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新型小檗碱衍生物的发展与构效关系研究。

Current development and structure-activity relationship study of berberine derivatives.

机构信息

School of Pharmacy, Lanzhou University, Lanzhou 730000, China.

Key Laboratory of Vector Biology and Pathogen Control of Zhejiang Province, College of Life Science, Huzhou University, Huzhou 313000, China.

出版信息

Bioorg Med Chem. 2024 Oct 1;112:117880. doi: 10.1016/j.bmc.2024.117880. Epub 2024 Aug 17.

Abstract

Berberine is a quaternary ammonium isoquinoline alkaloid derived from traditional Chinese medicines Coptis chinensis and Phellodendron chinense. It has many pharmacological activities such as hypoglycemic, hypolipidemic, anti-tumor, antimicrobial and anti-inflammatory. Through structural modifications at various sites of berberine, the introduction of different groups can change berberine's physical and chemical properties, thereby improving the biological activity and clinical efficacy, and expanding the scope of application. This paper reviews the research progress and structure-activity relationships of berberine in recent years, aiming to provide valuable insights for the exploration of novel berberine derivatives.

摘要

小檗碱是一种从黄连和黄柏等传统中药中提取的季铵型异喹啉类生物碱。它具有降血糖、降血脂、抗肿瘤、抗菌和抗炎等多种药理活性。通过对小檗碱的各个部位进行结构修饰,引入不同的基团可以改变小檗碱的物理化学性质,从而提高生物活性和临床疗效,扩大应用范围。本文综述了近年来小檗碱的研究进展和构效关系,旨在为新型小檗碱衍生物的探索提供有价值的参考。

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