Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370362 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
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.
Graphical abstractNovel mercaptoethylleonurine and mercaptoethylguanidine derivatives were designed, synthesized, and evaluated for their neuroprotective effects on H2O2-induced apoptosis in human SH-SY5Y cells, and the mechanism of compound 8k was studied.Figure optionsDownload full-size imageDownload as PowerPoint slide