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- Daikenchuto, a Traditional Kampo Medicine, Facilitates Mucosal Hyperemic
Responses through Activation of TRPA1- and TRPV1-Expressing Sensory Nerves
in Rat StomachPlanta Medica International Open 2022; 9: e123-e123
DOI: 10.1055/a-1868-2432
Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, Germany
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Planta Medica International Open 2022; 9: e123-e1232022-06-15T10:09:44+01:00
Issue No: Vol. 9, No. 01 (2022)
- Coix Seed Extract Prevents Inflammation-mediated Skin Dryness Induced by
Sodium Dodecyl Sulfate Exposure in HR-1 Hairless Mice
Authors: Li; Feng, Nakanishi, Yusuke, Murata, Kenta, Shinguchi, Kanako, Fujita, Nina, Chiba, Shigeki, Takahashi, Ryuji
Abstract: Skin inflammation and dryness are the features of surfactant-induced irritant contact dermatitis, a common skin disorder. In Japan, Coix seed (CS, Coix lacryma-jobi L. var. ma-yuen Stapf) is widely used as a traditional medicine and functional supplement to treat skin inflammation and dry skin. However, the efficacy of CS against surfactant-induced skin disorders has not been reported. Here, we investigated the effect of CS on inflammatory dry skin disorders induced by multiple topical applications of sodium dodecyl sulfate (SDS), a representative anionic surfactant. Male HR-1 hairless mice received a water extract of CS for four weeks. Three weeks after CS administration, the dorsal skin of the mice was exposed once daily to 10% SDS for five days. CS efficacy was then evaluated by measuring epidermal water content; erythema index; severity of skin scaling; epidermal thickness; inflammatory cell infiltration; production of pro-inflammatory mediators, such as interleukin-1α (IL-1α) and prostaglandin E2 (PGE2); and protein expression of cyclooxygenase 2 (COX-2), in the dorsal skin. Administration of CS markedly attenuated the SDS-induced reduction in epidermal water content, elevated erythema index, and severity of skin scaling. Histological analysis demonstrated that CS suppressed epidermal hyperplasia and macrophage infiltration in SDS-exposed skin. Furthermore, CS significantly prevented SDS-induced production of IL-1α and PGE2, as well as COX-2 upregulation. These results indicate that CS prevents SDS-induced inflammation-mediated skin dryness by inhibiting the production of pro-inflammatory mediators.
Citation: Planta Medica International Open 2022; 9: e108-e115
PubDate: 2022-05-30T00:00:00+01:00
DOI: 10.1055/a-1821-6332
Issue No: Vol. 9, No. 01 (2022)
- Studies of the Major Gene Expression and Related Metabolites in
Cannabinoids Biosynthesis Pathway Influenced by Ascorbic Acid
Authors: Soltan; Keyvan, Dadkhah, Behnoush
Abstract: Cannabis sativa L. is an annual dioecious plant that belongs to the Cannabaceae family and is essential for different pharmaceutical and nutritional properties. The most important and prevalent cannabinoids in cannabis are cannabidiol and delta-9-tetrahydrocannabinol. The application of elicitors is an effective method to improve secondary metabolite production, leading to a whole spectrum of molecular, genetic, and physiological modifications. Therefore, the expression changes of four key genes (THCAS, CBDAS, PT, and OLS) of the cannabinoids pathway along with the delta-9-tetrahydrocannabinol and cannabidiol metabolites fluctuation were surveyed following the application of ascorbic acid as an elicitor. Cannabis was sprayed immediately before flowering with ascorbic acid. Treated and untreated (control) plants were sampled in different time courses for real-time PCR and HPLC experiments. Results showed significant increases in THCAS, CBDAS, PT, and OLS expression after ascorbic acid treatments. The results of metabolite quantification also indicated that secondary metabolites, especially delta-9-tetrahydrocannabinol and cannabidiol, increased after the ascorbic acid application. This study contributes to the growing body of knowledge of the functions of key genes in the cannabinoids pathway to the engineering of cannabis for improving the production of delta-9-tetrahydrocannabinol and cannabidiol metabolites in this plant.
