A BENZOTHIOPHENE-CARBOXAMIDE IS A POTENT INHIBITOR OF IL-1-BETA INDUCED VCAM-1 GENE-EXPRESSION IN HUMAN ENDOTHELIAL-CELLS

Vascular endothelial cells respond to cytokines such as IL-1 beta or T NF-alpha by undergoing a number of functional alterations. Among these alterations is the induction of cell surface adhesion molecules, incl uding VCAM-1. In this report, ,ve investigated the effects of a 3-alko xybenzo[beta]thiophene-2-carboxamide (BZT) on the cytokine induction o f VCAM-1 expression and activation of the transcription factor NF-kapp a B in human endothelial cells. BZT blocked the IL-1 beta induced cell surface expression of VCAM-1 in human endothelial cells but did not p revent nuclear translocation of NF-kappa B. This study demonstrates th at BZT is a potent inhibitor of VCAM-1 expression in human endothelial cells.