Biflavones from Ginkgo biloba as novel pancreatic lipase inhibitors: Inhibition potentials and mechanism
Biflavones from Ginkgo biloba as novel pancreatic lipase inhibitors: Inhibition potentials and mechanism
复制标题
银杏叶双黄酮作为新型胰脂肪酶抑制剂：抑制潜力和机制
DOI：
10.1016/j.ijbiomac.2018.07.085
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发表时间：
2018-10-15
影响因子：
8.2
通讯作者：
Hou, Jie
中科院分区：
文献类型：
--
作者：
Liu, Ping-Kun;Weng, Zi-Miao;Hou, Jie
减少脂质吸收已被认为是发现治疗肥胖和超重的新药的有吸引力的方法。银杏叶提取物在东西方国家已被广泛用于治疗代谢性疾病（如高脂血症），但银杏叶中的生物活性成分及其作用机制尚未完全阐明。本研究旨在探讨甘草中主要黄酮类化合物的抑菌活性及其作用机制。银杏叶对胰脂肪酶（PL）的作用，这是调节脂质吸收的关键目标。结果清楚地表明，所有测试的双黄酮在G。银杏黄酮类化合物（包括异银杏黄酮、银杏黄酮、银杏黄酮和scidopitysin）对PL表现出强至中等的抑制作用，IC_（50）值在2.90 μ M至12.78 μ M之间。进一步的动力学分析和分子对接模拟研究表明，异银杏黄酮、银杏黄酮和银杏黄酮是有效的PL抑制剂（K-i
Reduction of lipid absorption has been recognized as an attractive approach for the discovery of new drugs to treat obesity and overweight. The leave extract of Ginkgo biloba has been widely used for the treatment of metabolic diseases (such as hyperlipidemia) in both eastern and western countries, but the bioactive compounds in Ginkgo biloba and the underlying mechanism have not been fully characterized. This study aimed to investigate the inhibition potentials and mechanism of major biflavones from G. biloba on pancreatic lipase (PL), a key target regulating lipid absorption. The results clearly demonstrated that all tested biflavones in G. biloba including isoginkgetin, bilobetin, ginkgetin and sciadopitysin, displayed strong to moderate inhibitory effects on PL with the IC50 values ranging from 2.90 mu M to 12.78 mu M. Further investigations on both inhibition kinetic analyses and docking simulations demonstrated that isoginkgetin, bilobetin and ginkgetin were potent PL inhibitors (K-i