Citation: Planta Medica International Open 2022; 9: e116-e122
PubDate: 2022-05-30T00:00:00+01:00
DOI: 10.1055/a-1809-7862
Issue No: Vol. 9, No. 01 (2022)
- Biochemical Characterization of the Pharmacological Effects of Yagari in
Experimentally Induced Benign Prostatic Hyperplasia
Authors: Agatemor; Uzuazokaro Mark-Maria, Nwodo, Okwesili Fred Chiligue
Abstract: Benign prostatic hyperplasia is a progressive pathologic condition common in ageing men, constituting a health burden. Benign prostatic hyperplasia is characterized by the proliferation of prostatic tissues, prostate enlargement, and lower urinary tract symptoms. The use of herbal medicine in the management and treatment of benign prostatic hyperplasia has shown some promise. The efficacy and potency of some polyherbal extracts have been scientifically proven in the management and treatment of diseases, while many others are yet to be investigated. The aim of this study was to determine the effect of the herbal mixture Yagari on experimentally induced benign prostatic hyperplasia in rats and to identify its pharmacologically active agents. The effect of the herbal mixture on experimentally induced benign prostatic hyperplasia in rats was determined using 36 male Wistar rats grouped randomly into 6 groups of 6 rats each. The test rats were treated subcutaneously using a combination of dihydrotestosterone and estradiol valerate in a 10:1 ratio for 28 days according to the standard method. The test rats were thereafter treated with the herbal mixture for 21 days. Prostate-specific antigen, inflammatory cytokines, assay of prostate function hormonal and prostate function enzyme activities, and kidney function test were evaluated in the blood samples collected by ocular puncture applying standard methods. Prostates were harvested and examined for histopathological changes. Biological activity-guided fractionation of Yagari in a silica gel column was carried out and using phospholipase A2 activity as a biomarker. The identity of the bioactive compounds was determined using mass spectroscopy and nuclear magnetic resonance. The herbal mixture showed a positive effect on prostatic hyperplasia by decreasing urinary obstruction through the inhibition of 5-alpha reductase, anti-inflammatory activity, and decreased level of sex hormones. Characterization by spectral studies revealed apigenin (4´,5,7-trihydroxyflavone, molecular weight).
Citation: Planta Medica International Open 2022; 9: e90-e107
PubDate: 2022-03-19T00:00:00+0100
DOI: 10.1055/a-1729-3499
Issue No: Vol. 9, No. 01 (2022)
- Time-Dependent Anti-inflammatory Effects of a Lipid Extract from
Macrocystis pyrifera on Toll-Like Receptor 2 Signaling in Human THP-1
Monocytes
Authors: Kok; Jamie Mei Lin, Dowd, Georgina, Cabral, Jaydee, Wise, Lyn
Abstract: Seaweeds reportedly contain anti-inflammatory compounds; however, little is known about the therapeutic potential of Macrocystis pyrifera. This study investigated the anti-inflammatory properties of a methanol:chloroform extract, chromatographic fractions, and fatty acids identified from M. pyrifera (Linnaeus) C. Agardh. In human THP-1 monocytes stimulated with the Toll-like receptor 2 agonist lipoteichoic acid, the extract decreased mRNA and protein levels of interleukin-1β, interleukin-8, and monocyte chemoattractant protein-1 to varied degrees at nontoxic concentrations. The greatest anti-inflammatory effects were elicited when the extract was applied between 6 h prior to, and 6 h after, the stimuli. Reduced levels of nuclear factor kappa-light-chain-enhancer of activated B cells signaling proteins were observed in extract-treated cells, with a significant decrease in the myeloid differentiation factor 88 protein abundance relative to stimulated THP-1 cells. Chromatographic fractionation of the extract yielded 40 fractions, of which fraction F25 exhibited the greatest inhibition of monocyte chemoattractant protein-1 production in activated THP-1 cells. Fatty acids abundant within the extract and F25 were identified then tested, individually and in combination, for their anti-inflammatory effects. Myristic acid, palmitoleic acid, and α-linolenic acid, but not the fatty acid combination, inhibited lipoteichoic acid-stimulated monocyte chemoattractant protein-1 production without compromising THP-1 cell viability. These findings indicate that the fatty acid-rich extract and fraction from M. pyrifera provide anti-inflammatory and cytoprotective effects that may be beneficial for use as a therapeutic.
Citation: Planta Medica International Open 2022; 9: e80-e89
PubDate: 2022-03-15T00:00:00+0100
DOI: 10.1055/a-1729-3654
Issue No: Vol. 9, No. 01 (2022)
- Anti-Alzheimer’s and Anti-inflammatory Activities of Compounds Isolated
from Solanum Mauritianum
Authors: Ticona; Luis Apaza, García, Borja Durán, Bastante, Marcos Humanes, Serban, Andreea Madalina, Sánchez, Ángel Rumbero
Abstract: Solanum mauritianum, commonly known as “Tabaquillo”, was one of the most used plants by tribes from South America as a remedy for headaches. Based on this ethnopharmacological use, a bioguided isolation of compounds with anti-inflammatory and anti-Alzheimer’s activities from S. mauritianum was carried out by measuring the inhibition of NF-κB in C8D1A, Neuro-2a, and EOC 13.31 cells, and by measuring the inhibition of acetylcholinesterase and β-amyloid. This allowed the isolation and characterisation by nuclear magnetic resonance and mass spectrometry of four compounds (1–4). Compounds 1–4 showed NF-κB inhibitory activity with IC50 values of 9.13–9.96, 17.17–17.77, 2.41–2.79, and 1.59–1.93 µM, respectively, while celastrol (the positive control) had an IC50 value of 7.41 µM. Likewise, compounds 1–4 showed anti-Alzheimer’s activity, inhibiting the acetylcholinesterase by 40.33, 20.57, 61.26, and 83.32%, respectively, while galantamine (positive control) showed an inhibition of 90.38%. In addition, concerning the inhibition of β-amyloid aggregation, compounds 1–4 showed an inhibition of 47, 23, 65, and 93%, respectively, while curcumin (positive control) had an inhibition of 71.19%.
