Liu Yuh-Hwa, Wu Wen-Chun, Lu Yeh-Lin, Lai Ying-Jang, Hou Wen-Chi
Division of Gastroenterology, Shin Kong Wu Ho-Su Memorial Hospital, Taipei, Taiwan.
Biosci Biotechnol Biochem. 2010;74(6):1256-60. doi: 10.1271/bbb.100096. Epub 2010 Jun 7.
Hydroxyurea (HU, NH(2)CONHOH), or hydroxycarbamide, is a hydroxamic acid derivative used as a drug for anti-neoplasm and sickle-cell disease. In this study, HU was found to have antioxidant activities against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and hydroxyl radicals and dose-dependent inhibitory activities against monoamine oxidase (MAO)-A, MAO-B, and semicarbazide-sensitive amine oxidase (SSAO) as compared to controls of clorgyline, deprenyl, and semicarbazide respectively. HU showed mixed-type, competitive-type, and competitive-type inhibition, respectively, with respect to substrates of MAO-A, MAO-B, and SSAO with apparent inhibition constants (Ki) of 19.46, 5.38, and 1.84 microM.
羟基脲(HU,NH(2)CONHOH),又称羟基脲素,是一种异羟肟酸衍生物,用作抗肿瘤和镰状细胞病的药物。在本研究中,与氯吉兰、司来吉兰和氨基脲对照相比,发现羟基脲对2,2-二苯基-1-苦基肼(DPPH)和羟基自由基具有抗氧化活性,对单胺氧化酶(MAO)-A、MAO-B和氨基脲敏感胺氧化酶(SSAO)具有剂量依赖性抑制活性。羟基脲分别对MAO-A、MAO-B和SSAO的底物表现出混合型、竞争型和竞争型抑制,表观抑制常数(Ki)分别为19.46、5.38和1.84 microM。