Department of Pharmacology, School of Pharmacy, The Fourth Military Medical University, Xi'an, Shaanxi Province 710032, PR China.
Neurotoxicology. 2013 Jan;34:219-25. doi: 10.1016/j.neuro.2012.09.009. Epub 2012 Sep 26.
Cytisine (CYT), one of the principal bioactive components derived from the seeds of Cytisus laborinum L, has been widely used for central nervous system (CNS) diseases treatment. The present study investigated the protective effect of CYT on cultured cortical neural injury induced by N-methyl-d-aspartate (NMDA). Our data showed that CYT conferred protective effect against loss of cellular viability induced by brief exposure to 200 μM NMDA in a concentration-dependent manner. CYT significantly inhibited the neuronal apoptosis induced by NMDA exposure by reversing intracellular Ca(2+) overload and balancing Bcl-2 and Bax expression levels. Furthermore, CYT significantly reversed the up-regulation of GluN2B-containing NMDA receptors by exposure to NMDA, but it did not affect the level of GluN2A-containing NMDA receptors. These findings suggest that CYT protects cortical neurons, at least partially, by inhibiting the level of GluN2B-containing NMDA receptors and regulating Bcl-2 family.
野靛碱（CYT）是从黎豆种子中提取的主要生物活性成分之一，已广泛用于治疗中枢神经系统（CNS）疾病。本研究探讨了 CYT 对 N-甲基-D-天冬氨酸（NMDA）诱导的培养皮质神经元损伤的保护作用。我们的数据表明，CYT 以浓度依赖的方式对短暂暴露于 200μM NMDA 引起的细胞活力丧失具有保护作用。CYT 通过逆转细胞内 Ca（2+）超载和平衡 Bcl-2 和 Bax 表达水平，显著抑制 NMDA 暴露引起的神经元凋亡。此外，CYT 显著逆转了 NMDA 暴露引起的 GluN2B 型 NMDA 受体的上调，但不影响 GluN2A 型 NMDA 受体的水平。这些发现表明，CYT 通过抑制 GluN2B 型 NMDA 受体的水平和调节 Bcl-2 家族来保护皮质神经元，至少部分如此。
