Bi Wei, Cai Jianhui, Xue Ping, Zhang Yanrong, Liu Sanguang, Gao Xiang, Li Meng, Wang Zhibo, Baudy-Floc'h Michèle, Green Sarah A, Bi Lanrong
Department of Surgery, Second Hospital of HeBei Medical University, Shijiazhuang 050000, PR China.
Bioorg Med Chem Lett. 2008 Mar 15;18(6):1788-94. doi: 10.1016/j.bmcl.2008.02.030. Epub 2008 Feb 16.
Stable nitroxides are potential antioxidant drugs. In this study, we have linked nitroxide to natural amino acids with the aim to improve therapeutic activity. The radical scavenging activities of two nitronyl nitroxide-amino acid conjugates (NNR and NNK) were evaluated in PC 12 cell survival assays. The NO scavenging activities of these compounds were confirmed in the acetylcholine-induced vasorelaxation assay. In addition, the protective effect of NNR was demonstrated in an in vivo rat model of hepatic ischemia-reperfusion (I/R) induced injury and oxidative change. Because NNR reduced hepatic I/R injury by minimizing oxidative stress, it might be possible to develop it into a possible therapeutic agent for hepatic I/R injury.
稳定的氮氧化物是潜在的抗氧化药物。在本研究中,我们将氮氧化物与天然氨基酸相连,旨在提高治疗活性。在PC 12细胞存活试验中评估了两种硝酮氮氧化物 - 氨基酸共轭物(NNR和NNK)的自由基清除活性。在乙酰胆碱诱导的血管舒张试验中证实了这些化合物的NO清除活性。此外,在肝缺血再灌注(I/R)诱导的损伤和氧化变化的体内大鼠模型中证明了NNR的保护作用。由于NNR通过最小化氧化应激减轻了肝I/R损伤,因此有可能将其开发成肝I/R损伤的潜在治疗剂。