Institute of Chinese Medicine, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong; State Key Laboratory of Phytochemistry and Plant Resources in West China, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong.
Phytother Res. 2014 Mar;28(3):395-404. doi: 10.1002/ptr.5002. Epub 2013 May 3.
The root of Astragalus membranaceus (AR), which has been widely used in Traditional Chinese herbal formulae for treating foot ulcer, was found to exhibit anti-inflammatory property, but its molecular mechanism still remains unknown. We previously identified the anti-inflammatory sub-fraction using bioassay-guided fractionation. The objective of the present study was to investigate the anti-inflammatory mechanism of the major active fraction (MAF) (0.039 to 0.156 mg/mL) using lipopolysaccharide (LPS)-stimulated mouse macrophage RAW 264.7 cells. MAF was shown to inhibit LPS-induced mRNA and protein expression of inducible nitric oxide synthase by 54.7% and 65.1%, respectively. Additionally, MAF down-regulated the protein expression of cyclooxygenase-2 and MAPK regulator by 45.0% to 74.6%, as well as the reduction of DNA binding activity of nuclear factor kappa B (NFκB) by 66.5%. It also attenuated the production of prostaglandin E2 , interleukin-1 beta (IL-1β), IL-6 and tumor necrosis factor alpha by 21.2% to 86.2%. Furthermore, the chemical constituents of MAF were identified. A total of 13 known chemical compounds were found in MAF, including five isoflavonoids and eight saponins. In conclusion, a bioactive fraction of AR was identified which possessed anti-inflammatory property by reducing the release of inflammatory mediators and inactivation of NFκB through MAPK signalling pathway.
黄芪（AR）的根部已广泛用于治疗足部溃疡的中药方剂中，具有抗炎特性，但分子机制尚不清楚。我们之前使用生物测定指导的分级分离法鉴定了抗炎亚组分。本研究的目的是使用脂多糖（LPS）刺激的小鼠巨噬细胞 RAW 264.7 细胞研究主要活性组分（MAF）（0.039 至 0.156 mg/mL）的抗炎机制。MAF 显示出抑制 LPS 诱导的诱导型一氧化氮合酶的 mRNA 和蛋白质表达分别为 54.7％和 65.1％。此外，MAF 将环氧化酶-2 和 MAPK 调节剂的蛋白表达下调 45.0％至 74.6％，并降低核因子 kappa B（NFκB）的 DNA 结合活性 66.5％。它还减弱了前列腺素 E2、白细胞介素-1β（IL-1β）、IL-6 和肿瘤坏死因子-α的产生，降低了 21.2％至 86.2％。此外，鉴定了 MAF 的化学成分。在 MAF 中发现了 13 种已知的化学化合物，包括五种异黄酮和八种皂苷。总之，鉴定出 AR 的生物活性组分具有抗炎作用，通过减少炎症介质的释放和通过 MAPK 信号通路失活 NFκB。
