Puttachary Sreekanth, Robertson Alan P, Clark Cheryl L, Martin Richard J
Department of Biomedical Sciences, Iowa State University, Ames, IA 50011-1250, USA.
Mol Biochem Parasitol. 2010 May;171(1):8-16. doi: 10.1016/j.molbiopara.2009.12.006. Epub 2010 Jan 11.
Resistance to antinematodal drugs like levamisole has increased and there is a need to understand what factors affect the responses to these anthelmintics. In our previous study, we examined the role of ryanodine receptors in muscle contraction pathways. Here we have examined interactions of levamisole receptors, ryanodine receptors (RyRs), the excitatory neuropeptide AF2, and coupling to electrophysiological responses. We examined the effects of a brief application of levamisole on Ascaris suum body muscle under current-clamp. The levamisole responses were characterized as an initial primary depolarization, followed by a slow secondary depolarizing response. We examined the effects of AF2 (KHEYLRFamide), 1 microM applied for 2 min. We found that AF2 potentiated the secondary response to levamisole and had no significant effect on the primary depolarization. Further, the reversal potentials observed during the secondary response suggested that more than one ion was involved in producing this potential. AF2 potentiated the secondary response in the presence of 30 microM mecamylamine suggesting the effect was independent of levamisole sensitive acetylcholine receptors. The secondary response, potentiated by AF2, appeared to be dependent on cytoplasmic events triggered by the primary depolarization. Ion-substitution experiments showed that the AF2 potentiated secondary response was dependent on extracellular calcium and chloride suggesting a role for the calcium-activated anion channel. Caffeine mimicked the AF2 potentiated secondary response and 0.1 microM ryanodine inhibited it. 1.0 microM ryanodine increased spiking showing that it affected membrane excitability. A model is proposed showing ryanodine receptors mediating effects of AF2 on levamisole responses.
对左旋咪唑等抗线虫药物的耐药性有所增加,因此有必要了解哪些因素会影响对这些驱虫药的反应。在我们之前的研究中,我们研究了兰尼碱受体在肌肉收缩途径中的作用。在此,我们研究了左旋咪唑受体、兰尼碱受体(RyRs)、兴奋性神经肽AF2之间的相互作用,以及它们与电生理反应的偶联。我们在电流钳制下研究了短暂应用左旋咪唑对猪蛔虫体肌的影响。左旋咪唑反应的特征是初始的初级去极化,随后是缓慢的次级去极化反应。我们研究了AF2(KHEYLRFamide)在1 μM浓度下作用2分钟的效果。我们发现AF2增强了对左旋咪唑的次级反应,而对初级去极化没有显著影响。此外,在次级反应期间观察到的反转电位表明,不止一种离子参与了该电位的产生。在存在30 μM美加明的情况下,AF2增强了次级反应,这表明该效应独立于对左旋咪唑敏感的乙酰胆碱受体。由AF2增强的次级反应似乎依赖于初级去极化触发的细胞质事件。离子替代实验表明,AF2增强的次级反应依赖于细胞外钙和氯,这表明钙激活阴离子通道发挥了作用。咖啡因模拟了AF2增强的次级反应,而0.1 μM的兰尼碱抑制了该反应。1.0 μM的兰尼碱增加了动作电位发放,表明它影响了膜兴奋性。我们提出了一个模型,显示兰尼碱受体介导AF2对左旋咪唑反应的影响。