Synthesis of mono-carbonyl analogues of curcumin and their effects on inhibition of cytokine release in LPS-stimulated RAW 264.7 macrophages

被引：82

作者：

Zhao, Chengguang ^{[1
]}

Yang, Ju ^{[1
]}

Wang, Yi ^{[1
]}

Liang, Donglou ^{[1
]}

Yang, Xuyi ^{[1
]}

Li, Xiaoxia ^{[1
]}

Wu, Jianzhang ^{[1
]}

Wu, Xiaoping ^{[1
]}

Yang, Shulin ^{[2
]}

Li, Xiaokun ^{[1
]}

Liang, Guang ^{[1
,2
]}

机构：

[1] Wenzhou Med Coll, Sch Pharm, Bioorgan & Med Chem Res Ctr, Wenzhou 325035, Zhejiang, Peoples R China

[2] Nanjing Univ Sci & Technol, Coll Chem Engn, Nanjing 210094, Jiangsu, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 07期

关键词：

Curcumin; Mono-carbonyl analogues; SAR; TNF-alpha; IL-6; Macrophage; NF-KAPPA-B; TNF-ALPHA; CANCER; INFLAMMATION; CELLS; ANTIOXIDANT; EXPRESSION; PROTECTION; REDUCTION; STABILITY;

D O I：

10.1016/j.bmc.2010.03.001

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

Curcumin has been reported to possess multifunctional bioactivities, especially the ability to inhibit pro-inflammatory induction. We previously demonstrated that the mono-carbonyl analogues of curcumin possessed improved pharmacokinetic profiles both in vitro and in vivo. In this study, we synthesized and examined a series of 5-carbon linker-containing mono-carbonyl analogues of curcumin with potent inhibitory activities against TNF-alpha and IL-6 release in LPS-stimulated RAW 264.7 macrophages. Discussion and conclusions are given regarding structure-activity relationships (SAR). The two most potent analogues among the tested compounds, B75 and C12, exhibited anti-inflammatory abilities in a dose-dependent manner in macrophages. This raises the possibility that mono-carbonyl analogues of curcumin might serve as potential agents for the treatment of various inflammatory diseases. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：2388 / 2393

页数：6

共 36 条

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