新5-FU衍生物氟糖啶的抗肿瘤作用、毒性以及和葡萄糖醛酸酐酶的关系

The Antitumor Effect, Toxicity Of A New 5-FU Derivative FU-O-G And The Relation Between The Antitumor Effect With Glucose And β-Glucuronidase

摘要: 合成5-FU衍生物是寻找新抗癌药的重要途径。1978年日本马场恒男等^1,2报道5-FU的氧位β-葡萄糖醛酸苷（FU-O-G）,在体内经β-葡萄糖醛酸苷酶（β-Glucuro-nidase,β-G）分解成5-FU后显示抗癌作用。给L₁210小鼠iv-FU OG的同时,ip葡萄糖比单独给予FU-OG的作用更明显。

Abstract: In this paper we have discovered that the new 6-FU derivative FU-O-G had obvious antitumor effect on EAC, S₁₆₀,H₂₂, L₆₁₅ and L₁₂₁₈ in mice,The inhibitory tumor rate of FU-O-G could be markedly elevated by oral 5g/kg glucose during glucose was administed before 30 minuts.Glucose might decrease the PH and increase the activity of β-glucuronidase(β-G) in tumor tissues, The results helpful promoted hydrolysis of FU-O-G in tumor and released to 5-FU,Using a colorimetric method determining the activity of β-G in tumor tissues was much higher than that of other organ，or serum, except for colon and rectum.