Sarciron M E, Delabre-Defayolle I, Audin P, Petavy A F, Paris J
Département de Parasitologie et Pathologie Exotique, Universitaire Rockefeller, Lyon, France.
Arzneimittelforschung. 1990 May;40(5):607-10.
Ethyl N-N-benzyl-methyl-oxamate is a N-substituted derivative of the oxamic acid, well-known as inhibitor of the lactate dehydrogenase activity. The biochemical and ultrastructural effects of this drug in Echinococcus multilocularis metacestodes and the repercussions in the livers of receptive host, Meriones unguiculatus, were investigated. This compound decreased the specific activity of the lactate dehydrogenase in the metacestodes and the host liver by 81 and 86.8%, respectively. This N-methyl compound has shown an important repercussion on the lactate dehydrogenase activity due to its greater lipophilicity and thus allows a better penetration of the molecule. In the host liver, a fall of the alkaline and acid phosphatases activity was observed. The glucose and glycogen concentrations were also decreased. The ultrastructural study provided an alteration of the tegument of the metacestodes and damages of the muscular system. The parenchyma was disorganized. In conclusion, these biochemical and ultrastructural data obtained with ethyl-N-N-benzyl-methyl oxamate in E. multilocularis metacestodes show clearly the importance of the lactate dehydrogenase activity in the metacestodes.
N - N - 苄基 - 甲基乙酰胺基乙酯是草氨酸的一种N - 取代衍生物,是众所周知的乳酸脱氢酶活性抑制剂。研究了该药物对多房棘球绦虫幼虫的生化和超微结构影响以及对受体宿主长爪沙鼠肝脏的影响。该化合物使幼虫和宿主肝脏中乳酸脱氢酶的比活性分别降低了81%和86.8%。这种N - 甲基化合物因其较强的亲脂性而对乳酸脱氢酶活性产生了重要影响,从而使分子具有更好的穿透力。在宿主肝脏中,观察到碱性和酸性磷酸酶活性下降。葡萄糖和糖原浓度也降低。超微结构研究显示幼虫的皮层发生改变,肌肉系统受损。实质组织紊乱。总之,用N - N - 苄基 - 甲基乙酰胺基乙酯处理多房棘球绦虫幼虫获得的这些生化和超微结构数据清楚地表明了乳酸脱氢酶活性在幼虫中的重要性。