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Coptis teeta Wall., an endangered but valuable medicinal species having various folklore uses in Indian and Chinese Traditional system of medicine. Its distribution is restricted to India, China and Tibet. In India, C. teeta is traditionally used in joint disorders, urinary infections and inflammatory diseases, however the scientific validation is missing. Thus, the present study aims to validate the anti-lithiatic and anti-gout activity of C. teeta rhizome extract (CTME) through in-vitro biological assays. The metabolic fingerprinting of CTME through reverse phase-high performance liquid chromatography-photodiode array (RP-HPLC-PDA) showed the presence of five benzyl-isoquinoline alkaloids, namely berberine (2.59%), coptisine (0.746%) jatrorrhizine (0.133%), palmatine (0.03%) and tetrahydropalmatine (0.003%). The anti-gout potency analysed via in-vitro xanthine oxidase (XOD) inhibition assay, followed by HPTLC (High performance thin layer chromatography) mediated bio-autographic inhibition of XOD signifies that CTME exhibit strong inhibition of XOD (IC50: 3.014 µg/ml), insignificantly different (p > 0.05) from allopurinol (IC50: 2.47 µg/ml). The XOD bioautographic assay advocates that the efficacy is primarily due to berberine and coptisine alkaloids. The CTME has significant anti-lithiatic activity, and thereby limiting the progression of crystal nidus formation, mediated via inhibition of calcium oxalate crystals nucleation and aggregation. Additionally, the extract also exhibits potential effect on inhibition of oxidative stress associated inflammation, which plays crucial role in alleviating urolithiasis and gouty conditions. Validating the traditional claims of C. teeta will not only confirm its medicinal benefits for targeted pathological conditions but also enhance its industrial demand.
Assuntos
Benzilisoquinolinas , Oxalato de Cálcio , Coptis , Extratos Vegetais , Ácido Úrico , Coptis/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Benzilisoquinolinas/farmacologia , Benzilisoquinolinas/isolamento & purificação , Rizoma/química , Xantina Oxidase/antagonistas & inibidores , Xantina Oxidase/metabolismo , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/isolamento & purificação , Índia , Supressores da Gota/farmacologia , Supressores da Gota/isolamento & purificação , Doenças Metabólicas/tratamento farmacológico , Estrutura MolecularRESUMO
Malnutrition and hunger is a serious global issue, however, wild fruits possess the potential of combatting it being rich in nutrients. Stereospermum chelonoides (L.f.) DC., commonly known as "Patala" in Ayurvedic text, is a large wild tree bearing edible, yet, underutilized fruits consumed by the locals in Western parts of India and neighboring countries. The present study focuses on the nutritional profile of S. chelonoides fruit along with quantification of bioactive constituents using RP-HPLC-PDA and evaluation of in-vitro anti-oxidant and, anti-microbial activity. The fruit was found rich in nutritional composition having protein (2.41 % ± 0.007), fibre (3.46 % ± 0.02) and carbohydrate (90.19 % ± 1.73) with energy value of 368.2 ± 3.94 Kcal/100g. The elemental analysis of fruit resulted in macronutrients Ca, Mg and Na and micronutrients Fe, Mn, Zn, and Cu in amounts comparable to common marketed fruits. The RP-HPLC-PDA analysis revealed the presence of six phenolic compounds in all 3 extracts made from the fruit in which highest amount are present in hydro-alcoholic extract. All the extracts exhibited potent antioxidant activity evaluated through DPPH assay and oxygen radical absorbing capacity (ORAC), with highest activity in hydro-alcoholic extract. All the analyzed extracts also exhibited potent inhibition, against four human pathogens namely Pseudomonas aeruginosa, Vibrio cholerae, Escherichia coli, and Shigella flexneri. Therefore, it is evident from the study that the fruit of S. chelonoides has immense potential as a nutraceutical supplement and may help in the management of nutrient deficiency and malnutrition among rural and tribal communities.
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Coscinium fenestratum (Goetgh.) Colebr. is widely used for urinary disorders and kidney stones by ethnic communities in southern India. The species is documented in various ancient Indian Ayurvedic literatures having therapeutic use in 'Ashmari' i.e., urolithiasis. The present study aims at validation of in-vitro anti-urolithiatic potential of various extracts of C. fenestratum stem along with identification and quantification of major bioactive alkaloids, i.e., berberine and palmatine through HPTLC and LC-MS/MS. Water extract showed maximum anti-urolithiatic activity which on further kinetic analysis, showed concentration dependent inhibitory delay in nucleation and aggregation of calcium oxalate crystals. Berberine and palmatine were quantified with maximum content in methanolic extract (0.478 ± 0.003 and 0.0358 ± 0.001) followed by chloroform and petroleum ether extracts. The study validates ethnobotanical use of C. fenestratum as anti-urolithiatic agent. Further, species can also be explored as a substitute for Berberis spp. for the alkaloid metabolites i.e., berberine and palmatine.
