Application of d-Penicillamine2,5-enkephalin to characterization of sandwich-cultured hepatocytes transport activities
Guo Cen1; He Lei1; Yao Dan2; Pan Guoyu2; Wang Guangji1
刊名Chinese Journal of Clinical Pharmacology and Therapeutics
2013
卷号18期号:5页码:506-512
关键词LC/MS/MS DPDPE Transporter Sandwich-cultured rat hepatocytes LC/MS/MS DPDPE
ISSN号1009-2501
其他题名d-Penicillamine2,5-enkephalin作为底物考察三明治大鼠原代肝细胞的转运体功能研究
文献子类Article
英文摘要AIM:To develop a sensitive and rapid method for determining the concentration of d-Penicillamine2,5-enkephalin (DPDPE)in hepatocytes and Hank's buffer by LC/MS/MS. And to evaluate the function of transporters in sandwich-cultured rat hepatocytes (SCRH)using DPDPE as the probe substrate.METHODS: Co-incubate DPDPE with SCRH treated by alpha-naphthylisothiocyanate, the model compound,and measure the accumulation and the efflux of DPDPE by SCRH.The concentration of DPDPE in hepatocytes or Hank's buffer was determined by LC/MS/MS.RESULTS:DPDPE had a good linearity from 0.5to 50ng/mL(r~2= 0.9995)in Hank's buffer and from 0.1to 5ng/ well(r~2=0.9997)in hepatocytes in the LC/MS/ MS method established in this study. This method was sensitive enough to quantify DPDPE used as probe substrate in SCRH transport studies.The inter-and intra-day precision (RSD) were less than 15% and the recoveries were above 65%.The basolateral uptake and canalicular efflux of DPDPE by SCRH was inhibited by ANIT without change in the basolateral efflux. CONCLUSION:The analytical method established here is selective,sensitive and feasible to determine DPDPE used as probe substrate in the evaluation of membrane transporters in SCRH.
资助项目国家自然科学基金项目[00000000] ; 江苏省药代动力学重点实验室提升项目[00000000]
WOS研究方向Pharmacology & Pharmacy (provided by Clarivate Analytics)
语种中文
CSCD记录号CSCD:4853330
内容类型期刊论文
源URL[http://119.78.100.183/handle/2S10ELR8/267776]  
专题药物安全性评价中心
通讯作者Pan Guoyu
作者单位1.Key Laborary of Drug Metabolism and Pharmacokinetics,China Pharmaceutical University, Nanjing, Jiangsu 210009, China.;
2.Center for Drug Safety Evaluation & Research,Shanghai Institute of Materia Medica,Chinese Academy of Sciences, Shanghai 201203, China.
推荐引用方式
GB/T 7714
Guo Cen,He Lei,Yao Dan,et al. Application of d-Penicillamine2,5-enkephalin to characterization of sandwich-cultured hepatocytes transport activities[J]. Chinese Journal of Clinical Pharmacology and Therapeutics,2013,18(5):506-512.
APA Guo Cen,He Lei,Yao Dan,Pan Guoyu,&Wang Guangji.(2013).Application of d-Penicillamine2,5-enkephalin to characterization of sandwich-cultured hepatocytes transport activities.Chinese Journal of Clinical Pharmacology and Therapeutics,18(5),506-512.
MLA Guo Cen,et al."Application of d-Penicillamine2,5-enkephalin to characterization of sandwich-cultured hepatocytes transport activities".Chinese Journal of Clinical Pharmacology and Therapeutics 18.5(2013):506-512.
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