Vanhanen H, Miettinen T A
Second Dept. of Medicine, University of Helsinki, Finland.
Scand J Gastroenterol. 1995 Jan;30(1):33-7. doi: 10.3109/00365529509093232.
Enprostil, a synthetic dehydroprostaglandin E2 structural analogue primarily developed for treatment of gastritis, has been shown also to lower serum cholesterol.
We studied cholesterol metabolism in seven hypercholesterolemic subjects before, during, and after a low-dose enprostil (18 micrograms/day) treatment, measuring serum lipids, cholesterol absorption by an oral double-isotope method, fecal cholesterol elimination by the balance technique, and fecal fat. In addition, an oral fat load test with vitamin A was performed.
The drug treatment reduced serum concentrations of total and low-density lipoprotein (LDL) cholesterol by 8.2% and 7.9% (p < 0.05), respectively, and cholesterol absorption efficiency by 18% (p < 0.05), and increased fecal output of neutral sterols by 20% (p < 0.05), bile acids by 24% (NS), and cholesterol synthesis by 30% (p < 0.05). Postabsorptive concentrations of triglycerides and vitamin A in chylomicrons were reduced 3-4 h after the intake of the test meal. Fecal fat excretion was doubled during the enprostil treatment.
Enprostil reduces serum cholesterol concentrations, apparently by inhibiting cholesterol absorption so that fecal cholesterol elimination is increased in association with a mild fat malabsorption. Enhanced intestinal motility may contribute to these changes, frequently causing abdominal fullness or mild pain without diarrhea.
恩前列素是一种合成的脱氢前列腺素E2结构类似物,最初开发用于治疗胃炎,现已证明它还能降低血清胆固醇。
我们研究了7名高胆固醇血症患者在低剂量恩前列素(18微克/天)治疗前、治疗期间和治疗后的胆固醇代谢情况,测量血清脂质、采用口服双同位素法测定胆固醇吸收、采用平衡技术测定粪便胆固醇排泄以及粪便脂肪。此外,还进行了维生素A口服脂肪负荷试验。
药物治疗使总胆固醇和低密度脂蛋白(LDL)胆固醇的血清浓度分别降低了8.2%和7.9%(p<0.05),胆固醇吸收效率降低了18%(p<0.05),中性固醇的粪便排出量增加了20%(p<0.05),胆汁酸增加了24%(无统计学意义),胆固醇合成增加了30%(p<0.05)。摄入试验餐后3-4小时,乳糜微粒中甘油三酯和维生素A的吸收后浓度降低。在恩前列素治疗期间,粪便脂肪排泄量增加了一倍。
恩前列素降低血清胆固醇浓度,显然是通过抑制胆固醇吸收,从而使粪便胆固醇排泄增加,同时伴有轻度脂肪吸收不良。肠道蠕动增强可能导致这些变化,常引起腹部饱胀或轻度疼痛,但无腹泻。