title: [The in vitro anti-atherosclerotic activity of compound IMB-1680].
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.
authors.forename: Ting-Ting
authors.initials: TT
authors.lastname: Feng
authors.forename: Yong-Zhen
authors.initials: YZ
authors.lastname: Li
authors.forename: Ni
authors.initials: N
authors.lastname: Li
authors.forename: Chang
authors.initials: C
authors.lastname: Liu
authors.forename: Xiao
authors.initials: X
authors.lastname: Wang
authors.forename: Yan-Ni
authors.initials: YN
authors.lastname: Xu
authors.forename: Shu-Yi
authors.initials: SY
authors.lastname: Si
mesh_terms: D000818:Animals; D018955:CD36 Antigens / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism*; D016466:CHO Cells; D002478:Cells, Cultured; D003412:Cricetulus; D004305:Dose-Response Relationship, Drug; D005487:Foam Cells / Q000166:cytology; D057166:High-Throughput Screening Assays; D006801:Humans; D008077:Lipoproteins, LDL / Q000378:metabolism*; D008264:Macrophages / Q000166:cytology / Q000378:metabolism; D051379:Mice; D015394:Molecular Structure; D010957:Plasmids; D051116:Receptors, Scavenger / Q000037:antagonists & inhibitors*; D061987:Sf9 Cells; D018411:Spodoptera; D014162:Transfection
chemical_list: D018955:CD36 Antigens; D008077:Lipoproteins, LDL; D051116:Receptors, Scavenger; C032629:acetyl-LDL; C099252:oxidized low density lipoprotein