Kelder P P, de Mol N J, Janssen L H
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Utrecht, The Netherlands.
Biochem Pharmacol. 1989 Oct 15;38(20):3593-9. doi: 10.1016/0006-2952(89)90132-9.
The possible role of hemoglobin in the sulfoxidation of chlorpromazine is still a controversial subject. Therefore this sulfoxidation was investigated with purified oxyhemoglobin and methemoglobin under various conditions: (i) in phosphate buffer pH 6.5; (ii) in monooxygenase mimicking systems with electron donors like ascorbic acid and NADPH, the last, with and without an electron carrier like methylene blue and cytochrome c reductase; (iii) in the presence of H2O2. Only in the presence of H2O2 chlorpromazine was converted into chlorpromazine sulfoxide in a considerable amount. This so-called peroxidase activity of hemoglobin appeared not to be based on a Fenton-type reaction. An oxidized reactive form of hemoglobin (i.e. ferrylhemoglobin) is responsible for the sulfoxidation. In the other systems only with ascorbic acid some chlorpromazine sulfoxide was produced. This is probably due to the production of H2O2 and the subsequent peroxidase activity of hemoglobin. Chlorpromazine enhanced the autoxidation of oxyhemoglobin, without being transformed itself.
血红蛋白在氯丙嗪硫氧化中可能发挥的作用仍是一个有争议的话题。因此,在各种条件下,用纯化的氧合血红蛋白和高铁血红蛋白对这种硫氧化进行了研究:(i)在pH 6.5的磷酸盐缓冲液中;(ii)在具有电子供体如抗坏血酸和NADPH的单加氧酶模拟系统中,后者在有或没有电子载体如亚甲蓝和细胞色素c还原酶的情况下;(iii)在H2O2存在的情况下。只有在H2O2存在时,氯丙嗪才会大量转化为氯丙嗪亚砜。血红蛋白的这种所谓过氧化物酶活性似乎不是基于芬顿型反应。血红蛋白的一种氧化反应形式(即高铁血红蛋白)负责硫氧化。在其他系统中,只有与抗坏血酸一起时才会产生一些氯丙嗪亚砜。这可能是由于H2O2的产生以及随后血红蛋白的过氧化物酶活性。氯丙嗪增强了氧合血红蛋白的自动氧化,而其本身并未发生转化。