pgp - publications

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1. J Asian Nat Prod Res. 2012 Jan;14(1):14-21.

Uptake characteristics of pinocembrin and its effect on p-glycoprotein at the
blood-brain barrier in in vitro cell experiments.

Yang ZH, Sun X, Qi Y, Mei C, Sun XB, Du GH.

a Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences
and Peking Union Medical College , Beijing , 100193 , China.

One purpose of the present study was to investigate the uptake characteristics of
pinocembrin (PCB) and its effect on p-glycoprotein (P-gp) at the blood-brain
barrier (BBB). Cultured rat brain microvascular endothelial cells (rBMECs) were
used as an in vitro BBB model. Experiments were conducted to examine time-,
concentration-, and temperature-dependent elements of PCB uptake, and the effect
of classical P-gp inhibitors, cyclosporin A (CsA) and verapamil (Ver), on the
steady-state uptake of PCB. Uptake of rhodamine 123 (Rho123), the typical P-gp
substance, was measured with or without PCB. Meanwhile, the protein level of P-gp
after incubation with PCB was detected by Western blot assay. The results
demonstrated that PCB uptake by rBMECs was in a time- and concentration-dependent
manner. CsA and Ver slightly increased PCB steady-state uptake by less than 10%
(p>0.05). Similar results were observed in Rho123 uptake by co-administration of
PCB. Further results were obtained by Western blot assay. PCB might not affect
P-gp expression in rBMECs. Overall, the findings demonstrate that the passive
transport process may be the main process for PCB to pass through the BBB, and
P-gp is likely to have a little effect on the PCB transport process. Furthermore,
PCB may not affect the functional activity and the protein expression of the P-gp
transporter at the BBB.

PMID: 22263589 [PubMed - in process]