Piao Xiang-Lan, Piao Xiang Shu, Kim Sung Woo, Park Jeong Hill, Kim Hyun Young, Cai Shao-Qing
School of Pharmaceutical Sciences, Peking University, Beijing, China.
Biol Pharm Bull. 2006 Sep;29(9):1911-5. doi: 10.1248/bpb.29.1911.
The objectives of this study were to investigate the radical-scavenging activity and protective potential of Sophora flavescens from oxidative damage by the radical generator 2,2'-azobis(2-amidinopropane)dihydrochloride (AAPH) in renal epithelial LLC-PK(1) cells and to identify the active components using the bioassay-linked fractionation method. The MeOH extract and fractions of CH(2)Cl(2), BuOH, and H(2)O from S. flavescens showed 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging effects in a dose-dependent manner (p<0.01),whereas only the BuOH and CH(2)Cl(2) fractions showed protective effects against LLC-PK(1) cellular damage induced by AAPH in a dose-dependent manner (p<0.01). In particular, the BuOH fraction had the most effective (p<0.05) antioxidative capacity. Employing a bioassay-linked HPLC/MS method, the active constituents from the BuOH fraction of S. flavescens were isolated and characterized as sophoraflavanone G and kurarinone with potent antioxidant effects against the DPPH radical, with IC(50) values of 5.26 and 7.73 microg/ml, respectively. Moreover, the compounds dose dependently recovered cell viability decreased by AAPH treatment (p<0.01), suggesting their protective roles against cellular oxidative damage. The results of this study suggest that S. flavescens has excellent antioxidative and kidney-protective potential and that flavonoids from S. flavescens, i.e., sophoraflavanone G and kurarinone, are the active constituents.
本研究的目的是研究苦参对肾上皮LLC-PK(1)细胞中由自由基引发剂2,2'-偶氮二(2-脒基丙烷)二盐酸盐(AAPH)所致氧化损伤的自由基清除活性和保护潜力，并采用生物活性导向分离法鉴定其活性成分。苦参的甲醇提取物以及二氯甲烷、正丁醇和水部位均呈剂量依赖性地表现出1,1-二苯基-2-苦基肼基(DPPH)自由基清除作用(p<0.01)，而只有正丁醇和二氯甲烷部位呈剂量依赖性地对AAPH诱导的LLC-PK(1)细胞损伤具有保护作用(p<0.01)。特别是，正丁醇部位具有最有效的抗氧化能力(p<0.05)。采用生物活性导向的高效液相色谱/质谱联用方法，从苦参正丁醇部位分离并鉴定出活性成分槐黄酮G和苦参酮，它们对DPPH自由基具有强大的抗氧化作用，IC(50)值分别为5.26和7.73 μg/ml。此外，这些化合物呈剂量依赖性地恢复了因AAPH处理而降低的细胞活力(p<0.01)，表明它们对细胞氧化损伤具有保护作用。本研究结果表明，苦参具有优异的抗氧化和肾脏保护潜力，苦参中的黄酮类化合物，即槐黄酮G和苦参酮，是活性成分。
