el-Sharkawy A, el-Toukhy M, Abdel-Rahman S Z, el-Kholy Z, Farag H, el-Zoghby S, Gaber N
Department of Applied Medical Chemistry, Medical Research Institute, Alexandria University, Egypt.
J Trop Med Hyg. 1993 Feb;96(1):28-34.
The in-vivo effect of the schistosomicidal drugs praziquantel and oltipraz on the activities of the liver lysosomal enzymes in Schistosoma mansoni-infected and non-infected mice was studied. The effect of S. mansoni infection and the administration of the schistosomicidal drugs on the activities of beta-glucuronidase, acid ribonuclease and alpha-naphthyl acetate esterases may be considered as indices for carcinogenicity. Drugs were given orally in subcurative doses, either in a single dose of 400 mg kg-1 for praziquantel or in five daily doses of 50 mg kg-1 oltipraz. The increase in enzymatic activities in infected animals was attributed to deranged metabolic function as a result of liver cell injury. Treatment of uninfected animals with either praziquantel or oltipraz significantly increased the activities of the three lysosomal enzymes. Praziquantel possesses reversible and less toxic effects on the liver than oltipraz. The role of these antischistosomal drugs cannot be ignored as a possible aetiological factor implicated in the process of carcinogenesis associated with schistosomiasis infection through modulation of the operating potential of the enzymes concerned with detoxification, protein and fat metabolism.
研究了杀血吸虫药物吡喹酮和奥替普拉对曼氏血吸虫感染和未感染小鼠肝脏溶酶体酶活性的体内作用。曼氏血吸虫感染及杀血吸虫药物给药对β-葡萄糖醛酸酶、酸性核糖核酸酶和α-萘乙酸酯酶活性的影响可被视为致癌性指标。药物以亚治疗剂量口服,吡喹酮单次剂量为400 mg/kg,奥替普拉为每日5次剂量,每次50 mg/kg。感染动物酶活性的增加归因于肝细胞损伤导致的代谢功能紊乱。用吡喹酮或奥替普拉治疗未感染动物可显著增加三种溶酶体酶的活性。吡喹酮对肝脏具有可逆且毒性低于奥替普拉的作用。这些抗血吸虫药物作为一个可能的病因因素,通过调节与解毒、蛋白质和脂肪代谢相关酶的作用潜能,在与血吸虫病感染相关的致癌过程中所起的作用不容忽视。