小檗碱衍生物的合成及抗菌活性研究  

Synthesis and Antibacterial Activity of Berberine Derivatives

作　　者：葛莲 程珊 吕钦 万升标[1,2] Ge Lian;Cheng Shan;Lv Qin;Wan Shengbiao(Key Laboratory of Marine Drugs,Ministry of Education,School of Medicine and Pharmacy,Ocean University of China,Qingdao 266003,China;Laboratory for Marine Drugs and Bioproducts,Pilot National Laboratory for Marine Science and Technology(Qingdao),Qingdao 266237,China)

机构地区：[1]中国海洋大学医药学院,海洋药物教育部重点实验室,山东青岛266003 [2]青岛海洋科学与技术试点国家实验室海洋药物与生物制品功能实验室,山东青岛266237

出　　处：《中国海洋大学学报（自然科学版）》2024年第2期106-113,共8页Periodical of Ocean University of China

基　　金：国家自然科学基金项目(81973170)资助。

摘　　要：小檗碱具有广谱抗菌活性,但抑菌效果不强。本文对小檗碱进行结构改造,获得了具有更高抗菌活性的小檗碱衍生物。将经典的FtsZ(Filamenting temperature-sensitive mutant Z)抑制剂PC190723衍生物的苯并噻唑类活性片段引入到小檗碱中,对小檗碱进行结构改造并对其进行体外抗菌活性实验。合成出了10个小檗碱衍生物,其中有5个化合物对金黄色葡萄球菌和耐甲氧西林金黄色葡萄球菌的抗菌活性明显优于小檗碱。Berberine has broad-spectrum antibacterial activity,but its antibacterial effect is not very good.The structure of berberine was modified to obtain berberine derivatives with higher antibacterial activity.The active benzothiazoles of PC190723 derivatives,a classical FtsZ inhibitor,were introduced into berberine,and the structure of berberine was modified and its antibacterial activity was tested in vitro.Ten berberine derivatives were synthesized,among which 5 compounds showed significantly better antibacterial activity against Staphylococcus aureus and methicillin-resistant Staphylococcus aureus.

关 键 词：小檗碱 苯并噻唑 FtsZ抑制剂 结构改造 抗菌活性 

分 类 号：R914[医药卫生—药物化学]