In vitro evaluation of the α-glucosidase inhibitory potential of methanolic extracts of traditionally used antidiabetic plants

Bhatia, Astha; Singh, Balbir; Arora, Rohit; Arora, Saroj

doi:10.1186/s12906-019-2482-z

Cited by 98 publications

(53 citation statements)

References 31 publications

(39 reference statements)

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“…Kidane et al [37] reported that the extraction of Psiadia punctulata leaves in a methanolic solvent produced an extract with high AGI activity. A similar result was found by Bhatia et al [38] who reported the high AGI activity of a methanolic extract of Cornus capitata Wall leaves. Extraction with aqueous methanol was shown to be better for the recovery of the largest amount of phenolic compounds from Moringa oleifera and rice bran, which are related to antioxidant activity [39,40].…”

Section: Discussionsupporting

confidence: 88%

Characterization of α-Glucosidase Inhibitors from Psychotria malayana Jack Leaves Extract Using LC-MS-Based Multivariate Data Analysis and In-Silico Molecular Docking

et al. 2020

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Psychotria malayana Jack has traditionally been used to treat diabetes. Despite its potential, the scientific proof in relation to this plant is still lacking. Thus, the present study aimed to investigate the α-glucosidase inhibitors in P.malayana leaf extracts using a metabolomics approach and to elucidate the ligand–protein interactions through in silico techniques. The plant leaves were extracted with methanol and water at five various ratios (100, 75, 50, 25 and 0% v/v; water–methanol). Each extract was tested for α-glucosidase inhibition, followed by analysis using liquid chromatography tandem to mass spectrometry. The data were further subjected to multivariate data analysis by means of an orthogonal partial least square in order to correlate the chemical profile and the bioactivity. The loading plots revealed that the m/z signals correspond to the activity of α-glucosidase inhibitors, which led to the identification of three putative bioactive compounds, namely 5′-hydroxymethyl-1′-(1, 2, 3, 9-tetrahydro-pyrrolo (2, 1-b) quinazolin-1-yl)-heptan-1′-one (1), α-terpinyl-β-glucoside (2), and machaeridiol-A (3). Molecular docking of the identified inhibitors was performed using Auto Dock Vina software against the crystal structure of Saccharomyces cerevisiae isomaltase (Protein Data Bank code: 3A4A). Four hydrogen bonds were detected in the docked complex, involving several residues, namely ASP352, ARG213, ARG442, GLU277, GLN279, HIE280, and GLU411. Compound 1, 2, and 3 showed binding affinity values of −8.3, −7.6, and −10.0 kcal/mol, respectively, which indicate the good binding ability of the compounds towards the enzyme when compared to that of quercetin, a known α-glucosidase inhibitor. The three identified compounds that showed potential binding affinity towards the enzymatic protein in molecular docking interactions could be the bioactive compounds associated with the traditional use of this plant.

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Section: Discussionsupporting

confidence: 88%

Characterization of α-Glucosidase Inhibitors from Psychotria malayana Jack Leaves Extract Using LC-MS-Based Multivariate Data Analysis and In-Silico Molecular Docking

et al. 2020

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“…The inhibition of these enzymes is able to delay the absorption of monosaccharides from dietary complex carbohydrates, preventing any sudden rise in mealinduced blood glucose level, and therefore are involved in controlling the glucose level in the blood 7 . This is well correlated with the interesting finding that reveals that the a-glucosidase enzyme inhibitor is capable of slowing carbohydrate digestion, resulting in less efficient glucose absorption and thus decreasing postprandial hyperglycaemia 8 .…”

Section: Introductionsupporting

confidence: 67%

Inhibitory evaluation ofCurculigo latifoliaon α-glucosidase, DPP (IV) andin vitrostudies in antidiabetic with molecular docking relevance to type 2 diabetes mellitus

