Department of Food and Nutrition, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, South Korea.
Food Chem Toxicol. 2010 Oct;48(10):2607-11. doi: 10.1016/j.fct.2010.06.029. Epub 2010 Jun 22.
Matrix metalloproteinases (MMPs) play an important role in tissue degradation in rheumatoid synovium and inflammatory cytokines are essential in the pathogenesis of rheumatoid arthritis (RA). This study was conducted to evaluate the efficacy of luteolin in regulating interleukin-1beta (IL-1beta)-induced production of MMPs (MMP-1 and -3) and cytokines (tumor necrosis factor (TNF)-alpha and IL-6) in human synovial cell line, SW982. Treatment with luteolin at 1 or 10 microM significantly (P<0.05) inhibited IL-1beta-induced MMPs (MMP-1 and -3) and cytokines (TNF-alpha and IL-6) production when measured by enzyme-linked immunosorbent assay (ELISA). The mitogen-activated protein kinases (MAPKs) represent an attractive target for RA because they can regulate MMP and cytokine expression. The effects of luteolin on the activation of MAPKs and transcription factors were also examined in SW982 cells by ELISA. IL-1beta-induced JNK and p38 activation were inhibited by luteolin. Moreover, IL-1beta-induced activator protein-1 (AP-1) and nuclear factor-kappaB (NF-kappaB) activation were inhibited by luteolin. These results suggest that luteolin reduces the production of MMPs and cytokines in SW982 cells by inhibiting MAPKs (JNK and p38) and transcription factors (AP-1 and NF-kappaB).
基质金属蛋白酶（MMPs）在类风湿滑膜组织降解中发挥重要作用，细胞因子在类风湿关节炎（RA）的发病机制中必不可少。本研究旨在评估木樨草素在调节白细胞介素-1β（IL-1β）诱导的人滑膜细胞系 SW982 中 MMPs（MMP-1 和 MMP-3）和细胞因子（肿瘤坏死因子（TNF）-α和 IL-6）产生中的作用。酶联免疫吸附试验（ELISA）结果表明，1 或 10 μM 的木樨草素可显著抑制 IL-1β诱导的 MMPs（MMP-1 和 MMP-3）和细胞因子（TNF-α和 IL-6）产生（P<0.05）。丝裂原激活蛋白激酶（MAPKs）是 RA 的一个有吸引力的治疗靶点，因为它们可以调节 MMP 和细胞因子的表达。还通过 ELISA 研究了木樨草素对 SW982 细胞中 MAPKs 和转录因子激活的影响。木樨草素抑制了 IL-1β诱导的 JNK 和 p38 的激活。此外，木樨草素抑制了 IL-1β诱导的激活蛋白-1（AP-1）和核因子-κB（NF-κB）的激活。这些结果表明，木樨草素通过抑制 MAPKs（JNK 和 p38）和转录因子（AP-1 和 NF-κB）减少了 SW982 细胞中 MMPs 和细胞因子的产生。
