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Bioassay-guided isolation and identification of antidiabetic compounds from Garcinia cowa leaf extract.

ABSTRACT: Garcinia cowa Roxb. ex Choisy (Clusiaceae) is a Thai local edible plant, which has been used for the treatment of diabetes. The aim of this study is to discover and identify bioactive compounds related to antidiabetic properties from the leaf extract of G. cowa. ?-Glucosidase inhibitory bioassay-guided isolation of the ethyl acetate extract of the leaves of G.cowa resulted in the isolation and identification of 11 compounds. Of these, a decahydro-1H-xanthene derivative, garciniacowone K (1), was identified as a novel compound. Their structures were characterized by spectroscopic data and by comparison of their NMR spectroscopic data with those previously reported. All compounds were evaluated for their ?-glucosidase inhibitory and glucose consumption activities. Compound 2 showed the highest efficacy in inhibiting ?-glucosidase enzyme and promoting glucose consumption activity by 3T3-L1 cells, with IC50 values of 0.5 ?M and 13.1 ?M, respectively, without causing toxicity to cells.

SUBMITTER: Phukhatmuen P

PROVIDER: S-EPMC7184531 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature

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Bioassay-guided isolation and identification of antidiabetic compounds from Garcinia cowa leaf extract.

Phukhatmuen Piyaporn P Raksat Achara A Laphookhieo Surat S Charoensup Rawiwan R Duangyod Thidarat T Maneerat Wisanu W

Heliyon 20200425 4

Garcinia cowa Roxb. ex Choisy (Clusiaceae) is a Thai local edible plant, which has been used for the treatment of diabetes. The aim of this study is to discover and identify bioactive compounds related to antidiabetic properties from the leaf extract of G. cowa. α-Glucosidase inhibitory bioassay-guided isolation of the ethyl acetate extract of the leaves of G.cowa resulted in the isolation and identification of 11 compounds. Of these, a decahydro-1H-xanthene de ...[more]

PMID: 32368636

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Project description:Acacia hydaspica possesses varied pharmacological attributes. We aimed to examine the antimicrobial potential and isolate the active antimicrobial metabolites. The plant extract was fractionated and the antimicrobial activity of the crude extract, fractions and compounds was tested by agar well diffusion and agar tube dilution and broth dilution methods. Bacterial strains selected for bioactivity testing were Staphylococcus aureus, Enterococcus faecalis, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Acinetobacter baumannii while selected strains from kingdom fungi were Candida albicans, Cryptococcus neoformans, Fusarium solani and Aspergillus. The active compounds were isolated from Acacia hydaspica by bioassay-guided fractionation and identified by nuclear magnetic resonance and spectroscopic techniques. S. aureus cell surface proteins, Autolysins (Atl), Clumping factor A (ClfA), and Fibronectin Binding Proteins (FnBP), were molecularly docked with Catechin 3-O-gallate (CG) and Methyl gallate (MG) and binding energy and molecular interactions between the proteins and compounds were analyzed. Ethyl acetate (AHE) and Butanol (AHB) fractions of A. hydaspica were the most active fractions against tested microbial strains. Therefore, both were subjected to bioassay-directed fractionation which led to the isolation of one pure active antimicrobial AHE and one active pure compound from AHB fraction besides active enriched isolates. Methyl-gallate (MG) and catechin-3-gallate (CG) are active compounds extracted from AHE and AHB fractions respectively. In antibacterial testing MG significantly inhibited the growth of E. coli (MIC50 = 21.5 µg/ml), B. subtilus (MIC50 = 23 µg/ml) and S. aureus (MIC50 = 39.1 µg/ml) while moderate to low activity was noticed against other tested bacterial strains. Antifungal testing reveals that MG showed potent antifungal activity against F. solani (MIC50 = 33.9 µg/ml) and A. niger (MIC50 = 41.5 µg/ml) while lower antifungal activity was seen in other tested strains. AHB fractions and pure compound (CG) showed specific antibacterial activity against S. aureus only (MIC50 = 10.1 µg/ml) while compound and enriched fractions showed moderate to no activity against other bacterial and fungal strains respectively. Molecular docking analysis revealed that CG interacted more strongly with the cell surface proteins than MG. Among these proteins, CG made a stronger complex with ClfA (binding affinity - 9.7) with nine hydrophobic interactions and five hydrogen bonds. Methyl gallate (MG) and catechin 3-O-gallate (CG) are the major antimicrobial compound from A. hydaspica that inhibit the growth of specific microbes. The occurrence of MG and CG endorse the traditional antimicrobial applicability of A. hydaspica, and it can be a legitimate alternative to control specific microbial infections.

Project description:BackgroundOptimal adoption of the malaria transmission-blocking strategy is currently limited by lack of safe and efficacious drugs. This has sparked the exploration of different sources of drugs in search of transmission-blocking agents. While plant species have been extensively investigated in search of malaria chemotherapeutic agents, comparatively less effort has been channelled towards exploring them in search of transmission-blocking drugs. Artemisia afra (Asteraceae), a prominent feature of South African folk medicine, is used for the treatment of a number of diseases, including malaria. In search of transmission-blocking compounds aimed against Plasmodium parasites, the current study endeavoured to isolate and identify gametocytocidal compounds from A. afra.MethodsA bioassay-guided isolation approach was adopted wherein a combination of solvent-solvent partitioning and gravity column chromatography was used. Collected fractions were continuously screened in vitro for their ability to inhibit the viability of primarily late-stage gametocytes of Plasmodium falciparum (NF54 strain), using a parasite lactate dehydrogenase assay. Chemical structures of isolated compounds were elucidated using UPLC-MS/MS and NMR data analysis.ResultsTwo guaianolide sesquiterpene lactones, 1α,4α-dihydroxybishopsolicepolide and yomogiartemin, were isolated and shown to be active (IC50 < 10 μg/ml; ~ 10 μM) against both gametocytes and intra-erythrocytic asexual P. falciparum parasites. Interestingly, 1α,4α-dihydroxybishopsolicepolide was significantly more potent against late-stage gametocytes than to early-stage gametocytes and intra-erythrocytic asexual P. falciparum parasites. Additionally, both isolated compounds were not overly cytotoxic against HepG2 cells in vitro.ConclusionThis study provides the first instance of isolated compounds from A. afra against P. falciparum gametocytes as a starting point for further investigations on more plant species in search of transmission-blocking compounds.

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Bioassay-guided isolation and identification of antidiabetic compounds from Garcinia cowa leaf extract.

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Bioassay-guided isolation and identification of antidiabetic compounds from <i>Garcinia cowa</i> leaf extract.

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