Martini L H, Souza C R, Marques P B, Calixto J B, Yunes R A, Souza D O
Departamento de Bioquímica, Instituto de Ciências Básicas da Saúde, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.
Neurochem Res. 2000 Feb;25(2):211-5. doi: 10.1023/a:1007567302504.
Glutamate is to be considered a nociceptive neurotransmitter and glutamatergic antagonists present antinoceptive activity. In this study we investigated the effects of the naturally occurring antinociceptive compounds rutin, geraniin and quercetine extracted from Phyllanthus, as well as the diterpene jatrophone, extracted from Jatropha elliptica on the binding of [3H]glutamate and [3H]GMP-PNP [a GTP analogue which binds to extracellular site(s), modulating the glutamatergic transmission] in rat brain membrane. Jatrophone inhibited [3H]glutamate binding and geraniin inhibited [3H]GMP-PNP binding. Quercetine inhibited the binding of both ligands. These results may indicate a neurochemical parameter possibly related to the antinoceptive activity of these natural compounds.
谷氨酸被认为是一种伤害性感受神经递质,谷氨酸能拮抗剂具有抗伤害感受活性。在本研究中,我们研究了从叶下珠中提取的天然抗伤害感受化合物芦丁、老鹳草素和槲皮素,以及从椭圆叶麻风树中提取的二萜麻风树酮对大鼠脑膜中[3H]谷氨酸和[3H]GMP-PNP(一种与细胞外位点结合、调节谷氨酸能传递的GTP类似物)结合的影响。麻风树酮抑制[3H]谷氨酸结合,老鹳草素抑制[3H]GMP-PNP结合。槲皮素抑制两种配体的结合。这些结果可能表明一个与这些天然化合物的抗伤害感受活性可能相关的神经化学参数。