Umezu K, Yuasa S, Sudoh A
Nihon Yakurigaku Zasshi. 1985 Mar;85(3):185-92. doi: 10.1254/fpj.85.185.
Tritoqualine (TRQ) administered at doses of 100 or 200 mg/kg, perorally, had a preventive effect on the liver injury in rats induced by the treatment with CCl4 for 12 weeks consecutively. Rats subjected to this chronic treatment with CCl4 showed a decrease in body weight gain and changes in several serum parameters that are indicators of hepatic function were observed: the increase of transaminases, as a parameter of hepatocyte breakdown; the increase of alkaline phosphatase, as a parameter of biliary system abnormalities, the reduction of prothrombin time, as a marker of protein biosynthesis in the liver; and the change of lipids concentrations, reflecting liver injury. After the administration of TRQ perorally, there was a notable suppression of the increment in leaked enzymes in the serum and a marked improvement of the parameters concerning protein biosynthesis and lipid metabolism in comparison with CCl4 control rats. Marked fibrosis in the liver was observed after CCl4 treatment for 12 weeks, and the collagen content in the liver was 5 times higher than that of control rats. TRQ suppressed the increment in collagen formation and also showed improvement of the decrease of the liver function with regards to protein biosynthesis in CCl4-treated rats. Judging from these results, it was concluded that TRQ had a remarkable protecting action on the liver injury chronically induced by CCl4 treatment and was a effective compound for restoring liver function.
以100或200毫克/千克的剂量口服曲喹啉（TRQ），对连续12周用四氯化碳处理诱导的大鼠肝损伤具有预防作用。接受四氯化碳这种慢性处理的大鼠体重增加减少，并且观察到几个作为肝功能指标的血清参数发生变化：转氨酶升高，作为肝细胞分解的参数；碱性磷酸酶升高，作为胆道系统异常的参数；凝血酶原时间缩短，作为肝脏中蛋白质生物合成的标志物；以及脂质浓度变化，反映肝损伤。口服TRQ后，与四氯化碳对照大鼠相比，血清中漏出酶的增加受到显著抑制，并且与蛋白质生物合成和脂质代谢有关的参数有明显改善。四氯化碳处理12周后观察到肝脏有明显纤维化，肝脏中的胶原蛋白含量比对照大鼠高5倍。TRQ抑制了胶原蛋白形成的增加，并且在四氯化碳处理的大鼠中，在蛋白质生物合成方面也改善了肝功能的下降。从这些结果判断，得出结论：TRQ对四氯化碳处理慢性诱导的肝损伤具有显著的保护作用，并且是恢复肝功能的有效化合物。
