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Volume 301, Issue 3 p. 307-309
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Quercetin, a bioflavonoid, inhibits the increase of human multidrug resistance gene (MDR1) expression caused by arsenite

Noriyuki Kioka

Noriyuki Kioka

Laboratory of Biochemistry, Department of Agricultural Chemistry, Chest Disease Research Institute, Kyoto University, Kyoto 606, Japan

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Nobuko Hosokawa

Nobuko Hosokawa

Department of Cell Biology, Chest Disease Research Institute, Kyoto University, Kyoto 606, Japan

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Tohru Komano

Tohru Komano

Laboratory of Biochemistry, Department of Agricultural Chemistry, Chest Disease Research Institute, Kyoto University, Kyoto 606, Japan

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Kazunori Hirayoshi

Kazunori Hirayoshi

Department of Cell Biology, Chest Disease Research Institute, Kyoto University, Kyoto 606, Japan

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Kazuhiro Nagate

Kazuhiro Nagate

Department of Cell Biology, Chest Disease Research Institute, Kyoto University, Kyoto 606, Japan

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Kazumitsu Ueda

Kazumitsu Ueda

Laboratory of Biochemistry, Department of Agricultural Chemistry, Chest Disease Research Institute, Kyoto University, Kyoto 606, Japan

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First published: April 27, 1992
Citations: 54
Correspondence address: K. Ueda, Laboratory of Biochemistry, Department of Agricultural Chemistry, Kyoto University, Kyoto 606, Japan. Fax: (81) (75) 753-6128

Abstract

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.