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目的:(1)了解脱氧氟尿苷(5-deoxy-5-fluorouridine,5-DFUR)在食管癌组织中转化为5-FU的情况及其高选择性抗肿瘤作用。方法:(1)选择拟行手术治疗的17例食管癌患者,术前5～7天口服5～DFUR1200mg/人/天后再行手术;(2)用柱切换反相高效液相色谱法检测食管癌组织、转移淋巴结、远癌正常食管组织及肝脏组织的5-氟尿嘧啶(5-fluorouracil,5-FU)浓度。结果:(1)在同一时点食管癌患者各组织的5-FU浓度分别是:癌组织214.18±92.53ng/g、转移淋巴结147.50±71.86ng/g、远癌食管组织50.67±20.24ng/g、肝脏组织17.80±9.09ng/g,P值<0.05。(2)不同分化程度的癌组织中5-FU浓度分别为:高分化鳞癌184.27±92.18ng/g、中分化鳞癌214.53±82.43ng/g、低分化鳞癌412.18±192.53ng/g,P值=0.024。(3)不同分期食管癌组织中的5-FU浓度为:Ⅱ期212.38±92.63ng/g,Ⅲ期247.50±91.99ng/g,P值=0.098。结论:5-DFUR能够高选择地在食管癌组织中转化为5-FU。不同分化程度的食管癌组织对5-DFUR的转化能力不同,分化能力愈低,转化为5-FU的能力愈强。
Objective: (1) To understand the 5-deoxy-5-fluorouridine (5-DFUR) in esophageal cancer into 5-FU and its high selective anti-tumor effect. Methods: (1) Seventeen patients with esophageal cancer who underwent surgical treatment were selected, and 5 ~ DFUR1200mg / person / day were given orally 5 ~ 7 days before operation. (2) The esophagus was detected by reversed phase high performance liquid chromatography 5-fluorouracil (5-FU) concentration in cancer tissues, metastatic lymph nodes, distant cancer normal esophageal tissues and liver tissues. Results: (1) The 5-FU concentrations of esophageal cancer tissues at the same time point were 214.18 ± 92.53ng / g, 147.50 ± 71.86ng / g, 50.67 ± 20.24ng / g , Liver tissue 17.80 ± 9.09ng / g, P value <0.05. (2) The concentration of 5-FU in differentiated cancer tissues were 184.27 ± 92.18ng / g for well differentiated squamous cell carcinoma, 214.53 ± 82.43ng / g for moderately differentiated squamous cell carcinoma, 412.18 ± 192.53ng / g for poorly differentiated squamous cell carcinoma, P value = 0.024. (3) The concentration of 5-FU in different staging esophageal cancer tissues was: 212.38 ± 92.63ng / g in stage Ⅱ, 247.50 ± 91.99ng / g in stage Ⅲ, P = 0.098. Conclusion: 5-DFUR can be selectively converted to 5-FU in esophageal cancer tissues with high selectivity. Different degrees of differentiation of esophageal cancer on the transformation of 5-DFUR different ability to differentiate lower, the stronger the ability to convert to 5-FU.