High throughput screening for intercellular adhesion molecule-1 inhibitor.
- Author:
De-cheng REN
1
;
Guan-hua DU
;
Jun-tian ZHANG
Author Information
- Publication Type:Journal Article
- MeSH: Cell Adhesion Molecules; antagonists & inhibitors; biosynthesis; Cells, Cultured; Chemistry, Pharmaceutical; methods; Drug Evaluation, Preclinical; methods; Endothelium, Vascular; cytology; metabolism; Humans; Intercellular Adhesion Molecule-1; drug effects; metabolism; Lipopolysaccharides; pharmacology; Umbilical Veins; cytology; metabolism
- From: Acta Pharmaceutica Sinica 2003;38(6):405-408
- CountryChina
- Language:English
-
Abstract:
AIMTo develop a high throughput screening assay to identify inhibitors of intercellular adhesion molecule-1 (ICAM-1) expression in human umbilical vein endothelial cells (HUVEC).
METHODSICAM-1 expression in lipopolysaccharide-stimulated endothelial cells was measured by ELISA. The cytotoxicity of the compounds was measured by MTT.
RESULTSLipopolysaccharide (LPS) increased ICAM-1 expression in HUVEC in a concentration- and time-dependent manner. Two thousand compounds were screened and the hit rate was 1.5%. Among these 30 compounds, 24 were cytotoxic.
CONCLUSIONThe ELISA method was inexpensive, reproducible and suitable for high throughput primary cell assay. This assay was feasible to identify inhibitors of ICAM-1 and simultaneously discriminate the activity from the cytotoxic effects.
