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

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.

journal_name

Anticancer Res

journal_title

Anticancer research

authors

Wesolowska O,Wisniewski J,Bielawska-Pohl A,Paprocka M,Duarte N,Ferreira MJ,Dus D,Michalak K

subject

Has Abstract

pub_date

2010-11-01 00:00:00

pages

4587-93

issue

11

eissn

0250-7005

issn

1791-7530

pii

30/11/4587

journal_volume

30

pub_type

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