Marinelli Sara, Pavone Flaminia, Luvisetto Siro
Institute of Biochemistry and Cellular Biology, National Research Council of Italy, via Ercole Ramarini 32, 00015 Monterotondo, Italy.
Toxins (Basel). 2025 Jul 28;17(8):374. doi: 10.3390/toxins17080374.
Botulinum neurotoxins (BoNTs) are known to inhibit synaptic transmission by targeting SNARE proteins, but their selectivity toward central excitatory and inhibitory pathways is not yet fully understood. In this study, the interaction of serotypes A (BoNT/A) and B (BoNT/B) with the glutamatergic and GABAergic systems has been investigated using a pharmacological approach in an animal model of inflammatory pain, i.e., the formalin test in mice. BoNTs were administered intracerebroventricularly, three days before testing, followed 15 min before testing by systemic administration of sub-analgesic doses of MK801, an NMDA receptor antagonist, or muscimol, a GABA_A receptor agonist. BoNT/A reduced the second phase of the formalin test without affecting both the first phase and the interphase, suggesting a selective action on excitatory glutamatergic circuits while sparing GABAergic inhibition. Co-administration of MK801 with BoNT/A did not enhance analgesia, and muscimol did not further reduce interphase, confirming preserved GABAergic transmission. In contrast, BoNT/B abolished the interphase, consistent with impaired GABA release. Co-administration of MK801 or muscimol with BoNT/B restored the interphase, indicating compensatory rebalancing of excitatory-inhibitory networks. These results demonstrate that BoNT/A and BoNT/B exert distinct effects on central neurotransmission and support the hypothesis that BoNT/A preferentially targets excitatory synapses, while BoNT/B targets inhibitory synapses. This work contributes to a deeper understanding of anti-inflammatory mechanisms of BoNTs and their selective interaction with central pain pathways.
肉毒杆菌神经毒素(BoNTs)已知通过靶向SNARE蛋白来抑制突触传递,但其对中枢兴奋性和抑制性通路的选择性尚未完全明确。在本研究中,利用炎性疼痛动物模型(即小鼠福尔马林试验),采用药理学方法研究了A型(BoNT/A)和B型(BoNT/B)肉毒杆菌神经毒素与谷氨酸能和γ-氨基丁酸能系统的相互作用。在测试前三天脑室内注射BoNTs,在测试前15分钟全身给予亚镇痛剂量的NMDA受体拮抗剂MK801或GABA_A受体激动剂蝇蕈醇。BoNT/A减少了福尔马林试验的第二阶段,而不影响第一阶段和中间阶段,表明其对兴奋性谷氨酸能回路有选择性作用,同时保留γ-氨基丁酸能抑制作用。MK801与BoNT/A联合给药并未增强镇痛效果,蝇蕈醇也未进一步减少中间阶段,证实γ-氨基丁酸能传递得以保留。相反,BoNT/B消除了中间阶段,这与γ-氨基丁酸释放受损一致。MK801或蝇蕈醇与BoNT/B联合给药恢复了中间阶段,表明兴奋性-抑制性网络的代偿性重新平衡。这些结果表明,BoNT/A和BoNT/B对中枢神经传递有不同影响,并支持以下假说:BoNT/A优先靶向兴奋性突触,而BoNT/B靶向抑制性突触。这项工作有助于更深入地了解BoNTs的抗炎机制及其与中枢疼痛通路的选择性相互作用。