Synthesis and Preliminary Biologic Activity Evaluation of Nitric Oxide-Releasing Andrographolide Derivatives in RIN-m Cells

被引：10

作者：

Liang, Zhibin

Du, Enming

Xu, Lipeng

Sun, Yewei ^{[1
]}

Zhang, Gaoxiao

Yu, Pei

Wang, Yuqiang

机构：

[1] Jinan Univ, Coll Pharm, Inst New Drug Res, Guangzhou 510632, Guangdong, Peoples R China

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2014年 / 62卷 / 06期

关键词：

andrographolide; synthesis; nitric oxide (NO) donor; beta cell protection; KAPPA-B; ROS;

D O I：

10.1248/cpb.c13-00959

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Pancreatic beta-cell dysfunction and death are important feature of diabetes mellitus. Beta-cell protection has demonstrated clinical benefits in the treatment of this disease. In the present study, andrographolide derivatives with nitric oxide (NO)-releasing capability were synthesized and their protective effects against tert-butyl hydroperoxide (t-BHP) induced cell damage were investigated in RIN-m cells. Compound 6b was found to release a moderate amount of NO and was more potent than its natural parent andrographolide in inhibiting cell apoptosis. These findings suggested that andrographolide derivatives with NO-releasing capacity may be a potential therapy for diabetes.

引用

收藏

页码：519 / 523

页数：5

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