A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox

作者：Kamogawa Erisa; Sueishi Yoshimi^*

来源：Bioorganic & Medicinal Chemistry Letters, 2014, 24(5): 1376-1379.

DOI：10.1016/j.bmcl.2014.01.045

• Edaravone
• Multiple free radical scavenging (MULTIS)
• ESR spin trapping
• Uric acid
• Glutathione

Edaravone (3-methyl-1-phenyl-2-pyrazoline-5-one) is a neuroprotective drug that has been used for brain ischemia injury treatment. Because its activity is speculated to be due to free radical scavenging activity, we carried out a quantitative determination of edaravone's free radical scavenging activity against multiple free radical species. Electron spin resonance (ESR) spin trapping-based multiple freeradical scavenging (MULTIS) method was employed, where target free radicals were hydroxyl radical, superoxide anion, alkoxyl radical, alkylperoxyl radical, methyl radical, and singlet oxygen. Edaravone showed relatively high scavenging abilities against hydroxyl radical (scavenging rate constant k = 2.98 x 10(11) M-1 s(-1)), singlet oxygen (k = 2.75 x 10(7) M-1 s(-1)), and methyl radical (k = 3.00 x 10(7) M-1 s(-1)). Overall, edaravone's scavenging activity against multiple free radical species is as robust as other known potent antioxidant such as uric acid, glutathione, and trolox. A radar chart illustration of the MULTIS activity relative to uric acid, glutathione, and trolox indicates that edaravone has a high and balanced antioxidant activity with low specificity.

• 出版日期2014-3-1