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Issue 7, 2015
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Synthesis and biological evaluation of novel semi-conservative monocarbonyl analogs of curcumin as anti-inflammatory agents

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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

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Publication details

The article was received on 24 Mar 2015, accepted on 26 May 2015 and first published on 26 May 2015


Article type: Concise Article
DOI: 10.1039/C5MD00114E
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Citation: Med. Chem. Commun., 2015,6, 1328-1339

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    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

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