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首页> 外文会议>International Conference on Food Factors >A bitter melon extract inhibits the P-glycoprotein activity in intestinal Caco-2 cells: Monoglyceride as an active compound
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A bitter melon extract inhibits the P-glycoprotein activity in intestinal Caco-2 cells: Monoglyceride as an active compound

机译：苦瓜提取物抑制肠道CaCo-2细胞中的p-糖蛋白活性：作为活性化合物的单甘油酯

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摘要

P-glycoprotein (P-gp) is a 170 kDa membrane protein that belongs to the ATP-binding cassette (ABC) transporter superfamily. In normal tissues, P-gp functions as an ATP-dependent efflux pump that excretes highly hydrophobic xenobiotic compounds, playing an important role in protecting the cells/tissues from xenobiotics. In the present study, chemical substances that could directly modulate the intestinal P-gp activity were searched in vegetables and fruits. By using human intestinal epithelial Caco-2cells as a model of the small intestinal cells, we observed that a bitter melon fraction extracted from 40% methanol showed the greatest increase of the rhodamine-123 accumulation by Caco-2 cells. Inhibitory compounds in the bitter melon fraction were then isolated by HPLC using Pegasil C4 and Pegasil ODS columns. The HPLC fraction having the highest activity was analyzed by :H-NMR and FAB-MS, and the active compound was identified as 1-monopalmitin. It is interesting that certain types of monoglyceridemight be involved in the drug bioavailability by specifically inhibiting the efflux mediated by P-gp.
机译：p-糖蛋白（P-GP）是170kDa膜蛋白，属于ATP结合盒（ABC）转运蛋白超家族。在正常组织中，P-GP用作ATP依赖性的外排泵，其排出高度疏水的异蛋白化合物，在保护细胞/组织免受异卵胞生物学中起着重要作用。在本研究中，在蔬菜和水果中搜索可直接调节肠P-GP活性的化学物质。通过使用人肠上皮的Caco-2cells作为小肠细胞的模型，我们观察到40％的甲醇提取的苦瓜级分显示通过Caco-2细胞的若丹明123积累的最大增加。然后，使用Pegasil C4和Pegasil ODS柱通过HPLC分离苦瓜级分中的抑制化合物。通过：H-NMR和Fab-MS分析具有最高活性的HPLC级分，并将活性化合物鉴定为1-单拷贝。有趣的是，某些类型的单甘油以通过特异性抑制P-GP介导的流出来参与药物生物利用性。

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