Tsuruo T, Iida H, Naganuma K, Tsukagoshi S, Sakurai Y
Cancer Chemother Pharmacol. 1980;4(2):83-7. doi: 10.1007/BF00254027.
1-Hexylcarbamoyl-5-fluorouracil (HCFU) and its parent compound 5-fluorouracil (5-FU) were tested PO for antitumor activity against mouse colon adenocarcinoma 26 (colon 26), colon adenocarcinoma 38 (colon 38), and Lewis lung carcinoma. The drugs were given orally at 2--4 days intervals for a total of ten doses. 5-FU was moderately active against colons 26 and 38 but not against Lewis lung carcinoma. In this treatment regimen the most impressive antitumor activity was obtained with HCFU against colons 26 and 38, especially colon 38 tumor. At 300 mg HCFU/kg, one out of seven mice inoculated with colon 26 and five out of ten mice inoculated with colon 38 became tumor-free. HCFU, however, was marginally effective in the prolongation of survival time of mice bearing Lewis lung carcinoma. 5-FU is approximately twice as active as HCFU against cultured cell lines from colon 26, colon 38, and Lewis lung carcinoma. Lewis lung carcinoma cells were most sensitive against HCFU, which is in contrast to the results obtained in the in vivo experiment. The IC50 value of HCFU against Lewis lung carcinoma cells was approximately half that against colon 26 and colon 38 cells. This higher sensitivity of Lewis lung cells against HCFU could be explained by the higher cellular uptake of the drug.
1-己基氨基甲酰基-5-氟尿嘧啶（HCFU）及其母体化合物5-氟尿嘧啶（5-FU）经口服给药，测试其对小鼠结肠腺癌26（结肠26）、结肠腺癌38（结肠38）和Lewis肺癌的抗肿瘤活性。药物每隔2至4天口服给药，共给药十次。5-FU对结肠26和结肠38有中等活性，但对Lewis肺癌无效。在该治疗方案中，HCFU对结肠26和结肠38，尤其是结肠38肿瘤表现出最显著的抗肿瘤活性。在300mg HCFU/kg剂量下，接种结肠26的七只小鼠中有一只、接种结肠38的十只小鼠中有五只肿瘤消失。然而，HCFU在延长荷Lewis肺癌小鼠的生存时间方面效果甚微。5-FU对来自结肠26、结肠38和Lewis肺癌的培养细胞系的活性约为HCFU的两倍。Lewis肺癌细胞对HCFU最为敏感，这与体内实验结果相反。HCFU对Lewis肺癌细胞的IC50值约为对结肠26和结肠38细胞IC50值的一半。Lewis肺癌细胞对HCFU的这种较高敏感性可以用该药物较高的细胞摄取来解释。
