Neuroprotective effects of mercaptoethylleonurine and mercaptoethylguanidine analogs on hydrogen peroxide-induced apoptosis in human neuronal SH-SY5Y cells

作者：Que, Zhao-Lin; Zhou, Wen-Jiang; Chang, Jun^*; Liu, Xin-Hua; Yu, Jian-Ming; Sun, Xun

来源：Bioorganic & Medicinal Chemistry Letters, 2013, 23(6): 1793-1796.

DOI：10.1016/j.bmcl.2013.01.038

• Mercaptoethylleonurine
• Mercaptoethylguanidine
• Neuroprotective effect
• SH-SY5Y cell

A series of mercaptoethylleonurine and mercaptoethylguanidine derivatives were designed and synthesized. Their neuroprotective effects toward H2O2-induced apoptosis were investigated in human SH-SY5Y cells. The results from these studies identified several potent compounds, with compound 8k emerging as the most effective. Further investigation demonstrated that 8k reduced H2O2-induced activation of mitochondrial apoptosis by inhibiting the expression of Bax and elevating the expression of Bcl-2. Moreover, the molecular mechanism underlying the observed neuroprotective effects of 8k was exerted via the Akt and JNK pathways. Compound 8k can be a lead compound for further discovery of neuroprotective medicine.

• 出版日期2013-3-15
• 单位复旦大学