Berginc Katja, Zakelj Simon, Ursic Darko, Kristl Albin
Faculty of Pharmacy, University of Ljubljana, Slovenia.
Biol Pharm Bull. 2009 Apr;32(4):694-9. doi: 10.1248/bpb.32.694.
The growing concomitant consumption of drugs and herbal preparations such as garlic, and the numerous reports about the influence of herbal preparations on intestinal transport, led us to evaluate the influence of aged garlic extract on the transport function and electrophysiological parameters of the small intestinal mucosa. Aged garlic extract induced increase of the absolute value of the transepithelial potential difference and of the short-circuit current in both permeability models tested (rat jejunum, Caco-2 cell monolayers) without affecting transepithelial electrical resistance. It also caused a significant increase of the P-glycoprotein and multidrug resistance associated protein 2 mediated effluxes through rat jejunum of marker substrates Rhodamine 123 and 2,4-dinitrophenyl-S-glutathione, respectively. Rhodamine 123 efflux through the Caco-2 cell monolayers was not altered by aged garlic extract, whereas the efflux of 2,4-dinitrophenyl-S-glutathione increased significantly. So altered activity of the important transport proteins could significantly change the pharmacokinetic properties of conventional medicines taken concomitantly with aged garlic extract.
药物与大蒜等草药制剂的同时服用日益增多，且有大量关于草药制剂对肠道转运影响的报道，这促使我们评估陈年大蒜提取物对小肠黏膜转运功能和电生理参数的影响。在两种测试的通透模型（大鼠空肠、Caco-2细胞单层）中，陈年大蒜提取物均使跨上皮电位差的绝对值和短路电流增加，而不影响跨上皮电阻。它还分别使标记底物罗丹明123和2,4-二硝基苯基-S-谷胱甘肽通过大鼠空肠的P-糖蛋白和多药耐药相关蛋白2介导的外排显著增加。通过Caco-2细胞单层的罗丹明123外排不受陈年大蒜提取物影响，而2,4-二硝基苯基-S-谷胱甘肽的外排则显著增加。因此，重要转运蛋白活性的改变可能会显著改变与陈年大蒜提取物同时服用的传统药物的药代动力学特性。
