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2019, Número 2

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Biotecnol Apl 2019; 36 (2)


Extractos metanólicos de secreciones de glándulas paratoideas de sapos cubanos del género Peltophryne contienen actividades inhibitorias de peptidasas de relevancia biomédica

Pascual-Alonso I, Alonso-Bosch R, Cabrera-Muñoz A, Perera WH, Charli JL

Idioma: Ingles.
Referencias bibliográficas: 41
Paginas: 2221-2227
Archivo PDF: 566.96 Kb.


RESUMEN

Las peptidasas regulan la mayoría de los procesos bioquímicos y fisiológicos de los organismos vivos y facilitan la propagación de agentes infecciosos. Muchas son blancos para el diseño de nuevos agentes terapéuticos. En este contexto, las secreciones de la piel de los anfibios han evolucionado con potentes mecanismos de defensa contra depredadores y microorganismos, aunque se ha informado sobre pocos inhibidores de peptidasas en ellas. En este trabajo se evaluó el efecto inhibitorio de extractos metanólicos obtenidos de las secreciones de las glándulas paratoides de cuatro especies de sapos endémicos cubanos (Peltophryne fustiger, P. florentinoi, P. peltocephala y P. taladai) contra nueve peptidasas de diferentes clases mecanísticas. El análisis químico cualitativo de los extractos indicó la presencia de triterpenoides y esteroides, azúcares reductores, compuestos fenólicos, aminoácidos, glucósidos cardíacos y alcaloides. Las actividades inhibitorias frente a pAPN, pAPA y pDPP-IV fueron dependientes de la dosis; la inhibición disminuyó al incrementar la concentración de sustrato. La secreción de P. fustiger inhibió a la papaína de forma dosis-dependiente, aunque la inhibición no dependió de la concentración del sustrato. Tampoco se detectó inhibición dosis-dependiente para tripsina, pepsina bovina, mPPII, pAPB ni pLAP. Además, Bufalina inhibió a pAPN (IC50 de 6.23 ± 0.11 μM) y el comportamiento cinético sugirió un modo de inhibición no competitivo (α >1 ) o competitivo. Los extractos metanólicos estudiados contienen actividades inhibidoras dirigidas contra peptidasas de tipo metalo, serino y cisteíno, cuya caracterización química podría generar nuevos inhibidores con relevancia biomédica. Además, Bufalina emerge como un nuevo inhibidor clásico de pAPN.


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