Effects of synthetic glycosides on steroid balance in Macaca fascicularis.
The predominantly beta-anomer of diosgenin glucoside (DG) was synthesized and its effects on cholesterol homeostasis were tested in monkeys. Cynomolgus macaques (Macaca fascicularis) were fed, during two 3-week periods, a semipurified diet with 0.1% cholesterol and a similar ration containing 1% DG, respectively. A Chow diet was given for 5 weeks between the experimental periods. Cholesterol and bile acid balance were analyzed during the last week of each semipurified diet. Diosgenin glucoside reduced cholesterolemia from 292 mg/dl to 172 mg/dl, decreased intestinal absorption of exogenous cholesterol from 62.4% to 26.0%, and increased secretion of endogenous cholesterol from -0.8 to 93.5 mg/day. The fecal excretion of neutral steroids rose from 40.7 to 157.3 mg/day; that of bile acids changed, nonsignificantly, from 23.1 to 16.0 mg/day. The cholesterol balance was -44 mg/day in the control period, and 88 mg/day in the DG-fed animals. No toxic signs were observed. Thus, when long-term studies demonstrate that the glucoside is well tolerated, DG and other synthetic glycosides with similar activities may be of use in the management of hypercholesterolemia and atherosclerosis.
D000818:Animals; D001647:Bile Acids and Salts / Q000378:metabolism*; D002250:Carbon Radioisotopes; D002784:Cholesterol / Q000378:metabolism*; D002791:Cholesterol, Dietary; D004144:Diosgenin / Q000031:analogs & derivatives / Q000494:pharmacology*; D004906:Erythrocyte Count / Q000187:drug effects; D005260:Female; D005960:Glucosides / Q000494:pharmacology*; D006027:Glycosides / Q000494:pharmacology*; D006400:Hematocrit; D006706:Homeostasis; D007408:Intestinal Absorption; D007700:Kinetics; D007958:Leukocyte Count / Q000187:drug effects; D008251:Macaca / Q000378:metabolism*; D008252:Macaca fascicularis / Q000378:metabolism*; D012502:Sapogenins / Q000494:pharmacology*; D014280:Triglycerides / Q000097:blood; D014316:Tritium
D001647:Bile Acids and Salts; D002250:Carbon Radioisotopes; D002791:Cholesterol, Dietary; D005960:Glucosides; D006027:Glycosides; D012502:Sapogenins; D014280:Triglycerides; D014316:Tritium; C051985:diosgenin glucoside; D002784:Cholesterol; D004144:Diosgenin