The in vitro anti-atherosclerotic activity of compound IMB-1680.
- Author:
Ting-Ting FENG
;
Yong-Zhen LI
;
Ni LI
;
Chang LIU
;
Xiao WANG
;
Yan-Ni XU
;
Shu-Yi SI
- Publication Type:Journal Article
- MeSH:
Animals;
CD36 Antigens;
antagonists & inhibitors;
genetics;
metabolism;
CHO Cells;
Cells, Cultured;
Cricetulus;
Dose-Response Relationship, Drug;
Foam Cells;
cytology;
High-Throughput Screening Assays;
Humans;
Lipoproteins, LDL;
metabolism;
Macrophages;
cytology;
metabolism;
Mice;
Molecular Structure;
Plasmids;
Receptors, Scavenger;
antagonists & inhibitors;
Sf9 Cells;
Spodoptera;
Transfection
- From:
Acta Pharmaceutica Sinica
2014;49(5):602-607
- CountryChina
- Language:Chinese
-
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.
