胰脂肪酶抑制剂电位滴定筛选法的研究

Extraction and isolation of baicalin and its inhibitory activity against pancreatic lipase

建立了一种简单快速的胰脂肪酶抑制剂筛选研究的新方法,特别适用于深颜色或浑浊体系的天然药物活性分析。本研究采用临床减肥药Orlistat论证了电位滴定筛选胰脂肪酶抑制活性的可靠性和稳定性,探讨了酶抑制活性测定的影响因素,并成功应用于天然药物活性成分—黄芩苷的抑制活性研究。研究结果显示,Orlistat对胰脂肪酶具有很强的抑制活性(IC50=0.011g/L),实验结果与临床效果吻合,表明构建的胰脂肪酶抑制活性电位滴定筛选法是可靠的。此外,黄芩苷也显示出良好的胰脂肪酶抑制活性,其IC50为0.027 g/L。本研究为从天然药物筛选胰脂肪酶抑制剂作为绿色减肥药提供了一种新颖的研究思路。

A simple and rapid method was developed for the screening of pancreatic lipase inhibitors, which is especially suitable for the activity analysis of dark or turbid natural medicines. Here, orlistat （clinical weight-loss drug） was used to demonstrate the reliability and stability of potentiometrie titration screening for inhibitory activity of pancreatic lipase, the influencing factors for the determination of enzyme inhibition were explored. Then, it was successfully applied to screening the inhibitory activity of the active ingredients of natural medicine baiealin. The research results show that orlistat has a strong inhibitory activity on pancreatic lipase （IC50= 0. 011g/L） , consistent with the clinical effect. It indicates that the developed screening method based on potentiometrie titration is reliable for screening pancreatic lipase inhibitory activity. In addition, baiealin also has good inhibitory activity for pancreatic lipase and its IC50 is 0. 027g/L. The study provides a new research method for screening of pancreatic lipase inhibitors from natural medicines as a green anti-obesity drug.