Watanabe T, Manna H, Suga T
J Pharmacobiodyn. 1981 Oct;4(10):743-50. doi: 10.1248/bpb1978.4.743.
Effects of vitamin B2-butyrate, nicomol, ML-236B, KF 1492 and pantethine, which are hypolipidemic drugs, on biochemical values and on hepatic peroxisomal enzymes of normolipemic rat. 1) Vitamin B2-butyrate (100 mg/kg) and nicomol (lg/Kg) increased carnitine acetyltransferase and D-amino acid oxidase activities, respectively, while these drugs had no influence on body weight, liver weight, serum and liver triglyceride, and serum and liver cholesterol levels. 2) ML-236B (300 mg/kg) had no influence on biochemical values and on activities of peroxisomal enzymes containing catalase. 3) KF 1492 (300 mg/kg) had no influence on the biochemical values, but an increase in the activities of fatty acyl-CoA oxidizing system (FAOS) and carnitine acetyltransferase (CAT) participating hepatic lipid metabolism was observed. 4) Pantethine (lg/kg) had no influence on the biochemical values, except a little decrease in the growth rate. However, increase by about 10% in the activities of urate oxidase and D-amino acid oxidase was observed. Catalase activity was decreased to 60% of control level. From these results, it is concluded that, in contrast to clofibrate, vitamin B2-butyrate, nicomol, ML-236B, KF 1492 and pantethine have little influence on the lipid metabolism of normolipemic animal and on the hepatic peroxisomal enzymes, indicating that the action mechanism of these drugs may be different from that of clofibrate and that the participation of hepatic peroxisomes in hypolipidemic activities of these drugs may be little if any.
维生素B2-丁酸盐、尼克莫尔、ML-236B、KF 1492和泛硫乙胺这些降血脂药物对血脂正常大鼠的生化指标及肝脏过氧化物酶体酶的影响。1)维生素B2-丁酸盐(100毫克/千克)和尼克莫尔(1克/千克)分别增加了肉碱乙酰转移酶和D-氨基酸氧化酶的活性,而这些药物对体重、肝脏重量、血清和肝脏甘油三酯以及血清和肝脏胆固醇水平没有影响。2)ML-236B(300毫克/千克)对生化指标及含过氧化氢酶的过氧化物酶体酶活性没有影响。3)KF 1492(300毫克/千克)对生化指标没有影响,但观察到参与肝脏脂质代谢的脂肪酰基辅酶A氧化系统(FAOS)和肉碱乙酰转移酶(CAT)的活性增加。4)泛硫乙胺(1克/千克)对生化指标没有影响,只是生长速率略有下降。然而,观察到尿酸氧化酶和D-氨基酸氧化酶的活性增加了约10%。过氧化氢酶活性降至对照水平的60%。从这些结果可以得出结论,与氯贝丁酯不同,维生素B2-丁酸盐、尼克莫尔、ML-236B、KF 1492和泛硫乙胺对血脂正常动物的脂质代谢及肝脏过氧化物酶体酶影响很小,这表明这些药物的作用机制可能与氯贝丁酯不同,并且肝脏过氧化物酶体对这些药物降血脂活性的参与可能很少(如果有参与的话)。