Zabidi

Ishak

Hamid

et al. 2020

Journal of Enzyme Inhibition and Medicinal Chemistry

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The inhibition of a-glucosidase and DPP enzymes capable of effectively reducing blood glucose level in the management of type 2 diabetes. The purpose of the present study is to evaluate the inhibitory potential of a-glucosidase and DPP (IV) activity including with the 2-NBDG uptake assay and insulin secretion activities through in vitro studies. The selected of active compounds obtained from the screening of compounds by LC-MS were docked with the targeted enzyme that involved in the mechanism of T2DM. From the results, root extracts displayed a better promising outcome in a-glucosidase (IC 50 2.72 ± 0.32) as compared with the fruit extracts (IC 50 3.87 ± 0.32). Besides, root extracts also displayed a better activity in the inhibition of DPP (IV), enhance insulin secretion and glucose uptake activity. Molecular docking results revealing that phlorizin binds strongly with a-glucosidase, DPP (IV) and Insulin receptor (IR) enzymes with achieving the lowest binding energy value. The present work suggests several of the compounds have the potential that contribute towards inhibiting a-glucosidase and DPP (IV) and thus effective in lowering post-prandial hyperglycaemia.

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“…The IC 50 value of sub fraction of chloroform of G . sylvestre against α-glucosidase is 85.73 ± 0.001 µg/mL and it is better as compared to extract of leaves of Petalostigma pubescens (IC 50 value of 167.83 ± 23.82 μg/mL) 26 and ethyl acetate fraction of Cornus capitata (IC 50 value of 50 μg/mL) 29 . The bioactive sub fraction derivative of F .…”

Section: Discussionmentioning

confidence: 94%

Characterization and evaluation of mycosterol secreted from endophytic strain of Gymnema sylvestre for inhibition of α-glucosidase activity

Ranjan

Singh

Khare

et al. 2019

Sci Rep

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Endophytic fungi produce various types of chemicals for establishment of niche within the host plant. Due to symbiotic association, they secrete pharmaceutically important bioactive compounds and enzyme inhibitors. In this research article, we have explored the potent α-glucosidse inhibitor (AGI) produced from Fusarium equiseti recovered from the leaf of Gymnema sylvestre through bioassay-guided fraction. This study investigated the biodiversity, phylogeny, antioxidant activity and α-glucosidse inhibition of endophytic fungi isolated from Gymnema sylvestre. A total of 32 isolates obtained were grouped into 16 genera, according to their morphology of colony and spores. A high biodiversity of endophytic fungi were observed in G. sylvestre with diversity indices. Endophytic fungal strain Fusarium equiseti was identified through DNA sequencing and the sequence was deposited in GenBank database (https://ncbi.nim.nih.gov) with acession number: MF403109. The characterization of potent compound was done by FTIR, LC-ESI-MS and NMR spectroscopic analysis with IUPAC name 17-(5-ethyl-6-methylheptan-2-yl)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a] phenanthren-3-ol. The isolated bioactive compound showed significant α-amylase and α-glucosidase inhibition activity with IC50 values, 4.22 ± 0.0005 µg/mL and 69.72 ± 0.001 µg/mL while IC50 values of acarbose was 5.75 ± 0.007 and 55.29 ± 0.0005 µg/mL respectively. This result is higher in comparison to other previous study. The enzyme kinetics study revealed that bioactive compound was competitive inhibitor for α-amylase and α-glucosidase. In-silico study showed that bioactive compound binds to the binding site of α-amylase, similar to that of acarbose but with higher affinity. The study highlights the importance of endophytic fungi as an alternative source of AGI (α-glucosidase inhibition) to control the diabetic condition in vitro.

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In vitro evaluation of the α-glucosidase inhibitory potential of methanolic extracts of traditionally used antidiabetic plants

Cited by 98 publications

References 31 publications

Characterization of α-Glucosidase Inhibitors from Psychotria malayana Jack Leaves Extract Using LC-MS-Based Multivariate Data Analysis and In-Silico Molecular Docking

Characterization of α-Glucosidase Inhibitors from Psychotria malayana Jack Leaves Extract Using LC-MS-Based Multivariate Data Analysis and In-Silico Molecular Docking

Inhibitory evaluation ofCurculigo latifoliaon α-glucosidase, DPP (IV) andin vitrostudies in antidiabetic with molecular docking relevance to type 2 diabetes mellitus

Characterization and evaluation of mycosterol secreted from endophytic strain of Gymnema sylvestre for inhibition of α-glucosidase activity

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