Tsuda H, Sarma D S, Rajalakshmi S, Zubroff J, Farber E, Batzinger R P, Cha Y N, Bueding E
Cancer Res. 1979 Nov;39(11):4491-6.
Experiments were designed to determine whether hycanthone methanesulfonate (1-([2-(diethylamino)ethyl]amino)-4-(hydroxymethyl)thioxanthen-9-one monomethanesulfonate), an antischistosomal drug, and its analog, IA-4-N-oxide (8-chloro-2-[2-(diethylamino)ethyl]-2H-[1]benzothiopyrano[4,3,2-cd]indazole 5-methanol monomethanesulfonate), will induce neoplastic lesions in the livers of mice not infected with Schistosoma mansoni. All the mice received a single i.m. injection of hycanthone methanesulfonate (76 mg/kg), IA-4-N-oxide (80 mg/kg), or an equivalent volume of the solvent, 0.9% NaCl solution, 42 hr after partial hepatectomy. Of the mice receiving hycanthone methanesulfonate and living 200 days or longer, hepatocellular carcinoma was seen in 11.5% and liver sarcoma was seen in 4.2%. This type of malignant neoplasm was not seen in the animals receiving either IA-4-N-oxide or 0.9% NaCl solution. In addition, mice receiving hycanthone methanesulfonate showed a significantly higher incidence of both type 1 (43% compared to 21% in controls) and type 2 (21% compared to 12% in controls) hepatocyte neoplasms. Mice receiving IA-4-N-oxide showed no increased incidence of neoplasms.
实验旨在确定抗血吸虫药物甲磺海蒽酮（1-([2-(二乙氨基)乙基]氨基)-4-(羟甲基)噻吨-9-酮甲磺酸盐）及其类似物IA-4-N-氧化物（8-氯-2-[2-(二乙氨基)乙基]-2H-[1]苯并硫代吡喃并[4,3,2-cd]吲唑5-甲醇甲磺酸盐）是否会在未感染曼氏血吸虫的小鼠肝脏中诱发肿瘤病变。所有小鼠在部分肝切除术后42小时接受一次甲磺海蒽酮（76毫克/千克）、IA-4-N-氧化物（80毫克/千克）或等体积溶剂（0.9%氯化钠溶液）的肌肉注射。在接受甲磺海蒽酮且存活200天或更长时间的小鼠中，11.5%出现肝细胞癌，4.2%出现肝肉瘤。在接受IA-4-N-氧化物或0.9%氯化钠溶液的动物中未观察到这种类型的恶性肿瘤。此外，接受甲磺海蒽酮的小鼠1型（对照组为21%，接受甲磺海蒽酮的小鼠为43%）和2型（对照组为12%，接受甲磺海蒽酮的小鼠为21%）肝细胞肿瘤的发生率均显著更高。接受IA-4-N-氧化物的小鼠肿瘤发生率没有增加。
