Tier 4 — mechanistic

Apigenin, a novel candidate involving herb-drug interaction (HDI), interacts with organic anion transporter 1 (OAT1)

Ting Wu, Haixin Li, Jiasheng Chen, Ying Cao, Weimin Fu, Pingzheng Zhou, Jianxin Pang
Pharmacological Reports 2017 69(6):1254-1262

Bibliography

PubMed
PMID 29128807
DOI
10.1016/j.pharep.2017.06.012
Funding
Supported by the Foundation of Science and Technology of Guangdong, China (2014A020210013).
Competing interests
The authors reported no conflict of interest.

Study snapshot

DesignIn vitro transporter study with in vivo pharmacokinetic interaction experiments
ModelMDCK cells stably expressing OAT1 and Sprague-Dawley rat in vivo pharmacokinetic experiments
SampleCell and animal experiments; total animal N was not stated in the PubMed abstract.
InterventionApigenin tested for OAT1 inhibition and co-administration effects with OAT1 substrates including acyclovir and adefovir
DurationAcute transporter and pharmacokinetic experiments
EndpointsOAT1 transport activity; Apigenin IC50; Time-dependent OAT1 inhibition; Acyclovir uptake; Acyclovir plasma exposure; Adefovir cytotoxicity

What the study showed, in plain terms

This study examined whether apigenin can interfere with OAT1, a kidney drug transporter involved in handling medicines such as acyclovir and adefovir.

Key findings

Apigenin inhibited OAT1 in the cell system with an IC50 of about 0.737 micromolar and showed time-dependent inhibition. It reduced OAT1-mediated acyclovir uptake in vitro and altered acyclovir exposure in the animal experiment, supporting a mechanistic interaction signal.

What this study can and cannot tell us

The evidence is preclinical. Transporter inhibition in engineered cells and altered pharmacokinetics in animals cannot be assumed to occur to the same extent in humans taking oral apigenin supplements. No clinical interaction trial was performed.

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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