Liang Guang, Li Xiaokun, Chen Li, Yang Shulin, Wu Xudong, Studer Elaine, Gurley Emily, Hylemon Phillip B, Ye Faqing, Li Yueru, Zhou Huiping
College of Pharmacy, Wenzhou Medical College, Wenzhou, Zhejiang 325035, PR China.
Bioorg Med Chem Lett. 2008 Feb 15;18(4):1525-9. doi: 10.1016/j.bmcl.2007.12.068. Epub 2008 Jan 1.
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.
姜黄素因其抗炎活性已得到广泛研究。然而,其对各种疾病预防和治疗的潜在有益作用受到其不稳定结构的限制。β - 二酮部分使姜黄素在肝脏中被醛糖还原酶迅速代谢。在本研究中,合成了一系列具有更稳定化学结构的姜黄素类似物,并且几种化合物在抑制巨噬细胞中脂多糖(LPS)诱导的肿瘤坏死因子 -α(TNF -α)和白细胞介素 -6(IL -6)合成方面表现出增强的能力。