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Un producto natural que reduce el colesterol como un ligando antagonista para la FXR
Nancy L Urizar1, Amy B Liverman, D'Nette T Dodds
1Department of Molecular and Cellular Biology, Baylor College of Medicine, 1 Baylor Plaza, Houston, TX 77030, USA.
Science (New York, N.Y.)
|May 4, 2002
Resumen
La guggulsterona, del árbol guggul, reduce el colesterol LDL al bloquear el receptor farnesoide X (FXR). Este descubrimiento revela un mecanismo para la reducción del colesterol por compuestos naturales.
Área de la Ciencia:
- La bioquímica es la bioquímica.
- Farmacología Farmacología.
- Productos Naturales Productos Naturales.
Sus antecedentes:
- Se sabe que el extracto de resina del árbol guggul (Commiphora mukul) reduce el colesterol LDL en los seres humanos.
- La gugulsterona se identifica como el fitosterol activo responsable de este efecto reductor del colesterol.
- El receptor farnesoide X (FXR) es un receptor nuclear activado por los ácidos biliares, que juega un papel en la regulación metabólica.
Objetivo del estudio:
- Para dilucidar el mecanismo molecular por el cual la guggulsterona ejerce sus efectos reductores del colesterol.
- Para investigar el papel del receptor farnesoide X (FXR) en la mediación de la actividad de la guggulsterona.
Principales métodos:
- Pruebas in vitro para determinar la interacción de la guggulsterona con el receptor farnesoide X (FXR).
- En estudios in vivo con ratones de tipo salvaje y ratones sin FXR alimentados con una dieta alta en colesterol.
- Medición de los niveles de colesterol hepático después del tratamiento con guggulsterona.
Principales resultados:
- La gugulsterona actúa como un potente antagonista del receptor farnesoide X (FXR, por sus siglas en inglés).
- El tratamiento con Guggulsterona disminuyó significativamente el colesterol hepático en ratones de tipo salvaje en una dieta alta en colesterol.
- El efecto reductor del colesterol de la guggulsterona fue abolido en ratones sin FXR.
Conclusiones:
- La actividad reductora del colesterol de la guggulsterona está mediada a través de la inhibición de la activación del receptor farnesóide X (FXR).
- Este estudio propone la inhibición de la FXR como el mecanismo principal para los efectos reductores de lípidos de la guggulsterona.
- Los productos naturales pueden modular la actividad de los receptores de hormonas nucleares como FXR, ofreciendo un potencial terapéutico.
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