Yamada K, Hase S, Yoshimura A, Haruyama K, Katsura Y, Sameshima T, Niwa K, Ishizawa T, Shimazu H
First Dept. of Surgery, Kagoshima University School of Medicine.
Gan To Kagaku Ryoho. 1990 Dec;17(12):2333-7.
5-fluorouracil (5-FU) concentrations in peripheral blood, portal blood, normal and cancer tissues were evaluated in 26 patients with colorectal cancer after SF-SP administration (800 mg/day for 10 days). Thymidine phosphorylase activity in cancer tissues was also evaluated. 5-FU concentration in cancer tissues was significantly higher than that in other three specimens, and much higher than 0.05 microgram/g which was reported to be the minimum effective concentration. 5-FU concentration in portal blood was lower than MEC (0.05 microgram/ml). As for the relationship with the pathological features of cancer, the protruding lesions showed a higher 5-FU concentration than the ulcerative ones, and the lesions invaded only to submucosa or proper muscle showed a higher concentration than others. 5-FU concentration ratio in cancer tissues per in peripheral blood (T/B ratio) was related to thymidine phosphorylase activity. The higher was the thymidine phosphorylase activity, the greater T/B ratio. The results suggest that the tumor with higher thymidine phosphorylase activity might have a more pronounced anticancer efficacy of 5-FU.
对26例结直肠癌患者在给予SF-SP（800毫克/天，共10天）后，评估其外周血、门静脉血、正常组织和癌组织中的5-氟尿嘧啶（5-FU）浓度。同时也评估癌组织中的胸苷磷酸化酶活性。癌组织中的5-FU浓度显著高于其他三个样本，且远高于据报道的最低有效浓度0.05微克/克。门静脉血中的5-FU浓度低于最低有效浓度（0.05微克/毫升）。至于与癌症病理特征的关系，突出性病变的5-FU浓度高于溃疡性病变，仅侵犯黏膜下层或固有肌层的病变浓度高于其他病变。癌组织中5-FU浓度与外周血浓度之比（T/B比）与胸苷磷酸化酶活性相关。胸苷磷酸化酶活性越高，T/B比越大。结果表明，胸苷磷酸化酶活性较高的肿瘤对5-FU的抗癌疗效可能更显著。
