Diapocynin versus apocynin as pretranscriptional inhibitors of NADPH oxidase and cytokine production by peripheral blood mononuclear cells

Marília P.P. Kanegae, Antonio Condino-Neto, Luis Alberto Pedroza, Ana Carolina de Almeida, Jussara Rehder, Luiz Marcos da Fonseca, Valdecir F. Ximenes

Producción científica: Contribución a una revistaArtículorevisión exhaustiva

33 Citas (Scopus)

Resumen

Apocynin has been extensively used as an inhibitor of NADPH oxidase (NOX) in many experimental models using phagocytic and non-phagocytic cells. Currently, there is some controversy about the efficacy of apocynin in non-phagocytic cells, but in phagocytes the reported results are consistent, which could be due to the presence of myeloperoxidase in these cells. This enzyme has been proposed as responsible for activating apocynin by generating its dimer, diapocynin, which is supposed to be the active compound that prevents NADPH oxidase complex assembly and activation. Here, we synthesized diapocynin and studied its effect on inhibition of gp91phox RNA expression. We found that diapocynin strongly inhibited the expression of gp91phoxmRNA in peripheral blood mononuclear cells (PBMC). Only at a higher concentration, apocynin was able to exert the same effect. We also compared the apocynin and diapocynin efficacy as inhibitors of tumor necrosis factor-alpha (TNF-α) and interleukin-10 (IL-10) production in response to lipopolysaccharide (LPS)-activated PBMC. Although apocynin did inhibit TNF-α production, diapocynin had a much more pronounced effect, on both TNF-α and IL-10 production. In conclusion, these findings suggest that the bioconversion of apocynin to diapocynin is an important issue not limited to enzymatic activity inhibition, but also for other biological effects as gp91phox mRNA expression and cytokine production. Hence, as diapocynin can be easily prepared from apocynin, a one-step synthesis, we recommend its use in studies where the biological effects of apocynin are searched.

Idioma originalInglés
Páginas (desde-hasta)551-554
Número de páginas4
PublicaciónBiochemical and Biophysical Research Communications
Volumen393
N.º3
DOI
EstadoPublicada - 12 mar. 2010
Publicado de forma externa

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