缺氧大鼠小肠中P-gp的变化及其对左氧氟沙星吸收的影响

发布时间：2018-01-17 03:19

本文关键词：缺氧大鼠小肠中P-gp的变化及其对左氧氟沙星吸收的影响　出处：《药学学报》2016年09期 　论文类型：期刊论文

【摘要】：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%(P0.05);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%(P0.05)。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。
[Abstract]:Drug transporters play an important role in promoting diffusion and active drug absorption. The changes of P-gpm RNA and protein levels in the small intestine after 72 h hypoxia were studied. The effect of P-gp on the absorption of levofloxacin in the small intestine was investigated. The relative expression levels of P-gpm RNA and protein in small intestine after hypoxia were down-regulated by 50.80% and 71.30, respectively. In the hypoxia group, the levels of PSD at each time period of 30 ~ 60 ~ 60 ~ 90 ~ 90 min and 120 ~ 150 min increased by 56.16% and 226.00%, respectively. The results showed that hypoxia could lead to the down-regulation of P-gp expression in the small intestine, decrease the efflux of levofloxacin and increase the absorption of levofloxacin in the intestine.
【作者单位】：兰州军区兰州总医院全军高原环境损伤防治重点实验室;
【基金】：国家自然科学基金资助项目(81403004,81673508) 全军后勤科研“十二五”计划重点项目(AWS14L005)
【分类号】：R965
【正文快照】： 越来越多的研究表明,急性高原缺氧会影响药物的药代动力学参数,使药物的疗效及不良反应发生改变,影响高原药代动力学参数的因素众多,包括胃排空、血液流变学、心肺功能、肝肾功能、细胞色素P450酶等[1-3]。缺氧对于药物代谢酶的影响是目前的研究热点[4-9],但是药物代谢酶主要

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