High throughput screening for intercellular adhesion molecule-1 inhibitor / 药学学报

ABSTRACT

<p><b>AIM</b>To develop a high throughput screening assay to identify inhibitors of intercellular adhesion molecule-1 (ICAM-1) expression in human umbilical vein endothelial cells (HUVEC).</p><p><b>METHODS</b>ICAM-1 expression in lipopolysaccharide-stimulated endothelial cells was measured by ELISA. The cytotoxicity of the compounds was measured by MTT.</p><p><b>RESULTS</b>Lipopolysaccharide (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.</p><p><b>CONCLUSION</b>The 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.</p>