Department of Nutrition and Food Hygiene, School of Public Health and Tropical Medicine, Southern Medical University, Guangzhou 510515, PR China.
Bioorg Med Chem Lett. 2011 Apr 15;21(8):2415-8. doi: 10.1016/j.bmcl.2011.02.071. Epub 2011 Feb 19.
The anti-inflammatory properties of soyasaponins (especially soyasaponins with different chemical structures) have scarcely been investigated. We investigated the inhibitory effects of five structural types of soyasaponins (soyasaponin A(1), A(2), I and soyasapogenol A, B) on the induction of nitric oxide (NO) and inducible NO synthase (iNOS) in murine RAW 264.7 cells activated with lipopolysaccharide (LPS). Soyasaponin A(1), A(2) and I (25-200 μg/mL) dose-dependently inhibited the production of NO and tumor necrosis factor α (TNF-α) in LPS-activated macrophages, whereas soyasapogenol A and B did not. Furthermore, soyasaponin A(1), A(2) and I suppressed the iNOS enzyme activity and down-regulated the iNOS mRNA expression both in a dose-dependent manner. The reporter gene assay revealed that soyasaponin A(1), A(2) and I decreased LPS-induced nuclear factor kappa B (NF-κB) activity. Soyasaponin A(1), A(2) and I exhibit anti-inflammatory properties by suppressing NO production in LPS-stimulated RAW 264.7 cells through attenuation of NF-κB-mediated iNOS expression. It is proposed that the sugar chains present in the structures of soyasaponins are important for their anti-inflammatory activities. These results have important implication for using selected soyasaponins towards the development of effective chemopreventive and anti-inflammatory agents.
大豆皂素(尤其是具有不同化学结构的大豆皂素)的抗炎特性几乎没有被研究过。我们研究了五种结构类型的大豆皂素(大豆皂素 A(1)、A(2)、I 和大豆皂醇 A、B)对脂多糖(LPS)激活的小鼠 RAW 264.7 细胞中一氧化氮(NO)和诱导型一氧化氮合酶(iNOS)诱导的抑制作用。大豆皂素 A(1)、A(2)和 I(25-200μg/mL)剂量依赖性地抑制 LPS 激活的巨噬细胞中 NO 和肿瘤坏死因子-α(TNF-α)的产生,而大豆皂醇 A 和 B 则没有。此外,大豆皂素 A(1)、A(2)和 I 还以剂量依赖性方式抑制 iNOS 酶活性和下调 iNOS mRNA 表达。报告基因检测表明,大豆皂素 A(1)、A(2)和 I 通过降低 LPS 诱导的核因子 kappa B(NF-κB)活性来抑制 iNOS 的表达。大豆皂素 A(1)、A(2)和 I 通过抑制 LPS 刺激的 RAW 264.7 细胞中 NO 的产生来发挥抗炎作用,这是通过减弱 NF-κB 介导的 iNOS 表达来实现的。据推测,大豆皂素结构中存在的糖链对其抗炎活性很重要。这些结果对于使用选定的大豆皂素开发有效的化学预防和抗炎药物具有重要意义。