Bioorganic & Medicinal Chemistry Research Center, School of Pharmacy, Wenzhou Medical College, 1210 College Town, Wenzhou, Zhejiang 325035, China.
Bioorg Med Chem. 2010 Apr 1;18(7):2388-93. doi: 10.1016/j.bmc.2010.03.001. Epub 2010 Mar 6.
Curcumin has been reported to possess multifunctional bioactivities, especially the ability to inhibit proinflammatory 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.
姜黄素具有多种生物活性，特别是抑制前炎症诱导的能力。我们之前的研究表明，姜黄素的单羰基类似物在体外和体内都具有改善的药代动力学特征。在这项研究中，我们合成并研究了一系列含有 5 碳键的单羰基姜黄素类似物，它们对 LPS 刺激的 RAW 264.7 巨噬细胞中 TNF-α和 IL-6 释放具有很强的抑制活性。对结构-活性关系（SAR）进行了讨论和总结。在所测试的化合物中，B75 和 C12 这两个最有效的类似物在巨噬细胞中表现出剂量依赖性的抗炎能力。这表明姜黄素的单羰基类似物可能作为治疗各种炎症性疾病的潜在药物。
