Tier 4 — mechanistic

Inhibitory effects of polyphenols on human cytochrome P450 3A4 and 2C9 activity

Yuka Kimura, Hideyuki Ito, Ryoko Ohnishi, Tsutomu Hatano
Food and Chemical Toxicology 2010 48(1):429-435

Bibliography

PubMed
PMID 19883715
DOI
10.1016/j.fct.2009.10.041
Funding
Not reported in the indexed record reviewed.
Competing interests
Not reported in the indexed record reviewed.

Study snapshot

DesignIn vitro comparative cytochrome P450 inhibition study
ModelHuman CYP3A4 and CYP2C9 enzyme activity assays
SampleSixty polyphenols and related compounds screened; not a human participant study.
InterventionApigenin and other polyphenols tested for inhibition of CYP3A4 and CYP2C9 activity
DurationIn vitro enzyme-assay experiments
EndpointsCYP3A4 activity; CYP2C9 activity; Inhibition kinetics; Mixed-type inhibition

What the study showed, in plain terms

This laboratory screening study tested apigenin and dozens of other polyphenols for their ability to inhibit two major human drug-metabolizing enzymes, CYP3A4 and CYP2C9.

Key findings

Apigenin was among the flavonoids that significantly suppressed CYP3A4 or CYP2C9 activity in vitro, and kinetic analysis indicated mixed-type inhibition. This supports a theoretical pathway for supplement-drug interactions.

What this study can and cannot tell us

Enzyme inhibition in vitro does not establish that orally consumed apigenin reaches sufficient unbound concentrations in humans to cause a clinically important interaction. Clinical pharmacokinetic interaction studies are needed before quantifying risk.

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Dr. Khaled Mahmoud, MBBChCritical Care Medicine, Longevity Science & Editorial Direction Dr. Amr Yasser, PhDCardiometabolic, Musculoskeletal, Gut & Bioavailability Dr. Abdulla Mostafa, PhDCellular Senescence, Neurological, Mitochondrial & Brain-Ageing Biology