RESUMO
The present study has been planned to evaluate the impact of seasonal variation in labdane-type diterpenoids namely isoforskolin, forskolin, 1,9-dideoxyforskolin and 1-deoxyforskolin in Coleus forskholii (roots). The plant samples were harvested in different seasons from our experimental field located at CSIR-NBRI garden, Lucknow (India) and metabolite contents were estimated through validated high performance thin layer chromatography (HPTLC) method. The HPTLC plate was developed in tertiary mobile phase of toluene-ethyl acetate-methanol (8.5-1-0.05 v/v) for separation of all the four metabolites. The metabolite content viz. isoforskolin, forskolin, 1,9-dideoxyforskolin and 1-deoxyforskolin varies from 0.0247% to 0.198%, 0.238 to 0.730%, 0.056 to 0.161% and 0.0401 to 0.332% on dry weight basis respectively. The maximum content of metabolites was recorded in winter season and was found optimum for harvesting of C. forskholii roots. Optimization of harvesting season for this industrially valuable medicinal plant will lead to sustainable sources of good quality raw material to herbal drug industry.
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ETHNO PHARMACOLOGICAL RELEVANCE: Eulophia nuda, locally known as "Amarkand" is an edible orchid, traditionally used as food and ethnomedicine in arthritis, as a blood purifier, vermifuge, in bronchitis, scrofulous glands etc. AIM: The present study focuses on the proximate-nutrient analysis, metabolic profiling of bioactive phenolic acids (PA's) and validation of anti-arthritic activity in E. nuda. MATERIALS: The proximate, nutrition and element (macro-micro) content were evaluated as per standard protocols. The anti-arthritic activity was evaluated via different Invitro models and bioactive phenolics were quantified through calibrated HPLC-UV (PDA) method, as per ICH guidelines. RESULTS: The species contains a considerable amount of proximate i.e. ash, fiber, crude alkaloid, total phenolics, and flavonoid. It is a rich source of macro-micro nutrients, carbohydrates and energy, at par with conventional cereals and super-foods like finger millet, foxtail millet etc. It also contains seven PA's viz. gallic acid, protocatechuic acid, caffeic acid, syringic acid, vanillin acid, ferulic acid and quercetin. The PA's content varies from 4.00 to 83.50 µg/ml. The anti-arthritic potential of the plant extract based on several in-vitro-models showed a promising inhibitory effect on inflammation and uric acid synthesis. CONCLUSION: The study scientifically validates the traditional claims of this traditional orchid as food and ethnomedicine. The species can be commercially explored as a supplement to combat nutritional deficiency among rural communities.
Assuntos
Antioxidantes , Extratos Vegetais , Antioxidantes/farmacologia , Extratos Vegetais/farmacologia , Fenóis/farmacologia , Flavonoides/farmacologia , Suplementos Nutricionais/análiseRESUMO
Gloriosine, the predominant metabolite of Gloriosa superba L., shares chemical properties with colchicine. We analyze the microtubule-binding affinity of gloriosine at the colchicine binding site (CBS) using an in silico-in vivo approach. The In silico docking of gloriosine showed a binding score of (-) 7.5 kcal/Mol towards ß-tubulin at CBS and was validated by overlapping the coupling pose of the docked ligand with co-crystallized colchicine. 2D plots (Ligplot +) showed > 85% overlap between gloriosine and colchicine. The ADMET profile of gloriosine was in accordance with Lipinski's rule of five. Gloriosine belongs to class II toxicity with anLD50 value of 6 mg/kg. In vivo and transmission electron microscopy studies revealed that gloriosine induces abnormalities in cell division such as condensed chromosomes in C-metaphase and enlarged nucleus with increased nuclear material. Gloriosine treated cells exhibited mitotic index of about 14% compared to control of 24% and high anti-proliferative activity i.e. 63.94% cell viability at a low concentration (0.0004 mg/ml). We conclude that gloriosine has a strong affinity for ß-tubulin at CBS and thus can be used as a colchicine alternative in cytology and other clinical conditions.