Inhibitors of pancreatic a-amylase offer an effective strategy to lower the levels of postprandial hyperglycemia by controlof starch breakdown. Among 86 fungal endophytes isolated from 15 medicinal plants Aspergillus ...Inhibitors of pancreatic a-amylase offer an effective strategy to lower the levels of postprandial hyperglycemia by controlof starch breakdown. Among 86 fungal endophytes isolated from 15 medicinal plants Aspergillus terreus-AFl04S, Aspergillusegypticus-HT166S and Penicillium sp.-CC200 exhibited strong pancreatic amylase inhibitory potential were selected. Endophyteswere subjected to ethyl acetate extraction and tested for a-amylase inhibition, in order to assess and evaluate their inhibitory potentialon pancreatic a-amylase. Analysis showed concentration dependent enzyme inhibition up to 83% with half inhibition （IC50） valuesfor less 25 mg.mL1, which is lower than acarbose as control. It was observed 3-fold increasing of Vmax and maintenance Km atcontrol level in the presence of extracts A. terreus-AFl04S and Penicillium sp.-CC200, while in presence of extract A.egypticus-HT166S Km was doubled, and Vmax was maintained at the control level. Kinetic studies allow proposing the competitivemode of a-amylase inhibition by extracts A. egypticus-HT166S and uncompetitive inhibition by extracts A, terreus-AFl04S andPenicillium sp.-CC200.展开更多
文摘Inhibitors of pancreatic a-amylase offer an effective strategy to lower the levels of postprandial hyperglycemia by controlof starch breakdown. Among 86 fungal endophytes isolated from 15 medicinal plants Aspergillus terreus-AFl04S, Aspergillusegypticus-HT166S and Penicillium sp.-CC200 exhibited strong pancreatic amylase inhibitory potential were selected. Endophyteswere subjected to ethyl acetate extraction and tested for a-amylase inhibition, in order to assess and evaluate their inhibitory potentialon pancreatic a-amylase. Analysis showed concentration dependent enzyme inhibition up to 83% with half inhibition （IC50） valuesfor less 25 mg.mL1, which is lower than acarbose as control. It was observed 3-fold increasing of Vmax and maintenance Km atcontrol level in the presence of extracts A. terreus-AFl04S and Penicillium sp.-CC200, while in presence of extract A.egypticus-HT166S Km was doubled, and Vmax was maintained at the control level. Kinetic studies allow proposing the competitivemode of a-amylase inhibition by extracts A. egypticus-HT166S and uncompetitive inhibition by extracts A, terreus-AFl04S andPenicillium sp.-CC200.
