Screening And Inhibition Kinetics Of A-Glucosidase Inhibitors In Vitro

Diabetes mellitus is a kind of systemic disease which is characterized by high blood sugar and marked by metabolic disorder. Moreover, it's closely related to insulin secretion. In recent years, the incidence of diabetes has increased year by year, and this disease has become a "health killer" that threat to mankind in the third place. Therefore it's a worldwide problem how to prevent and control diabetes effectivelyA-glucosidase inhibitors can retard the absorption of glucose to improve postprandial hyperglycemia effectively. They are helpful for impeding the progress of diabetes and its complications. A-glucosidase inhibitors are applied for the treatment of diabetes extensively. Currently there are three kinds used for clinical treatment: acarbose, voglibose and miglitol. The type of these drugs are small and there is also some side effects though they have good curative effects. Consequently, it's significant to develop new bettera-glucosidase inhibitors. Screening a-glucosidase inhibitors from traditional Chinese medicines (TCM) is a popular pathway to develop natural medicines to reduce blood glucose.We established an a-glucosidase inhibitors screening model in vitro. Then we screened effective a-glucosidase inhibitors from 111 kinds of extracts in the TCM. Results: Forty-eight extracts among the 21 kinds of TCM tested inhibite a-glucosidase at the concentration of 50mg/ml, and eight extracts are as effective as acarbose.Our cooperators in Chengdu Biological Research Institute of The Chinese Academy of Sciences have separated and purified broussonetinine B and broussonetine B on the basis of the screening results. We use the reverted gut sac method to study the a-glucosidase activity inhibition of this two substances. The results showed that the inhibition of both alkaloids was enhanced with the dose increased. And the 50% inhibitory concentration were 0.530 mg / ml, 0.445 mg / ml.This paper studies provide the basis of lead compounds for further research and development of new a-glucosidase inhibitors.