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
Affiliation: Centre of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, Jiangsu 210009, China.
Keywords: Andrographolide, Combination-principle, Derivatives, Hepatoprotective, Natural products, Synthesis.
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.
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