Reinke L A, Towner R A, Janzen E G
Department of Clinical Studies, Ontario Veterinary College, University of Guelph, Canada.
Toxicol Appl Pharmacol. 1992 Jan;112(1):17-23. doi: 10.1016/0041-008x(92)90274-v.
A single dose of ethanol, when administered 18 hr prior to CCl4, potentiates the hepatotoxicity of the halocarbon. In these studies, spin trapping and electron spin resonance (ESR) spectroscopy methods were utilized to determine whether a single ethanol dose increased the metabolism of CCl4 to free radical intermediates. When hepatic microsomes from ethanol-treated or control rats were incubated with CCl4 and the spin trapping agent alpha-phenyl-N-tert-butylnitrone (PBN), the ESR signal of the trichloromethyl radical adduct of PBN was of similar intensity in both groups. The ethanol dose also failed to induce p-nitrophenol hydroxylase activity. When PBN and CCl4 were administered to rats, liver extracts contained ESR signals resulting primarily from the trichloromethyl radical adduct of PBN, and the signals were of similar intensity in both experimental groups. Higher concentrations of the carbon dioxide anion radical adduct of PBN were detected in plasma samples from ethanol-treated rats. However, when hepatocytes from ethanol-treated and control rats were incubated with PBN and CCl4, ESR signals of the carbon dioxide adduct were of similar intensity. These data suggest that the higher concentrations of the carbon dioxide adduct in the blood of ethanol-treated rats may be explained by early CCl4-induced damage to liver cell membranes, rather than increased rates of formation. The data in this report fail to support the hypothesis that a single dose of ethanol stimulates the hepatic metabolism of CCl4 to the trichloromethyl radical. Alternatively, ethanol may potentiate CCl4 toxicity by affecting some critical metabolic step subsequent to trichloromethyl radical formation.
在四氯化碳给药前18小时给予单剂量乙醇,会增强卤代烃的肝毒性。在这些研究中,采用自旋捕获和电子自旋共振(ESR)光谱法来确定单剂量乙醇是否会增加四氯化碳向自由基中间体的代谢。当用四氯化碳和自旋捕获剂α-苯基-N-叔丁基硝酮(PBN)孵育乙醇处理组或对照组大鼠的肝微粒体时,两组中PBN的三氯甲基自由基加合物的ESR信号强度相似。乙醇剂量也未能诱导对硝基苯酚羟化酶活性。当给大鼠同时给予PBN和四氯化碳时,肝提取物中的ESR信号主要来自PBN的三氯甲基自由基加合物,且两组中的信号强度相似。在乙醇处理组大鼠的血浆样本中检测到更高浓度的PBN二氧化碳阴离子自由基加合物。然而,当用PBN和四氯化碳孵育乙醇处理组和对照组大鼠的肝细胞时,二氧化碳加合物的ESR信号强度相似。这些数据表明,乙醇处理组大鼠血液中较高浓度的二氧化碳加合物可能是由于早期四氯化碳诱导的肝细胞膜损伤,而非形成速率增加所致。本报告中的数据不支持单剂量乙醇刺激四氯化碳在肝脏中代谢为三氯甲基自由基这一假说。另外,乙醇可能通过影响三氯甲基自由基形成后的某些关键代谢步骤来增强四氯化碳的毒性。