Suppression of multidrug resistance via inhibition of heat shock factor by quercetin in mdr cells

ABSTRACT MDR1 promoter has been shown to contain heat shock elements (HSE), and it has been reported that FM3A/M and P388/M MDR cells show a constitutively activated heat shock factor (HSF),

suggesting that HSF might be an important target for reversing the multidrug resistance. Therefore, it was examined whether quercetin, which has been shown to interfere with the formation

of the complex between HSE and HSF, and to downregulate the level of HSF1, can sensitize MDR cells against anticancer drugs by inhibition of HSF DNA-binding activity. In this study,

quercetin appeared to inhibit the constitutive HSF DNA-binding activity and the sodium arsenite-induced HSF DNA-binding activity in the MDR cells. The basal and sodium arsenite-induced

MDRCAT activities were remarkably suppressed by the treatment of quercetin. These results were well consistent with the finding that the treatment of quercetin decreased the expression level

of P-gp, MDR1 gene product, in dose-dependent manner, and markedly increased the sensitivity of MDR cells to vincristine or vinblastine. These results suggest that quercetin can decrease

the expression of P-gp via inhibition of HSF DNA-binding activity, and might be useful as a chemosensitizer in MDR cells. SIMILAR CONTENT BEING VIEWED BY OTHERS C0818, A NOVEL CURCUMIN

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Biochemistry, College of Medicine, Pusan National University, Korea Sun-Hee Kim Authors * Sun-Hee Kim View author publications You can also search for this author inPubMed Google Scholar *

Gae-Sun Yeo View author publications You can also search for this author inPubMed Google Scholar * Young-Sun Lim View author publications You can also search for this author inPubMed Google

Scholar * Chi-Dug Kang View author publications You can also search for this author inPubMed Google Scholar * Cheol-Min Kim View author publications You can also search for this author

inPubMed Google Scholar * Byung-Seon Chung View author publications You can also search for this author inPubMed Google Scholar RIGHTS AND PERMISSIONS This is an Open Access article

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distribution, and reproduction in any medium, provided the original work is properly cited. Reprints and permissions ABOUT THIS ARTICLE CITE THIS ARTICLE Kim, SH., Yeo, GS., Lim, YS. _et

al._ Suppression of multidrug resistance via inhibition of heat shock factor by quercetin in MDR cells. _Exp Mol Med_ 30, 87–92 (1998). https://doi.org/10.1038/emm.1998.13 Download citation

* Published: 01 June 1998 * Issue Date: 01 June 1998 * DOI: https://doi.org/10.1038/emm.1998.13 SHARE THIS ARTICLE Anyone you share the following link with will be able to read this content:

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multidrug resistance (mdr) * heat shock factor (HSF) * quercetin