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Research ArticleArticle

Curcumin, Piperine, and Capsaicin: A Comparative Study of Spice-Mediated Inhibition of Human Cytochrome P450 Isozyme Activities

Suhaili Shamsi, Huong Tran, Renee Seok Jin Tan, Zee Jian Tan and Lee Yong Lim
Drug Metabolism and Disposition January 2017, 45 (1) 49-55; DOI: https://doi.org/10.1124/dmd.116.073213
Suhaili Shamsi
Laboratory for Drug Delivery, Centre for Optimization of Medicines, Pharmacy, School of Medicine and Pharmacology, University of Western Australia, Crawley, Australia (S.S., H.T., R.S.J.T., Z.J.T., L.Y.L.); Department of Biochemistry, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, Serdang, Malaysia (S.S.)
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Huong Tran
Laboratory for Drug Delivery, Centre for Optimization of Medicines, Pharmacy, School of Medicine and Pharmacology, University of Western Australia, Crawley, Australia (S.S., H.T., R.S.J.T., Z.J.T., L.Y.L.); Department of Biochemistry, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, Serdang, Malaysia (S.S.)
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Renee Seok Jin Tan
Laboratory for Drug Delivery, Centre for Optimization of Medicines, Pharmacy, School of Medicine and Pharmacology, University of Western Australia, Crawley, Australia (S.S., H.T., R.S.J.T., Z.J.T., L.Y.L.); Department of Biochemistry, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, Serdang, Malaysia (S.S.)
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Zee Jian Tan
Laboratory for Drug Delivery, Centre for Optimization of Medicines, Pharmacy, School of Medicine and Pharmacology, University of Western Australia, Crawley, Australia (S.S., H.T., R.S.J.T., Z.J.T., L.Y.L.); Department of Biochemistry, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, Serdang, Malaysia (S.S.)
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Lee Yong Lim
Laboratory for Drug Delivery, Centre for Optimization of Medicines, Pharmacy, School of Medicine and Pharmacology, University of Western Australia, Crawley, Australia (S.S., H.T., R.S.J.T., Z.J.T., L.Y.L.); Department of Biochemistry, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, Serdang, Malaysia (S.S.)
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Abstract

Inhibition of cytochrome P450 (P450) enzymes (CYP) has been shown to lower the metabolism of drugs that are P450 substrates and to consequently alter their pharmacokinetic profiles. Curcumin (CUR), piperine (PIP), and capsaicin (CAP) are spice components (SC) that inhibit the activities of a range of P450 enzymes, but the selection of which SC to be prioritized for further development as an adjuvant will depend on the ranking order of the inhibitory potential of the SCs on specific P450 isozymes. We used common human recombinant enzyme platforms to provide a comparative evaluation of the inhibitory activities of CUR, PIP, and CAP on the principal drug-metabolizing P450 enzymes. SC-mediated inhibition of CYP3A4 was found to rank in the order of CAP (IC50 1.84 ± 0.71 µM) ∼ PIP (2.12 ± 0.45 µM) > CUR (11.93 ± 3.49 µM), while CYP2C9 inhibition was in the order of CAP (11.95 ± 4.24 µM) ∼ CUR (14.58 ± 4.57 µM) > PIP (89.62 ± 9.17 µM). CAP and PIP were significantly more potent inhibitors of CYP1A2 (IC50 2.14 ± 0.22 µM and 14.19 ± 4.15 µM, respectively) than CUR (IC50 > 100 µM), while all three SCs exhibited weak activity toward CYP2D6 (IC50 95.42 ± 12.09 µM for CUR, 99.99 ± 5.88 µM for CAP, and 110.40 ± 3.23 µM for PIP). Of the three SCs, CAP thus has the strongest potential for further development into an inhibitor of multiple CYPs for use in the clinic. Data from this study are also useful for managing potential drug–SC interactions.

Footnotes

    • Received August 24, 2016.
    • Accepted November 3, 2016.
  • This study was supported by grants from the University of Western Australia, Australia. Suhaili Shamsi was the recipient of a graduate scholarship from the Ministry of Higher Education, Malaysia.

  • dx.doi.org/10.1124/dmd.116.073213.

  • Copyright © 2016 by The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 45 (1)
Drug Metabolism and Disposition
Vol. 45, Issue 1
1 Jan 2017
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Research ArticleArticle

Comparative Study of Spice-Mediated Inhibition of Human P450

Suhaili Shamsi, Huong Tran, Renee Seok Jin Tan, Zee Jian Tan and Lee Yong Lim
Drug Metabolism and Disposition January 1, 2017, 45 (1) 49-55; DOI: https://doi.org/10.1124/dmd.116.073213

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Research ArticleArticle

Comparative Study of Spice-Mediated Inhibition of Human P450

Suhaili Shamsi, Huong Tran, Renee Seok Jin Tan, Zee Jian Tan and Lee Yong Lim
Drug Metabolism and Disposition January 1, 2017, 45 (1) 49-55; DOI: https://doi.org/10.1124/dmd.116.073213
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