川芎嗪结构改造与活性研究进展

Derivatives Research Progress on Structural Modification and Activity of Ligustrazine

川芎嗪(TMP)是从传统中药川芎的根茎中提取的一种生物碱,化学名为四甲基吡嗪,是川芎的主要活性成分之一,临床中用于治疗缺血性心脑血管等疾病。但由于其生物活性较低、半衰期短等的缺点,限制了在临床上的使用。因此需要对川芎嗪进行结构修饰和改造以改善其缺点,本文旨在从药物设计与结构改造的方向,综述近年来对川芎嗪及其衍生物的研究进展。

Ligustrazine(TMP)is a kind of alkaloid extracted from the root of traditional medicine known as Chuanxiong hort which is one of the main active components of ligusticum chuanxiong Hort.Ligustrazine has been used as clincal medication for ischemic cardiovascular and cerebrovascular diseases.However,as its short half life of ligustrazine seriously limits its application in clinical practice.In order to improve its shortcomings,it is necessary to modify the structure of ligustrazine.Hence,this review aims to conclude the recent prominent advances of ligustrazine and ligustrazine derivatives from the drug design and the modify of the structure in the past five years.