Reactive oxygen species generation through NADH oxidation by pterin derivatives.

Pterin is an electron transfer compound in biological systems. Among the analogs, 6-formylpterin (6FP) has been demonstrated to have many marked physiological and pharmacological activities. In previous study, we have elucidated that 6FP derivatives in which the 3-position is modified possess reactive oxygen species (ROS), which are involved in the modulation of a variety of cell functions, generation activities through the oxidation of NADH to NAD(+) in the dark at neutral pH. In the present study, we have demonstrated that the ROS generation activity by 6FP derivative is enhanced in the presence of 3-methyl-1-phenyl-2-pyrazolin-5-one. In this reaction, 3-methyl-1-phenyl-2-pyrazolin-5-one is reacted with the formyl group on the 6-position of 6FP derivative to give the activated product. The present results would be helpful for designing pharmaceutical ROS generation system in vivo.