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齐墩果酸释放一氧化氮衍生物作为HepG2细胞凋亡抑制剂的合成及生物学评价

Synthesis and biological evaluation of nitric oxide-releasing derivatives of oleanolic acid as inhibitors of HepG2 cell apoptosis.

作者信息

Chen Li, Zhang Yihua, Kong Xiangwen, Peng Sixun, Tian Jide

机构信息

Center of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China.

出版信息

Bioorg Med Chem Lett. 2007 Jun 1;17(11):2979-82. doi: 10.1016/j.bmcl.2007.03.068. Epub 2007 Mar 25.

Abstract

A total of 106 nitric oxide-releasing derivatives of oleanolic acid were synthesized and their effects on the inhibition of anti-Fas-mediated HepG2 cell apoptosis were evaluated in vitro. Several compounds inhibited anti-Fas-mediated HepG2 cell apoptosis in a dose-dependent manner. Within this series of compounds, 8b is the most potent inhibitor. The development of new NO-releasing derivatives of oleanolic acid may aid in the design of NO-based medicines for the intervention of human liver inflammatory diseases.

摘要

共合成了106种齐墩果酸的一氧化氮释放衍生物,并在体外评估了它们对抑制抗Fas介导的HepG2细胞凋亡的作用。几种化合物以剂量依赖性方式抑制抗Fas介导的HepG2细胞凋亡。在这一系列化合物中,8b是最有效的抑制剂。新型齐墩果酸一氧化氮释放衍生物的开发可能有助于设计用于干预人类肝脏炎症性疾病的基于一氧化氮的药物。

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