大黄素结构修饰及其生物活性研究进展  

Advances in Study on Structural Modification and Bioactivity of Emodin

作　　者：邢志华[1,2] 徐志远 申光焕 张凤阳 韩维娜 程美池[1,2] XING Zhi-hua;XU Zhi-yuan;SHEN Guang-huan;ZHANG Feng-yang;HAN Wei-na;CHENG Mei-chi(School of Pharmacy,Harbin University of Commerce,Harbin150076,China;Key Laboratory for Drug Research on Preven-tion and Treatment of Geriatric Diseases of Heilongjiang Province,Harbin150076,China;School of Pharmacy,Harbin Medical University,Harbin150081,China)

机构地区：[1]哈尔滨商业大学药学院,哈尔滨150076 [2]黑龙江省预防与治疗老年病药物研究重点实验室,哈尔滨150076 [3]哈尔滨医科大学药学院,哈尔滨150081

出　　处：《中国药学杂志》2022年第16期1316-1322,共7页Chinese Pharmaceutical Journal

基　　金：黑龙江省自然科学基金面上项目资助(H2016001);黑龙江省留学回国人员择优资助项目资助(18930101);黑龙江省博士后科研启动基金资助(LBH⁃Q15111);哈尔滨商业大学研究生科研创新项目资助(YJSCX2020⁃684HSD)。

摘　　要：近年来,研究人员为提高大黄素的生物利用度及生物活性,对其结构进行修饰与改造得到许多大黄素类衍生物。本文通过查阅并整理近几年的国内外相关文献,对季铵盐、季膦盐、甲基化物、糖苷、金属配合物等79个大黄素衍生物的生物活性进行综述。其中绝大多数衍生物的生物活性研究是围绕体外抗肿瘤活性展开的,其他衍生物活性涉及灭蚊活性、清除自由基、抗金黄色葡萄球菌及抗烟草花叶病毒等。该综述为大黄素的构效关系研究及开发大黄素类药物提供参考。In recent years,in order to improve the bioavailability and bioactivity of emodin,researchers have modified its structure to obtain many emodin derivatives.In this paper,the bioactivities of 79 emodin derivatives including quaternary ammonium salts,quater⁃nary phosphonium salts,methylated salts,glycosides and metal complexes were reviewed by referring to and sorting out relevant literatures domestic and overseas in recent years.The biological activities of most of the derivatives revolve around antitumor activityin vitro,and the other derivatives involve anti⁃mosquito activities,free radical scavenging,anti⁃Staphylococcus aureusand anti⁃tobacco mosaic virus,etc.This review provides reference for the research on the structure⁃activity relationship of emodin and the development of emodin drugs.

关 键 词：大黄素 蒽醌化合物 衍生物 生物活性 

分 类 号：R282.71[医药卫生—中药学]