TY - JOUR
T1 - P-glycoprotein as the drug efflux pump in primary cultured bovine brain capillary endothelial cells
AU - Tsuji, Akira
AU - Terasaki, Tetsuya
AU - Takabatake, Yasushi
AU - Tenda, Yoshiyuki
AU - Tamai, Ikumi
AU - Yamashima, Tetsumori
AU - Moritani, Shuzo
AU - Tsuruo, Takashi
AU - Yamashita, Junkoh
N1 - Funding Information:
The authors thank Mr. Saburo Okabe, Meat Inspection Center of Kanazawa City (Kanazawa, Japan) for providingu s with fresh bovine brains. This work was supported in part by a Grant-in-Aidf or ScientificR esearch fromt he Ministryo f Education,S cience
Funding Information:
and Culture, Japan, and grants from the Project Research Foundation of the Graduate School of Natural Science and Technology, Kanazawa University, and the Hokkoku Cancer Research Foundation.
Copyright:
Copyright 2014 Elsevier B.V., All rights reserved.
PY - 1992
Y1 - 1992
N2 - The expression of a functional P-glycoprotein (P-gp) which pumps drugs out of brain capillary endothelial cells (BCEC) into blood was studied by evaluating the steady-state uptake and efflux of vincristine (VCR) by primary cultured bovine BCEC. The steady-state uptake of VCR was increased in the presence of metabolic inhibitors, and an anti-P-gp monoclonal antibody, MRK16, as well as verapamil and steroid hormones which are known to reverse multidrug resistance in tumor cells. Furthermore, efflux of VCR from BCEC was inhibited by verapamil. By immunohistochemistry, P-gp was localized at the luminal side of the capillary endothelial cells in both gray matter of bovine brain and primary cultured BCEC. These data suggest that P-gp functions as a drug efflux pump at the luminal side of BCEC and regulates the transfer of certain lipophilic drugs from the blood into the brain.
AB - The expression of a functional P-glycoprotein (P-gp) which pumps drugs out of brain capillary endothelial cells (BCEC) into blood was studied by evaluating the steady-state uptake and efflux of vincristine (VCR) by primary cultured bovine BCEC. The steady-state uptake of VCR was increased in the presence of metabolic inhibitors, and an anti-P-gp monoclonal antibody, MRK16, as well as verapamil and steroid hormones which are known to reverse multidrug resistance in tumor cells. Furthermore, efflux of VCR from BCEC was inhibited by verapamil. By immunohistochemistry, P-gp was localized at the luminal side of the capillary endothelial cells in both gray matter of bovine brain and primary cultured BCEC. These data suggest that P-gp functions as a drug efflux pump at the luminal side of BCEC and regulates the transfer of certain lipophilic drugs from the blood into the brain.
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U2 - 10.1016/0024-3205(92)90537-Y
DO - 10.1016/0024-3205(92)90537-Y
M3 - Article
C2 - 1357522
AN - SCOPUS:0026760889
VL - 51
SP - 1427
EP - 1437
JO - Life Sciences
JF - Life Sciences
SN - 0024-3205
IS - 18
ER -