[Hypocholesterolemic effect of phytoecdysones during experimental hypercholesterolemia in rats]

The most active hypocholesterolemic preparation, affecting the absorption of 3H1-cholesterol in small intestine of rats with experimental hypercholesterolemia, proved to be I-hydroxyecdisterone; the activity was gradually decreased in the following series of preparations: ecdisterone, steroid sapogenine allyogenone, ciasterone and ecdisterone 25 acetate. Thus, the hypocholesterolemic activity of the preparations was increased with an increase in the content of hydroxy groups in the molecules. After daily administration of ecdisterone at a dose of 2.5 mg/kg into the animals with hypercholesterolemia within 3, 6 and 8 weeks, content of cholesterol in blood plasma was decreased by 7.0%, 16.9% and 29%, respectively; this phenomenon was accompanied by a decrease of the cholesterol content in erythrocyte membranes as well as in microfilaments of erythrocyte border by 26% and 34%, respectively. Amount of phospholipids and the ratio cholesterol/phospholipids were also normalized in the membranes studied. The data obtained suggest that competitive relationship occurs between cholesterol and the hypocholesterolemic drugs during binding with the membrane sites depending on their concentrations in blood plasma, intestine lumen and on the content in the membranes.