Bioorganic & Medicinal Chemistry Letters 2013-03-15

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

Zhao-Lin Que, Wen-Jiang Zhou, Jun Chang, Xin-Hua Liu, Jian-Ming Yu, Xun Sun

文献索引：Bioorg. Med. Chem. Lett. 23(6) , 1793-6, (2013)

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摘要

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.Copyright © 2013 Elsevier Ltd. All rights reserved.