丹参脂溶性成分结构优化研究进展  

Research Progress on Structural Optimization on the Lipid-Soluble Ingredients of Salvia miltiorrhiza

作　　者：李兴军 王江 柳红 Li Xingjun;Wang Jiang;Liu Hong(State Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203;School of Pharmacy,China Pharmaceutical University,Nanjing 211198;Lingang Laboratory,Shanghai 200031)

机构地区：[1]中国科学院上海药物研究所新药研究国家重点实验室,上海201203 [2]中国药科大学药学院,南京211198 [3]临港实验室,上海200031

出　　处：《有机化学》2023年第2期471-490,共20页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.82130105)资助项目。

摘　　要：丹参作为一种传统中药在临床上广泛应用于心脑血管疾病的治疗,对其有效成分及衍生物的研究一直是国内外的研究热点.丹参的有效成分主要分为脂溶性成分和水溶性成分,其脂溶性成分具有多种药理活性,但因其水溶性不足、生物利用度低的缺点限制了临床应用.为了能够推进丹参脂溶性成分的临床应用,研究人员以丹参脂溶性成分为先导化合物进行结构优化,以期能够提高其类药性.综述了近年来丹参主要脂溶性成分的结构优化及相关药理活性的研究进展,总结了主要脂溶性成分的成药性结构优化策略以及该类衍生物的合成方法,阐述了不同位置结构优化对药理活性的影响,旨在为丹参脂溶性成分创新药物的研发提供新的研究思路.As a traditional Chinese medicine,Salvia miltiorrhiza has been widely applied in the treatment of cardiovascular diseases in clinical.Research on its active components and derivatives has become an issue of great focus both domestically and internationally.The active ingredients of Salvia miltiorrhiza are mainly divided into lipid-soluble and water-soluble ingredients with the lipid-soluble ones performing various pharmacological properties.However,their poor solubility and bioavailability have limited their clinical applications.In order to promote the clinical application of lipid-soluble ingredients of Salvia miltiorrhiza,these components are used as lead compounds to perform structural optimization to improve drug-like properties.In order to generate novel research ideas for the development of novel drugs based on lipid-soluble ingredients of Salvia miltiorrhiza,the research progress of structural optimization and related biological activities of the major lipid-soluble ingredients of Salvia miltiorrhiza in recent years is reviewed,the structural optimization strategy of the drug-like properties of these compounds and the synthetic approaches of their derivatives are summarized,and the effects of different structure modifications on pharmacological activities are described.

关 键 词：丹参 脂溶性成分 结构优化 

分 类 号：R284[医药卫生—中药学]