酚红外排水平评价肺上皮细胞多药耐药相关蛋白1的功能

中国临床药理学与治疗学 ›› 2013, Vol. 18 ›› Issue (2): 127-131.

酚红外排水平评价肺上皮细胞多药耐药相关蛋白1的功能

陶秀华, 汪电雷, 曹银, 汪辰吟, 陈金佩, 杨丽丽

安徽中医学院,合肥 230038,安徽

收稿日期:2012-08-06 修回日期:2012-08-06 出版日期:2013-02-26 发布日期:2013-02-28
通讯作者: 汪电雷,通信作者,男,博士,副教授,硕士研究生导师,研究方向:药物代谢动力学。 Tel: 0551-5169230 E-mail: dlwang@ahtcm.edu.cn
作者简介:陶秀华,男,硕士在读,研究方向:药物代谢动力学。 Tel: 13721072550 E-mail: xiuhuatao@163.com
基金资助:
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)

Evaluation on the function of MRP1 in pulmonary epithelial cells by the efflux level of phenolsulfonphthalein

TAO Xiu-hua, WANG Dian-lei, CAO Yin, WANG Chen-yin, CHEN Jin-pei, YANG Li-li

Anhui University of Traditional Chinese Medicine, Hefei 230038, Anhui, China

Received:2012-08-06 Revised:2012-08-06 Online:2013-02-26 Published:2013-02-28

摘要/Abstract

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(250 mg/kg),30 min 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(150 mg/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 60 min 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。

关键词: 酚红, 外排水平, 多药耐药相关蛋白1, 丙磺舒

Abstract: AIM: To evaluate the function of MRP1 in pulmonary epithelial cells by the efflux level of substrate using phenolsulfonphthalein as MRP1 substrate and probenecid as MRP1-specific 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 min after phenolsulfonphthalein (250 mg/kg) was administered to the control group mouse by intravenous injection. The inhibitor inhaled groups mouse was administered phenolsulfonphthalein (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 after phenolsulfonphthalein administration. The phenolsulfonphthalein concentration in BALF and plasma was determined and the concentration 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. Compared with control group, the phenolsulfonphthalein concentration in BALF and the phenolsulfonphthalein concentration of in BALF/plasma 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 pulmonary epithelial cells MRP1.

Key words: Phenolsulfonphthalein, Efflux level, MRP1, Probenecid

中图分类号:

R965.2

陶秀华, 汪电雷, 曹银, 汪辰吟, 陈金佩, 杨丽丽. 酚红外排水平评价肺上皮细胞多药耐药相关蛋白1的功能[J]. 中国临床药理学与治疗学, 2013, 18(2): 127-131.

TAO Xiu-hua, WANG Dian-lei, CAO Yin, WANG Chen-yin, CHEN Jin-pei, YANG Li-li. Evaluation on the function of MRP1 in pulmonary epithelial cells by the efflux level of phenolsulfonphthalein[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2013, 18(2): 127-131.

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