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Interindividual variations in human liver cytochrome P-450 enzymes involved in the oxidation of drugs, carcinogens and toxic chemicals: studies with liver microsomes of 30 Japanese and 30 Caucasians
Abstract
Interindividual variations in the level and activity of cytochrome P-450 enzymes were investigated in the liver microsomes of 30 Japanese and 30 Caucasian patients. The P-450 enzymes used in this study included P-450 1A2, 2A6, 2B6, 2C, 2D6, 2E1 and 3A, and the monooxygenase activities determined were 13 typical P-450 substrates and 9 procarcinogens. Although the total P-450 content was higher in Caucasian (mean, 0.43 nmol/mg of protein) than in Japanese populations (mean, 0.26 nmol/mg of protein), the relative levels (percent of total P-450) of individual forms of P-450 determined immunochemically were not very different except that P-450 2A6 and 2B6 levels were higher in the Caucasians. About 70% of liver P-450 could be accounted for by P-450 1A2, 2A6, 2B6, 2C, 2D6, 2E1 and 3A proteins, and P-450 3A (about 30% of total P-450) and 2C (about 20%) enzymes were found to be the major forms. Considerable levels of P-450 1A2 (about 13%) and 2E1 (about 7%) could be determined, whereas the P-450 2A6 (about 4%), 2D6 (about 2%) and 2B6 (< 1%) were the minor P-450 forms. Differences in some of the P-450 1A2-, 2A6-, 2D6-, 2E1- and 3A4-dependent activities were observed in Japanese and Caucasian populations. No clear sex-related differences in individual P-450 contents and drug- and carcinogen-metabolizing activities were detected in 60 human samples, except that P-450 1A2-dependent activities were found to be higher in mean than in women in the Caucasian population only. A single neonate sample tended to be lower in P-450 1A2-, 2A6- and 2E1-dependent activities. In contrast to rat counterparts, we could not detect apparent developmental changes in P-450 content and activity in humans between 12 and 73 years old. Thus, the results presented in this study provide useful information for the study of drug biotransformation in humans and for the basis of drug toxicities, carcinogenesis and teratogenesis.
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“CYP3A4 is the most abundant CYP expressed in the adult liver [121,122]”
From Human steroid biosynthesis, metabolism and excretion are differentially reflected by serum and urine steroid metabolomes: a comprehensive review (2019) · cites this paper as [122]
In the citing paper
“makes the major contribution to steroid metabolism.”
From Human steroid biosynthesis, metabolism and excretion are differentially reflected by serum and urine steroid metabolomes: a comprehensive review (2019) · cites this paper as [122]
In the citing paper
“CYP3A4 is the most abundant P450 in the liver (∼30%) (Shimada et al., 1994) and predominantly, though not exclusively, catalyses the 6β-hydroxylation of T and the 16α- and 7α-hydroxylation of DHEA (Niwa et al., 2015).”
From Intracrine androgen biosynthesis, metabolism and action revisited (2018) · cites this paper as Shimada et al., 1994
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Cytochrome P450 2E1 is the Principal Catalyst of Human Oxidative Halothane Metabolism in Vitro
Spracklin, D. K., Hankins, D. C., Fisher, J. M., et al. (1997) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)36603-0 · Cited by 122
Neonatal Hepatic Drug Elimination
Gow, P. J., Ghabrial, H., Smallwood, R. A., et al. (2001) · Pharmacology & Toxicology · doi:10.1034/j.1600-0773.2001.088001003.x · Cited by 122
Regioselective hydroxylation of steroid hormones by human cytochromes P450
Niwa, T., Murayama, N., Imagawa, Y., & Yamazaki, H. (2015) · Drug Metabolism Reviews · doi:10.3109/03602532.2015.1011658 · Cited by 121
Characterization of hepatic cytochrome P4503A activity in patients with end‐stage renal disease
Dowling, T. C., Briglia, A., Fink, J. C., et al. (2003) · Clinical Pharmacology & Therapeutics · doi:10.1016/s0009-9236(03)00056-0 · Cited by 121
Giraud, C., Tran, A., Rey, E., Vincent, J., Tréluyer, J., & Pons, G. (2004) · Drug Metabolism and Disposition · doi:10.1124/dmd.32.11.1279 · Cited by 123
“In human liver, CYP3A4 and CYP2C19 account, respectively, for about 30% (Shimada et al., 1994) and 1.”
BackgroundInfluentialIn vitro assessment of human cytochrome P450
Clarke, S. E. (1998) · Xenobiotica · doi:10.1080/004982598238877 · Cited by 121
Genetic Polymorphism in Cytochrome P450 2D6 (CYP2D6): Population Distribution of CYP2D6 Activity
Neafsey, P. J., Ginsberg, G., Hattis, D. B., & Sonawane, B. R. (2009) · Journal of Toxicology and Environmental Health Part B · doi:10.1080/10937400903158342 · Cited by 121
Inhibition of Caffeine Metabolism by Estrogen Replacement Therapy in Postmenopausal Women
Pollock, B. G., Wylie, M. E., STACK, J. A., Sorisio, D. A., Thompson, D. S., Kirshner, M. A., Folan, M., & Condifer, K. A. (1999) · The Journal of Clinical Pharmacology · doi:10.1177/00912709922008560 · Cited by 121
“The CYP1A2 isozyme is a lower capacity isozyme than CYP3A4, making competitive inhibitory interactions between estrogen and CYP1A2 substrate drugs distinctly possible.(4) It is also of interest that systemic clearances of caffeine and theophylline, two typical CYP1A2 drugs, have been noted to be lower in the late lute…”
Background
Metadata
- Authors
- Shimada, T., Yamazaki, H., Mimura, M., Inui, Y., & Guengerich, F. P.
- Affiliations
- Osaka Prefectural Institute of Public Health (JP)
- Venue
- The Journal of Pharmacology and Experimental Therapeutics
- Publisher
- Elsevier BV
- Published
- 1994-07
- Volume
- 270
- Issue
- 1
- Pages
- 414-423
- ISSN
- 0022-3565 (ISSN-L)
- OpenAlex
- W2155268095
- Cited by
- 2,785
- References
- 0
- Citations by year
- 2026: 14 · 2025: 28 · 2024: 24 · 2023: 40 · 2022: 36 · 2021: 55 · 2020: 41 · 2019: 59 · 2018: 52 · 2017: 53 · 2016: 75 · 2015: 81 · 2014: 121 · 2013: 104 · 2012: 118
- FWCI
- 64.47
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Pharmacology and Experimental Therapeutics (publishedVersion)
- PubMed (publishedVersion)
- PubMed
- Funders
- National Institutes of Health (5r35ca044353-14)
- National Cancer Institute (CA 44353)
- National Institute of Environmental Health Sciences (ES00267)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Drug-Induced Hepatotoxicity and Protection
- Physical Sciences › Chemistry › Inorganic Chemistry › Metal-Catalyzed Oxygenation Mechanisms
- Keywords
- cytochrome P450, interindividual variability, liver microsomes, CYP1A2, CYP2A6, CYP2B6, CYP2C, CYP2D6, CYP2E1, CYP3A4, monooxygenase activity, procarcinogen metabolism, drug metabolism, sex differences
- MeSH terms
- Adolescent, Adult, Aged, Aging, Biotransformation, Carcinogens, Child, Cytochrome P-450 Enzyme System, Pharmaceutical Preparations, Female, Humans, Individuality, Infant, Isoenzymes, Japan, Liver, Male, Microsomes, Liver, Middle Aged, Oxidation-Reduction, Sex Factors, Hazardous Substances, White People
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