Citation: Planta Medica International Open 2022; 9: e1-e11
PubDate: 2022-02-07T00:00:00+0100
DOI: 10.1055/a-1696-6741
Issue No: Vol. 9, No. 01 (2022)
- Isolated Compounds from Buddleja Coriacea with Antibacterial and
Anti-Inflammatory Activities in the Urinary Tract
Authors: Ticona; Luis Apaza, Rico, Francisco Aguilar, Sánchez-Corral, Javier Sánchez, Domenech, Montserrat Ortega, Sánchez, Ángel Rumbero
Abstract: Buddleja coriacea Remy is one of the plant species used by the Bolivian population for the treatment of urinary infections. This study aimed to identify the extract, fractions, and compounds responsible for the antibacterial and anti-inflammatory activities of B. coriacea leaves. Bioguided isolation of compounds with antibacterial and anti-inflammatory activities was carried out by measuring the antibacterial effect against specific pathogenic microbial strains, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, and Serratia marcescens, and the inhibition of NF-κB in RM-2 and MM.14Ov cells. Bioassay-guided isolation led to the isolation and characterisation of (4aR,4bS,5 S,6aS,6bS,9aR,10aS,10bS)-6b-glycoloyl-5-hydroxy-4a,6a-dimethyl-8-propyl-4a,4b,5,6,6a,6b,9a,10,10a,10b,11,12-dodecahydro-2H-naphtho [2',1':4,5] indeno [1,2-d][1,3] dioxol-2-one (1), 3-[3-(2-dimethylaminoethyl)-1H-indol-5-yl]-N-(4-methoxybenzyl) acrylamide (2), and (1β,11β,12α)-1,11,12-trihydroxy-11,20-epoxypicrasa-3,13(21)-diene-2,16-dione (3) by nuclear magnetic resonance and mass spectroscopy. All compounds showed antibacterial activity with minimum inhibitory concentration values of 11.64–11.81, 0.17–0.19, and 0.34–0.36 µM, respectively, on the tested strains, while the positive control, ofloxacin, had a minimum inhibitory concentration of 27.66 µM. Finally, all the compounds showed NF-κB inhibitory activity with IC50 values of 11.25–11.34, 0.15–0.16, and 0.33–0.36 µM, respectively, in all cell lines, while the positive control, celastrol, had an IC50 of 7.96 µM. Thus, this study managed to isolate and evaluate for the first time the pharmacological potential of three compounds present in the leaves of B. coriacea with antibacterial and anti-inflammatory activities.
Citation: Planta Medica International Open 2022; 9: e12-e22
PubDate: 2022-02-07T00:00:00+0100
DOI: 10.1055/a-1696-6851
Issue No: Vol. 9, No. 01 (2022)
- Biosynthesis and Chemopreventive Potential of Jute (Corchorus capsularis
and C. olitorius) Flavonoids and Phylogeny of Flavonoid Biosynthesis
Pathways
Authors: Satya; Pratik, Sarkar, Debabrata, Chatterjee, Amitava, Pal, Srikumar, Ray, Soham, Sharma, Laxmi, Roy, Suman, Bera, Amit, Ghosh, Srinjoy, Mitra, Jiban, Kar, Gouranga, Singh, Nagendra Kumar
Abstract: Flavonoids are valuable phytochemicals for human health and nutrition. Jute (Corchorus capsularis and C. olitorius), a vegetable rich in phenolics and flavonoids, is globally consumed for its health benefit, but the biosynthesis pathways and metabolic profiles of its flavonoids are poorly characterized. Elucidating the flavonoid biosynthesis pathways would augment the broader use of jute, including targeted synthesis of its specific flavonoids. We reconstructed the core flavonoid biosynthesis pathways in jute by integrating transcriptome mining, HPLC and flavonoid histochemistry. In C. capsularis (white jute), the flavonoid biosynthesis pathways’ metabolic flux was driven toward the biosynthesis of proanthocyanidins that mediate the acquisition of abiotic stress tolerance. However, higher levels of flavonols in C. olitorius (tossa jute) render it more suitable for nutritional and medicinal use. Jute flavonoid extract exhibited in vitro inhibition of matrix metalloproteinase-2, suggesting its potential chemopreventive and immunity-boosting roles. Using the flavonoid biosynthesis pathways profiles of 93 plant species, we reconstructed the flavonoid biosynthesis pathways phylogeny based on distance-based clustering of reaction paths. This reaction-path flavonoid biosynthesis pathways phylogeny was quite distinct from that reconstructed using individual gene sequences. Our flavonoid biosynthesis pathways-based classification of flavonoid groups corroborates well with their chemical evolution, suggesting complex, adaptive evolution of flavonoid biosynthesis pathways, particularly in higher plants.
