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La unión nanomolar de esteroides a las urillas de cucurbita: selectividad y aplicaciones

Alexandra I Lazar¹, Frank Biedermann², Kamila R Mustafina¹

¹Department of Life Sciences and Chemistry, Jacobs University Bremen , Campus Ring 1, 28759 Bremen, Germany.

Journal of the American Chemical Society

|September 28, 2016

Resumen

Cucurbit[n]urils (CBn) son potentes receptores artificiales para esteroides, que muestran altas afinidades de unión y selectividad. Estos complejos estables ofrecen un potencial significativo para aplicaciones de administración y detección de fármacos.

Área de la Ciencia:

Química supramolecular
Biología Química

Sus antecedentes:

Los esteroides, incluidas las hormonas y los medicamentos, son biomoléculas cruciales con interacciones complejas.
El desarrollo de receptores artificiales eficaces para el reconocimiento selectivo de esteroides sigue siendo un desafío.

Objetivo del estudio:

Para investigar cucurbit[n]urils (CBn) como receptores artificiales para una amplia gama de esteroides.
Caracterizar las afinidades de unión, selectividades y estabilidad de los complejos CBn-esteroides.
Explorar las aplicaciones potenciales de estos complejos en la administración y detección de fármacos.

Principales métodos:

Titraciones por desplazamiento de fluorescencia
Calorimetría por titulación isotérmica (ITC)
Espectroscopia de resonancia magnética nuclear (RMN)
Difracción de los cristales de rayos X
Cálculos químicos cuánticos

Principales resultados:

CBn (n=7, 8) demostró altas afinidades de unión (rango nanomolar) para 21 esteroides probados.
Se observaron selectividades de unión excepcionales, incluso para parejas de esteroides estructuralmente similares.
Los complejos CBn-esteroides mostraron una notable estabilidad en diversos ambientes acuosos, incluido el ácido gástrico artificial y el suero sanguíneo.
Se logró un aumento significativo de la solubilidad (hasta 100 veces) de los esteroides en presencia de CBn.

Conclusiones:

Cucurbit[n]urils representan una nueva clase de receptores artificiales altamente efectivos para los esteroides.
La estabilidad y la selectividad de los complejos CBn-esteroides abren vías para sistemas avanzados de administración de fármacos.
Los sistemas basados en CBn son prometedores para la detección diferencial de esteroides y los ensayos enzimáticos en tiempo real.

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