Dan N, Li X J, Zhao B L, Zhang T M, Xin W J
Zhongguo Yao Li Xue Bao. 1989 Sep;10(5):443-7.
Probimane, dl-1,2-bis (4-morpholine-methyl-3, 5-dioxopiperazin-1-yl) propane, is a new antitumor agent synthesized by Shanghai Institute of Materia Medica, Chinese Academy of Sciences. The scavenging effects of probimane on active oxygen radicals produced in 3 different systems were studied with the ESR spin trapping methods. In Fenton's reaction, probimane remarkably scavenged hydroxyl radicals (.OH) and the rate of scavenging .OH by probimane 0.05 mmol/L was 47%, compared to 5% by vitamin E (VE) and 30% by ascorbic acid (AA). In irradiation riboflavin system, in which superoxide (O2-.) was produced, the agent also had the scavenging effects on O2(-.). The rate of scavenging O2-. by probimane 0.05 mmol/L was 13%, higher than that by VE (7%) but lower than that by AA (90%). In cell system where the active oxygen radicals were produced during the respiratory burst of human neutrophils (Neu) stimulated by TPA (tetradecanoylphorbol acetate), probimane exhibited a dose-dependent scavenging action on the radicals. The rate of the radical scavenging by probimane 0.05 mmol/L was 37%, much higher than that by VE (9%) but lower than that by AA (68%). Probimane had no effect on the rate of oxygen consumption by human Neu, measured with spin probe oxymetry.
丙亚胺,即dl-1,2-双(4-吗啉甲基-3,5-二氧代哌嗪-1-基)丙烷,是中国科学院上海药物研究所合成的一种新型抗肿瘤药物。采用电子自旋共振(ESR)自旋捕集法研究了丙亚胺对3种不同体系中产生的活性氧自由基的清除作用。在芬顿反应中,丙亚胺能显著清除羟基自由基(·OH),0.05 mmol/L丙亚胺对·OH的清除率为47%,相比之下,维生素E(VE)为5%,抗坏血酸(AA)为30%。在产生超氧阴离子(O2-·)的核黄素光照体系中,该药物对O2-·也有清除作用。0.05 mmol/L丙亚胺对O2-·的清除率为13%,高于VE(7%)但低于AA(90%)。在由十四酰佛波醇乙酸酯(TPA)刺激人中性粒细胞(Neu)呼吸爆发过程中产生活性氧自由基的细胞体系中,丙亚胺对自由基表现出剂量依赖性的清除作用。0.05 mmol/L丙亚胺对自由基的清除率为37%,远高于VE(9%)但低于AA(68%)。用自旋探针测氧法测定,丙亚胺对人中性粒细胞的耗氧率无影响。