Malinow M R, Elliott W H, McLaughlin P, Upson B
J Lipid Res. 1987 Jan;28(1):1-9.
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.
合成了薯蓣皂苷元葡萄糖苷（DG）的主要β-异构体，并在猴子身上测试了其对胆固醇稳态的影响。在两个为期3周的时间段内，分别给食蟹猴（食蟹猕猴）喂食含0.1%胆固醇的半纯化饮食和含1% DG的类似日粮。在实验周期之间给予5周的普通饮食。在每种半纯化饮食的最后一周分析胆固醇和胆汁酸平衡。薯蓣皂苷元葡萄糖苷使胆固醇血症从292毫克/分升降至172毫克/分升，将外源性胆固醇的肠道吸收从62.4%降至26.0%，并使内源性胆固醇的分泌从-0.8毫克/天增加至93.5毫克/天。中性类固醇的粪便排泄量从40.7毫克/天增至157.3毫克/天；胆汁酸的排泄量从23.1毫克/天变化至16.0毫克/天，变化不显著。对照组的胆固醇平衡为-44毫克/天，喂食DG的动物为88毫克/天。未观察到毒性迹象。因此，当长期研究表明该葡萄糖苷耐受性良好时，DG和其他具有类似活性的合成糖苷可能可用于治疗高胆固醇血症和动脉粥样硬化。
