Major active components in grapefruit, orange, and apple juices responsible for OATP2B1-mediated drug interactions.

@article{Shirasaka2013MajorAC,
  title={Major active components in grapefruit, orange, and apple juices responsible for OATP2B1-mediated drug interactions.},
  author={Y. Shirasaka and Megumi Shichiri and Takanori Mori and T. Nakanishi and I. Tamai},
  journal={Journal of pharmaceutical sciences},
  year={2013},
  volume={102 9},
  pages={
          3418-26
        }
}
We aimed to explore the major active components in grapefruit juice (GFJ), orange juice (OJ), and apple juice (AJ) that are responsible for OATP2B1-mediated drug interactions, by means of in vitro studies using Xenopus oocytes expressing OATP2B1 with a typical OATP2B1 substrate, estrone-3-sulfate. All three juices inhibited OATP2B1-mediated estrone-3-sulfate uptake with half-maximum inhibition (IC50 ) values of 0.222% (GFJ), 0.807% (OJ), and 2.27% (AJ). Eight major flavonoids (naringin… Expand
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