Department of Pharmaceutical Analysis, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, PR China.
J Pharm Biomed Anal. 2012 Nov;70:194-201. doi: 10.1016/j.jpba.2012.06.030. Epub 2012 Jun 28.
A new method employing HPLC, LC-MS, liposomes and cell membranes for the screening of bioactive compounds in traditional Chinese medicines (TCMs) has been proposed. We hypothesized that exposure of the TCM extracts to liposome membranes or cell membranes should decrease the concentration of membrane-permeable compounds in the solution. Using this approach, the permeability of the compounds in Radix Salviae Miltiorrhizae was investigated. By comparing chromatograms of samples prepared both before and after interaction with liposome membranes, erythrocyte membranes and cardiac myocyte membranes, 12 permeable compounds of Radix Salviae Miltiorrhizae were identified, and they were proven to be biologically active, with the exception of vanillic acid. There was a good correlation between the liposome model and the erythrocyte membranes, which was determined by comparing the binding degree of the permeable compounds (n=0.9059). Additionally, it was found that dihydrotanshinone I, cryptotanshinone, tanshinone I, tanshinone IIA combined specifically with cardiac myocyte membranes, which might indicate a useful approach for revealing the cardiovascular effects of Radix Salviae Miltiorrhizae. Based on these results, this method could be a novel approach for identifying potentially bioactive components in other TCMs.
一种新的方法，采用 HPLC、LC-MS、脂质体和细胞膜，用于筛选中药（TCM）中的生物活性化合物。我们假设，将 TCM 提取物暴露于脂质体膜或细胞膜中，应该会降低溶液中膜通透性化合物的浓度。使用这种方法，研究了丹参中化合物的通透性。通过比较与脂质体膜、红细胞膜和心肌细胞膜相互作用前后样品的色谱图，鉴定出 12 种丹参的通透性化合物，除香草酸外，它们均被证明具有生物活性。脂质体模型与红细胞膜之间具有良好的相关性，通过比较通透性化合物的结合程度（n=0.9059）来确定。此外，还发现二氢丹参酮 I、隐丹参酮、丹参酮 I、丹参酮 IIA 特异性地与心肌细胞膜结合，这可能表明揭示丹参心血管作用的一种有用方法。基于这些结果，这种方法可能成为鉴定其他 TCM 中潜在生物活性成分的新方法。
