关于抗肿瘤药物的研究Ⅸ.N-甲酰溶肉瘤素的一些药理作用

抗肿瘤药N-甲酰溶肉瘤素(简称N-甲)的毒性低.小鼠于每天口服25-150毫克/公斤连续10天,游泳耐力不减,肝脏破坏戊巴比妥钠功能正常.小鼠于腹腔注射N-甲10-20毫克/公斤/天,连续10天,或150毫克/公斤一次,对因戊巴比妥钠产生的睡眠时间无改变.大鼠于每天腹腔注射N-甲10毫克/公斤,连续10天,其利尿功能,肾上腺内维生素C含量及微血管渗进性均无明显改变.麻醉兔于静脉注射N-甲10-40毫克/公斤后,血压亦无明显改变.当N-甲20毫克/公斤/天,连续10天时,于注射后5天,大鼠利尿功能受到抑制,但于停药后3天逐渐恢复正常.大鼠于腹腔注射N-甲80毫克/公斤后2小时,肾上腺内维生素C含量明显下降,微血管渗透性显著增加.

STUDIES ON ANTITUMOUR DRUGS Ⅸ. SOME PHARMACOLOGICAL ACTIONS OF N-FORMYLSARCOLYSINE

In earlier communications, we reported that N-Formylsarcolysine (N-F) was an effec- tive antitumour agent with low toxicity.The present paper is a report on some phar- macological actions of N-F. After oral administration of N-F at 25-150 mg/kg/day to mice for 10 days, the drug did not decrease the swimming time, nor did it prolong the pentobarbital sleeping time.When mice were injected intraperitoneally with 10-20 mg/kg of N-F daily for 10 days, there was no prolongation of pentobarbital sleeping time.Intraperitoneal injec- tion of N-F at 10 mg/kg/day to rats for 10 days produced no marked change in diuresis, the contents of the adrenal ascorbic acid, and the permeability of the capillaries.In- travenous injection of N-F 10-40 mg/kg to anaesthetized rabbits did not alter the blood pressure. When rats were injected intraperitoneally with N-F at 20 mg/kg for 10 days, an inhibition of diuresis was observed beginning 5 days after the treatment. However, the diuretic function of rats became normal three days after cessation of N-F. Two hours after intraperitoneal injection of 80 mg/kg of N-F to rats the content of the adrenal ascorbic acid was significantly reduced and the permeability of the capillary increased markedly.