蔓性千斤拔黄酮类成分对乙酰胆碱酯酶抑制作用

王岩; 袁凤娟; 张萌; 于璐; 刘文宇; 吴红艳; 高建伟; 王拓一

doi:10.13386/j.issn1002-0306.2021040243

蔓性千斤拔黄酮类成分对乙酰胆碱酯酶抑制作用

Acetylcholinesterase Inhibition Effect of Flavonoids from Flemigia philippinensis

摘要

摘要: 为研究蔓性千斤拔活性成分对乙酰胆碱酯酶（Acetylcholinesterase, AChE）的抑制作用，本文以蔓性千斤拔的根为研究对象，采用不同溶剂系统针对黄酮成分进行分级萃取，进一步分离纯化出四种黄酮化合物，采用可逆抑制动力学方法研究了不同溶剂提取物和四种黄酮化合物对AChE的抑制作用及相关抑制常数。结果表明，蔓性千斤拔根的不同溶剂提取物及四种黄酮化合物（Genistein、Philippin C、Philippin D和Flemiphilippinone A）对AChE有较强的抑制作用, 抑制类型为混合型抑制（Mix type），半抑制浓度（IC₅₀）在（57.86±0.67）~（127.28±1.22）µmol/L之间，抑制常数K_i为（54.8±0.43）~（120.58±1.35）µmol/L。研究结果可为发现高效乙酰胆碱酯酶抑制剂先导化合物及千斤拔食品的开发和综合利用提供理论基础及试验依据。

Abstract: In order to study the inhibitory effect of the active ingredients of the Flemigia philippinensis roots on acetylcholinesterase (AChE), the roots of the Flemigia philippinensis were used as raw materials, and different solvent systems were applied to fractionate and extract flavonoids, and then further separate and purify them. Reversible inhibition kinetics method were applied to study the inhibitory effect of different solvent extracts and four flavonoids on AChE and related constants. The results showed that the different solvent extracts and the four favonoids (Genistein, Philippin C, Philippin D and Flemiphilippinone A) from the roots of Flemigia philippinensis had a strong inhibitory effect on AChE. The inhibition type was mixed type inhibition, and the half inhibition concentration (IC₅₀) was (57.86±0.67)~(127.28±1.22) µmol/L, the inhibition constant K_i was (54.8±0.43)~(120.58±1.35) µmol/L. The research results could provide a theoretical basis and experimental basis for the discovery of high-efficiency acetylcholinesterase inhibitor lead compounds and the development and comprehensive utilization of Flemigia philippinensis related foods.