Lin Chun-Mao, Huang Sheng-Tung, Lee Fu-Wei, Kuo Hsien-Saw, Lin Mei-Hsiang
Department of Biochemistry, Taipei Medical University, Taiwan, ROC.
Bioorg Med Chem. 2006 Jul 1;14(13):4402-9. doi: 10.1016/j.bmc.2006.02.042. Epub 2006 Mar 15.
A series of coumarin derivatives were synthesized in two steps from phloroglucinol. The anti-inflammatory activities of these derivatives were evaluated by means of inhibiting NO production in LPS-induced RAW 264.7 cells. Derivatives 3, 8, 10, 11, and 13 exhibited low micromolar levels of anti-inflammatory activities, and these derivatives also protected DNA against hydroxyl radical attack. Coumarin derivative 8 was the most potent derivative among those tested herein against NO production in LPS-induced RAW 264.7 cells with an IC(50) value of 7.6 microM, and it effectively reduced the hydroxyl radical production by 50% at 100 microM in the electron spin resonance study.
一系列香豆素衍生物由间苯三酚分两步合成。通过抑制脂多糖诱导的RAW 264.7细胞中一氧化氮的产生来评估这些衍生物的抗炎活性。衍生物3、8、10、11和13表现出低微摩尔水平的抗炎活性，并且这些衍生物还能保护DNA免受羟基自由基攻击。香豆素衍生物8是本文测试的对脂多糖诱导的RAW 264.7细胞中一氧化氮产生最有效的衍生物，其IC(50)值为7.6微摩尔，并且在电子自旋共振研究中，它在100微摩尔时能有效降低50%的羟基自由基产生。
