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Research ArticleArticle

Subcellular Events Occurring during Aryl Hydrocarbon Hydroxylase Induction: No Requirement for Metabolism of Polycyclic Hydrocarbon Inducer

ITSU KANO, JACQUES E. GIELEN, HARUHIKO YAGI, DONALD M. JERINA and DANIEL W. NEBERT
Molecular Pharmacology November 1977, 13 (6) 1181-1186;
ITSU KANO
Developmental Pharmacology Branch, National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, Maryland 20014; Laboratoire de Chimie Médicale, Toxicologie et Hygiène, Université de Liège, B-4000 Liège, Belgium; and Laboratory of Chemistry, National Institute of Arthritis, Metabolism, and Digestive Diseases, National Institutes of Health, Bethesda, Maryland 20014
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JACQUES E. GIELEN
Developmental Pharmacology Branch, National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, Maryland 20014; Laboratoire de Chimie Médicale, Toxicologie et Hygiène, Université de Liège, B-4000 Liège, Belgium; and Laboratory of Chemistry, National Institute of Arthritis, Metabolism, and Digestive Diseases, National Institutes of Health, Bethesda, Maryland 20014
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HARUHIKO YAGI
Developmental Pharmacology Branch, National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, Maryland 20014; Laboratoire de Chimie Médicale, Toxicologie et Hygiène, Université de Liège, B-4000 Liège, Belgium; and Laboratory of Chemistry, National Institute of Arthritis, Metabolism, and Digestive Diseases, National Institutes of Health, Bethesda, Maryland 20014
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DONALD M. JERINA
Developmental Pharmacology Branch, National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, Maryland 20014; Laboratoire de Chimie Médicale, Toxicologie et Hygiène, Université de Liège, B-4000 Liège, Belgium; and Laboratory of Chemistry, National Institute of Arthritis, Metabolism, and Digestive Diseases, National Institutes of Health, Bethesda, Maryland 20014
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DANIEL W. NEBERT
Developmental Pharmacology Branch, National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, Maryland 20014; Laboratoire de Chimie Médicale, Toxicologie et Hygiène, Université de Liège, B-4000 Liège, Belgium; and Laboratory of Chemistry, National Institute of Arthritis, Metabolism, and Digestive Diseases, National Institutes of Health, Bethesda, Maryland 20014
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Abstract

The induction of aryl hydrocarbon (benzo[a]pyrene) hydroxylase (EC 1.14.14.2) activity in the rat Reuber hepatoma H-4-II-E established cell line was studied with 3-methylcholanthrene and its K-region oxide and diol and with benzo[a]pyrene and 23 of its oxygenated derivatives, including 12 phenols, three diols, three quinones, three oxides, and two diol-epoxides. Compared with the parent benzo[a]pyrene molecule, the naturally occurring benzo[a]pyrene 6,12-quinone is approximately as potent, the chemically synthesized 12-hydroxy derivative is at least 50% more potent, and the chemically synthesized 4-hydroxy derivative is about one-half as potent in inducing the hydroxylase activity. The naturally occurring benzo[a]pyrene 7,8-oxide is also about one-half as potent as benzo[a]pyrene, and all other analogues examined are poorer inducers than the four compounds mentioned. trans-7,8-Dihydroxy-7,8-dihydrobenzo[a]pyrene is more polar than benzo[a]pyrene and enters the cells in culture more readily than benzo[a]pyrene. Knowing the amount of polycyclic hydrocarbon metabolized and the percentage of various metabolites of benzo[a]pyrene that exist in these cells, we have found no metabolite sufficiently potent to induce the hydroxylase activity more than the parent benzo[a]pyrene molecule. It is concluded, therefore, that metabolism of the parent polycyclic hydrocarbon is not a requirement for the induction process to proceed.

ACKNOWLEDGMENTS We thank Dr. Olavi Pelkonen and Dr. Mortimer B. Lipsett for helpful suggestions in reviewing this manuscript, and Ms. Ingrid E. Jordan for her expert secretarial assistance.

  • Copyright © 1977 by Academic Press, Inc.

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Molecular Pharmacology
Vol. 13, Issue 6
1 Nov 1977
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Research ArticleArticle

Subcellular Events Occurring during Aryl Hydrocarbon Hydroxylase Induction: No Requirement for Metabolism of Polycyclic Hydrocarbon Inducer

ITSU KANO, JACQUES E. GIELEN, HARUHIKO YAGI, DONALD M. JERINA and DANIEL W. NEBERT
Molecular Pharmacology November 1, 1977, 13 (6) 1181-1186;

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Research ArticleArticle

Subcellular Events Occurring during Aryl Hydrocarbon Hydroxylase Induction: No Requirement for Metabolism of Polycyclic Hydrocarbon Inducer

ITSU KANO, JACQUES E. GIELEN, HARUHIKO YAGI, DONALD M. JERINA and DANIEL W. NEBERT
Molecular Pharmacology November 1, 1977, 13 (6) 1181-1186;
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