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Letters in Drug Design & Discovery

Editor-in-Chief

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

Improved Pharmacokinetic Profile and Anti-Inflammatory Property of a Novel Curcumin Derivative, A50

Author(s): Xiangjian Chen, Luqing Ren, Xiuhua Zhang, Lu Guo, Jianmin Zhou, Guang Liang and Yi Wang

Volume 10 , Issue 6 , 2013

Page: [535 - 542] Pages: 8

DOI: 10.2174/1570180811310060010

Price: $65

Abstract

Extensive researches within the last decade have supported the anti-inflammatory properties of curcumin. However, the development and clinical application of curcumin have been limited significantly by its instability and poor metabolic property resulting from the β-diketone moiety decomposition and phenolic glucuronides. In this paper, a curcumin derivative (A50) without β-diketone and phenolic hydroxyl groups was designed and reported. The X-ray diffraction analysis showed a more rigid structure of A50 than that of curcumin. A pharmacokinetic study of A50 in rats indicated that its metabolic parameters were significantly improved compared to those of curcumin. Furthermore, A50 exhibited stronger anti-inflammatory activity than curcumin did via the mechanism, at least partly, associated with inhibiting ERK and JNK phosphorylation in macrophages. These results suggest that the structural modification is both pharmacokinetically and pharmacologically beneficial, and A50 may be a promising anti-inflammatory candidate to treat various inflammatory diseases.

Keywords: Anti-inflammatory property, Curcumin, Crystal structure, (2E, 5E)-2, 5-bis(2, 5-dimethylbenzylidene) cyclopentanone, Mono-carbonyl analogue of curcumin, Pharmacokinetic profile.


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