Bachur N R, Felsted R L
Drug Metab Dispos. 1976 May-Jun;4(3):239-43.
Oxisuran, 2-((methylsulfinyl)acetyl)pyridine is reduced to alpha-((methylsulfinyl)methyl-2-pyridinemethanol, oxisuranol, by cytoplasmic enzymes from rabbit liver, kidney, brain, intestine, and lung. The cytoplasmic enzyme from liver is dependent on NADPH as cofactor and has an optimal pH of 6.0. Enzymatic activity is also present in liver mitochondria but at a lower specific activity. The cytoplasmic extracts catalyze the formation of two oxisuranol products, presumably the diastereoisomers described by Di Carlo and associates from in vivo studies. Verification of the product as oxisuranol was accomplished by thin-layer chromatography and mass spectrometry.
奥昔舒仑,即2 - ((甲基亚磺酰基)乙酰基)吡啶,可被来自兔肝、肾、脑、肠和肺的细胞质酶还原为α - ((甲基亚磺酰基)甲基 - 2 - 吡啶甲醇,即奥昔舒仑醇。来自肝脏的细胞质酶以NADPH作为辅因子,最适pH为6.0。肝脏线粒体中也存在酶活性,但比活性较低。细胞质提取物催化形成两种奥昔舒仑醇产物,推测是迪卡罗及其同事在体内研究中描述的非对映异构体。通过薄层色谱法和质谱法对产物为奥昔舒仑醇进行了验证。