and HEL were 336 ± 26 ng/mL × h and 170 ± 5 ng/mL × h. After oral administration at 10 mg/kg, the AUC0-t of LAS was much lower than that of HEL (18.2 ± 3.8 ng/mL × h vs. 396 ± 18 ng/mL × h), while the Cmax of LAS was lower than that of HEL (51.7 ± 22.5 ng/mL × h vs. 320 ± 26 ng/mL × h). The absolute oral bioavailability of LAS was 0.5%, which was significantly lower than that of HEL (23.3%). The results revealed that the pharmacokinetic behaviors of LAS differed from that of HEL.
Citation: Planta Med ; : -
PubDate: 2022-09-28T14:57:17+01:00
DOI: 10.1055/a-1915-5456
Issue No: Vol. eFirst

Pharmacological and Toxicological Study of Coumarinolignoids from Cleome
viscosa in Small Animals for the Management of Rheumatoid Arthritis

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Authors: Babu; Vineet, Singh, Rupali, Kashyap, Praveen K., Washimkar, Kaveri R., Mugale, Madhav N., Tandon, Sudeep, Bawankule, Dnyaneshwar Umrao
Abstract: This study aims to explore the possible pharmacological potential of Cleome viscosa Linn (Cleomaceae), an annual weed, into therapeutic value-added products. In the present study, we have explored the pharmacological and toxicological profile of coumarinolignoids isolated from Cleome viscose for the management of rheumatoid arthritis and related complications in a small animal model. To avoid the biasness during experiments on animals, we have coded the isolated coumarinolignoids as CLIV-92 to perform the experimental pharmacological study. CLIV-92 was orally administrated (30,100, 300 mg/kg) to animal models of collagen-induced arthritis (CIA), carrageenan-induced acute inflammation, thermal and chemical-induced pain, and Brewerʼs yeast-induced pyrexia. Oral administration of CLIV-92 significantly decreases the arthritis index, arthritis score, and increases the limb withdrawal threshold in the CIA model in experimental rats. The anti-arthritis studies revealed that the anti-inflammatory effect of CLIV-92 was associated with inhibition of the production of inflammatory mediators like TNF-α, IL-6, IL-17A, MMP-1, MMP-9, Nitric oxide, and C-RP in CIA ratʼs serum, and also reduced the NFкB-p65 expression as evidence of immunohistochemistry in knee joint tissue of CIA rats, in a dose-dependent manner. Further individual experiments related to arthritis-related complications in experimental animals demonstrated the analgesic, anti-inflammatory, and antipyretic potential of CLIV-92 in a dose-dependent manner. Further, an in-vivo acute oral toxicity study concluded that CLIV-92 is safe in experimental animals up to 2,000 mg/kg dose. The results of this study suggested that the oral administration of CLIV-92 may be a therapeutic candidate for further investigation in the management of rheumatoid arthritis and related complications.
Citation: Planta Med ; : -
PubDate: 2022-09-27T17:47:00+01:00
DOI: 10.1055/a-1906-1837
Issue No: Vol. eFirst

Resveratrol Protects BEAS-2B Cells against Erastin-Induced Ferroptosis
through the Nrf2/Keap1 Pathway

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Authors: Huang; Wenhan, Yu, Liuda, Cai, Wanru, Ma, Chunfang
Abstract: Ferroptosis is a newly discovered type of cell death that is different from other types of cell death morphologically and biologically. It is considered to play an important role in many pulmonary diseases. Currently, the regulatory roles of antioxidation in lung epithelial ferroptosis have not been fully explored. In this study, we show that resveratrol protected erastin-induced ferroptosis in BEAS-2B cells. Erastin led to increased reactive oxygen species production and iron deposition in BEAS-2B cells, which could be rescued by resveratrol. Furthermore, we observed that resveratrol led to modulating ferroptosis-associated gene glutathione peroxidase 4 expression and regulating glutathione in BEAS-2B cells. Resveratrol exerted an antioxidant property in erastin-induced ferroptosis of BEAS-2B cells by activating the nuclear factor-erythroid 2-related factor 2/Kelch-like ECH-associated protein signaling pathway. Finally, these findings demonstrate that resveratrol protects BEAS-2B from erastin-induced ferroptosis.
Citation: Planta Med ; : -
PubDate: 2022-09-27T17:39:18+01:00
DOI: 10.1055/a-1923-4399
Issue No: Vol. eFirst