CYP3A4 inhibitors isolated from Licorice

  • Biol Pharm Bull. 2005 Oct;28(10):2000-2. doi: 10.1248/bpb.28.2000.
Sachiko Tsukamoto  1 ,  Maki Aburatani ,  Tomohiro Yoshida ,  Yuko Yamashita ,  Ahmed Atef El-Beih ,  Tomihisa Ohta
Affiliations
  • 1. Graduate School of Natural Science and Technology, Kanazawa University; Kakuma-machi, Kanazawa 920-1192, Japan.
PMID: 16204965 DOI: 10.1248/bpb.28.2000
Abstract

The extract of licorice (Glycyrrhiza uralensis FISHER, Leguminosae) showed CYP3A4 inhibitory activity with the IC50 value of 0.022 mg/ml. Bioassay-guided purification afforded nine compounds, 3-(p-hydroxyphenyl)propionic acid (1), isoliquiritigenin (2), (3R)-vestitol (3), licopyranocoumarin (4), 4-hydroxyguaiacol apioglucoside (5), liquiritin (6), liquiritigenin 7,4'-diglucoside (7), liquiritin apioside (8), and glucoliquiritin apioside (9). Among these compounds, 3, 7, and 5 showed potent CYP3A4 inhibitory activities with IC50 values of 3.6, 17, and 20 microM, respectively. Glycyrrhizin (10), a main constituent of licorice, however, was inactive for CYP3A4 inhibition.

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