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Food Sci Nutr. 2014 Sep;2(5):500-20. doi: 10.1002/fsn3.122. Epub 2014 Jun 10.

Cytochrome P450 induction properties of food and herbal-derived compounds using a novel multiplex RT-qPCR in vitro assay, a drug-food interaction prediction tool.

Author information

1
Malaysian Institute of Pharmaceuticals & Nutraceuticals, Ministry of Science, Technology & Innovation (MOSTI) Halaman Bukit Gambir, 11700, Georgetown, Pulau Pinang, Malaysia.
2
School of Fundamental Science, Universiti Malaysia Terengganu 21030, Kuala Terengganu, Terengganu, Malaysia.
3
Malaysian Institute of Pharmaceuticals & Nutraceuticals, Ministry of Science, Technology & Innovation (MOSTI) Halaman Bukit Gambir, 11700, Georgetown, Pulau Pinang, Malaysia ; The Centre for Chemical Biology, Universiti Sains Malaysia Georgetown, Pulau Pinang, Malaysia.
4
Malaysian Institute of Pharmaceuticals & Nutraceuticals, Ministry of Science, Technology & Innovation (MOSTI) Halaman Bukit Gambir, 11700, Georgetown, Pulau Pinang, Malaysia ; School of Pharmaceutical Sciences, Universiti Sains Malaysia Georgetown, Pulau Pinang, Malaysia.
5
Malaysian Institute of Pharmaceuticals & Nutraceuticals, Ministry of Science, Technology & Innovation (MOSTI) Halaman Bukit Gambir, 11700, Georgetown, Pulau Pinang, Malaysia ; Advanced Medical & Dental Institute, Universiti Sains Malaysia Georgetown, Pulau Pinang, Malaysia.

Abstract

A multiplex RT-qPCR was developed to examine CYP1A2, CYP2D6, and CYP3A4 induction properties of compounds from food and herbal sources. The induction of drug metabolizing enzymes is an important pharmacokinetic interaction with unique features in comparison with inhibition of metabolizing enzymes. Cytochrome induction can lead to serious drug-drug or drug-food interactions, especially if the coadministered drug plasma level is critical as it can reduce therapeutic effects and cause complications. Using this optimized multiplex RT-qPCR, cytochrome induction properties of andrographolide, curcumin, lycopene, bergamottin, and resveratrol were determined. Andrographolide, curcumin, and lycopene produced no significant induction effects on CYP1A2, CYP2D6, and CYP3A4. However, bergamottin appeared to be a significant in vitro CYP1A2 inducer starting from 5 to 50 μmol/L with induction ranging from 60 to 100-fold changes. On the other hand, resveratrol is a weak in vitro CYP1A2 inducer. Examining the cytochrome induction properties of food and herbal compounds help complement CYP inhibition studies and provide labeling and safety caution for such products.

KEYWORDS:

CYP1A2; CYP2D6; CYP3A4; drug–food interactions; multiplex RT-qPCR

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