Van Gelder J, Deferme S, Annaert P, Naesens L, De Clercq E, Van den Mooter G, Kinget R, Augustijns P
Laboratorium voor Farmacotechnologie en Biofarmacie, Campus Gasthuisberg O&N, Katholieke Universiteit, Leuven, Belgium.
Drug Metab Dispos. 2000 Dec;28(12):1394-6.
Previous studies have shown that strawberry extract increases the transepithelial transport of tenofovir disoproxil, an esterase-sensitive prodrug of the antiviral compound tenofovir (formerly PMPA), across Caco-2 monolayers. This increase in transport was at least partially due to inhibition of its intestinal metabolism. To further study the feasibility of this absorption enhancing strategy, the influence of various concentrations of strawberry extract (0-2%) on the intestinal absorption of tenofovir disoproxil (100 microM) was assessed using an in situ perfusion model with immediate blood sampling from the mesenteric vein, a model closer to the in vivo situation than the in vitro Caco-2 system. Inclusion of strawberry extract (1%) resulted in a 7-fold increase in the appearance of tenofovir equivalents. The metabolism of tenofovir disoproxil in the intestinal perfusate was significantly lower in the presence of strawberry extract (1%), showing that the metabolism of tenofovir disoproxil is reduced by the flavoring extract.
先前的研究表明，草莓提取物可增加替诺福韦酯（一种抗病毒化合物替诺福韦的酯酶敏感前药，原称PMPA）跨Caco-2单层细胞的跨上皮转运。转运的增加至少部分归因于其肠道代谢受到抑制。为了进一步研究这种吸收增强策略的可行性，使用一种原位灌注模型并从肠系膜静脉立即采血，评估了不同浓度（0-2%）的草莓提取物对替诺福韦酯（100微摩尔）肠道吸收的影响，该模型比体外Caco-2系统更接近体内情况。加入1%的草莓提取物使替诺福韦等效物的出现量增加了7倍。在存在1%草莓提取物的情况下，替诺福韦酯在肠道灌注液中的代谢显著降低，表明调味提取物可降低替诺福韦酯的代谢。
