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Mol Cell Endocrinol ; 426: 146-54, 2016 May 05.
Artigo em Inglês | MEDLINE | ID: mdl-26930569

RESUMO

Aminopeptidases (APs) are involved in various physiological and pathological processes. In tumor tissues the expression of APs, cyclooxygenase-2 and its metabolites are increased. The objective was to determine the effect of certain NSAIDs on the AP activity of osteoblasts. Primary cultures of osteoblast were treated with different concentrations of indomethacin, meloxicam, naproxen, nimesulide, and piroxicam. The AP activity was fluorimetrically determined using aminoacyl-ß-naphthylamides (aa-ßNAs) as substrates: Ala-ßNA, Arg-ßNA, Gly-ßNA, Leu-ßNA, Lys-ßNA, Met-ßNA, and Phe-ßNA. The five NSAIDs showed an inhibitory effect of AP activity against the study substrates depending on the dose tested. Meloxicam and piroxicam had the highest inhibitory effect on enzymatic activity, with an IC50 of around 70 µM. Our results suggest that the physiological alteration of osteoblasts in the presence of NSAIDs may be a consequence of AP inhibition, suggesting a potential clinical role for these drugs against cancer in combination with chemotherapeutic agents.


Assuntos
Aminopeptidases/metabolismo , Anti-Inflamatórios não Esteroides/farmacologia , Osteoblastos/enzimologia , Adulto , Células Cultivadas , Avaliação Pré-Clínica de Medicamentos , Feminino , Humanos , Masculino , Osteoblastos/efeitos dos fármacos , Adulto Jovem
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