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.
|
Authors | Guangcheng Wang, Chongyang Deng, Caifeng Xie, Liang Ma, Jincheng Yang, Neng Qiu, Qinyuan Xu, Tao Chen, Fei Peng, Jinying Chen, Jingxiang Qiu, Aihua Peng, Yuquan Wei, Lijuan Chen |
Journal | European journal of medicinal chemistry
(Eur J Med Chem)
Vol. 46
Issue 12
Pg. 5941-8
(Dec 2011)
ISSN: 1768-3254 [Electronic] France |
PMID | 22019226
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
|
Copyright | Copyright © 2011. Published by Elsevier Masson SAS. |
Chemical References |
- Anti-Inflammatory Agents, Non-Steroidal
- Biphenyl Compounds
- Lipopolysaccharides
- bifendate
- Concanavalin A
- Nitric Oxide
|
Topics |
- Animals
- Anti-Inflammatory Agents, Non-Steroidal
(chemical synthesis, chemistry, pharmacology, therapeutic use)
- Biphenyl Compounds
(chemical synthesis, chemistry, pharmacology, therapeutic use)
- Cell Line
- Concanavalin A
- Edema
(chemically induced, drug therapy, pathology)
- Female
- Hepatitis, Animal
(chemically induced, drug therapy, pathology)
- Lipopolysaccharides
(immunology)
- Liver
(drug effects, pathology)
- Macrophages
(drug effects, immunology)
- Male
- Mice
- Mice, Inbred BALB C
- Nitric Oxide
(immunology)
- Rats
|