Induction of drug metabolizing enzymes in human liver cell line Hep G2

J. R. Dawson; D. J. Adams; C. R. Wolf

doi:10.1016/0014-5793(85)80780-8

Induction of drug metabolizing enzymes in human liver cell line Hep G2

J. R. Dawson
, D. J. Adams
, C. R. Wolf

Research output: Contribution to journal › Article › peer-review

96 Citations (Scopus)

Abstract

Human cytochrome P-450, UDP-glucuronosyltransferase and sulphotransferase activities have been measured in the cell line Hep G2 following treatment of cells with 3-methylcholanthrene or phenobarbital. 3-Methylcholanthrene treatment caused a 20-30-fold increase in the O-deethylation of 7-ethoxycoumarin. The glucuronidation and sulphation of the product 7-hydroxycoumarin were increased 36 and 7 fold, respectively. In comparison, phenobarbital treatment did not increase these activities significantly. However, phenobarbital-inducible proteins were identified on 'Western blots' using antibodies to a rat liver phenobarbital inducible P-450 form. The molecular masses of the proteins did not coincide with those expected for cytochromes P-450. However, characteristic of P-450 forms, the synthesis of these proteins was suppressed by 3-methylcholanthrene treatment. The Hep G2 cell line represents a potentially useful model for studying the regulation of human P-450 genes.

Original language	English
Pages (from-to)	219-222
Number of pages	4
Journal	FEBS Letters
Volume	183
Issue number	2
DOIs	https://doi.org/10.1016/0014-5793(85)80780-8
Publication status	Published - 22 Apr 1985

Keywords

Cell line
Cytochrome
Drug metabolism
Enzyme induction
Hep G2
P-450
UDP-glucoronosyltransferase

ASJC Scopus subject areas

Biophysics
Structural Biology
Biochemistry
Molecular Biology
Genetics
Cell Biology

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10.1016/0014-5793(85)80780-8

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@article{cfc6c391cde04da89e60e18ec5224bfc,

title = "Induction of drug metabolizing enzymes in human liver cell line Hep G2",

abstract = "Human cytochrome P-450, UDP-glucuronosyltransferase and sulphotransferase activities have been measured in the cell line Hep G2 following treatment of cells with 3-methylcholanthrene or phenobarbital. 3-Methylcholanthrene treatment caused a 20-30-fold increase in the O-deethylation of 7-ethoxycoumarin. The glucuronidation and sulphation of the product 7-hydroxycoumarin were increased 36 and 7 fold, respectively. In comparison, phenobarbital treatment did not increase these activities significantly. However, phenobarbital-inducible proteins were identified on 'Western blots' using antibodies to a rat liver phenobarbital inducible P-450 form. The molecular masses of the proteins did not coincide with those expected for cytochromes P-450. However, characteristic of P-450 forms, the synthesis of these proteins was suppressed by 3-methylcholanthrene treatment. The Hep G2 cell line represents a potentially useful model for studying the regulation of human P-450 genes.",

keywords = "Cell line, Cytochrome, Drug metabolism, Enzyme induction, Hep G2, P-450, UDP-glucoronosyltransferase",

author = "Dawson, \{J. R.\} and Adams, \{D. J.\} and Wolf, \{C. R.\}",

year = "1985",

month = apr,

day = "22",

doi = "10.1016/0014-5793(85)80780-8",

language = "English",

volume = "183",

pages = "219--222",

journal = "FEBS Letters",

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T1 - Induction of drug metabolizing enzymes in human liver cell line Hep G2

AU - Dawson, J. R.

AU - Adams, D. J.

AU - Wolf, C. R.

PY - 1985/4/22

Y1 - 1985/4/22

N2 - Human cytochrome P-450, UDP-glucuronosyltransferase and sulphotransferase activities have been measured in the cell line Hep G2 following treatment of cells with 3-methylcholanthrene or phenobarbital. 3-Methylcholanthrene treatment caused a 20-30-fold increase in the O-deethylation of 7-ethoxycoumarin. The glucuronidation and sulphation of the product 7-hydroxycoumarin were increased 36 and 7 fold, respectively. In comparison, phenobarbital treatment did not increase these activities significantly. However, phenobarbital-inducible proteins were identified on 'Western blots' using antibodies to a rat liver phenobarbital inducible P-450 form. The molecular masses of the proteins did not coincide with those expected for cytochromes P-450. However, characteristic of P-450 forms, the synthesis of these proteins was suppressed by 3-methylcholanthrene treatment. The Hep G2 cell line represents a potentially useful model for studying the regulation of human P-450 genes.

AB - Human cytochrome P-450, UDP-glucuronosyltransferase and sulphotransferase activities have been measured in the cell line Hep G2 following treatment of cells with 3-methylcholanthrene or phenobarbital. 3-Methylcholanthrene treatment caused a 20-30-fold increase in the O-deethylation of 7-ethoxycoumarin. The glucuronidation and sulphation of the product 7-hydroxycoumarin were increased 36 and 7 fold, respectively. In comparison, phenobarbital treatment did not increase these activities significantly. However, phenobarbital-inducible proteins were identified on 'Western blots' using antibodies to a rat liver phenobarbital inducible P-450 form. The molecular masses of the proteins did not coincide with those expected for cytochromes P-450. However, characteristic of P-450 forms, the synthesis of these proteins was suppressed by 3-methylcholanthrene treatment. The Hep G2 cell line represents a potentially useful model for studying the regulation of human P-450 genes.

KW - Cell line

KW - Cytochrome

KW - Drug metabolism

KW - Enzyme induction

KW - Hep G2

KW - P-450

KW - UDP-glucoronosyltransferase

UR - https://www.scopus.com/pages/publications/0021846279

U2 - 10.1016/0014-5793(85)80780-8

DO - 10.1016/0014-5793(85)80780-8

M3 - Article

C2 - 3921402

AN - SCOPUS:0021846279

SN - 0014-5793

VL - 183

SP - 219

EP - 222

JO - FEBS Letters

JF - FEBS Letters

IS - 2

ER -

Induction of drug metabolizing enzymes in human liver cell line Hep G2

Abstract

Keywords

ASJC Scopus subject areas

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