1275576-99-2Relevant academic research and scientific papers
Synthesis and biological evaluation of novel semi-conservative monocarbonyl analogs of curcumin as anti-inflammatory agents
Wang, Zhe,Zou, Peng,Li, Chenglong,He, Wenfei,Xiao, Bing,Fang, Qilu,Chen, Wenbo,Zheng, Suqing,Zhao, Yunjie,Cai, Yuepiao,Liang, Guang
, p. 1328 - 1339 (2015)
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.
COMPOUNDS USEFUL AGAINST KINETOPLASTIDEAE PARASITES
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Page/Page column 22, (2012/09/05)
Dibenzylidene and heterobenzylideneacetone derivatives, related 4-piperidones, related 4-thiopyranones and the corresponding sulfinyl- and sulfonyl-analogues for their use for prophylaxis or treatment of trypanosomiasis and leishmaniasis.