Citation: Planta Medica International Open 2022; 9: e23-e33
PubDate: 2022-02-07T00:00:00+0100
DOI: 10.1055/a-1712-7978
Issue No: Vol. 9, No. 01 (2022)
- Tea Tree Oil and Terpinen-4-Ol Induce Cytoskeletal Reorganization of Human
Melanoma Cells
Authors: Bozzuto; Giuseppina, Mariano, Fulvia, Costa, Ilaria, Calcabrini, Annarica, Molinari, Agnese
Abstract: Tea tree oil is an essential oil distilled from the leaves of Melaleuca alternifolia, a plant native to Australia. It has been used in traditional medicine for its antiseptic and anti-inflammatory properties to treat various skin conditions and infections. It has also been incorporated into many topical formulations to treat cutaneous infections and speed wound healing. In vivo and in vitro studies report antiproliferative effects in skin disorders but the molecular mechanisms underlying this effect remain to be still elucidated. In this study MTT assay, scanning electron microscopy-field emission gun, flow cytometry, cell cycle assays, and laser scanning confocal microscopy were utilized to investigate a novel mechanism underlying the antiproliferative effects of tea tree oil and terpinen-4-ol on transformed skin (melanoma) M14 cells. The analysis of the actin cytoskeleton by laser scanning confocal microscopy evidenced a clear action of both essential oil and its main active component on F-actin, which interfered with bundling of actin microfilaments in stress fibers. As for the microtubular network, both tea tree oil and terpinen-4-ol induced a disorganization of the perinuclear cage with the rupture and collapse of microtubules. Finally, they noticeably changed the intermediate filaments architecture by inducing the formation of large vimentin cables. Results obtained in the present study point to the cytoskeleton as a further target of tea tree oil and terpinen-4-ol and could account for the inhibition of proliferation and invasion of skin transformed M14 cells. In our experimental conditions, vimentin intermediate filaments appear to be the cytoskeletal element more affected by the treatments. Moreover, the role of cross-linker proteins in the mechanism of action of tea tree oil has been discussed.
Citation: Planta Medica International Open 2022; 9: e34-e53
PubDate: 2022-02-07T00:00:00+0100
DOI: 10.1055/a-1623-2938
Issue No: Vol. 9, No. 01 (2022)
- Libocedroquinone: A Promising Anticancer Lead against Lung Cancer from
Calocedrus Decurrens
Authors: Subramanyan; Santhi, Karunakaran, Varsha, Deepika, Selvakumar, Gracy, Anuja Joseph, Sheeba, Veluthoor, Joseph, Karchesy, Maiti, Kaustabh Kumar, Varma, Ramavarma Luxmi, Radhakrishnan, Kokkuvayil Vasu
Abstract: A focus on evaluating anticancer potency of various extracts of the heartwood of Calocedrus decurrens against human lung adenocarcinoma (A549) cell line was performed using in vitro MTT assay. The hexane extract displayed excellent cytotoxic effect, and the phytochemical investigation of the hexane and acetone extracts resulted in the isolation of five major compounds. The structure of the compounds was established as libocedrol (1), thymoquinone (2), libocedroquinone (3), diethylphthalate (4), and (1 R, 2 R, 4 R)-p-menthane-1,2,4-triol (5). Compounds 4 and 5 are reported for the first time from the Calocedrus genus. Compounds 1–3 were evaluated for their cytotoxicity against the lung cancer cell line along with a healthy control. Compound 3 was more potent than other compounds against the A549 cell line with an IC50 of 4.8 µM at 24 h. Moreover, compound 3 exhibited less toxicity with the normal lung fibroblast cell line WI-38. This is the first anticancer study of the species Calocedrus decurrens.
Citation: Planta Medica International Open 2022; 9: e54-e59
PubDate: 2022-02-07T00:00:00+0100
DOI: 10.1055/a-1699-8748
Issue No: Vol. 9, No. 01 (2022)
- Antidiabetic Activity of Caulerpa racemosa: Role of Proinflammatory
Mediators, Oxidative Stress, and Other Biomarkers
Authors: Mandlik; Rahul V., Naik, Suresh R., Zine, Sandip, Ved, Hemen, Doshi, Gaurav
Abstract: A marine alga, Caulerpa racemose (seaweed), exhibits few biological activities, such as antinociceptive/anti-inflammatory, antitumor, and growth regulator. This study aimed to determine the antidiabetic activity of this seaweed. High-performance thin-layer chromatography of C. racemosa ethanolic extract was performed to identify its active constituents. Antidiabetic activity of C. racemosa ethanolic extract (100 and 200 mg/kg) was evaluated using various biochemical paradigms against glipizide (5 mg/kg) in a streptozotocin-induced diabetes rat model. High-performance thin-layer chromatography revealed β-sitosterol as an active constituent and also indicated the presence of saponins and alkaloids. Treatment with C. racemosa ethanolic extract significantly reduced blood glucose levels in diabetic rats, and the degree of glucose reduction was comparable to that attained by glipizide treatment. The C. racemosa ethanolic extract treatment restored the impaired glycosylated hemoglobin level, liver glycogen level, glucose uptake by hemidiaphragm, and glucose transport by hepatic cells. Pretreatment with C. racemosa ethanolic extract also restored lipid abnormalities, elevated liver enzymes, elevated inflammatory markers, and depleted endogenous antioxidants. A superior effect was shown by C. racemosa ethanolic extract (200 mg/kg) over glipizide (5 mg/kg). Moreover, the restoration of the histoarchitecture of the pancreas by C. racemosa ethanolic extract (200 mg/kg) was comparable to that of the glipizide (5 mg/kg) treatment group. The present experimental findings demonstrate significant antidiabetic activity of C. racemosa ethanolic extract in diabetic rats using various biochemical paradigms. Further, C. racemosa ethanolic extract seems to be safe and does not affect vital organs adversely.
