Issue 7, 2015

Synthesis and biological evaluation of novel semi-conservative monocarbonyl analogs of curcumin as anti-inflammatory agents

Abstract

Curcumin, a natural product, has been shown to exhibit notable anti-inflammatory activities. However, the clinical application of curcumin was restricted by its poor stability and bioavailability. We have reported a series of monocarbonyl analogs of curcumin (MACs) previously. In the present study, we synthesized 32 semi-conservative MACs and evaluated their anti-inflammatory effects in RAW 264.7 macrophages. Most of them showed enhanced abilities to inhibit the lipopolysaccharide (LPS)-induced expression of tumor necrosis factor alpha (TNF-α). The preliminary structure–activity relationship was discussed and the preliminary anti-inflammatory mechanism was also explored. The most potent analog compound, WZ35, exhibits significant protection against LPS-induced death in septic mice. These findings suggest that this kind of curcumin derivative may be used to develop promising anti-inflammatory agents to treat inflammatory diseases.

Graphical abstract: Synthesis and biological evaluation of novel semi-conservative monocarbonyl analogs of curcumin as anti-inflammatory agents

Associated articles

Supplementary files

Article information

Article type
Concise Article
Submitted
24 Mar 2015
Accepted
26 May 2015
First published
26 May 2015

Med. Chem. Commun., 2015,6, 1328-1339

Author version available

Synthesis and biological evaluation of novel semi-conservative monocarbonyl analogs of curcumin as anti-inflammatory agents

Z. Wang, P. Zou, C. Li, W. He, B. Xiao, Q. Fang, W. Chen, S. Zheng, Y. Zhao, Y. Cai and G. Liang, Med. Chem. Commun., 2015, 6, 1328 DOI: 10.1039/C5MD00114E

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Spotlight

Advertisements