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Pro-portadores receptivos a las enzimas capaces de transportar iones cloruro a través de las membranas lipídicas y
Ye Rin Choi1, Bom Lee1, Jinhong Park2
1Department of Chemistry, Yonsei University , Seoul 120-749, Korea.
Journal of the American Chemical Society
|December 10, 2016
Resumen
Los investigadores desarrollaron procarios activados por enzimas para el transporte controlado de iones cloruro a través de membranas. Estos procariadores mejoran la administración del fármaco al mejorar la solubilidad y permitir la activación dirigida.
Área de la Ciencia:
- Transporte por membrana
- La bioquímica
- Sistemas de administración de medicamentos
Sus antecedentes:
- El transporte de iones cloruro es crucial para las funciones celulares.
- El desarrollo de sistemas de entrega dirigidos para moléculas hidrofóbicas sigue siendo un desafío.
- Las estrategias de Procarrier ofrecen potencial para la activación y la entrega controladas.
Objetivo del estudio:
- Introducir y validar el concepto de procarrier para el transporte controlado de iones cloruro.
- Investigar la activación por medio de enzimas de los procariantes en condiciones específicas.
- Evaluar el impacto de los apéndices hidrófilos en la solubilidad de los procariones y en el particionamiento de la membrana.
Principales métodos:
- Síntesis de procariones con apéndices hidrofílicos vinculados por enlaces de éster y de glucósilo.
- Hidrólisis enzimática de los apéndices mediante esterasa (PLE) y glucosilasa (AOG).
- Ensayos de transporte de iones cloruro a través de las bicapas lipídicas y las membranas celulares.
- Estudios de activación dependientes del pH.
Principales resultados:
- Los procariantes fueron inicialmente inactivos en las membranas lipofílicas pero activados por enzimas específicas.
- Los procariadores de enlace de éster fueron activados por el PLE a un pH de 7,4.
- Los procariadores de enlaces de glucosilo fueron activados por AOG a un pH de 5,5-6.
- Los apéndices hidrófilos mejoran la solubilidad en agua de los procariones, lo que facilita el parto.
Conclusiones:
- La estrategia del procariador permite la activación controlada y específica de la enzima del transporte de iones cloruro.
- La activación condicional permite la entrega y el transporte dirigidos a través de las membranas.
- Este enfoque es prometedor para mejorar la administración de medicamentos hidrofóbicos.
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