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AT-16是由氯霉素基团与氮芥結合而成的新的化合物。根据其原有基团的性貭,推想到二者結合后的可能效用,我們研究了它对动物的实驗性抗癌作用及毒性表現。結果发現:(1)AT-16对大白鼠肉瘤M-57、Jensen瘤及小白鼠肉瘤180、脑瘤53、淋巴白血病固体型均有显著的抑制作用;其中以对肉瘤M-57及Jensen瘤的疗效最好,抑制率可达到94—99％以上,并可使长大的肉瘤M-57消退。(2)能使吉田腹水瘤大白鼠的生存时間比对照組延长6倍以上。(3)将AT-16給家兔連續灌胃10日,在接近中毒剂量组,可見到有白血球下降、食量減退、体重減輕等現象。(4)用不同剂量的AT-16給猴子連續灌胃14日,观察呼吸、心率、血压、心电图、血象、体重及粪便常規,結果只是50毫克/公斤/日剂量組有輕度白血球下降現象,停药后随即恢复。其他均未見异常。
AT-16 is a new compound formed by combining a chloramphenicol group with nitrogen mustard. Based on the nature of the original group, the possible effects of the combination of the two were deduced. We studied its experimental anti-cancer effects and toxicity on animals. The results showed that: (1) AT-16 significantly inhibited the sarcoma M-57, Jensen’s tumor, and mouse sarcoma 180, brain tumor 53, and lymphoid leukemia solid type. Among them, sarcoma M-57 and Jensen The curative effect of the tumor is best, the inhibition rate can reach more than 94-99%, and can make the growth of sarcoma M-57 subsided. (2) The survival time of Yoshida ascites tumor mice can be extended by more than 6 times compared with the control group. (3) AT-16 rabbits were given intragastric administration for 10 consecutive days. In the near poisoning group, white blood cells decreased, food intake decreased, and body weight decreased. (4) Continuously gavage the monkeys with different doses of AT-16 for 14 days to observe the respiratory, heart rate, blood pressure, electrocardiogram, hemogram, weight, and stool routines. The result was only a mild white blood cell drop in the 50 mg/kg/day group. After the withdrawal, it will resume immediately. No other abnormality.