Letters in Drug Design & Discovery

Author(s): Chunlei Tang, Guolong Gu, Baowei Yang, Xuekun Wang, Hai Qian, Wenlong Huang, Xiaoyun Zhu and Jing Li

DOI: 10.2174/1570180810666131123002409

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Synthesis and In Vivo Hepatoprotective Activity of Some Novel Andrographolide Derivatives

Page: [677 - 685] Pages: 9

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Abstract

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.

Keywords: Andrographolide, Combination-principle, Derivatives, Hepatoprotective, Natural products, Synthesis.