Literature DB >> 24902789

Quercetin sensitizes human glioblastoma cells to temozolomide in vitro via inhibition of Hsp27.

Dong-Ping Sang1, Ru-Jun Li2, Qing Lan2.   

Abstract

AIM: Quercetin is an effective Hsp27 inhibitor and has been reported to facilitate tumor cell apoptosis. The aim of this study was to investigate whether quercetin could sensitize human glioblastoma cells to temozolomide (TMZ) in vitro.
METHODS: Both U251 and U87 human glioblastoma cells were treated with quercetin and/or TMZ for 48 h. Cell viability was detected using the MTT assay. Cell apoptosis was analyzed with caspase-3 activity kits and flow cytometry. Hsp27 expression and phosphorylation were examined using Western blot analysis. RNA interference using Hsp27 siRNA oligos was performed to knock down the gene expression of Hsp27.
RESULTS: TMZ (200 or 400 μmol/L) alone effectively inhibited the viability of U251 and U87 cells. When combined with quercetin (30 μmol/L), TMZ (100 μmol/L) significantly inhibited the cell viability, and the inhibition of TMZ (200 and 400 μmol/L) was enhanced. TMZ or quercetin anole did not affect caspase-3 activity and cell apoptosis, while TMZ combined with quercetin significantly increased caspase-3 activity and induced cell apoptosis. TMZ anole significantly increased Hsp27 phosphorylation in U251 and U87 cells, while quercetin or Hsp27 siRNA oligos combined with TMZ attenuated TMZ-induced Hsp27 phosphorylation and significantly inhibited Hsp27 expression.
CONCLUSION: Combined treatment with TMZ and quercetin efficiently suppressed human glioblastoma cell survival in vitro.

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Year:  2014        PMID: 24902789      PMCID: PMC4086384          DOI: 10.1038/aps.2014.22

Source DB:  PubMed          Journal:  Acta Pharmacol Sin        ISSN: 1671-4083            Impact factor:   6.150


  24 in total

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6.  Induction of apoptosis by quercetin: involvement of heat shock protein.

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Journal:  Cancer Res       Date:  1994-09-15       Impact factor: 12.701

7.  Graded methylation in the promoter and body of the O6-methylguanine DNA methyltransferase (MGMT) gene correlates with MGMT expression in human glioma cells.

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9.  Quercetin suppresses drug-resistant spheres via the p38 MAPK-Hsp27 apoptotic pathway in oral cancer cells.

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Journal:  EMBO Mol Med       Date:  2013-07-01       Impact factor: 12.137

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  28 in total

1.  Effects of temozolomide (TMZ) on the expression and interaction of heat shock proteins (HSPs) and DNA repair proteins in human malignant glioma cells.

Authors:  Gisela Natalia Castro; Niubys Cayado-Gutiérrez; Felipe Carlos Martín Zoppino; Mariel Andrea Fanelli; Fernando Darío Cuello-Carrión; Mayra Sottile; Silvina Beatriz Nadin; Daniel Ramón Ciocca
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Review 2.  Glucose transport: meeting the metabolic demands of cancer, and applications in glioblastoma treatment.

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Review 7.  Advances in HSP27 and HSP90-targeting strategies for glioblastoma.

Authors:  Randy van Ommeren; Michael D Staudt; Hu Xu; Matthew O Hebb
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8.  The Monocarboxylate transporter inhibitor Quercetin induces intracellular acidification in a mouse model of Glioblastoma Multiforme: in-vivo detection using magnetic resonance imaging.

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Authors:  Ana Isabel Oliveira; Cláudia Pinho; Bruno Sarmento; Alberto C P Dias
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Review 10.  Natural Compounds in Glioblastoma Therapy: Preclinical Insights, Mechanistic Pathways, and Outlook.

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