Transepithelial transport of Cerulenin across Caco-2 cell monolayers.
The transepithelial transport of Cerulenin across Caco-2 cell monolayers was examined in this study. The permeated amounts of Cerulenin were measured by HPLC method to calculate the permeation rate and the apparent permeability coefficient (P(app)). The transport of Cerulenin was independent on apical pH and exhibited concentration-dependent and nonsatuable even at 10 mM Cerulenin. The permeation rate at 1 mM Cerulenin in the apical-to-basolateral direction was 0.151 ng/min/mg of protein and the P(app) was 3.76 x 10(-6) cm/second. The permeation rate of Cerulenin was affected by neither metabolic inhibitors nor inhibitors for P-glycoprotein, as was the same case in monolayers treated with cytochalasin D. All these data from experiments indicated that transport of Cerulenin across Caco-2 cell monolayers was not mediated by ATP-dependent transport systems nor via paracellular pathway, but via passive diffusion without efflux by P-glycoprotein.
Fu
Da-Hua
DH
Department of Medicine, Zhangzhou Health College, Zhangzhou Fujian, P.R. China.
Liu
Zhi-Li
ZL
Liu
Jun-Shi
JS
Luo
Yun
Y
Shu
Yong
Y
Huang
Shan-Hu
SH
Han
Zhi-Min
ZM
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism; D001692:Biological Transport; D018938:Caco-2 Cells; D002569:Cerulenin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D004058:Diffusion; D004305:Dose-Response Relationship, Drug; D054872:Fatty Acid Synthesis Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D007408:Intestinal Absorption; D007413:Intestinal Mucosa / Q000378:metabolism; D010539:Permeability
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D054872:Fatty Acid Synthesis Inhibitors; D002569:Cerulenin