Kojima S, Iizuka H, Yamaguchi H, Tanuma S, Kochi M, Ueno Y
Research Institute for Biosciences, Science University of Tokyo, Chiba, Japan.
Anticancer Res. 1994 Sep-Oct;14(5A):1875-80.
The in vitro antioxidative activity of benzylideneascorbate (SBA) and the in vivo effect on adriamycin (ADR)-induced cardiotoxicity in a mouse model were investigated. The radical-scavenging activity of SBA was assayed in terms of reduction of chemiluminescence induced by O2-, generated in xanthine/xanthine oxidase and macrophage/phorbol myristate acetate reaction systems. SBA showed a strong antioxidative activity (IC50 = 3 to 4 microM) in both assay systems, though its activity was weaker than that of ascorbic acid (Asc). In the assay of the antioxidative activity against auto-oxidation of linolenic acid, SBA was stable and retained its potency for a long period of time in comparison with Asc, 6-palmitoylascorbic acid (6-P-Asc) and cysteamine (CysNH2). Electron spin resonance examination indicated that SBA strongly scavenged both superoxide anion and hydroxy radical. The in vivo protective effect of SBA against ADR-induced cardiotoxicity, in which active oxygen radicals play a role, was examined. The serum creatine phosphokinase activity, a parameter of cardiotoxicity, was remarkably increased from the 3rd day until the 4th day after ADR treatment. This elevation was significantly suppressed by SBA treatment, whereas Asc, 6-P-Asc and CysNH2 were ineffective. SBA could have clinical potential for the treatment of diabetes and other disorders in which active oxygen species play a pathogenic role.
研究了亚苄基抗坏血酸（SBA）的体外抗氧化活性及其对阿霉素（ADR）诱导的小鼠模型心脏毒性的体内影响。通过检测在黄嘌呤/黄嘌呤氧化酶和巨噬细胞/佛波酯肉豆蔻酸酯反应体系中产生的O2-诱导的化学发光的降低来测定SBA的自由基清除活性。在两个检测体系中，SBA均表现出较强的抗氧化活性（IC50 = 3至4 microM），尽管其活性比抗坏血酸（Asc）弱。在亚麻酸自动氧化的抗氧化活性检测中，与Asc、6-棕榈酰抗坏血酸（6-P-Asc）和半胱胺（CysNH2）相比，SBA稳定且能长时间保持其效力。电子自旋共振检测表明，SBA能强烈清除超氧阴离子和羟基自由基。研究了SBA对ADR诱导的心脏毒性的体内保护作用，其中活性氧自由基起作用。作为心脏毒性参数的血清肌酸磷酸激酶活性在ADR治疗后第3天至第4天显著升高。SBA治疗可显著抑制这种升高，而Asc、6-P-Asc和CysNH2则无效。SBA在治疗糖尿病和其他活性氧起致病作用的疾病方面可能具有临床潜力。
