利用体外血脑屏障模型结合高压液相-质谱技术筛选传统中药——朝鲜淫羊藿有效成分(英文)

Screening of Effective Ingredients of Traditional Chinese Herb Epimediumkoreanum Nakai by Combination of Co-cultured ECV304/C6 Cells as an in vitro BBB Model with HPLC-MS Analysis

血脑屏障(blood-brain barrier,BBB)是位于中枢神经系统(central nervous system,CNS)和中枢系统环境间的一层生理保护屏障.凡是作用于CNS的药物,必须先通过BBB.为了寻找能够进入CNS的药物,通过细胞培养时间优化和跨膜电阻测定等,建立了ECV304/C6共培养通过BBB药物筛选模型.并将该模型应用于从传统中药淫羊藿的提取物中,筛选可能作用于CNS的活性成分,结合高压液相色谱-质谱联用技术(HPLC-MS),对筛选出的化合物进行鉴定分析.研究结果表明,淫羊藿提取物中至少有13种成分能够穿越BBB模型,其中2种成分被确认为淫羊藿苷和宝藿苷Ⅰ,为CNS药物开发的早期快速筛选提供了实验依据.

The blood-brain barrier（BBB） serves as a physiological protective barrier between the central nervous system（CNS） and the systemic circulation.For CNS drugs,ready permeating across the BBB is necessary for efficacy.To select BBB permeable drug candidates,an in vitro BBB model using co-cultured ECV304/C6 cells was adopted in this study.The transendothelial electrical resistance showed that the cultured ECV304 cell monolayer was of integrity and vitality.The active components of Epimedium koreanum Nakai,a widely used traditional Chinese herb,were screened with this in vitro BBB model,and then analyzed by HPLC-MS.We found that 13 compounds at least from the extract of Epimedium could permeate across BBB model,in which icariin and baohuoside-Ⅰ were identified.These results indicated that the co-cultured ECV304/C6 model combined with HPLC-MS analysis was a potential tool for screening of BBB permeable drug candidates from plant-derived materials.