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作 者:陶秀华[1] 汪电雷[1] 曹银[1] 汪辰吟[1] 陈金佩[1] 杨丽丽[1]
机构地区:[1]安徽中医学院
出 处:《中国临床药理学与治疗学》2013年第2期127-131,共5页Chinese Journal of Clinical Pharmacology and Therapeutics
基 金:国家自然科学基金(81001592);教育部科学技术重点项目资助(210101);安徽高校省级自然科学研究重点项目资助(KJ2010A210)
摘 要:目的:以酚红为多药耐药相关蛋白1(MRP1)的底物,丙磺舒为其抑制剂,通过酚红的外排水平建立评价肺上皮细胞MRP1的功能的方法。方法:小鼠静脉注射酚红(250mg/kg),30min后进行肺泡灌洗,测定灌洗液中酚红的浓度,并以雾化吸入MRP1特异性抑制剂丙磺舒(150mg/kg)作为对照,观察给予抑制剂前后灌洗液中酚红浓度及灌洗液中酚红浓度/血浆中酚红浓度比值的变化,来评价小鼠肺上皮细胞MRP1功能的改变。结果:与未给予抑制剂相比,给予MRP1抑制剂丙磺舒后,血浆中酚红浓度无显著性差异,但与未给予抑制剂相比,给予MRP1抑制剂丙磺舒60min后,其肺泡灌洗液中酚红浓度、灌洗液中酚红浓度/血浆中酚红浓度比值显著性降低。结论:肺泡灌洗液中酚红的外排水平反映小鼠肺上皮细胞MRP1功能的改变。AIM: To evaluate the function of MRP1 in pulmonary epithelial cells by the efflux level of suhstrate using pheno[sulfonphthalein as MRP1 substrate and prohenecid as MRPl-specif- ic inhibitor. METHODS: The mouse was divided into the control group and inhibitor inhaled groups. The bronchoalveolar lavage fluid (BALF) and plasma samples were collected at 30 rain after phenolsulfonphthalein (250 mg/kg) was administered to the intravenous injection. control group mouse by The inhibitor inhaled groups mouse was administered phenolsulfonph- thalein (250 mg/kg) at 10, 30 and 60 min after inhaled probenecid (150 mg/kg), and the BALF and plasma samples were collected at 30 min af- ter phenolsulfonphthalein administration. The phenolsulfonphthalein concentration in BALF and plasma was determined and the concentra- tion of in BALF/plasma ratio was calculated. RESULTS:There was no difference in the plasma concentration of phenolsulfonphthalein between the control group and inhibitor groups, Com- pared with control group, the phenolsulfonph- thalein concentration in BALF and the phenol- sulfonphthalein concentration of in BALF/plas- ma ratio of the 60 min after inhaled probenecid group had significant difference. CONCLUSION: The efflux level of phenolsulfonphthalein in BALF could reflect the function of mouse pul- monary epithelial cells MRP1.
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