V. Kenche, C. Tumpach, K. Barnham
2013
Citations
0
Influential Citations
2
Citations
Journal
Oxidants and Antioxidants in Medical Science
Abstract
The compound 4-{[(4-hydroxyphenyl)amino]methyl}-2,6-di-tert-butylphenol (TRS1) was developed using a “mix-and-match” drug design approach for antioxidant-based neuroprotection and therapy. The commonly-used antipyretic drug, paracetamol, which is also found to act as a mild anti-inflammatory, was further modified by attaching a radical scavenger moiety to design a bifunctional bioactive molecule. Using a cell-free 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical reduction assay, and a 2',7'-dichlorofluorescein (DCFH) oxidation assay in cultured N2a mouse neuroblastoma and SH-SY5Y human neuroblastoma cells exposed to oxidative insult (serum deprivation), the radical scavenging ability of TRS1 was found to be comparable with other well-studied antioxidants such as Trolox. The maintenance of antioxidant action of this compound in cells suggests this avenue and other multi-targeted drug discovery paradigms may provide potential therapeutic strategies for targeting complicated neurodegenerative conditions.