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 Resjournal_title
Anticancer researchauthors
Wesolowska O,Wisniewski J,Bielawska-Pohl A,Paprocka M,Duarte N,Ferreira MJ,Dus D,Michalak Ksubject
Has Abstractpub_date
2010-11-01 00:00:00pages
4587-93issue
11eissn
0250-7005issn
1791-7530pii
30/11/4587journal_volume
30pub_type
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