The effect of lycopene on cytochrome P450 isoenzymes and P-glycoprotein by using human liver microsomes and Caco-2 cell monolayer model |
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| Authors: | Lingti Kong Chunli Song Linhu Ye Jian Xu Daohua Guo |
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| Affiliation: | 1. Department of Pharmacy, The First Affiliated Hospital of Bengbu Medical College, Bengbu, China;2. Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China;3. Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China;4. Department of Pharmacy, The First People’s Hospital of Bijie, Bijie, China |
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| Abstract: | Lycopene is widely used as a dietary supplement. However, the effects of lycopene on cytochrome P450 (CYP) enzymes or P-glycoprotein (P-gp) are not comprehensive. The present study was performed to investigate the effects of lycopene on the CYP enzymes and P-gp activity. A cocktail method was used to evaluate the activities of CYP3A4, CYP2C9, CYP2C19, CYP2D6 and CYP2E1. Caco-2 cell monolayer model was carried out to assay lycopene on P-gp activity. The results indicated that lycopene had a moderate inhibitory effect on CYP2E1, with IC50 value of 43.65?μM, whereas no inhibitory effects on CYP3A4, CYP2C19, CYP2D6 and CYP2E1, with IC50 values all over 100?μM. In addition, lycopene showed almost no inhibitory effect on rhodamine-123 efflux and uptake (p?>?.05), indicated no effects on P-gp activity. In conclusion, there should be required attention when lycopene are coadministered with other drugs that are metabolised by CYP2E1. |
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| Keywords: | Lycopene cytochrome P450 isoenzymes cocktail P-glycoprotein |
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