Mechanism-based CYP2D6 inactivation by acridone alkaloids of Indonesian medicinal plant Lunasia amara.

@article{Takahashi2012MechanismbasedCI,
  title={Mechanism-based CYP2D6 inactivation by acridone alkaloids of Indonesian medicinal plant Lunasia amara.},
  author={Naoto Takahashi and Subehan and Shigetoshi Kadota and Yasuhiro Tezuka},
  journal={Fitoterapia},
  year={2012},
  volume={83 4},
  pages={774-9}
}
Fourteen acridone alkaloids isolated from Lunasia amara Blanco were tested for their mechanism-based inhibition on human liver microsomal dextromethorphan O-demethylation activity, a prototype marker for cytochrome P450 2D6 (CYP2D6). Among the 14 compounds, 5-hydroxygraveroline (1), 8-methoxyifflaiamine (2), lunamarine (3), and lunine (12) increased their inhibitory activity with increasing preincubation time. Then, we further examined the possibility of mechanism-based inhibition on 5… CONTINUE READING

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