Beske Phillip H, Bradford Aaron B, Grynovicki Justin O, Glotfelty Elliot J, Hoffman Katie M, Hubbard Kyle S, Tuznik Kaylie M, McNutt Patrick M
Cellular and Molecular Biology Branch, Research Division, United States Army Medical Research Institute of Chemical Defense, Aberdeen Proving Ground, Maryland.
Cellular and Molecular Biology Branch, Research Division, United States Army Medical Research Institute of Chemical Defense, Aberdeen Proving Ground, Maryland
Toxicol Sci. 2016 Feb;149(2):503-15. doi: 10.1093/toxsci/kfv254. Epub 2015 Nov 28.
Clinical manifestations of tetanus and botulism result from an intricate series of interactions between clostridial neurotoxins (CNTs) and nerve terminal proteins that ultimately cause proteolytic cleavage of SNARE (soluble N-ethylmaleimide-sensitive factor attachment protein receptor) proteins and functional blockade of neurotransmitter release. Although detection of cleaved SNARE proteins is routinely used as a molecular readout of CNT intoxication in cultured cells, impaired synaptic function is the pathophysiological basis of clinical disease. Work in our laboratory has suggested that the blockade of synaptic neurotransmission in networked neuron cultures offers a phenotypic readout of CNT intoxication that more closely replicates the functional endpoint of clinical disease. Here, we explore the value of measuring spontaneous neurotransmission frequencies as novel and functionally relevant readouts of CNT intoxication. The generalizability of this approach was confirmed in primary neuron cultures as well as human and mouse stem cell-derived neurons exposed to botulinum neurotoxin serotypes A-G and tetanus neurotoxin. The sensitivity and specificity of synaptic activity as a reporter of intoxication was evaluated in assays representing the principal clinical and research purposes of in vivo studies. Our findings confirm that synaptic activity offers a novel and functionally relevant readout for the in vitro characterizations of CNTs. They further suggest that the analysis of synaptic activity in neuronal cell cultures can serve as a surrogate for neuromuscular paralysis in the mouse lethal assay, and therefore is expected to significantly reduce the need for terminal animal use in toxin studies and facilitate identification of candidate therapeutics in cell-based screening assays.
破伤风和肉毒中毒的临床表现源于梭菌神经毒素(CNTs)与神经末梢蛋白之间一系列复杂的相互作用,这些相互作用最终导致可溶性N - 乙基马来酰亚胺敏感因子附着蛋白受体(SNARE)蛋白的蛋白水解裂解以及神经递质释放的功能阻断。尽管检测裂解的SNARE蛋白通常被用作培养细胞中CNT中毒的分子读数,但突触功能受损是临床疾病的病理生理基础。我们实验室的研究表明,在联网神经元培养物中突触神经传递的阻断提供了一种CNT中毒的表型读数,它更紧密地复制了临床疾病的功能终点。在这里,我们探讨测量自发神经传递频率作为CNT中毒的新型且功能相关读数的价值。在原代神经元培养物以及暴露于A - G型肉毒杆菌神经毒素和破伤风神经毒素的人及小鼠干细胞衍生神经元中证实了这种方法的普遍性。在代表体内研究主要临床和研究目的的试验中评估了突触活动作为中毒报告指标的敏感性和特异性。我们的研究结果证实,突触活动为CNTs的体外表征提供了一种新型且功能相关的读数。它们进一步表明,神经元细胞培养物中突触活动的分析可以作为小鼠致死试验中神经肌肉麻痹的替代指标,因此有望显著减少毒素研究中终末动物的使用需求,并促进基于细胞的筛选试验中候选治疗药物的鉴定。