Hall I H, Williams W L, Gilbert C J, McPhail A T, Spielvogel B F
J Pharm Sci. 1984 Jul;73(7):973-7. doi: 10.1002/jps.2600730728.
A binuclear copper(II) complex was shown to have potent hypolipidemic activity in rats and mice at low doses, i.e., 2.5-10 mg/kg/d. The agent moderately lowered liver ATP-dependent citrate lyase, acetyl CoA synthetase, and phosphatidate phosphohydrolase activities in vivo. The appetite of the animal was reduced by drug treatment, and orally administered cholesterol absorption from the intestine was markedly lowered. Higher lipid levels were found in the chyme and the feces, indicating accelerated excretion of lipids by the drug, probably via the biliary route. Organs, e.g., liver and small intestine, as well as serum lipoprotein levels, demonstrated lower lipid content after drug administration. Thus, this chemical class of agents may have potential as a hypolipidemic agent in humans.
一种双核铜(II)配合物在大鼠和小鼠中低剂量(即2.5 - 10毫克/千克/天)时显示出有效的降血脂活性。该药物在体内适度降低了肝脏中依赖ATP的柠檬酸裂解酶、乙酰辅酶A合成酶和磷脂酸磷酸水解酶的活性。药物治疗降低了动物的食欲,并且口服给药后肠道胆固醇吸收显著降低。在食糜和粪便中发现了更高的脂质水平,表明该药物可能通过胆汁途径加速了脂质的排泄。给药后,肝脏和小肠等器官以及血清脂蛋白水平的脂质含量均降低。因此,这类化学药物可能具有作为人类降血脂药物的潜力。