大黄酸的结构修饰及其生物活性研究进展  

Structural modification and biological research progress of rhein

作　　者：高鑫 方方 GAO Xin;FANG Fang(College of Pharmacy,Anhui University of Chinese Medicine,Hefei 230012,China;Department of Medicinal Chemistry,Anhui Academy of Chinese Medicine,Hefei 230012,China;Anhui Province Key Laboratory of Research&Development of Chinese Medicine,Hefei 230012,China)

机构地区：[1]安徽中医药大学药学院,合肥230012 [2]安徽省中医药科学院药物化学研究所,合肥230012 [3]中药研究与开发安徽省重点实验室,合肥230012

出　　处：《中国新药杂志》2023年第1期35-45,共11页Chinese Journal of New Drugs

基　　金：安徽省高校优秀青年人才支持计划重点项目资助(gxyqZD2016129)。

摘　　要：大黄酸是大黄素型羟基蒽醌,主要存在于大黄等中药中。大黄酸具有抗癌、抗炎、抗菌、抗阿尔茨海默病等广泛的药理活性,但由于其水溶性差、生物利用度低等缺点,限制了其临床应用。为了克服这些缺点,研究者通过对其进行结构修饰研究,设计并合成了大量生物活性更为突出的大黄酸衍生物。本文综述了近年来大黄酸的结构修饰及其生物活性研究进展,为大黄酸类衍生物的进一步研究提供参考依据。Rhein is a kind of emodin-type hydroxy-anthraquinone,which mainly exists in traditional Chinese medicines like rhubarb.Rhein is well acknowledged for its pharmacological activities,such as anti-cancer,anti-inflammatory,anti-bacterial and anti-Alzheimer’s disease;however,its clinical application is limited due to its poor water solubility and low bioavailability.In order to overcome these shortcomings,a large number of more bioactive Rhein derivatives were designed and synthesized by structural modification of Rhein.In this paper,the structural modification and pharmacological activity of rhein are reviewed,providing reference for future development of rhein derivatives.

关 键 词：大黄酸 衍生物 结构修饰 生物活性 

分 类 号：R961[医药卫生—药理学]