文献类型：期刊文献

中文题名：川芎嗪类衍生物药理活性的研究进展

英文题名：Research progress on pharmacological activities of ligustrazine derivatives

作者：赵君利[1];程菊[2];陈建军[3];谢小冬[1,2]

第一作者：赵君利

机构：[1]甘肃中医药大学基础医学院,甘肃兰州730020;[2]兰州大学基础医学院遗传学研究所,甘肃兰州730020;[3]兰州大学功能有机分子化学国家重点实验室,甘肃兰州730000

第一机构：甘肃中医药大学基础医学院（敦煌医学研究所）

年份：2023

卷号：38

期号：3

起止页码：340

中文期刊名：华西药学杂志

外文期刊名：West China Journal of Pharmaceutical Sciences

收录：CSTPCD;;CSCD:【CSCD_E2023_2024】；

基金：兰州市新冠肺炎防控技术研究项目(2020-XG-37)。

语种：中文

中文关键词：川芎;川芎嗪类衍生物;抗氧化;抗心血管疾病;抗肿瘤;神经保护;抗菌;抗炎

外文关键词：Ligustrazine;Ligustrazine derivatives;Antioxidant;Anti-cardiovascular disease;Antitumor;Neuroprotection;Antibacterial;Anti-inflammatory

摘要：川芎嗪是中药川芎的主要活性成分,已用于临床治疗脑血栓、冠心病和心绞痛药。因川芎嗪的代谢快、半衰期短、生物利用度低,严重制约了其在临床上的应用。故对其进行了化学结构改造和修饰,设计并合成川芎嗪的衍生物,成为提高川芎疗效的研究热点之一。目前,在人工合成哌嗪、肉桂酸、苯乙烯、酰基胍、酰胺、姜黄素和三萜衍生物等化合物方面已取得了一定成果,并获得了抗氧化、治疗心血管疾病、抗肿瘤、神经保护、抗菌及抗炎等药理学特性。现针对川芎嗪的化学结构修饰及其药理学活性研究进行综述,为川芎嗪的深入研究和临床合理应用提供参考。
Ligustrazine is the main active ingredient of the traditional medicine Ligusticum chuanxiong,which has recently been used as a clinical drug for the treatment of cerebral thrombosis,coronary heart disease and angina pectoris.Ligustrazine′s fast metabolism,short half-life and low bioavailability severely restrict its clinical application.Therefore,to design and synthesize derivatives of ligustrazine based on the metabolic characteristics of ligustrazine have become a research hotspot to improve the curative effect of ligustrazine.Some achievements have been made in compounds such as triterpenoid derivatives,and have pharmacological properties such as antioxidant,anti-cardiovascular disease,anti-cancer,neuroprotective,antibacterial and anti-inflammatory properties.In this paper,the chemical structure modification and pharmacological activity of ligustrazine are reviewed,which can provide a reference for the in-depth research and clinical rational application of ligustrazine.