川芎嗪类衍生物药理活性的研究进展  

Research progress on pharmacological activities of ligustrazine derivatives

作　　者：赵君利 程菊 陈建军 谢小冬 ZHAO Junli;CHENG Ju;CHEN Jianjun;XIE Xiaodong(School of Basic Medicine,Gansu University of Traditional Chinese Medicine,Lanzhou,Gansu,730020 P.R.China;Institute of Genetics,School of Basic Medicine,Lanzhou University,Lanzhou,Gansu,730020 P.R.China;State Key Laboratory of Functional Organic Molecular Chemistry,Lanzhou University,Lanzhou,Gansu,730000 P.R.China)

机构地区：[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

出　　处：《华西药学杂志》2023年第3期340-344,共5页West China Journal of Pharmaceutical Sciences

基　　金：兰州市新冠肺炎防控技术研究项目(2020-XG-37)。

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.

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 

分 类 号：R96[医药卫生—药理学]