青蒿素C-16位新型衍生物及生物活性的研究进展  

Research progress on novel derivatives of artemisinin C-16 and their biological activities

作　　者：荣丽 周文[2] 赵云辉[1] Rong Li;Zhou Wen;Zhao Yunhui(College of Chemistry and Chemical Engineering,Hunan University of Science and Technology,Xiangtan Hunan 411201,China;Department of Sixth Affliated Hospital,School of Medicine,South China University of Technology,Foshan Guangdong 528200,China)

机构地区：[1]湖南科技大学化学化工学院,湖南湘潭411201 [2]华南理工大学附属第六医院,广东佛山528200

出　　处：《遵义医科大学学报》2025年第2期202-212,共11页Journal of Zunyi Medical University

基　　金：湖南省教育厅重点项目(NO:23A0358);广东省自然科学基金面上项目(NO:2020A1515010185)。

摘　　要：青蒿素是一种含有过氧基团结构的倍半萜内酯化合物,是全新的天然抗疟药,且不易产生耐药性。但因其存在溶解性差、生物利用率低、复燃率高等缺点,限制了其广泛应用。研究发现,以青蒿烯为母核合成青蒿素C-16位新型衍生物,不仅抗疟,还具有抗癌、抗炎等药理功效。目前少有文章对青蒿素C-16位新型衍生物进行综合报道,本文将对近年来国内外学者在有关其结构修饰和生物活性研究方面的新进展进行简要阐述,为该类化合物的进一步研究提供参考。Objective Artemisinin,a sesquiterpene lactone compound with a peroxide group structure,is a new natural antimalarial drug that is not susceptible to drug resistance.However,its wide application is limited due to its disadvantages of poor solubility,low bioavailability,and high relapse rate.A novel derivative of artemisinin at C-16 position was synthesized by using artemisinene as parent nucleus,and it was found that it is not only anti-malarial,but also has the pharmacological efficacy of anti-cancer and anti-inflammation.At present,few articles has been reported on the synthesis of new artemisinin derivatives at the C-16 position.In this paper,the recent progress in the structure modification and biological activity of artemisinin derivatives is briefly described,which can provide illumination for the further study of this kind of compounds.

关 键 词：青蒿烯 C-16位 抗疟 抗癌 抗炎 结构修饰 

分 类 号：R914.2[医药卫生—药物化学]