Curcumin analogues as selective fluorescence imaging probes for brown adipose tissue and monitoring browning.
Sci Rep
; 5: 13116, 2015 Aug 13.
Article
en En
| MEDLINE
| ID: mdl-26269357
Manipulation of brown adipose tissue (BAT) and browning of white adipose tissue (WAT) can be promising new approaches to counter metabolic disorder diseases in humans. Imaging probes that could consistently monitor BAT mass and browning of WAT are highly desirable. In the course of our imaging probe screening, we found that BAT could be imaged with curcumin analogues in mice. However, the poor BAT selectivity over WAT and short emissions of the lead probes promoted further lead optimization. Limited uptake mechanism studies suggested that CD36/FAT (fatty acid transporter) probably contributed to the facilitated uptake of the probes. By increasing the stereo-hindrance of the lead compound, we designed CRANAD-29 to extend the emission and increase the facilitated uptake, thus increasing its BAT selectivity. Our data demonstrated that CRANAD-29 had significantly improved selectivity for BAT over WAT, and could be used for imaging BAT mass change in a streptozotocin-induced diabetic mouse model, as well as for monitoring BAT activation under cold exposure. In addition, CRANAD-29 could be used for monitoring the browning of subcutaneous WAT (sWAT) induced by ß3-adrenoceptor agonist CL-316, 243.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Tejido Adiposo Pardo
/
Curcumina
/
Colorantes Fluorescentes
Límite:
Animals
Idioma:
En
Revista:
Sci Rep
Año:
2015
Tipo del documento:
Article
Pais de publicación:
Reino Unido