植物来源的脂肪酶抑制剂的筛选

Screening Lipase Inhibitors from Plant Sources

目的:随着人们生活水平的不断提高,肥胖问题日趋严重。胰脂肪酶抑制剂是药物治疗肥胖的有效途径之一,本文主要通过筛选一些植物来源的化合物来寻找具有胰脂肪酶抑制作用的天然活性物。方法:以4-甲基伞形酮油酸酯作为底物,用荧光检测的方法测定对胰脂肪酶(triacylglycerol lipase,EC 3.1.1.3)的抑制活性。结果:皂苷类化合物可有效地抑制胰脂肪酶的活性,其中薯蓣皂苷,毛地黄皂苷和皂树皂苷的活性较强,IC50值分别为3.5μM、2.7μM和3.0μg/mL。黄酮类化合物也有抑制脂肪酶活性的作用,在浓度为100μM时,对胰脂肪酶活性的抑制率在35.7%到68.2%之间。相比之下,相同浓度的苷元类化合物和咖啡酸衍生物对胰脂肪酶活性的抑制作用低于50%,而氨基糖类化合物的抑制率则低于15%。结论:皂苷这类植物的次级代谢产物具有良好的抑制脂肪酶活力的作用,黄酮次之,并且这两类化合物是从植物中提取的,毒性小,安全性高,可以为进一步研发治疗肥胖药物提供理论依据。

Objective： With the improvement of living standards, the obesity has become a serious problem all over the world. Pancreatic lipase inhibitors are one class of the effective anti-obesity agents. In this work, the plant derived compounds were screened to identify pancreatic lipase inhibitor from natural sources. Methods： Plant derived compounds were screened against porcine pancreatic lipase （triacylglycerol lipase, EC 3.1.1.3） by using 4-methylumbelliferyl oleate as the substrate. Results： The saponins could inhibite the activation of pancreatic lipase effectively. Dioscin, digit0nin and quillaja showed potential inhibitory activity with the ICs0s of 3.5 txM, 2.7 ixM and 3.0 txg/mL, respectively. In addition, flavones exhibited effective lipase inhibition, the inhibition ratio was from 35.7% to 68.2%. But the inhibitory ratio ofsapogenins and flavones on pancreatic lipase were less than 50%, and the inhibitor ratio ofimino sugar.was less than 15%. Conclusions： Saponins and fiavones, plant derived compounds, showed effective inhibition on pancreatic lipase with low toxicity, which could be a support for the development of antiobesity drugs.