Citation: Planta Medica International Open 2022; 9: e60-e71
PubDate: 2022-01-31T00:00:00+0100
DOI: 10.1055/a-1712-8178
Issue No: Vol. 9, No. 01 (2022)
- Daikenchuto, a Traditional Kampo Medicine, Facilitates Mucosal Hyperemic
Responses through Activation of TRPA1- and TRPV1-Expressing Sensory Nerves
in Rat Stomach
Authors: Yoshikubo; Masatoshi, Tashima, Kimihito, Raimura, Masaki, Watanabe, Yuto, Noma, Yukiko, Horie, Syunji
Pages: 72 - 79
Abstract: Daikenchuto is a traditional Kampo medicine used to treat cold sensations and dysmotility in the abdomen. This study investigated the roles of transient receptor potential ankyrin 1- and transient reporter potential vanilloid 1-expressing sensory nerves in daikenchuto-induced gastric mucosal blood flow by pharmacological and immunohistochemical analyses using male Sprague-Dawley rats. Gastric mucosal blood flow was measured in ex vivo stomachs using a laser Doppler flowmeter. Transient receptor potential ankyrin 1 activator allyl isothiocyanate or transient reporter potential vanilloid 1 activator capsaicin were applied for 10 min, and daikenchuto was applied for 10 or 30 min to the rat stomach. Transient reporter potential vanilloid 1 blocker N-(4-t-butylphenyl)-4-(3-chlopyridin-2-yl) tetrahydropyrazine-1(2H)-carboxamide and transient receptor potential ankyrin 1 blocker A-967079 were also administered intragastrically. Capsaicin and allyl isothiocyanate increased gastric mucosal blood flow immediately after the intragastric application, which was almost completely inhibited by N-(4-t-butylphenyl)-4-(3-chlopyridin-2-yl) tetrahydropyrazine-1(2H)-carboxamide and A-967079, respectively. Daikenchuto increased gastric mucosal blood flow in a concentration-dependent manner. A-967079 significantly inhibited the increase in gastric mucosal blood flow induced by daikenchuto. In contrast, N-(4-t-butylphenyl)-4-(3-chlopyridin-2-yl) tetrahydropyrazine-1(2H)-carboxamide inhibited the responses to daikenchuto only in the late phase but not in the initial phase. Interestingly, in the deafferentation of capsaicin-sensitive sensory fiber in rats, the increased gastric mucosal blood flow induced by daikenchuto was only decreased in the late phase. Although transient receptor potential ankyrin 1- and transient reporter potential vanilloid 1-immunoreactive fibers were observed around the submucosal blood vessels of normal subjects, they were completely absent in the deafferentation of capsaicin-sensitive sensory fibers. Thus, daikenchuto increases gastric mucosal blood flow via transient receptor potential ankyrin 1- and transient reporter potential vanilloid 1-co-expressing sensory nerves in rat stomachs.
Citation: Planta Medica International Open 2022; 9: 72-79
PubDate: 2022-03-07T00:00:00+0100
DOI: 10.1055/a-1712-8391
Issue No: Vol. 9, No. 01 (2022)
- Effect of Environmental Factors on Plectranthus Neochilus Volatile
Composition: A GC-MS-Based Metabolomics Approach
Authors: Galbiatti; Maria Isabel, Pinheiro, Guilherme Perez, Antunes, Elisa Ribeiro Miranda, Hernandes, Vinicius Verri, Sawaya, Alexandra Christine Helena Frankland
Abstract: Plectranthus neochilus Schltr. is an aromatic species, commonly used for digestive, antispasmodic, and analgesic purposes. Although many studies have reported the chemical composition of its essential oil, variations in the volatile profile were observed, which may be due to multiple factors linked to growth and field conditions. In order to detect metabolic variations in this species, we employed a GC-MS-based untargeted metabolomics approach analyzing samples of four P. neochilus individuals collected over a year. From all analyses, 24 mass features were detected and 21 were identified according to their respective chromatographic peaks. All features varied among samples, particularly (2E)-hexenal, 3-octanone and δ-3-carene, which showed the highest coefficient of variation percentage in our study. Although the four individuals presented the same peaks in the chromatograms, significant differences in the intensity of specific mass features were detected between individuals throughout the year. Time of sampling did not affect P. neochilus volatile composition; the chemical profile remained constant throughout the day. Seasonal trends were observed for the species. Winter months coincided with a drop in the intensity of most components. Air temperature showed a positive correlation with some feature intensities, while myrcene and α-thujene resulted in a positive and a negative correlation with rainfall, respectively. This study was the first attempt to correlate metabolic variation and environmental factors in P. neochilus. Our approach was successful in identifying the composition and variation of the headspace volatiles of P. neochilus leaves.
