中药活性成分含笑内酯的结构修饰和抗肿瘤活性研究进展  

Advances on structural modifications and antitumor activities of micheliolide,an active ingredient from Chinese medicines

作　　者：孟祥伟 曹原[1] 张剑桥 任帅 庞晓明 MENG Xiang-wei;CAO Yuan;ZHANG Jian-qiao;REN Shuai;PANG Xiao-ming(Department of Drug Clinical Trials,Zibo Central Hospital,Zibo 255000,China;Department of Medicinal Chemistry,School of Pharmacy,Qingdao University,Qingdao 266021,China)

机构地区：[1]淄博市中心医院临床试验研究中心,山东淄博255400 [2]青岛大学药学院,山东青岛266021

出　　处：《化学研究与应用》2024年第5期931-941,共11页Chemical Research and Application

基　　金：国家自然科学基金项目(81600348)资助;山东省自然科学基金项目(ZR202111230327)资助;山东省中医药科技项目项目(Q-2022012)资助;淄博市卫生健康青年卓越人才孵化项目(淄卫办字<2022>156)资助;山东省医学会治疗药物监测科研基金项目(YXH2020ZX051)资助。

摘　　要：含笑内酯(Micheliolide)是一种愈创木烷型倍半萜内酯,主要存在于黄兰、含笑等传统中药中,具有抗肿瘤、抗炎及抗肺纤维化等药理作用,在药学领域受到广泛关注。近年来,研究人员围绕含笑内酯作了大量的结构修饰工作,已成功开发了多个具有潜在活性的抗癌药物,其衍生物ACT001已在多个国家开展了临床试验研究。本文通过查阅近年来国内外相关文献,综述了天然药物含笑内酯的来源、结构修饰方法、抗肿瘤活性和药理作用机制研究进展,以期为探索愈创木烷型天然药物在临床上的应用提供参考。Micheliolide,a natural guaiane-type sesquiterpenoid,is primarily found in traditional Chinese medicines such as Huanglan and Hanxiao.It exhibits pharmacological effects,including anti-tumor,anti-inflammatory,and anti-pulmonary fibrosis properties that have attracted widespread attention in the field of pharmacy.In recent years,researchers have conducted extensive studies on structural modifications of micheliolide.Currently,several anti-tumor drugs have been approved based on micheliolide,and its derivative ACTO01 has entered the clinical stage in several countries.In this paper the occurrences,structural modifications,and mechanisms of micheliolide were reviewed to provide references for the development and clinical research of basic guaiane-type sesquiterpenes.

关 键 词：含笑内酯 作用机制 结构修饰 抗肿瘤活性 

分 类 号：O623.624[理学—有机化学]