2,2′-Pyridoin derivatives protect HL-60 cells against oxidative stress

Keio University, Faculty of Pharmacy, Department of Pharmaceutical Sciences, Shibakoen 1-5-30, Minato-ku 105-8512, Tokyo, Japan.
Bioorganic & medicinal chemistry letters (Impact Factor: 2.42). 10/2008; 18(19):5290-3. DOI: 10.1016/j.bmcl.2008.08.057
Source: PubMed


Focusing on 2,2'-pyridoin (1, 1,2-di(2-pyridyl)-1,2-ethenediol) and its synthetic derivatives as the lead compound of the potent antioxidative enediol, their protective effect against oxidative stress was evaluated on the HL-60 cell system. 2,2'-Pyridoins showed no remarkable cytotoxic effect on HL-60 cells. The derivatives 1, 2, 3, 5, and 6 inhibited H(2)O(2)-induced cell death and intracellular oxidative stress more significantly than ascorbic acid. Since 2,2'-pyridoins are oxidized to the diketones, 2,2'-pyridils, in a protic solvent, the antioxidant activity of 2,2'-pyridils was also investigated. 2,2'-Pyridils showed antioxidant activity in the cell; however, the activity was lower than that of 2,2'-pyridoins. These results suggested that 2,2'-pyrdoin derivatives can be good cytoprotective agents against oxidative stress.

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