Synthesis and anti-inflammatory activities of mono-carbonyl analogues of curcumin
Synthesis and anti-inflammatory activities of mono-carbonyl analogues of curcumin
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DOI：
10.1016/j.bmcl.2007.12.068
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发表时间：
2008-02-15
影响因子：
2.7
通讯作者：
Zhou, Huiping
中科院分区：
文献类型：
--
作者：
Liang, Guang;Li, Xiaokun;Zhou, Huiping
姜黄素因其抗炎活性而被广泛研究。然而，由于其结构不稳定，其在各种疾病预防和治疗中的潜在有益作用受到限制。β-二酮部分使姜黄素在肝脏中被醛酮还原酶快速代谢。本研究合成了一系列化学结构更为稳定的姜黄素类似物，其中几个化合物对脂多糖(LPS)诱导的巨噬细胞产生的肿瘤坏死因子-α(TNF-α)和白介素6(IL-6)具有较强的抑制作用。(C)2007爱思唯尔有限公司。保留所有权利。
Curcumin has been extensively studied for its anti-inflammatory activities. However, its potential beneficial effects on various disease preventions and treatments are limited by its unstable structure. The beta-diketone moiety renders curcumin to be rapidly metabolized by aldo -keto reductase in liver. In the present study, a series of curcumin analogues with more stable chemical structures were synthesized and several compounds showed an enhanced ability to inhibit lipopolysaccharide ( LPS)-induced TNF-alpha and IL-6 synthesis in macrophages. (C) 2007 Elsevier Ltd. All rights reserved.