Department of Pharmaceutical Analysis, School of Pharmacy, Fudan University, Shanghai, PR China.
J Sep Sci. 2014 Feb;37(3):250-6. doi: 10.1002/jssc.201301020. Epub 2013 Dec 27.
A new method employing HPLC, LC-MS, and hepatocyte membranes for the screening of bioactive compounds in traditional Chinese medicines (TCMs) has been proposed. We hypothesized that exposure of the TCM extracts to hepatocyte membranes should decrease the concentration of membrane-permeable compounds in the solution. Using this approach, the permeability of the compounds in Rhizoma Polygoni Cuspidati was investigated. By comparing chromatograms of samples prepared both before and after interaction with hepatocyte membranes, seven permeable compounds of Rhizoma Polygoni Cuspidati were identified. Additionally, it was found that piceid, resveratrol, emodin-8-β-d-glucoside, physcion-8-β-d-glucoside, aloe-emodin, emodin, and physcion combined specifically with hepatocyte membranes, which might indicate a useful approach for revealing the antiatherosclerotic effects of Rhizoma Polygoni Cuspidati. Therefore, the proposed method could be a good approach to predict the potential bioactivities of multiple compounds in TCMs simultaneously. Based on the significance of these results, this method could be a novel approach for identifying potentially bioactive components in other TCMs.
已提出一种采用 HPLC、LC-MS 和肝细胞膜筛选中药（TCM）中生物活性化合物的新方法。我们假设 TCM 提取物暴露于肝细胞膜应该会降低溶液中膜通透性化合物的浓度。使用这种方法，研究了虎杖中化合物的通透性。通过比较与肝细胞膜相互作用前后样品的色谱图，鉴定出了虎杖中的七种通透性化合物。此外，还发现白藜芦醇苷、白藜芦醇、大黄素-8-β-D-葡萄糖苷、大黄素-8-β-D-葡萄糖苷、芦荟大黄素、大黄素和大黄素与肝细胞膜特异性结合，这可能表明这是一种揭示虎杖抗动脉粥样硬化作用的有用方法。因此，所提出的方法可能是同时预测 TCM 中多种化合物潜在生物活性的好方法。基于这些结果的重要性，该方法可能是鉴定其他 TCM 中潜在生物活性成分的一种新方法。
