Synthesis and In Vivo Hepatoprotective Activity of Some Novel Andrographolide Derivatives
Chunlei Tang, Guolong Gu, Baowei Yang, Xuekun Wang, Hai Qian, Wenlong Huang, Xiaoyun Zhu and Jing Li
In this study, combination-principle was reported to improve the hepatoprotective activity of andrographolide. Ten andrographolide derivatives were synthesized and evaluated for in vivo hepatoprotective activity in CCl4-induced liver injury mice. The pharmacological results revealed that 6 derivatives exhibited significant hepatoprotective activity. The most promising compound 6b significantly improved liver enzymes (ALT and AST) activity as compared with andrographolide, with high potency to be a new lead.
Andrographolide, Combination-principle, Derivatives, Hepatoprotective, Natural products, Synthesis
Centre of Drug Discovery China Pharmaceutical University 24 Tongjiaxiang Nanjing, Jiangsu 210009 China.