Fang Haiyang, Yue Rongcai, Ga Yang, Zhang Yi, Shan Lei, Zhao Jing
Department of Mathematics, Logistical Engineering University, Chongqing, China.
Department of Natural Medicinal Chemistry, Second Military Medical University, Shanghai, China; School of Pharmacy, Shanghai Jiao Tong University, Shanghai, China.
PLoS One. 2015 May 8;10(5):e0124632. doi: 10.1371/journal.pone.0124632. eCollection 2015.
Ischemic stroke is the third leading cause of death in the world. Our previous study found that cynandione A (CYNA), the main component from the root of Cynanchum bungei, exhibits anti-ischemic stroke activity. In this work, we investigated the therapeutic mechanisms of CYNA to ischemic stroke at protein network level. First, PC12 cells and cerebellar granule neurons were prepared to validate the effects of CYNA against glutamate injury. Our experiments suggested that CYNA could dose-dependently mitigate glutamate-induced neurons neurotoxicity and inhibit glutamate-induced upregulation of KHSRP and HMGB1, further confirming the neuroprotective effects of CYNA in vivo. Then, on the pathway sub-networks, which present biological processes that can be impacted directly or in periphery nodes by drugs via their targets, we found that CYNA regulates 11 pathways associated with the biological process of thrombotic or embolic occlusion of a cerebral artery. Meanwhile, by defining a network-based anti-ischemic stroke effect score, we showed that CYNA has a significantly higher effect score than random counterparts, which suggests a synergistic effect of CYNA to ischemic stroke. This study may shed new lights on the study of network based pharmacology.
缺血性中风是全球第三大致死原因。我们之前的研究发现,白首乌根中的主要成分白首乌二苯乙烯苷A(CYNA)具有抗缺血性中风活性。在这项研究中,我们在蛋白质网络水平上研究了CYNA对缺血性中风的治疗机制。首先,制备PC12细胞和小脑颗粒神经元以验证CYNA对谷氨酸损伤的作用。我们的实验表明,CYNA可以剂量依赖性地减轻谷氨酸诱导的神经元神经毒性,并抑制谷氨酸诱导的KHSRP和HMGB1上调,进一步证实了CYNA在体内的神经保护作用。然后,在通路子网(其呈现可通过药物靶点直接或在外围节点受到影响的生物学过程)上,我们发现CYNA调节与脑动脉血栓形成或栓塞闭塞生物学过程相关的11条通路。同时,通过定义基于网络的抗缺血性中风效应评分,我们表明CYNA的效应评分明显高于随机对照,这表明CYNA对缺血性中风具有协同作用。本研究可能为基于网络的药理学研究提供新的思路。