Chen Su, Rong Yi, Liu Mengxue, Cheng Song, Liu Xiangming, Li Xiaohong, Yu Yi, Yang Guangzhong, Yang Xiaofei
Key Laboratory of Cognitive Science, Hubei Key Laboratory of Medical Information Analysis and Tumor Diagnosis & Treatment, Laboratory of Membrane Ion Channels and Medicine, College of Biomedical Engineering, South-Central University for Nationalities, Wuhan, China.
Gongqing Institute of Science and Technology, Gongqing, China.
Front Pharmacol. 2018 Nov 12;9:1302. doi: 10.3389/fphar.2018.01302. eCollection 2018.
Triterpenoid saponins from (TSS) are potential therapeutic agents because of its analgesic properties. However, the underlying mechanisms of the anti-nociceptive activity of TSS are largely unclear, especially in CNS. The present study confirmed the analgesic effect of TSS using four models of acute pain based on thermal or chemical stimuli. TSS treatment specifically impaired the threshold of thermal- and chemical-stimulated acute pain. Naloxone did not block the anti-nociceptive effects of TSS, which showed no participation of the opioid system. We investigated the electrical signal in cultured cortical neurons to explore whether TSS treatment directly affected synaptic transmission. TSS treatment selectively increased spontaneous inhibitory synaptic release and GABA induced charge transfer in mouse cortical neurons. The effects of TSS were maintained for at least 8 h in cultured neurons and in injected mice. Taken together, our results suggest that the analgesic role of TSS in cortex occurs via a particular increase in the inhibitory synaptic response at resting state, which supports TSS as a potential candidate for inflammatory pain relief.
来自[具体来源未提及]的三萜皂苷（TSS）因其镇痛特性而成为潜在的治疗药物。然而，TSS抗伤害感受活性的潜在机制在很大程度上尚不清楚，尤其是在中枢神经系统中。本研究使用基于热刺激或化学刺激的四种急性疼痛模型证实了TSS的镇痛作用。TSS处理特异性地降低了热刺激和化学刺激引起的急性疼痛阈值。纳洛酮并未阻断TSS的抗伤害感受作用，这表明阿片类系统未参与其中。我们研究了培养的皮质神经元中的电信号，以探讨TSS处理是否直接影响突触传递。TSS处理选择性地增加了小鼠皮质神经元中自发抑制性突触释放和GABA诱导的电荷转移。TSS的作用在培养的神经元和注射的小鼠中至少维持8小时。综上所述，我们的结果表明，TSS在皮质中的镇痛作用是通过静息状态下抑制性突触反应的特定增加而发生的，这支持TSS作为缓解炎性疼痛的潜在候选药物。
