Ishihara T, Kohno K, Ushio S, Iwaki K, Ikeda M, Kurimoto M
Fujisaki Institute, Hayashibara Biochemical Laboratories, Inc., 675-1 Fujisaki, 702-8006, Okayama, Japan.
Eur J Pharmacol. 2000 Oct 27;407(1-2):197-204. doi: 10.1016/s0014-2999(00)00674-9.
Nitric oxide (NO) and prostaglandins have been implicated in the pathogenesis of several inflammatory diseases. In this study, we investigated the effect of tryptanthrin (6,12-dihydro-6, 12-dioxoindolo-(2,1-b)-quinazoline), an antimicrobial and antitumoral plant compound isolated from Porigonum tinctorium, on NO and prostaglandin E(2) production by interferon-gamma and lipopolysaccharide-stimulated murine macrophage-like RAW 264.7 cells. Tryptanthrin markedly inhibited both NO and prostaglandin E(2) production in a dose-dependent manner. Tryptanthrin at 20 microM fully inhibited expression of inducible NO synthase, suggesting that the inhibitory effect on NO synthesis was mediated by inhibited expression of the enzyme. On the other hand, tryptanthrin had no effect on the levels of cyclooxygenase-2 protein, but inhibited cyclooxygenase enzyme activity with a ICM(50) value of 1.5 microM. Thus, tryptanthrin has the dual functions of inhibiting both NO and prostaglandin E(2) production by activated macrophages, suggesting that tryptanthrin exhibits anti-inflammatory properties.
一氧化氮（NO）和前列腺素与多种炎症性疾病的发病机制有关。在本研究中，我们调查了从蓼蓝中分离出的一种具有抗菌和抗肿瘤作用的植物化合物靛玉红（6,12 - 二氢 - 6,12 - 二氧代吲哚并 - (2,1 - b) - 喹唑啉）对经干扰素 - γ和脂多糖刺激的小鼠巨噬细胞样RAW 264.7细胞产生NO和前列腺素E2的影响。靛玉红以剂量依赖性方式显著抑制NO和前列腺素E2的产生。20微摩尔的靛玉红完全抑制诱导型一氧化氮合酶的表达，这表明对NO合成的抑制作用是由该酶表达的抑制介导的。另一方面，靛玉红对环氧合酶 - 2蛋白水平没有影响，但以1.5微摩尔的半数抑制浓度（IC50）值抑制环氧合酶活性。因此，靛玉红具有抑制活化巨噬细胞产生NO和前列腺素E2的双重功能，表明靛玉红具有抗炎特性。
