title: Expression of P-glycoprotein and multidrug resistance-associated protein on human brain-microvascular endothelial cells with electromagnetic stimulation.
abstract: This study investigates the effect of electromagnetic field (EMF) on the expression of P-glycoprotein (P-gp) and multidrug resistance-associated protein (MRP) on human brain-microvascular endothelial cells (HBMECs). A monolayer of HBMECs was cocultured with human astrocytes for developing apical/basolateral membrane properties. The results revealed that an increase in the frequency of an EMF enhanced the endocytotic uptake of calcein-AM. Probenecid demonstrated a stronger inhibition to the efflux pumps than verapamil under the exposure to an EMF. The expressed quantities of P-gp and MRP1 after transcytosis of saquinavir were higher than those of azidothymidine, suggesting that the former induced a stronger drug resistance than the latter. In addition, an EMF with 750 Hz could effectively inhibit the expression of P-gp and MRP1. An appropriate exposure to an EMF can be efficient to deliver antiretroviral drugs into the brain via reducing the expressed efflux transporters on HBMECs.
authors: Department of Chemical Engineering, National Chung Cheng University, Chia-Yi, Taiwan, ROC. chmyck@ccu.edu.tw
authors: Yung-Chih
authors: YC
authors: Kuo
authors: Chin-Hsun
authors: CH
authors: Lu
mesh_terms: D018435:ATP Binding Cassette Transporter, Subfamily B / Q000378:metabolism*; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism*; D001921:Brain / Q000098:blood supply*; D004574:Electromagnetic Fields; D004705:Endocytosis; D004730:Endothelium, Vascular / Q000166:cytology / Q000378:metabolism*; D006801:Humans
chemical_list: D018435:ATP Binding Cassette Transporter, Subfamily B; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1