Raso G M, Meli R, Di Carlo G, Pacilio M, Di Carlo R
Department of Experimental Pharmacology, University of Naples Federico II, Italy.
Life Sci. 2001 Jan 12;68(8):921-31. doi: 10.1016/s0024-3205(00)00999-1.
The present study focuses on the effect of various naturally occurring flavonoids (apigenin, galangin, morin, naringenin, quercetin, and silymarin) on nitric oxide (NO) and prostaglandin E2 (PGE2) production induced by lipopolysaccharide (LPS) in the macrophage cell line J774A.1. Moreover, we evaluated flavonoid modulation of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) enzyme expression by western blot analysis. Apigenin and quercetin (0.5-50 microM) were the most potent inhibitors of NO production and this effect was concentration-dependent and significant at 5 and 50 microM. These data were consistent with the modulation of iNOS enzyme expression. A similar pattern was observed considering the inhibitory effect of flavonoids on LPS-induced PGE2 release and COX-2 expression. Quercetin, galangin, apigenin, and naringenin markedly decreased PGE2 release and COX-2 expression in a concentration-dependent manner. This study suggests that inhibition of iNOS and COX-2 expression by flavonoids may be one of the mechanisms responsible for their anti-inflammatory effects.
本研究聚焦于多种天然存在的类黄酮（芹菜素、高良姜素、桑色素、柚皮素、槲皮素和水飞蓟素）对巨噬细胞系J774A.1中脂多糖（LPS）诱导的一氧化氮（NO）和前列腺素E2（PGE2）生成的影响。此外，我们通过蛋白质印迹分析评估了类黄酮对诱导型一氧化氮合酶（iNOS）和环氧化酶-2（COX-2）酶表达的调节作用。芹菜素和槲皮素（0.5 - 50微摩尔）是NO生成的最有效抑制剂，且这种作用呈浓度依赖性，在5和50微摩尔时具有显著性。这些数据与iNOS酶表达的调节一致。考虑到类黄酮对LPS诱导的PGE2释放和COX-2表达的抑制作用，观察到了类似的模式。槲皮素、高良姜素、芹菜素和柚皮素以浓度依赖性方式显著降低了PGE2释放和COX-2表达。本研究表明，类黄酮对iNOS和COX-2表达的抑制可能是其抗炎作用的机制之一。
