%A QIAN Yu-jun1, QIN Chun-xia1, SUN Li-li1, DING Hua-min1, LI Tie-jun1, 2 %T Screening of the anti-atherogenic drugsusing THP-1-HIF-1&alpha;-HER-Luciferase cell model %0 Journal Article %D 2019 %J Journal of Shanghai Jiao Tong University (Medical Science) %R 10.3969/j.issn.1674-8115.2019.01.007 %P 33- %V 39 %N 1 %U {https://xuebao.shsmu.edu.cn/CN/abstract/article_12120.shtml} %8 2019-01-28 %X Objective · To screen the anti-atherosclerosis (AS) activity of the compoundsusing THP-1-HIF-1α-HER-Luciferase high-throughput model, and to verify the anti-AS function of the effective compounds. Methods · THP-1-HIF-1α-HER-Luciferase cells were pretreated with different concentrations of compounds (1, 10, and 100 μg/mL) for 2 h, then cultured under hypoxia for 24 h. Luciferase activity of cells was detected and compounds with anti-AS activity were screenedluciferase activity evaluation. THP-1 and U937 cells were pretreated with effective compounds, and then induced for 24 hoxidized low density lipoprotein (OX-LDL). The formation of foam cells was observedoil red staining. The mRNA level of hypoxia-inducible factor 1α (HIF-1α) was detectedreal-time quantitative PCR (qPCR). HIF-1α protein was detectedWestern blotting. Anti-AS activity of effective compounds were evaluated. Results · Among the 200 compounds, 11 compounds could significantly inhibit the increase of luciferase activity in THP-1-HIF-1α-HER-Luciferase cells inducedhypoxia (all P<0.05), and compound numbered 14 (C14) had the most significant inhibitory effect. THP-1 and U937 cells formed foam cells induced for 24 hOX-LDL. However, cells were pretreated with C14 for 2 h, which could significantly inhibit the formation of foam cells inducedOX-LDL. Cells were induced for 24 hOX-LDL, which could significantly increase the of HIF-1α mRNA and protein (all P<0.05), while cells pretreated with C14 could significantly inhibit the increase of HIF-1α mRNA and protein in a gradient-dependent manner (all P<0.05). Conclusion · THP-1-HIF-1α-HER-Luciferase high-throughput model can be reliability used in screening of compounds with anti-AS activity. C14 has the good anti-AS activity characteristics.