抄録
Effects of trapidil (Rocornal®) on the metabolism of cholesterol and lipoprotein in rats were studied. Trapidil increased serum high density lipoprotein cholesterol (HDL-cholesterol) level and decreased serum low density lipoprotein cholesterol (LDL-cholesterol) level and the ratio of HDL-cholesterol to LDL-cholesterol. On the basis of these data, a possible mechanism of action of trapidil was investigated. Uptakes of 14C-acetate into cholesterol in serum, liver and small intestine were suppressed with trapidil. Both blood and bile 14C-cholesterol were significantly decreased and the radioactivity excretion in bile was markedly increased with trapidil. Trapidil increased HDL-apoprotein, HDL-apoprotein A-I in serum and apoprotein A-I in lymph of small intestine. Moreover, half life of 125I-HDL in plasma was significantly prolonged and that of 125I-LDL was significantly shortened with trapidil. These date suggested that trapidil inhibits the cholesterol biosynthesis and stimulates the catabolism and excretion of cholesterol, and biosynthesis of HDL-apoprotein, especially apoprotein A-I.
