Ahn Kwang Seok, Noh Eun Jung, Cha Kwang-Hyun, Kim Yeong Shik, Lim Soon Sung, Shin Kuk Hyun, Jung Sang Hoon
Department of Experimental Therapeutics, The University of Texas M. D. Anderson Cancer Center, 1515 Holcombe Boulevard, Houston, USA.
Life Sci. 2006 Apr 11;78(20):2336-42. doi: 10.1016/j.lfs.2005.09.041. Epub 2005 Nov 22.
In the present study, we investigated antiinflammatory effects of six flavonoids isolated from the rhizomes of Belamcanda chinensis (Iridaceae) in RAW 264.7 macrophages. The results indicated that irigenin concentration dependently inhibited lipopolysaccharide (LPS)-induced nitric oxide (NO) and prostaglandin (PG) E(2) production. Furthermore, this compound inhibited the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2 proteins and mRNAs without an appreciable cytotoxic effect. Treatment of the transfectant RAW 264.7 cells with irigenin reduced the level of nuclear factor-kappaB (NF-kappaB) activity, also effectively lowered NF-kappaB binding measured by electrophoretic mobility shift assay (EMSA), which was associated with decreased p65 protein levels in the nucleus. On the basis of the above data, we suggest that the effect of irigenin in decreasing LPS-induced NO and PGE(2) synthesis is due to diminish the mRNA and protein expression of iNOS and COX-2, respectively, also may be due to under the suppression of NF-kappaB activation. Therefore, irigenin isolated from the rhizomes of Belamcanda chinensis could be offered as a leading compound for anti-inflammation.
在本研究中,我们研究了从射干(鸢尾科)根茎中分离出的六种黄酮类化合物对RAW 264.7巨噬细胞的抗炎作用。结果表明,鸢尾苷元浓度依赖性地抑制脂多糖(LPS)诱导的一氧化氮(NO)和前列腺素(PG)E2的产生。此外,该化合物抑制诱导型一氧化氮合酶(iNOS)和环氧化酶(COX)-2蛋白及mRNA的表达,且无明显细胞毒性作用。用鸢尾苷元处理转染的RAW 264.7细胞可降低核因子-κB(NF-κB)活性水平,通过电泳迁移率变动分析(EMSA)测定也能有效降低NF-κB结合,这与细胞核中p65蛋白水平降低有关。基于上述数据,我们认为鸢尾苷元降低LPS诱导的NO和PGE2合成的作用分别是由于减少了iNOS和COX-2的mRNA和蛋白表达,也可能是由于NF-κB激活受到抑制。因此,从射干根茎中分离出的鸢尾苷元可作为抗炎的先导化合物。