Synthesis and anti-inflammatory evaluation of novel mono-carbonyl analogues of curcumin in LPS-stimulated RAW 264.7 macrophages
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- 作者：Chengguang Zhao ; Yuepiao Cai ; Xuzhi He ; Jianling Li ; Li Zhang ; Jianzhang Wu ; Yunjie Zhao ; Shulin Yang ; Xiaokun Li ; Wulan Li ; Guang Liang
- 关键词：Curcumin ; Mono-carbonyl analogues ; QSAR ; TNF-α ; IL-6 ; Anti-inflammation
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2010
- 出版时间：December 2010
- 年：2010
- 卷：45
- 期：12
- 页码：5773-5780
- 全文大小：400 K
文摘
Curcumin is a multifunctional natural product with regulatory effects on inflammation. However, a major limitation for the application of curcumin is its poor bioavailability. We previously demonstrated that the mono-carbonyl analogues of curcumin possessed improved pharmacokinetic profiles. In this study, 33 novel mono-carbonyl analogues of curcumin were synthesized and their inhibition against TNF-α and IL-6 release was evaluated in LPS-stimulated RAW 264.7 macrophages. Based on the screening data, quantitative structure–activity relationship was conducted, indicating that electron-withdrawing groups in benzene ring are favourable to anti-inflammatory activities of B-class compounds. Furthermore, compounds AN1 and B82 demonstrated anti-inflammatory abilities in a dose-dependent manner. These raise the possibility that these compounds might serve as potential agents for the treatment of inflammatory diseases.