Hatanaka Masashi, Nishizawa Chiho, Kakinoki Tomohiro, Takahashi Kyoko, Nakamura Shigeo, Mashino Tadahiko
Keio University, Faculty of Pharmacy, Department of Pharmaceutical Sciences, Shibakoen 1-5-30, Minato-ku 105-8512, Tokyo, Japan.
Bioorg Med Chem Lett. 2008 Oct 1;18(19):5290-3. doi: 10.1016/j.bmcl.2008.08.057. Epub 2008 Sep 12.
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.
以2,2'-吡啶二醇（1,1,2-二(2-吡啶基)-1,2-乙烯二醇）及其合成衍生物作为强效抗氧化烯二醇的先导化合物，在HL-60细胞体系上评估了它们对氧化应激的保护作用。2,2'-吡啶二醇对HL-60细胞无显著细胞毒性作用。衍生物1、2、3、5和6比抗坏血酸更显著地抑制H(2)O(2)诱导的细胞死亡和细胞内氧化应激。由于2,2'-吡啶二醇在质子溶剂中会被氧化为二酮，即2,2'-吡啶二酮，因此也研究了2,2'-吡啶二酮的抗氧化活性。2,2'-吡啶二酮在细胞中表现出抗氧化活性；然而，其活性低于2,2'-吡啶二醇。这些结果表明，2,2'-吡啶二醇衍生物可能是对抗氧化应激的良好细胞保护剂。
