Quercetin, a bioflavonoid, inhibits the increase of human multidrug resistance gene ( MDR1) expression caused by arsenite

Expression of the MDR1 gene, which encodes P-glycoprotein, is increased under some stress conditions. We have reported that quercetin, a bioflavonoid, inhibits the expression of heat-shock proteins. We have identified the effects of quercetin on the MDR1 gene expression in the human hepatocarcinoma...

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Bibliographic Details
Published in:FEBS letters 1992-04, Vol.301 (3), p.307-309
Main Authors: Kioka, Noriyuki, Hosokawa, Nobuko, Komano, Tohru, Hirayoshi, Kazunori, Nagate, Kazuhiro, Ueda, Kazumitsu
Format: Article
Language:English
Subjects:
Arsenic - pharmacology
Arsenites
ATP Binding Cassette Transporter, Subfamily B, Member 1
Biological and medical sciences
Blotting, Northern
Carcinoma, Hepatocellular - metabolism
CAT
chloramphenicol acetyltransferase
Chloramphenicol O-Acetyltransferase - genetics
Chloramphenicol O-Acetyltransferase - metabolism
Drug Antagonism
Drug Resistance
Fundamental and applied biological sciences. Psychology
Gene expression
Gene Expression - drug effects
Heat shock
heat shock factor
heat shock responsive element
HSE
HSF
MDR1
Membrane Glycoproteins - biosynthesis
Membrane Glycoproteins - genetics
Molecular and cellular biology
Molecular genetics
Multidrug resistance
P-Glycoprotein
Plasmids
Quercetin - pharmacology
RNA, Messenger - genetics
RNA, Messenger - metabolism
Stress protein
Transcription, Genetic
Tumor Cells, Cultured
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Summary:Expression of the MDR1 gene, which encodes P-glycoprotein, is increased under some stress conditions. We have reported that quercetin, a bioflavonoid, inhibits the expression of heat-shock proteins. We have identified the effects of quercetin on the MDR1 gene expression in the human hepatocarcinoma cells line, HepG2. The increase of P-glycoprotein synthesis and MDR1 mRNA accumulation caused by exposure to arsenite were inhibited by quercetin. The CAT assay suggested that quercetin suppressed the transcriptional activation of the MDR1 gene after exposure to arsenite. Although many drugs that prevent the P-glycoprotein function have been reported, this is the first report to describe the inhibition of MDR1 expression by a reagent.
ISSN:0014-5793
1873-3468
DOI:10.1016/0014-5793(92)80263-G