Citation: Planta Medica International Open 2021; 8: e153-e160
PubDate: 2021-12-20T00:00:00+0100
DOI: 10.1055/a-1648-8111
Issue No: Vol. 8, No. 03 (2021)
- In vitro Inhibitory Action of the Essential Oils of Origanum Vulgare and
Rosmarinus Officinalis against Aspergillus Fumigatus
Authors: Monteiro; Antonia Carolina Melo, Drame, Aminata Doucoure, Nascimento, Francisca Melo, Miranda-Vilela, Ana Luisa, Lima, Alexandre Vasconcelos, da Silva, Mirra Angelina Neres, Ribeiro, Ieler Ferreira
Abstract: Aspergillus fumigatus is the main etiological agent of aspergillosis. Considering azole antifungal drug resistance in A. fumigatus, which compromises treatment, new alternatives are needed. Among them, essential oils (EOs) can be an alternative treatment, having shown positive results in inhibiting phytopathogenic fungi in vitro. We aimed to determine the in vitro antifungal activity of Origanum vulgare L. subsp. hirtum (Link) (oregano) and Rosmarinus officinalis L. (rosemary) EOs alone and in association (O. vulgare+R. officinalis) against A. fumigatus. EOs were analyzed by gas chromatography (GC-FID and GC/MS systems), and analyses showed that the major components of O. vulgare EO were carvacrol (67.8%), p-cymene (14.8%), and thymol (3.9%); for R. officinalis, they were the monoterpenes 1,8-cineole (49.1%), camphor (18.1%) and α-pinene (8.1). For biological assays, five EO concentrations, 0.2; 0.4; 0.6; 0.8 and 1.0%, were used in disk diffusion and agar dilution tests for 21 days. In disk diffusion, O. vulgare EO alone and in association (O. vulgare+R. officinalis) showed fungicidal activity at all concentrations. In agar dilution, inhibitory action was demonstrated from 0.6% for O. vulgare EO and in association (O. vulgare+R. officinalis). R. officinalis EO at 1.0% showed no fungal growth, determining the minimum inhibitory concentration (MIC). The present study demonstrated inhibitory actions of O. vulgare and R. officinalis EOs in A. fumigatus. GC analyses corroborated the literature regarding their antibacterial and antifungal effects. However, further in vitro and in vivo studies are needed to evaluate EOs as alternative antifungals for treating aspergillosis.
Citation: Planta Medica International Open 2021; 8: e143-e152
PubDate: 2021-11-17T00:00:00+0100
DOI: 10.1055/a-1588-2875
Issue No: Vol. 8, No. 03 (2021)
- Anticipate, Target and Characterize: MS²-anticipated C-glycosylflavones
from Erythrococca anomala
Authors: Kouamé; Tapé, Okpekon, Timothée, Bony, Nicaise F., Ferron, Solenn, Bonnaffé, David, Vanheuverzwijn, Jérôme, Zhou, Zhiyu, Fontaine, Véronique, N’Tamon, Amon Diane, Gallard, Jean-François, Leblanc, Karine, Jullian, Jean-Christophe, Miel, Corto, Champy, Pierre, Beniddir, Mehdi A., Le Pogam, Pierre
Abstract: We herein report on the first chemical assessment of Erythrococca anomala (Juss. ex Poir.) Prain (Euphorbiaceae), a genus that was – to the best of our knowledge – not studied yet from a phytochemical perspective. A molecular networking strategy was implemented to rapidly identify the known specialized metabolites from untargeted MS/MS analyses of E. anomala leaves ethanolic extract. This strategy allowed for the identification of diverse C-glycosyl flavones and a cursory examination of MS/MS spectra could extend the GNPS-provided annotation to pinpoint the structural novelty of further derivatives. The isolation of the sought-after structures could be streamlined based on MS-guidance and their structures, determined through extensive NMR analyses, displayed structural features in line with MS²-based predictions. Anticipating sharp structural features at an early stage of the dereplication process through a critical assessment of the tandem mass spectrometric landmarks was essential to embark on the isolation of the newly reported structures owing to the elevated number of flavonoid glycosides isomers thereof formerly known, which would have deterred us from isolating them without the support of additional tandem mass spectrometric information. The isolation of the main components of the ethanolic extract completed the currently provided chemical report on E. anomala, also resulting in the description of a new phenylethanoid derivative (3) and of a new orcinol-based dimer (4). Anomaloflavone (1) exhibit significant activities with minimal inhibitory concentration values of 25 µg/mL against Staphylococcus aureus and Mycobacterium smegmatis while failing to exert an antibacterial activity against Pseudomonas aeruginosa, while being devoid of cytotoxicity against SiHa cells.
