5 alpha-Cholest-8(14)-en-3 beta-ol-15-one lowers serum cholesterol and induces profound changes in the levels of lipoprotein cholesterol and apoproteins in monkeys fed a diet of moderate cholesterol content.
5 alpha-Cholest-8(14)-en-3 beta-ol-15-one has been found to have significant hypocholesterolemic activity upon oral administration at a daily dosage of 75 mg/kg of body weight to Rhesus monkeys fed a diet of moderate cholesterol (Chol) content [0.19 mg/kcal (1 cal = 4.184 J) of diet]. The reductions in total serum Chol levels (mean, -41%) were associated with even more striking reductions (mean, -61%) in the levels of low density lipoprotein (LDL) plus very low density lipoprotein (VLDL) Chol and also with increases in high density lipoprotein (HDL) Chol levels (mean, +61%). The mean increase in HDL Chol was 33 mg/dl. In one animal, that with the lowest pretreatment HDL Chol level, the extent of the rise was 49 mg/dl (+120%). These changes were associated with reductions in the % of total serum Chol associated with LDL/VLDL, in the ratios of total Chol to HDL Chol and of LDL/VLDL Chol to HDL Chol, and in the levels of LDL protein. The 15-ketosterol also increased the % of total Chol associated with HDL, increased the level of HDL protein, and induced a shift in the HDL profile to one in which the HDL2 species was the predominant species. All of these changes are those generally considered desirable for the treatment and/or prevention of atherosclerosis.
D000818:Animals; D002782:Cholestenes / Q000494:pharmacology*; D002783:Cholestenones / Q000494:pharmacology*; D002784:Cholesterol / Q000097:blood*; D002791:Cholesterol, Dietary / Q000008:administration & dosage*; D008076:Cholesterol, HDL / Q000097:blood; D008078:Cholesterol, LDL / Q000097:blood; D015243:Cholesterol, VLDL; D007700:Kinetics; D008074:Lipoproteins / Q000097:blood*; D008079:Lipoproteins, VLDL / Q000097:blood; D008253:Macaca mulatta; D008297:Male; D014280:Triglycerides / Q000097:blood
D002782:Cholestenes; D002783:Cholestenones; D002791:Cholesterol, Dietary; D008076:Cholesterol, HDL; D008078:Cholesterol, LDL; D015243:Cholesterol, VLDL; D008074:Lipoproteins; D008079:Lipoproteins, VLDL; D014280:Triglycerides; C015073:cholest-8(14)-en-3-ol-15-one; D002784:Cholesterol