Abstract
In this paper, we reported the synthesis of bifendate derivatives and evaluation of anti-inflammatory activity by detecting the production of the Nitric Oxide (NO) in the lipopolysaccharide(LPS)-stimulated RAW 264.7 cell lines. Among the newly derivatives, compound 7k was the most potent one and two other compounds (7e and 7f) also exhibited greater anti-inflammatory activity than bifendate. Further in vivo studies confirmed that 7k significantly and dose-dependently inhibited carrageenan-induced paw edema and decreased the serum levels of alanine aminotransaminase, and aspartate aminotransaminase in concanavalin A-induced hepatitis model. Histopathological evaluation demonstrated that 7k has better hepatoprotective effect on acute liver injury induced by concanavalin A than bifendate, suggesting that 7k is a potential drug candidate for the treatment of hepatic injuries.
Copyright © 2011. Published by Elsevier Masson SAS.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
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Anti-Inflammatory Agents, Non-Steroidal / chemistry*
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology
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Anti-Inflammatory Agents, Non-Steroidal / therapeutic use*
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Biphenyl Compounds / chemical synthesis
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Biphenyl Compounds / chemistry*
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Biphenyl Compounds / pharmacology
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Biphenyl Compounds / therapeutic use*
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Cell Line
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Concanavalin A
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Edema / chemically induced
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Edema / drug therapy
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Edema / pathology
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Female
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Hepatitis, Animal / chemically induced
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Hepatitis, Animal / drug therapy*
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Hepatitis, Animal / pathology
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Lipopolysaccharides / immunology
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Liver / drug effects*
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Liver / pathology
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Macrophages / drug effects
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Macrophages / immunology
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Male
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Mice
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Mice, Inbred BALB C
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Nitric Oxide / immunology
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Rats
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Biphenyl Compounds
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Lipopolysaccharides
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bifendate
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Concanavalin A
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Nitric Oxide