Department of Physiology, Faculty of Medicine, Chiang Mai University, Chiang Mai 50200, Thailand.
J Nat Med. 2012 Apr;66(2):400-5. doi: 10.1007/s11418-011-0599-6. Epub 2011 Oct 13.
The chemically modified analogs, the demethylated analogs 4-6, the tetrahydro analogs 7-9 and the hexahydro analogs 10-12, of curcumin (1), demethoxycurcumin (2) and bisdemethoxycurcumin (3) were evaluated for their inhibitory activity on lipopolysaccharide activated nitric oxide (NO) production in HAPI microglial cells. Di-O-demethylcurcumin (5) and O-demethyldemethoxycurcumin (6) are the two most potent compounds that inhibited NO production. The analogs 5 and 6 were twofold and almost twofold more active than the parent curcuminoids 1 and 2, respectively. Moreover, the mRNA expression level of inducible NO synthase was inhibited by these two compounds. The strong neuroprotective activity of analogs 5 and 6 provide potential alternative compounds to be developed as therapeutics for neurological disorders associated with activated microglia.
姜黄素（1）、脱甲氧基姜黄素（2）和双脱甲氧基姜黄素（3）的化学修饰类似物、去甲基类似物 4-6、四氢类似物 7-9 和六氢类似物 10-12 被评估了其对脂多糖激活的 HAPI 小胶质细胞中一氧化氮（NO）产生的抑制活性。二-O-去甲氧基姜黄素（5）和 O-去甲氧基脱甲氧基姜黄素（6）是两种最有效的抑制 NO 产生的化合物。类似物 5 和 6 的活性分别比母体姜黄素 1 和 2 高两倍和近两倍。此外，这两种化合物还抑制了诱导型一氧化氮合酶的 mRNA 表达水平。类似物 5 和 6 的强烈神经保护活性为开发用于治疗与激活小胶质细胞相关的神经紊乱的治疗药物提供了潜在的替代化合物。
