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Phosphoramidon inhibits the intracellular conversion of big endothelin-1 to endothelin-1 in cultured endothelial cells

1991; Elsevier BV; Volume: 174; Issue: 2 Linguagem: Inglês

10.1016/0006-291x(91)91485-u

1090-2104

Tatsuya Sawamura, Yoshitoshi Kasuya, Yoh‐ichi Matsushita, Nobuhiro Suzuki, Osamu Shinmi, Naoya Kishi, Yoshiki Sugita, Masashi Yanagisawa, Katsutoshi Goto, Tomoh Masaki, Sadao Kimura,

Renin-Angiotensin System Studies

Effects of various protease inhibitors on the conversion of big endothelin (ET)-1 to ET-1 in cultured endothelial cells were analyzed. A metal protease inhibitor, phosphoramidon, decreases the amount of ET-1 and increase that of big ET-1 released. This effect is dose-dependent and not nonspecific. When the contents of ET-1 and big ET-1 in the cells after culturing in the medium with or without phosphoramidon were measured, the ratio of ET-1: big ET-1 in the cells was 3.3 : 1 and phosphoramidon inverted the ratio in the cells to 1 : 3.5. These data strongly suggest that a phosphoramidon-sensitive protease converts big ET-1 to mature ET-1 intracellularly.