Department of Bacteriology, University of Wisconsin, Madison, WI 53706, USA.
Curr Top Microbiol Immunol. 2013;364:257-85. doi: 10.1007/978-3-642-33570-9_12.
Botulinum neurotoxins (BoNTs) are the most potent human toxins known and the causative agent of botulism, and are widely used as valuable pharmaceuticals. The BoNTs are modular proteins consisting of a heavy chain and a light chain linked by a disulfide bond. Intoxication of neuronal cells by BoNTs is a multi-step process including specific cell binding, endocytosis, conformational change in the endosome, translocation of the enzymatic light chain into the cells cytosol, and SNARE target cleavage. The quantitative and reliable potency determination of fully functional BoNTs produced as active pharmaceutical ingredient (API) requires an assay that considers all steps in the intoxication pathway. The in vivo mouse bioassay has for years been the 'gold standard' assay used for this purpose, but it requires the use of large numbers of mice and thus causes associated costs and ethical concerns. Cell-based assays are currently the only in vitro alternative that detect fully functional BoNTs in a single assay and have been utilized for years for research purposes. Within the last 5 years, several cell-based BoNT detection assays have been developed that are able to quantitatively determine BoNT potency with similar or greater sensitivity than the mouse bioassay. These assays now offer an alternative method for BoNT potency determination. Such quantitative and reliable BoNT potency determination is a crucial step in basic research, in the development of pharmaceutical BoNTs, and in the quantitative detection of neutralizing antibodies.
肉毒神经毒素(BoNTs)是已知最有效的人类毒素,也是肉毒中毒的病原体,被广泛用作有价值的药物。BoNTs 是由重链和轻链通过二硫键连接而成的模块化蛋白质。BoNTs 使神经元细胞中毒是一个多步骤的过程,包括特异性细胞结合、内吞作用、内体中的构象变化、酶轻链向细胞胞质溶胶的易位以及 SNARE 靶标切割。作为活性药物成分(API)生产的具有完全功能的 BoNTs 的定量和可靠效力测定需要考虑中毒途径中所有步骤的测定。体内小鼠生物测定法多年来一直是为此目的使用的“金标准”测定法,但它需要使用大量的小鼠,因此会引起相关的成本和道德问题。基于细胞的测定法是目前唯一可在单次测定中检测到具有完全功能的 BoNTs 的体外替代方法,并且多年来一直用于研究目的。在过去的 5 年中,已经开发出几种基于细胞的 BoNT 检测测定法,这些测定法能够以与小鼠生物测定法相似或更高的灵敏度定量测定 BoNT 效力。这些测定法现在为 BoNT 效力测定提供了替代方法。这种定量和可靠的 BoNT 效力测定是基础研究、药物 BoNTs 开发以及中和抗体定量检测的关键步骤。