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依达拉奉多种自由基清除活性的剂量依赖性。

Dose-dependency of multiple free radical-scavenging activity of edaravone.

作者信息

Tokumaru Osamu, Shuto Yachiko, Ogata Kazue, Kamibayashi Masato, Bacal Kira, Takei Hidehiro, Yokoi Isao, Kitano Takaaki

机构信息

Faculty of Welfare and Health Sciences, Oita University, Oita City, Oita Pref., Japan.

Department of Neurophysiology, Oita University Faculty of Medicine, Yufu City, Oita Pref., Japan; Nursing School, Beppu University, Beppu City, Oita Pref., Japan.

出版信息

J Surg Res. 2018 Aug;228:147-153. doi: 10.1016/j.jss.2018.03.020. Epub 2018 Apr 11.

Abstract

BACKGROUND

Edaravone is a powerful free radical scavenger that is in clinical use. However, data concerning its dose-response relationship against multiple free radicals remain sparse. The purpose of the present study was to demonstrate the dose-dependency of direct scavenging activity of edaravone against multiple free radical species.

MATERIALS AND METHODS

Free radical-scavenging activities of edaravone against six free radical species were evaluated by electron spin resonance spectroscopy using spin-trapping method.

RESULTS

Edaravone scavenged the following free radicals in dose-dependent manners with reaction rate constants (k) or 50% inhibitory concentration (IC) as indicated: hydroxyl radical (k = 5.2 × 10 M s), superoxide anion (k/k = 0.63), tert-butyl peroxyl radical (k/k = 8.8), ascorbyl free radical (IC = 0.17 ± 0.06 mM), 2,2-diphenyl-1-picrylhydrazyl (DPPH, IC = 4.7 ± 0.3 μM), and nitric oxide (k = 7.0 × 10 M s).

CONCLUSIONS

The dose-dependent scavenging activities of edaravone against multiple free radical species were clearly illustrated. It is speculated that edaravone acts as antioxidant by dose-dependently scavenging multiple free radical species along the chain reactions of oxidative stress in surgery.

摘要

背景

依达拉奉是一种临床上使用的强效自由基清除剂。然而,关于其对多种自由基的剂量反应关系的数据仍然稀少。本研究的目的是证明依达拉奉对多种自由基的直接清除活性的剂量依赖性。

材料与方法

采用自旋捕获法,通过电子自旋共振光谱评估依达拉奉对六种自由基的自由基清除活性。

结果

依达拉奉以剂量依赖性方式清除以下自由基,反应速率常数(k)或50%抑制浓度(IC)如下所示:羟基自由基(k = 5.2×10 M s)、超氧阴离子(k/k = 0.63)、叔丁基过氧自由基(k/k = 8.8)、抗坏血酸自由基(IC = 0.17±0.06 mM)、2,2-二苯基-1-苦基肼(DPPH,IC = 4.7±0.3 μM)和一氧化氮(k = 7.0×10 M s)。

结论

依达拉奉对多种自由基的剂量依赖性清除活性得到了清晰的说明。推测依达拉奉通过在手术氧化应激的链式反应中剂量依赖性地清除多种自由基而发挥抗氧化作用。

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