吴茱萸次碱的结构修饰研究进展  

Research progress in structural modification of rutaecarpine

作　　者：宋继庭 魏洪卓 赵长阔 王先恒 SONG Ji-ting;WEI Hong-zhuo;ZHAO Chang-kuo;WANG Xian-heng(Key Laboratory of Basic Pharmacology of Ministry of Education and Joint International Research Laboratory of Ethnomedicine of Ministry of Education,Zunyi Medical University,Zunyi 563000,China;Pharmacy School,Zunyi Medical University,Zunyi 563000,China)

机构地区：[1]遵义医科大学基础药理教育部重点实验室暨特色民族药教育部国际合作联合实验室,遵义563000 [2]遵义医科大学药学院,遵义563000

出　　处：《中国新药杂志》2024年第2期138-145,共8页Chinese Journal of New Drugs

摘　　要：吴茱萸次碱(rutaecarpine)是从传统中药吴茱萸中分离出来的一种喹唑啉类生物碱,具有广泛的生物学和药理学活性,吸引了大量学者和专业人员对其进行研究.迄今,对吴茱萸次碱的研究主要包括从新的天然来源中分离提取和开发新的全合成方法,发现新的生物活性、代谢、毒理学性质、结构修饰与活性的关系、含量测定分析方法的建立等.随着研究的不断深入,发现吴茱萸次碱的溶解性很低,这影响了其吸收效率,其高细胞毒性也阻碍了其作为药物的发展.于是,众多学者对吴茱萸次碱结构修饰和改造做了大量研究,发现了一些新的、更好的生物活性结构.本文综述了近年来吴茱萸次碱结构修饰方面的研究,以期为寻找具有开发前景的吴茱萸次碱衍生物提供依据.Rutecarpine is a quinazoline alkaloid isolated from the traditional Chinese medicine Evodia rutaecarpa.It has a wide range of biological and pharmacological activities,attracting the attention of a large number of scholars and professionals.Up to now,the research on rutaecarpine mainly includes separating and extracting rutaecarpine from new natural sources,developing new total synthesis methods,discovering new biological activity,metabolism,toxicological properties,structure modification-activity relationship,establishing analytical methods for content determination,etc.With the deepening of research,it was found that the solubility of rutaecarpine was very low,which affected its absorption efficiency,and its high cytotoxicity also hindered its development as a drug.Therefore,many scholars have done a great deal of research on the structural modification and transformation of rutaecarpine and found some new and better bioactive structures.This paper reviews the research on structural modification of rutaecarpine in recent years,hoping to provide a basis for finding promising derivatives of rutaecarpine in the future.

关 键 词：吴茱萸次碱 结构修饰 生物活性 类似物 研究进展 

分 类 号：R966[医药卫生—药理学]