首页|苦参碱类衍生物的合成及其活性研究进展

苦参碱类衍生物的合成及其活性研究进展

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苦参碱是从豆科植物苦参、苦豆子等植物中分离得到的一类生物碱.苦参是其主要来源之一,因此以苦参碱命名.研究发现,苦参碱具有抗肿瘤,抗炎和抗病毒的活性,能够调节相关细胞的分子表达,诱导细胞凋亡.但苦参碱体内活性不高,药效时间短,存在毒性作用.许多专家学者对苦参碱参与临床治疗疾病以及相关作用机理的研究情况进行了不同角度和不同方向的深度探索和研究,主要通过修饰苦参碱来增强其活性,降低使用计量.苦参碱的主要结构修饰位点可以大大提高其活性.本文以苦参碱类衍生物在13-位,14-位,15-位及D环开环4 个方面的结构修饰为切入点,综述了苦参碱类衍生物的合成及其活性研究进展,以期为苦参碱类药物的研发提供参考.
Research Progress on Synthesis and Activity of Matrine Derivatives
Matrine is a class of alkaloids isolated from plants in the legume family,such as bitter gin-seng and bitter bean seeds.Bitter ginseng is one of its main sources,hence the name matrine.Studies have shown that matrine has anti-tumor,anti-inflammatory,and antiviral properties,and can regulate the molecular expression of related cells and induce cell apoptosis.However,matrine is not active in vivo,has a short duration of efficacy,and has toxic effects.Many experts and scholars have carried out in-depth exploration and research on the participation of matrine in the clinical treatment of diseases and related mechanisms of action from different angles and directions,and scholars have mainly modi-fied matrine to enhance its activity and reduce the use of measurement.The major structural modifica-tion sites of matrine can greatly enhance its activity.In this paper,we reviewed the progress of the synthesis and activity studies of the matrine derivatives by taking the structural modifications of the ma-trine derivatives in four aspects,namely,13-position,14-position,15-position,and D-ring opening,in order to provide a reference for the research and development of the matrine derivatives.

matrinestructural modificationmolecular expressionanti-inflammatorantiviral

席宇、申光焕、崔琳琳、王艺儒、邢志华、张雪琪

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哈尔滨商业大学 药学院,黑龙江 哈尔滨 150076

黑龙江省预防与治疗老年病药物研究重点实验室,黑龙江 哈尔滨 150076

哈尔滨商业大学药物研究所博士后科研工作站,黑龙江 哈尔滨 150076

苦参碱 结构修饰 分子表达 抗肿瘤 抗病毒

黑龙江省博士后面上资助项目

LBH-Z21066

2024

合成化学
四川省化学化工学会 中国科学院成都有机化学研究所

合成化学

CSTPCD
影响因子:0.42
ISSN:1005-1511
年,卷(期):2024.32(4)
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