Interaction of isoflavonoids with human liver microsomal cytochromes P450: inhibition of CYP enzyme activities.

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Kopecna-Zapletalova M, Krasulova K, Anzenbacher P, Hodek P, Anzenbacherova E

Interaction of isoflavonoids with human liver microsomal cytochromes P450: inhibition of CYP enzyme activities.

Xenobiotica. 2017 Apr;47(4):324-331. doi: 10.1080/00498254.2016.1195028. Epub 2016 Jun 17.

PubMed ID

27312150 [ View in PubMed

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Abstract

1. The possibility of interaction of isoflavonoids with concomitantly taken drugs to determined isoflavonoids safety was studied. Inhibition of nine forms of cytochrome P450 (CYP3A4, CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C19, CYP2C9, CYP2D6 and CYP2E1) by 12 isoflavonoids (daidzein, genistein, biochanin A, formononetin, glycitein, equol and six glucosides, daidzin, puerarin, genistin, sissotrin, ononin and glycitin) was studied systematically. 2. The most potent inhibitors were genistein and daidzein inhibiting noncompetitively the CYP2C9 with Ki of 35.95 +/- 6.96 and 60.56 +/- 3.53 mumol/l and CYP3A4 (inhibited by genistein with Ki of 23.25 +/- 5.85 mumol/l also by a noncompetitive mechanism). Potent inhibition of CYP3A4 was observed also with biochanin A (Ki of 57.69 +/- 2.36 mumol/l) and equol (Ki of 38.47 +/- 2.32 mumol/l). 3. Genistein and daidzein inhibit noncompetitively CYP3A4 and CYP2C9. With plasma levels in micromolar range, a clinically important interaction with concomitantly taken drugs does not seem to be probable.

DrugBank Data that Cites this Article

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Genistein	Cytochrome P450 2C9	Protein	Humans	Unknown	Inhibitor	Details