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山柑(Capparis spinosa L.)果实中的双黄酮类化合物及其抑制 NF-κB 激活的作用。

Biflavonoids from Caper (Capparis spinosa L.) fruits and their effects in inhibiting NF-kappa B activation.

机构信息

Shanghai Institute of Pharmaceutical Industry, 1320 West Beijing Road, Shanghai 200040, PR China.

出版信息

J Agric Food Chem. 2011 Apr 13;59(7):3060-5. doi: 10.1021/jf105017j. Epub 2011 Mar 7.

DOI:10.1021/jf105017j
PMID:21381749
Abstract

Caper (Capparis spinosa L.) fruits have been widely used as food and folk medicine in the Mediterranean basin and in central and west Asia. In this study, two biflavonoids, isoginkgetin, and ginkgetin, together with three other flavonoids, were isolated from caper fruits. Their chemical structures were elucidated by spectroscopic analyses and comparison with literature. To our knowledge, isoginkgetin, ginkgetin and sakuranetin were identified in caper for the first time. Notably, it is also the first time that biflavonoids have ever been found in the Capparidaceae. Concentrations of the two biflavonoids were measured in caper fruits collected from four major growing areas in northwest China. The anti-inflammatory effects of the flavonoids from caper fruits were evaluated by secreted placental alkaline phosphatase (SEAP) reporter assay, which was designed to measure nuclear factor-kappa B (NF-κB) activation. Isoginkgetin and ginkgetin showed inhibitory effects in initial screen at 20 μM, while the effect of ginkgetin was much greater than that of isoginkgetin. In a dose-response experiment, the IC(50) value of ginkgetin was estimated at 7.5 μM, suggesting it could be a strong NF-κB inhibitor and worthy of study in vivo.

摘要

刺山柑(Capparis spinosa L.)的果实被广泛应用于地中海盆地和中亚及西亚地区的食品和民间药物。在这项研究中,从刺山柑果实中分离得到了两种双黄酮类化合物,异银杏素和银杏素,以及另外三种类黄酮。通过光谱分析和与文献比较确定了它们的化学结构。据我们所知,异银杏素、银杏素和樱花素是首次在刺山柑中被鉴定出来的。值得注意的是,双黄酮类化合物也首次在山柑科中被发现。测量了来自中国西北部四个主要种植区的刺山柑果实中两种双黄酮的浓度。通过设计用于测量核因子-κB(NF-κB)激活的胎盘碱性磷酸酶(SEAP)报告基因测定,评估了刺山柑果实中类黄酮的抗炎作用。异银杏素和银杏素在 20μM 的初始筛选中表现出抑制作用,而银杏素的作用明显大于异银杏素。在剂量反应实验中,银杏素的 IC50 值估计为 7.5μM,表明它可能是一种很强的 NF-κB 抑制剂,值得在体内进行研究。

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