Toriyama K, Fujita H, Ishida N
J Antibiot (Tokyo). 1975 Jan;28(1):64-72. doi: 10.7164/antibiotics.28.64.
Distribution, excretion and toxicity of an antitumor protein, neocarzinostatin (NCS) were examined in mice after oral administration. The oral LD50 1 g/kg after intravenous injection. After oral administration of 200 mg/kg of NCS, the tissue level was low but detectable in lung, skin and pancreas in addition to the tissues of the gastrointestinal tract. The NCS level in lung and skin remained constant through 6 hours. In gastrointestinal tissues after oral administration the level was higher in the stomach than the large intestine or small intestine. The total recovery of orally administered NCS in feces of mice was 26.5% of the given dose during the first 12 hours. Inactivation of NCS by homogenates of small and large intestines (about 50%) was found in in vitro experiments.
口服给药后,在小鼠体内检测了抗肿瘤蛋白新制癌菌素(NCS)的分布、排泄及毒性。静脉注射后的口服半数致死量为1 g/kg。口服200 mg/kg的NCS后,除胃肠道组织外,肺、皮肤和胰腺中的组织水平较低但可检测到。肺和皮肤中的NCS水平在6小时内保持恒定。口服给药后,胃肠道组织中胃内的水平高于大肠或小肠。在最初12小时内,小鼠粪便中口服NCS的总回收率为给药剂量的26.5%。体外实验发现,小肠和大肠匀浆对NCS有灭活作用(约50%)。