Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.2.1.20 (alpha-glucosidase)
 4,237 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Extracts of eleven traditional Chinese medicines (TCM) with a reputation of usefulness in treating diabetes mellitus were examined for alpha-glucosidase and alpha-amylase inhibitory activities in vitro. The extract with the highest activity was selected for further characterization. The extract of the root bark of Aralia taibaiensis (EAT) outperformed other extracts in the assays with IC50 values of 0.48 +/- 0.01 mg/mL (BSG), 0.41 +/- 0.02mg/mL (SCG), 0.61 +/- .03mg/mL (BLA) and 0.77 +/- 0.03mg/mL (PPA), respectively. To identify which constituents were responsible for the activities, thirteen triterpenoid saponins were isolated from EAT and examined for their inhibitory effects against alpha-glucosidase and alpha-amylase. The results revealed that saponins 2, 3, 4 (IC50: 0.83 +/- 0.05 microM for BSG and IC50: 0.72 +/- 0.03 microM for SCG), 5, 6, 7, 9, 10, 11 and 12 (IC50: 1.07 +/- 0.04 micro.M for BSG and IC50: 0.93 +/- 0.05 micro.M for SCG) showed alpha-glucosidase inhibitory activities, while 2, 3, 4 (IC50: 0.93 +/- 0.04 micro.M for PPA), 5, 6, 7, 9, 10, 11 and 12 (IC50: 1.02 +/- 0.03 micro.M for PPA) possessed significant alpha-amylase inhibitory activities. In addition, the structure-activity relationship of the thirteen saponins was discussed based on their structure features and diabetes mellitus related activities. It is suggested that the glucuronic acid unit at C-3 of the aglycone is the imperative functional group of the antidiabetic activities, and two characteristic structural features are responsible for the remarkable alpha-glucosidase and alpha-amylase inhibitory activities.
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PMID:alpha-Glucosidase and alpha-amylase inhibitory activities of saponins from traditional Chinese medicines in the treatment of diabetes mellitus. 2370 Jul 98