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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 for the screening of pancreatic lipase inhibitors was developed. It is especially suitable for the analysis of natural drug activity in dark-colored or turbid systems. In this study, the clinical slimming drug Orlistat was used to demonstrate the reliability and stability of pancrelipase inhibition by potentiometric titration. The factors affecting the determination of enzyme inhibition activity were discussed. The inhibitory activity of baicalin, a natural active ingredient, was also successfully investigated. The results showed that Orlistat had a strong inhibitory activity on pancreatic lipase (IC50 = 0.011g / L). The experimental results were in good agreement with clinical results, indicating that the constructed pancreatic lipase inhibition potentiometric titration method is reliable. In addition, baicalin also showed good pancreatic lipase inhibitory activity with an IC50 of 0.027 g / L. This study provides a novel research approach for screening pancreatic lipase inhibitors from natural medicines as green diet pills.