A cell model for high-throughput screening lead compounds targeting HIF-1α for atherosclerosis treatment / 药学实践杂志

ABSTRACT

Objective To establish a high-throughput in-vitro screening cell model for anti-atherosclerosis leading compounds.Methods Hypoxia response element (HRE) was cloned into a luciferase reporter vector, pGL3-Enhancer, to construct pGL3-HIF-1α-HRE.The THP-1human monocyte cell line was infected with the pGL3-HIF-1α-HRE and a stable cell line, THP-1-HIF-1α-HRE, was screened.Results Real-time PCR assay showed that HIF-1αexpression and luciferase activity in THP-1-HIF-1α-HRE cells was effectively upregulated by hypoxia.The increase of HIF-1αexpression and luciferase activity induced by hypoxia was significantly inhibited by lovastatin or curcumin.Conclusion THP1-HIF-1α-HRE, an in-vitro cell model for high-throughput screening lead compounds for anti-atherosclerosis (AS) was successfully established.