Moretto M B, Franco J, Posser T, Nogueira C W, Zeni G, Rocha J B T
Departamento de Análises Clínicas e Toxicológicas, Centro de Ciências da Saúde, Universidade Federal de Santa Maria, Santa Maria, Brazil.
Neurochem Res. 2004 Oct;29(10):1801-6. doi: 10.1023/b:nere.0000042205.08917.f2.
The goal of this study was to investigate the isolated and combined effect of ebselen and Hg2+ on calcium influx and on glutamatergic system. We examined the in vitro effects of 2 phenyl-1,2-benzisoselenazol-3(2H)-ona), (Ebselen) on 45Ca2+ influx in synaptosomes of rat at rest and during depolarization and glutamate uptake into synaptosomes. Entry of 45Ca was measured during exposure to mercury in non-depolarizing and depolarizing solutions. Ebselen abolished the inhibition of 45Ca2+ influx on non-depolarizing conditions; however, ebselen did no modify inhibition uptake of 45Ca2+ caused by Hg2+ in high K+ depolarizing medium. Ebselen did not modify glutamate uptake inhibition caused by Hg2+ in synaptosomes. These results indicate that ebselen has an in vitro protective effect against Hg2+ induced inhibition of Ca2+ influx into synaptosomes, depending on the depolarizing conditions of the assay. The effects of Hg2+ on glutamate uptake were not modified by ebselen, suggesting that its protection is dependent on the target protein considered.
本研究的目的是探讨依布硒啉和Hg2+对钙内流和谷氨酸能系统的单独及联合作用。我们研究了2-苯基-1,2-苯并异硒唑-3(2H)-酮(依布硒啉)对大鼠突触体在静息和去极化状态下45Ca2+内流以及对突触体摄取谷氨酸的体外作用。在非去极化和去极化溶液中暴露于汞期间测量45Ca的进入。依布硒啉消除了非去极化条件下对45Ca2+内流的抑制;然而,依布硒啉并未改变高钾去极化培养基中Hg2+引起的45Ca2+摄取抑制。依布硒啉未改变Hg2+引起的突触体中谷氨酸摄取抑制。这些结果表明,依布硒啉在体外对Hg2+诱导的突触体钙内流抑制具有保护作用,这取决于测定的去极化条件。依布硒啉未改变Hg2+对谷氨酸摄取的影响,表明其保护作用取决于所考虑的靶蛋白。