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大蓟提取的刺儿菜素的抗炎作用及相应机制

Anti-inflammatory effects and corresponding mechanisms of cirsimaritin extracted from Cirsium japonicum var. maackii Maxim.

作者信息

Shin Myoung-Sook, Park Jun Yeon, Lee Jaemin, Yoo Hye Hyun, Hahm Dae-Hyun, Lee Sang Cheon, Lee Sanghyun, Hwang Gwi Seo, Jung Kiwon, Kang Ki Sung

机构信息

Natural Constituents Research Center, Korea Institute of Science and Technology Gangneung, Institute of Natural Products, 210-340, Republic of Korea.

College of Korean Medicine, Gachon University, Seongnam 13120, Republic of Korea.

出版信息

Bioorg Med Chem Lett. 2017 Jul 15;27(14):3076-3080. doi: 10.1016/j.bmcl.2017.05.051. Epub 2017 May 17.

Abstract

In this study, we investigated the anti-inflammatory effects and mechanisms of cirsimaritin isolated from an ethanol extract of the aerial parts of Cirsium japonicum var. maackii Maxim. using RAW264.7 cells. The extract and its flavonoid cirsimaritin inhibited nitric oxide (NO) production and inducible nitric oxide synthase expression in RAW264.7 cells. Cirsimaritin inhibited interleukin-6, tumor necrosis factor-α, and NO production in a concentration-dependent manner in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. From a western blot study, pretreatment with cirsimaritin inhibited phosphorylation/degradation of IκBα and phosphorylation of Akt in LPS-stimulated RAW264.7 cells. Moreover, cirsimaritin suppressed activation of LPS-induced transcription factors, such as c-fos and signal transducer and activator of transcription 3 (STAT3), in RAW264.7 cells. Collectively, these results show that cirsimaritin possesses anti-inflammatory activity, which is regulated by inhibition of c-fos and STAT3 phosphorylation in RAW264.7 cells.

摘要

在本研究中,我们利用RAW264.7细胞研究了从大蓟(Cirsium japonicum var. maackii Maxim.)地上部分乙醇提取物中分离得到的刺槐素的抗炎作用及其机制。该提取物及其类黄酮刺槐素抑制了RAW264.7细胞中一氧化氮(NO)的产生和诱导型一氧化氮合酶的表达。在脂多糖(LPS)刺激的RAW264.7细胞中,刺槐素以浓度依赖的方式抑制白细胞介素-6、肿瘤坏死因子-α和NO的产生。从蛋白质印迹研究来看,用刺槐素预处理可抑制LPS刺激的RAW264.7细胞中IκBα的磷酸化/降解和Akt的磷酸化。此外,刺槐素在RAW264.7细胞中抑制了LPS诱导的转录因子如c-fos和信号转导及转录激活因子3(STAT3)的激活。总体而言,这些结果表明刺槐素具有抗炎活性,其通过抑制RAW264.7细胞中c-fos和STAT3的磷酸化来调节。

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