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硫酸培普利欧霉素(NK631)的器官分布、吸收及排泄研究(作者译)

[Studies on organ distribution, absorption and excretion of pepleomycin sulfate (NK631) (author's transl)].

作者信息

Abe F, Yoshioka O, Ebihara K, Koyu A, Suzuki H, Inoue H, Kodaka A, Matsuda A

出版信息

Jpn J Antibiot. 1978 Dec;31(12):886-94.

PMID:83411
Abstract
  1. Organ distribution of pepleomycin (NK631) in mice and rats was studied. NK631 was found at higher levels than bleomycin (BLM) in skin, lung, stomach, solid tumor, etc. in mice and rats. Furthermore NK631 was detected in the mesenteric and lumbar lymph node, esophagus and prostate in rats and also distributed at about twice as high levels as BLM in the AH109A hepatoma cell-metastasized lymph nodes. 2. For the elucidation of reason on low pulmonary toxicity of NK631 which is in spite of 1.5 times highly distribution in lung compared with BLM, inactivation of various BLMs by high molecular fraction of lung of mice and rats was determined. The order of inactivation rate of various BLMs in lung was as follows: BLM-M5196 greater than NK631 greater than BLM greater than BLM-HPE. There is an encouraging coincidence between index of pulmonary fibrosis in mice and inactivating rate in lung. 3. A comparative study on the serum level and urinary excretion of NK631 and BLM was performed in dogs. The blood level and urinary excretion rate of both drugs were almost similar. 4. The blood levels of NK631 were comparable to those of BLM in cancer patients.
摘要
  1. 研究了培普利欧霉素(NK631)在小鼠和大鼠体内的器官分布。在小鼠和大鼠的皮肤、肺、胃、实体瘤等部位,发现NK631的含量高于博来霉素(BLM)。此外,在大鼠的肠系膜和腰淋巴结、食管和前列腺中检测到了NK631,并且在AH109A肝癌细胞转移的淋巴结中,NK631的分布水平约为BLM的两倍。2. 为了阐明NK631肺毒性低的原因,尽管其在肺中的分布比BLM高1.5倍,仍测定了小鼠和大鼠肺高分子组分对各种博来霉素的失活情况。肺中各种博来霉素的失活率顺序如下:BLM-M5196大于NK631大于BLM大于BLM-HPE。小鼠肺纤维化指数与肺失活率之间存在令人鼓舞的一致性。3. 对狗体内NK631和BLM的血清水平及尿排泄情况进行了比较研究。两种药物的血药水平和尿排泄率几乎相似。4. 癌症患者体内NK631的血药水平与BLM相当。

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