School of Pharmacy, Shanghai Jiao Tong University, MinHang DongChuan Rd800, Shanghai 200240, PR China.
Bioorg Med Chem Lett. 2013 Apr 1;23(7):2207-11. doi: 10.1016/j.bmcl.2013.01.091. Epub 2013 Feb 4.
The inhibitory activity of 4,4'-dihydroxy-α-truxillic acid and its derivatives (5-1a-5-35a) on nitric oxide (NO) release was evaluated in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. Compounds 5-3a, 5-4a, 5-5a, 5-10a, 5-24a, 5-26a and 5-30a exhibited significant inhibitory effects on NO production, with IC50 values of 19.8, 21.1, 16.4, 17.5, 20.8, 22.6 and 17.6 μM, respectively. Their cytotoxicities were also estimated using a CCK-8 assay. Among them, compound 5-10a showed no cytotoxic effect on cells up to a concentration of 50 μM. The structure-activity relationships of the compounds are also discussed.
4,4'-二羟基-α-土木香酸及其衍生物（5-1a-5-35a）对脂多糖（LPS）刺激的 RAW 264.7 巨噬细胞中一氧化氮（NO）释放的抑制活性进行了评估。化合物 5-3a、5-4a、5-5a、5-10a、5-24a、5-26a 和 5-30a 对 NO 生成表现出显著的抑制作用，IC50 值分别为 19.8、21.1、16.4、17.5、20.8、22.6 和 17.6 μM。还使用 CCK-8 测定法评估了它们的细胞毒性。其中，化合物 5-10a 在高达 50 μM 的浓度下对细胞没有细胞毒性作用。还讨论了化合物的构效关系。
