Effect of new oxicam derivatives on efflux pumps overexpressed in resistant a human colorectal adenocarcinoma cell line.
Anticancer Res
; 35(5): 2835-40, 2015 May.
Article
em En
| MEDLINE
| ID: mdl-25964564
ABSTRACT
BACKGROUND:
Oxicams are non-steroidal anti-inflammatory drugs (NSAIDs). Antitumor potential of NSAIDs has often been reported in literature. We studied antitumor activity of newly synthesized oxicam derivatives (PR17 and PR18) against doxorubicin-sensitive and resistant human colorectal adenocarcinoma cells (LoVo and LoVo/Dx). MATERIALS ANDMETHODS:
The cytotoxicity of oxicam derivatives alone and in combination with doxorubicin was assessed. Inhibition of P-glycoprotein (ABCB1) transport activity was monitored by flow cytometry. Expression of ABCB1 gene was analyzed by semi-quantitative reverse transcription PCR, while ABCB1 protein expression was assessed by western blotting.RESULTS:
Oxicam derivative PR18 was more cytotoxic to cancer cells than PR17. PR18 was observed to sensitize LoVo/Dx cells to doxorubicin and was identified as an effective multidrug resistance modulator. Additionally, ABCB1 expression was reduced in the presence of PR18.CONCLUSION:
PR18 was identified as an effective modulator in LoVo/Dx resistant human colorectal adenocarcinoma cells which overexpressed ABCB1 efflux pump.Palavras-chave
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Base de dados:
MEDLINE
Assunto principal:
Tiazinas
/
Adenocarcinoma
/
Neoplasias do Colo
/
Resistencia a Medicamentos Antineoplásicos
/
Óxidos S-Cíclicos
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article