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Ginger and Its Purified Major Components Inhibit Clinically Relevant Uptake and Efflux Transporters In Vitro.
Tamás Varga1,2, Nóra Szilvásy2, Zsuzsanna Schelz3
1Doctoral School of Biology, ELTE Eötvös Loránd University, H-1117 Budapest, Hungary.
Ginger extract components, [6]-gingerol and [6]-shogaol, interact with numerous drug transporters. High-dose ginger may risk herb-drug interactions (HDIs) with medications by affecting transporters like OAT3.
Area of Science:
- Pharmacology and Toxicology
- Natural Product Chemistry
Background:
- Ginger (Zingiber officinale) is widely used for medicinal purposes.
- Its potential for herb-drug interactions (HDIs) via drug transporters is under-investigated.
Purpose of the Study:
- To investigate ginger extract and its components ([6]-gingerol, [6]-shogaol) interactions with drug transporters.
- To assess the risk of HDIs from ginger consumption.
Main Methods:
- Utilized transporter-overexpressing cell lines and membrane vesicles.
- Measured interactions with uptake and efflux transporters.
- Determined IC50 values for risk assessment.
Main Results:
- Ginger extract interacted with 17 of 33 transporters.
- [6]-gingerol and [6]-shogaol interacted with 7 and 16 transporters, respectively.
- Identified novel interactions with OAT3, URAT1, OCT1, BSEP, and ENT1, with [6]-shogaol showing potent OAT3 inhibition.
Conclusions:
- Prolonged high-dose ginger may cause transporter-mediated HDIs.
- Concomitant use of ginger supplements with certain medications requires caution.
- Further in vivo studies are recommended to validate these findings.
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