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Abstract Title:

Stilbenes as multidrug resistance modulators and apoptosis inducers in human adenocarcinoma cells.

Abstract Source:

Anticancer Res. 2010 Nov;30(11):4587-93. PMID: 21115910

Abstract Author(s):

Olga Wesolowska, Jerzy Wisniewski, Aleksandra Bielawska-Pohl, Maria Paprocka, Noelia Duarte, Maria-José U Ferreira, Danuta Dus, Krystyna Michalak

Article Affiliation:

Department of Biophysics, Wrocław Medical University, 50-368 Wrocław, Poland. olawes@biofiz.am.wroc.pl

Abstract:

BACKGROUND: The search for promising modulators of cancer multidrug resistance (MDR) that are able to reduce the activity of P-glycoprotein, thus restoring the cytotoxicity of anticancer drugs, is ongoing. The identification of compounds that overcome the apoptosis deficiency that frequently accompanies MDR is also of great therapeutic importance.

MATERIALS AND METHODS: Four stilbenes, resveratrol, piceatannol and its two derivatives, were tested for their MDR-modulating and apoptosis-inducing activity in drug-sensitive (LoVo) and doxorubicin-resistant human adenocarcinoma cell line (LoVo/Dx) by means of flow cytometry and fluorescence microscopy.

RESULTS: Trans-3,5,3',4'-tetramethoxystilbene (PicMet) was identified as a promising modulator that efficiently increased accumulation of both rhodamine 123 and doxorubicin inside resistant cells. It also increased sensitivity of LoVo/Dx cells to doxorubicin. Resveratrol and trans-3,5,3',4'-tetracetoxystilbene (PicAcet) were identified as apoptosis inducers in LoVo/Dx cells.

CONCLUSION: The stilbene structure may constitute a promising chemical scaffold for the synthesis of potential MDR modulators.

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