Curcumin, piperine, and capsaicin: a comparative study of spice-mediated inhibition of human cytochrome P450 isozyme activities
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 o...
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| Format: | Article |
| Language: | English |
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American Society for Pharmacology and Experimental Therapeutics (ASPET)
2017
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| Online Access: | http://psasir.upm.edu.my/id/eprint/61267/ http://psasir.upm.edu.my/id/eprint/61267/1/Curcumin%2C%20piperine%2C%20and%20capsaicin%20a%20comparative%20study%20of%20spice-mediated%20inhibition%20of%20human%20cytochrome%20P450%20isozyme%20activities.pdf |
| _version_ | 1848854377939337216 |
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| author | Suhaili, Shamsi Huong, Tran Seok, Renee Jin Tan Zee, Jian Tan Lee, Yong Lim |
| author_facet | Suhaili, Shamsi Huong, Tran Seok, Renee Jin Tan Zee, Jian Tan Lee, Yong Lim |
| author_sort | Suhaili, Shamsi |
| building | UPM Institutional Repository |
| collection | Online Access |
| description | 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. |
| first_indexed | 2025-11-15T11:08:54Z |
| format | Article |
| id | upm-61267 |
| institution | Universiti Putra Malaysia |
| institution_category | Local University |
| language | English |
| last_indexed | 2025-11-15T11:08:54Z |
| publishDate | 2017 |
| publisher | American Society for Pharmacology and Experimental Therapeutics (ASPET) |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | upm-612672018-09-05T08:19:57Z http://psasir.upm.edu.my/id/eprint/61267/ Curcumin, piperine, and capsaicin: a comparative study of spice-mediated inhibition of human cytochrome P450 isozyme activities Suhaili, Shamsi Huong, Tran Seok, Renee Jin Tan Zee, Jian Tan Lee, Yong Lim 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. American Society for Pharmacology and Experimental Therapeutics (ASPET) 2017 Article PeerReviewed text en http://psasir.upm.edu.my/id/eprint/61267/1/Curcumin%2C%20piperine%2C%20and%20capsaicin%20a%20comparative%20study%20of%20spice-mediated%20inhibition%20of%20human%20cytochrome%20P450%20isozyme%20activities.pdf Suhaili, Shamsi and Huong, Tran and Seok, Renee Jin Tan and Zee, Jian Tan and Lee, Yong Lim (2017) Curcumin, piperine, and capsaicin: a comparative study of spice-mediated inhibition of human cytochrome P450 isozyme activities. Drug Metabolism and Disposition, 45 (1). pp. 49-55. ISSN 0090-9556; ESSN: 1521-009X http://dmd.aspetjournals.org/content/dmd/45/1/49.full.pdf 10.1124/dmd.116.073213 |
| spellingShingle | Suhaili, Shamsi Huong, Tran Seok, Renee Jin Tan Zee, Jian Tan Lee, Yong Lim Curcumin, piperine, and capsaicin: a comparative study of spice-mediated inhibition of human cytochrome P450 isozyme activities |
| title | Curcumin, piperine, and capsaicin: a comparative study of spice-mediated inhibition of human cytochrome P450 isozyme activities |
| title_full | Curcumin, piperine, and capsaicin: a comparative study of spice-mediated inhibition of human cytochrome P450 isozyme activities |
| title_fullStr | Curcumin, piperine, and capsaicin: a comparative study of spice-mediated inhibition of human cytochrome P450 isozyme activities |
| title_full_unstemmed | Curcumin, piperine, and capsaicin: a comparative study of spice-mediated inhibition of human cytochrome P450 isozyme activities |
| title_short | Curcumin, piperine, and capsaicin: a comparative study of spice-mediated inhibition of human cytochrome P450 isozyme activities |
| title_sort | curcumin, piperine, and capsaicin: a comparative study of spice-mediated inhibition of human cytochrome p450 isozyme activities |
| url | http://psasir.upm.edu.my/id/eprint/61267/ http://psasir.upm.edu.my/id/eprint/61267/ http://psasir.upm.edu.my/id/eprint/61267/ http://psasir.upm.edu.my/id/eprint/61267/1/Curcumin%2C%20piperine%2C%20and%20capsaicin%20a%20comparative%20study%20of%20spice-mediated%20inhibition%20of%20human%20cytochrome%20P450%20isozyme%20activities.pdf |