Inhibition of vinblastine efflux mediated by P-glycoprotein by grapefruit juice components in caco-2 cells.

@article{Takanaga1998InhibitionOV,
  title={Inhibition of vinblastine efflux mediated by P-glycoprotein by grapefruit juice components in caco-2 cells.},
  author={Hitomi Takanaga and Akiko Ohnishi and Hirotaka Matsuo and Yasufumi Sawada},
  journal={Biological & pharmaceutical bulletin},
  year={1998},
  volume={21 10},
  pages={1062-6}
}
We investigated the effect of components in grapefruit juice (GFJ) on the transport of vinblastine, a substrate of P-glycoprotein (P-gp), across Caco-2 cells. The apical to basolateral flux of [3H]vinblastine was increased in the presence of GFJ extracts. The steady-state uptake of [3H]vinblastine from the apical side was significantly increased in the presence of GFJ in a dose-dependent manner within the range of 2.5 to 50% (v/v) of GFJ. Although naringin and naringenin reduced apical efflux… CONTINUE READING

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