A cell model for high-throughput screening lead compounds targeting HIF-1α for atherosclerosis treatment
10.3969/j.issn.1006-0111.2019.01.007
- VernacularTitle:建立以HIF-1α为靶标的高通量筛选防治动脉粥样硬化先导化合物的细胞模型
- Author:
Yujun QIAN
1
;
Chunxia QIN
;
Lili SUN
;
Huamin DING
;
Tiejun LI
Author Information
1. 上海市浦东新区浦南医院药剂科
- Keywords:
hypoxia inducible factor-1α;
high-throughput;
luciferase;
atherosclerosis;
screen
- From:
Journal of Pharmaceutical Practice
2019;37(1):27-31
- CountryChina
- Language:Chinese
-
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.