Citation: Planta Medica International Open 2021; 8: e131-e142
PubDate: 2021-10-29T00:00:00+01:00
DOI: 10.1055/a-1576-4351
Issue No: Vol. 8, No. 03 (2021)
- Thymol and Piperine-Loaded Poly(D,L-lactic-co-glycolic acid) Nanoparticles
Modulate Inflammatory Mediators and Apoptosis in Murine Macrophages
Authors: Dzoyem; Jean Paul, Boulens, Nathalie, Allémann, Eric, Delie, Florence
Abstract: This study aimed at preparing and characterizing thymol, eugenol, and piperine-loaded poly(D,L-lactic-co-glycolic acid) nanoparticles and evaluating the effect on inflammatory mediators secretion and apoptosis in Raw 264.7 macrophage cells. Nanoparticles were produced by the solvent evaporation technique. Dynamic light scattering and scanning electron microscopy were used to study the physicochemical characteristics. Raw 264.7 macrophage cells were used as a model for in vitro assays. The 2-(4-iodophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium assay was used to determine the cytotoxicity of the formulated nanoparticles. An annexin V apoptosis detection kit was used to assess apoptosis. Nitric oxide production was determined using the Griess reagent, and the inflammatory mediators level was evaluated with Th1/Th2 cytokine and fluorometric cyclooxygenase kits. The loaded nanoparticles showed a particle size around 190 nm with a low polydispersity between 0.069 and 0.104 and a zeta potential between–1.2 and–9.5 mV. Reduced cytotoxicity of nanoparticles compared to free molecules against Raw 264.7 macrophage cells was observed and seemed to occur through a mechanism associated with apoptosis. A decrease in cyclooxygenase enzyme activity with an increasing concentration was observed. Both free molecules and nanoparticles showed their capacity to modulate the inflammatory process mostly by inhibiting the investigated inflammatory cytokines. The data presented in this study indicate that thymol and piperine-loaded poly(D,L-lactic-co-glycolic acid nanoparticles could serve as a novel anti-inflammatory colloidal drug delivery system with reduced toxicity. However, further study should be considered to optimize the formulation’s loading capacity and thereby probably enhance their bioactivity in treating inflammatory diseases.
Citation: Planta Medica International Open 2021; 8: e122-e130
PubDate: 2021-09-21T00:00:00+01:00
DOI: 10.1055/a-1543-1190
Issue No: Vol. 8, No. 03 (2021)
- Triterpenoids from Alisma orientale and their NF-кB Inhibitory
Activity
Authors: Yang; Qian, Li, Yinqing, Liu, Xizi, Han, Shiyi, Fan, Siyang
Abstract: The rhizome of Alisma orientale (sam.) Juz. is used in clinics for eliminating dampness, reducing edema, and promoting diuresis. This study aimed to elucidate the compounds and investigate their nuclear factor-kappa inhibitory activities in human embryonic kidney 293 cells. A new triterpene, alismaketone B (1); a new natural nortriterpene, noralisolic acid A (2); and 13 known protostane-type triterpenes were isolated from the rhizome of A. orientale. The new structures and their absolute configurations were established using HRESIMS, NMR, and electronic circular dichroism experiments. All isolated compounds were evaluated for their inhibitory activity on NF-κB. The compounds 8, 9, 10, and 14 showed moderate NF-κB inhibitory activities with their IC50 values being 64.7, 32.3, 47.3, and 37.3 μM, respectively.
Citation: Planta Medica International Open 2021; 8: e114-e121
PubDate: 2021-08-25T00:00:00+01:00
DOI: 10.1055/a-1543-1261
Issue No: Vol. 8, No. 03 (2021)
- Neuroprotective Effects of Delta-9-Tetrahydrocannabinol against FeSO4- and
H2O2-Induced Cell Damage on Dopaminergic Neurons in Primary Mesencephalic
Cell Culture
Authors: Moldzio; Rudolf, Unterberger, Alexander, Krewenka, Christopher, Kranner, Barbara, Radad, Khaled
Abstract: Delta-9-Tetrahydrocannabinol and other phytocannabinoids have been previously demonstrated to possess neuroprotective effects in murine mesencephalic cell culture models of Parkinson’s disease, in which increased levels of superoxide radicals led to the loss of dopaminergic neurons. In these models, delta-9-tetrahydrocannabinol did not scavenge these radicals but displayed antioxidative capacity by increasing glutathione levels. Based on these findings, in the present study, we investigated whether the neuroprotective effect of delta-9-tetrahydrocannabinol can also be detected in FeSO4- and H2O2-stressed cells. Mesencephalic cultures were concomitantly treated with FeSO4 (350 μM) or H2O2 (150 μM) and delta-9-tetrahydrocannabinol (0.01, 0.1, 1, 10 μM) on the 12th days in vitro for 48 h. On the 14th DIV, dopaminergic neurons were stained immunocytochemically by tyrosine hydroxylase, and fluorescently using crystal violet, Hoechst 33342, and JC-1. FeSO4 and H2O2 significantly reduced the number of dopaminergic neurons by 33 and 36%, respectively, and adversely affected the morphology of surviving neurons. Moreover, FeSO4, but not H2O2, significantly decreased the fluorescence intensity of crystal violet and Hoechst 33342, and reduced the red/green ratio of JC-1. Co-treatment with delta-9-tetrahydrocannabinol at the concentrations 0.01 and 0.1 μM significantly rescued dopaminergic neurons in FeSO4 and H2O2-treated cultures by 16 and 30%, respectively. delta-9-Tetrahydrocannabinol treatment also led to a higher fluorescence intensity of crystal violet and Hoechst 33342, and increased the red/green fluorescence ratio of JC-1 when concomitantly administered with FeSO4 but not H2O2. To conclude, delta-9-tetrahydrocannabinol rescues dopaminergic neurons against FeSO4- and H2O2-induced neurotoxicity. Using fluorescence dyes, this effect seems to be mediated partially by restoring mitochondrial integrity and decreasing cell death, particularly in FeSO4-treated cultures.
