The in vitro anti-atherosclerotic activity of compound IMB-1680 / 药学学报
Acta Pharmaceutica Sinica
;
(12): 602-607, 2014.
Artículo
en Chino
| WPRIM
| ID: wpr-245040
ABSTRACT
In the previous study, a high-throughput screening method was established to find the antagonists of CD36. In the present study, a new compound named IMB-1680 was found using this method. The anti-atherosclerotic activities of IMB-1680 were then evaluated. Dose-dependent activities of IMB-1680 were detected by using Sf9 [hCD36] and CHO [hCD36] models. Fluorescence microscopic photography and flow cytometry were used to analyze uptake of mLDL. Foam cell test with RAW264.7 macrophages was used to examine lipid accumulation. The results showed that IMB-1680 inhibited CD36 activity with IC50 of 2.80 and 8.79 micromol x L(-1) in Sf9[hCD36] and CHO [hCD36] cells, respectively. Fluorescence microscopic photography and flow cytometry revealed that IMB-1680 could significantly reduce DiI-AcLDL uptake. Meanwhile, IMB-1680 also could reduce lipids accumulation in RAW264.7 macrophages. In all, the data indicated that IMB-1680 might be a potent effective anti-atherosclerotic leading compound.
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Plásmidos
/
Transfección
/
Estructura Molecular
/
Células Cultivadas
/
Cricetulus
/
Células CHO
/
Spodoptera
/
Antígenos CD36
/
Biología Celular
/
Relación Dosis-Respuesta a Droga
Límite:
Animales
/
Humanos
Idioma:
Chino
Revista:
Acta Pharmaceutica Sinica
Año:
2014
Tipo del documento:
Artículo
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