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药物转运体对于促进扩散及主动转运药物的吸收具有重要作用,研究其在缺氧时的变化将为提高药物在小肠的吸收提供重要依据。本实验研究了缺氧72 h后P-gp m RNA水平及蛋白水平的变化,并考察了P-gp变化后对其特异性底物(左氧氟沙星)在小肠吸收的影响。结果显示,缺氧后小肠组织中P-gp m RNA与蛋白的相对表达水平分别下调了50.80%和71.30%(P<0.05);缺氧组30~60、60~90、90~120和120~150 min各时间段的P_(eff)分别增加了56.16%、226.00%、77.74%和141.00%(P<0.05)。这一结果说明缺氧会导致小肠中P-gp的表达下调,使左氧氟沙星的外排减少,增加其在肠道的吸收。
Drug transporters play an important role in promoting diffusion and active transport of drugs, and studying their changes during hypoxia will provide important evidence for improving drug absorption in the small intestine. The present study investigated the changes of P-gp m RNA and protein levels 72 h after hypoxia, and investigated the effect of P-gp on the absorption of levofloxacin. The results showed that the relative expression levels of P-gp m RNA and protein in the small intestine were decreased by 50.80% and 71.30%, respectively (P <0.05), while those in the hypoxic group were 30-60, 60-90, 90-120 and 120 P eff increased by 56.16%, 226.00%, 77.74% and 141.00% (P <0.05) in each time period of ~ 150 min. This result indicates that hypoxia leads to the down-regulation of P-gp expression in the small intestine and reduces the efflux of levofloxacin and increases its absorption in the intestine.