Citation: Planta Medica International Open 2021; 8: e88-e95
PubDate: 2021-08-11T00:00:00+01:00
DOI: 10.1055/a-1516-4182
Issue No: Vol. 8, No. 03 (2021)
- Effects of Chronic Administration of P-Cymene in an Animal Model of
LPS-Induced Autism
Authors: de Camargo; Rick Wilhiam, da Silva, Marina Goulart, Daros, Guilherme Cabreira, de Medeiros, Fabiana Durante, da Rosa, Naiana, Menschhein Medeiros, Caroline Liana, de Medeiros Peretti, Eduardo, Palandi, Juliete, Bobinski, Franciane, Fortunato, Jucélia Jeremias, de Bitencourt, Rafael Mariano
Abstract: p-Cymene is a monoterpene found in over 100 plant species. It shows a range of biological activity, including anti-inflammatory and antimicrobial effects. It is possibly a new therapeutic alternative for autism spectrum disorder characterized by deficits in interaction and behavioral abnormalities. These symptoms can occur in response to maternal immune activation through prenatal exposure to lipopolysaccharide. Thus, this study aimed to evaluate the behavioral, memory, and biochemical effects of chronic administration of p-cymene in an animal model of autism by prenatal maternal exposure to lipopolysaccharide. Twenty-four pregnant Wistar rats were used, who received 100 μg/kg of lipopolysaccharide or saline intraperitoneally (i.p.) on the 9.5 gestational day. After birth, the male offspring remained with the mothers until weaning and underwent model validation tests on postnatal day 30. From postnatal day 31 on, chronic administration, via i.p., of saline (1 mL/kg), risperidone (0.2 mg/kg), or p-cymene (100 mg/kg) for 22 days was performed. The animals were submitted to behavioral (postnatal day 52) and memory tests (postnatal days 52–53) and subsequently sacrificed (postnatal day 54) when their brain structures were removed for quantification of proinflammatory cytokines (TNF-α, interleukin 1β, and interleukin 6). Prenatal exposure to lipopolysaccharide significantly increased episodes of stereotyped movement (p=0.0001) and decreased parameters of social interaction in offspring, including sniffing, following, mounting, and allowing mounting (p=0.0043, p
Citation: Planta Medica International Open 2021; 8: e104-e113
PubDate: 2021-08-11T00:00:00+01:00
DOI: 10.1055/a-1491-1866
Issue No: Vol. 8, No. 03 (2021)
- Screening of 20 Pantanal Wetland Plants for Anti-Candida Activity using
HPLC-DAD-MS/MS and Bioautography to Characterize Active Compounds
Authors: de Brito; Daniela Z., Cassemiro, Nadla S., de Souza, Jeana M. E., Damasceno-Junior, Geraldo A., Oliveira, Rodrigo J., Carollo, Carlos A., Chang, Marilene R.
Abstract: The Pantanal wetland harbors a rich flora with uncharted pharmacological potential. This study evaluated 20 Brazilian Pantanal plants against Candida albicans, C. parapsilosis, C. tropicalis, and C. krusei. Fungal susceptibility was determined by agar diffusion and broth microdilution; active compounds were identified by bioautography and HPLC-DAD-MS/MS. Sesbania virgata, Polygala molluginifolia, and Cantinoa mutabilis extracts and their chloroform and ethyl acetate (EtOAc) fractions exhibited the best activity against all Candida species tested. The EtOAc fraction of P. molluginifolia proved to be more efficient in inhibiting C. parapsilosis and C. krusei growth (Minimum inhibitory concentration of 125 and 62.5 μg/mL, respectively). Bioautography of this fraction revealed two active bands, characterized by HPLC-DAD-MS/MS as a mixture of podophyllotoxin derivatives blumenol, besides some flavonoids. This work demonstrated antifungal potential of P. molluginifolia podophyllotoxin derivatives and the versatility of bioautography with HPLC-DAD-MS/MS to identify the bioactive compounds.
Citation: Planta Medica International Open 2021; 8: e96-e103
PubDate: 2021-07-14T00:00:00+01:00
DOI: 10.1055/a-1494-1117
Issue No: Vol. 8, No. 03 (2021)
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