[Effects of morphine and pethidine on the expression of P-glycoprotein in mouse brain microvascular endothelial cells].
OBJECTIVE
To observe the effects of morphine and pethidine on P-glycoprotein (P-gp) expression in mouse brain microvascular endothelial cells and investigate the role of nuclear factor-kappaB (NF-kappaB) signaling pathway in morphine-induced up-expression of P-gp.


METHODS
The mouse brain microvascular endothelial cell line (b.END3) was subjected to pre-incubation with NF-kappaB inhibitor PDTC (5 micromol/L) for 1 h followed by stimulation with morphine (1 microg/ml) or pethidine (1 microg/ml) for 24 h. The bEnd.3 cells were then collected for Western blotting for P-gp expression.


RESULTS
A 24-h morphine stimulation induced an up-expression of P-gp in bEnd.3 cells by almost 200%. Pethidine in similar conditions did not affect P-gp expression in the cells. PDTC, the specific inhibitor of NF-kappaB, inhibited morphine-induced up-expression of P-gp in the cells.


CONCLUSIONS
Morphine can induce up-expression of endogenous P-gp in mouse brain microvascular endothelial cells. NF-kappaB signaling pathway is involved in the morphine-induced up-expression of P-gp.
Su
Jian
J
Department of Anesthesiology, First Municipal Hospital of Guangzhou Affiliated to Guangzhou Medical College, Guangzhou 510180, China. 434800989@qq.com
Ruan
Xiang-cai
XC
Zhang
Yue-hong
YH
She
Shou-zhang
SZ
Xu
Li-xin
LX
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism*; D000818:Animals; D001812:Blood-Brain Barrier / Q000187:drug effects / Q000378:metabolism; D001921:Brain / Q000098:blood supply; D002460:Cell Line; D042783:Endothelial Cells / Q000187:drug effects* / Q000378:metabolism; D008614:Meperidine / Q000494:pharmacology*; D051379:Mice; D009020:Morphine / Q000494:pharmacology*; D016328:NF-kappa B / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D016328:NF-kappa B; D009020:Morphine; D008614:Meperidine