Synthesis and In Vivo Hepatoprotective Activity of Some Novel Andrographolide Derivatives

ISSN: 1875-628X (Online)
ISSN: 1570-1808 (Print)


Volume 13, 10 Issues, 2016


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Letters in Drug Design & Discovery

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University of Texas
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Synthesis and In Vivo Hepatoprotective Activity of Some Novel Andrographolide Derivatives



Letters in Drug Design & Discovery, 11(5): 677-685.

Author(s): 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.

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.



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Article Details

Volume: 11
Issue Number: 5
First Page: 677
Last Page: 685
Page Count: 9
DOI: 10.2174/1570180810666131123002409
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