Synthesis and hypoglycemic activity of 9-O-(lipophilic group substituted) berberine derivatives

详细信息    查看全文

• 作者：Shanshan Zhang^a ; Xiaohong Wang^a ; Weicheng Yin^b ; Zhenbao Liu^c ; Mi Zhou^b ; Daipeng Xiao^a ; Yanfei Liu^a ; ^{liuyfcsu@163.com" class="auth_mail" title="E-mail the corresponding author} ; Dongming Peng^b ; ^{pdmcsu@126.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Berberine derivatives ; Synthesis ; Cytotoxicity ; Hypoglycemic activity ; Structure&ndash ; activity analysis
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 October 2016
• 年：2016
• 卷：26
• 期：19
• 页码：4799-4803
• 全文大小：1446 K

文摘

A series of 9-O-(lipophilic group substituted) berberine derivatives were synthesized and evaluated for their cytotoxicity and hypoglycemic activity against HepG2 cells. All the results indicated that most of the synthesized compounds exhibited lower cytotoxicity and a certain degree of hypoglycemic activity. Especially the compounds 5g and 5h displayed dramatically increased hypoglycemic activity compared with berberine, and the cytotoxicity maintained or even lower than berberine, indicating that they are potential candidates for new anti-type 2 diabetes mellitus drugs.