[Establishment of a drug screening model for identifying up-regulator of human high density lipoprotein receptor].

Abstract

OBJECTIVE:

To establish a new drug screening model based on transcriptional regulation of human high density lipoprotein (HDL) receptor gene CD36 and LIMPII analogous-1 (CLA-1) for discovering up-regulator of this receptor.

METHODS:

The upstream regulatory sequence of CLA-1 was obtained by polymerase chain reaction. A recombinant reporter plasmid pGL3-CLAP was constructed by inserting the regulatory sequence upstream of luciferase gene of pGL3-Basic. Human hepatoma cell line BEL-7402 was transfected with pGL3-CLAP. Samples were detected by testing luciferase activity of transfected BEL-7402 cells in microtiter wells.

RESULTS:

The drug screening model was established and optimized. Significant difference was present between pGL3-CLAP and pGL3-Basic transfected BEL-7402 cells (P< 0.001), and coefficient of variation was less than 10%. After primary and secondary screening, 1 compounds and 3 fermentation extracts had up-regulating activities.

CONCLUSION:

This new drug screening model may be efficiently used to screen up-regulators of human HDL receptor expression, which might become lead compounds for new anti-atherosclerosis drugs.

• Authors: Xiao-hui Liu, Bin Hong, Li-fei Wang, Yuan Yang, Shu-yi Si, Yuan Li
• Journal: Zhongguo yi xue ke xue yuan xue bao. Acta Academiae Medicinae Sinicae (Zhongguo Yi Xue Ke Xue Yuan Xue Bao) Vol. 26 Issue 4 Pg. 354-8 (Aug 2004) ISSN: 1000-503X [Print] China
• PMID: 15379255 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• CD36 Antigens
• Cholesterol Esters
• Hypolipidemic Agents
• Lipoproteins, HDL
• RNA, Messenger
• RNA-Binding Proteins
• Receptors, Immunologic
• Receptors, Lipoprotein
• Receptors, Scavenger
• SCARB1 protein, human
• Scavenger Receptors, Class B
• high density lipoprotein receptors

Topics

• CD36 Antigens
• Cholesterol Esters (metabolism)
• Drug Evaluation, Preclinical (methods)
• Gene Expression Regulation (drug effects)
• Humans
• Hypolipidemic Agents (chemical synthesis, pharmacology)
• Lipoproteins, HDL (genetics, metabolism)
• RNA, Messenger (metabolism)
• RNA-Binding Proteins
• Receptors, Immunologic (genetics)
• Receptors, Lipoprotein (genetics)
• Receptors, Scavenger
• Scavenger Receptors, Class B
• Transcription, Genetic (drug effects)
• Up-Regulation