Synthetic Models Related to Furanocoumarin-CYP 3A4 Interactions. Comparison of Furanocoumarin, Coumarin, and Benzofuran Dimers as Potent Inhibitors of CYP3A4 Activity

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  • Oda Kazuaki
    Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
  • Yamaguchi Yuki
    Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
  • Yoshimura Teruki
    Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
  • Wada Keiji
    Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
  • Nishizono Naozumi
    Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido

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Furanocoumarin derivatives (dimers and monomers) present in commercially available grapefruit juice have the capacity to inhibit the activity of human CYP3A4. Such interactions are believed to result from the mechanism-based inhibition of CYP3A4 activity in the intestine. The aim of this work was to synthesize and test a series of dimers with a view to determining the relationship between structure and inhibitory activity and determining whether they might make suitable probes of CYP3A4 activity. We prepared a series of furanocoumarin, coumarin, and benzofuran derivatives that have inhibitory effects on the activity of human CYP3A4. A synthetic benzofuran dimer, which is more accessible than furanocoumarin dimers, exhibited activity against CYP3A4 comparable to that of furanocoumarin dimers.

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