Heparin regulates transcription of endothelin-1 gene in endothelial cells.

Heparin, which is widely used as an anticoagulant, has been shown to have antiatherosclerotic and antihypertensive effects in animals and humans. These effects are mediated by the inhibition of endothelin-1 (ET-1) production in endothelial cells. To clarify the mechanism of this inhibition, we investigated the effect of heparin on transcriptional regulation of the ET-1 gene in bovine aortic endothelial cells (BAEC) cultured in fetal calf serum.

Endothelin-1 gene expression in endothelial cells is potently inhibited by a vasodilator, dilazep.

Endothelin-1 (ET-1) is considered to be involved in various cardiovascular and renal disorders. The objective of this study was to investigate whether a vasodilator and antiplatelet agent, 1,4-bis[3-(3,4,5-trimethoxybenzoyloxy) propyl]perhydro-1,4-diazepine dihydrochloride monohydrate (dilazep, DZ), has an ET-1-inhibiting effect in vitro. Bovine aortic endothelial cells (BAEC) and human umbilical vein endothelial cells (HUVEC) pretreated with fetal calf serum were treated with DZ and preproET-1 (PpET-1) transcription was evaluated by Northern blot analysis.