Cunha V M, Noël F
Departamento de Farmacologia Básica e Clínica, Instituto de CiênciasBiomédicas, Universidade Federal do Rio de Janeiro, Brazil.
Life Sci. 1997;60(20):PL 289-94. doi: 10.1016/s0024-3205(97)00144-6.
Therapeutic concentrations of praziquantel produce a rapid and intense contraction of the human flatworm Schistosoma mansoni. As an action on ATPases responsible for calcium homeostasis arises as a possible explanation for the molecular mechanism of this effect, we tested here the effect of praziquantel on different preparations from male adult worms that were previously characterized for their content in (Na(+)+K+)-ATPase and (Ca2(+)-Mg2+)ATPase activities from different origins. Concentrations as high as 100 microM praziquantel did not inhibit (Na(+)+K+)-ATPase from tegument and carcass nor (Ca2(+)-Mg2+)ATPase from heterogeneous (P1) and microsomal (P4) fractions. As 100 microM praziquantel was also without effect on calcium permeability of microsomal vesicles actively loaded with 45Ca2+, the present results discard three hypotheses recently raised for the mechanism of praziquantel-induced contraction of S. mansoni.
吡喹酮的治疗浓度可使人体扁虫曼氏血吸虫迅速且强烈地收缩。由于对负责钙稳态的ATP酶的作用可能是这种效应分子机制的一种解释,我们在此测试了吡喹酮对雄性成虫不同制剂的影响,这些制剂先前已根据其来自不同来源的(Na⁺ + K⁺)-ATP酶和(Ca²⁺ - Mg²⁺)ATP酶活性的含量进行了表征。高达100微摩尔的吡喹酮浓度既不抑制来自体表和虫体的(Na⁺ + K⁺)-ATP酶,也不抑制来自异质(P1)和微粒体(P4)组分的(Ca²⁺ - Mg²⁺)ATP酶。由于100微摩尔的吡喹酮对主动装载有⁴⁵Ca²⁺的微粒体囊泡的钙通透性也没有影响,目前的结果摒弃了最近提出的关于吡喹酮诱导曼氏血吸虫收缩机制的三种假设。