UFT and its metabolites inhibit the angiogenesis induced by murine renal cell carcinoma, as determined by a dorsal air sac assay in mice.
UFT and its metabolites inhibit the angiogenesis induced by murine renal cell carcinoma, as determined by a dorsal air sac assay in mice.
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通过小鼠背气囊试验确定，UFT 及其代谢物可抑制小鼠肾细胞癌诱导的血管生成。
DOI：
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发表时间：
1999
影响因子：
11.5
通讯作者：
Yuji Yamada
中科院分区：
文献类型：
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作者：
K. Yonekura;Y. Basaki;L. Chikahisa;S. Okabe;A. Hashimoto;K. Miyadera;K. Wierzba;Yuji Yamada
UFT是一种由替加氟（FT）和尿嘧啶以1：4的摩尔比组成的抗癌剂，在日本临床实践中广泛用于治疗需要长期化疗的癌症患者，并且其副作用（如果有的话）很少。在这项研究中，我们评估了UFT对RENCA细胞诱导的血管生成的抑制作用，通过背气囊试验。通过将含有RENCA细胞的腔室植入小鼠中来诱导显著的血管生成。在该模型中，UFT显示出较强的血管生成抑制作用，而5-氟尿嘧啶（5-FU）和去氧氟尿苷的效果较差。其他实验显示FT是UFT的有效成分;尿嘧啶在抑制血管生成方面仍然无效。此外，我们已经发现，γ-羟基丁酸和γ-丁内酯，FT的代谢产物，具有有效的血管生成抑制作用，当化合物通过连续输注给药时，这种抑制作用被放大。这可能反映了UFT给药导致的每种代谢物的血药浓度变化。对于5-FU也获得了类似的结果。这表明UFT具有比其他氟化嘧啶更强的血管生成抑制作用，部分原因是其药代动力学特性，其特征是维持更高和持久的5-FU血液水平，部分原因是UFT特异性代谢产物γ-羟基丁酸和γ-丁内酯的抑制作用。
UFT, an anticancer agent that is composed of tegafur (FT) and uracil at a molar ratio of 1:4, is widely used in clinical practice in Japan to treat cancer patients requiring a long-term chemotherapy, and it is associated with few side effects, if any. In this study, we have evaluated the inhibitory effect of UFT against RENCA cell-induced angiogenesis by a dorsal air sac assay. Marked angiogenesis is induced by implantation of a chamber containing RENCA cells into mice. In this model, UFT showed a strong angiogenesis-inhibitory effect, whereas 5-fluorouracil (5-FU) and doxifluridine were less effective. Additional experiments revealed FT to be effective component of UFT; uracil remained ineffective in the inhibition of angiogenesis. Moreover, we have found that gamma-hydroxybutyric acid and gamma-butyrolactone, the metabolites of FT, possess a potent angiogenesis inhibitory effect that is amplified when the compounds are administered by a continuous infusion. This may reflect a transition in blood concentration of each metabolite resulting from the administration of UFT. Similar results were also obtained with respect to 5-FU. It was suggested that UFT has a stronger angiogenesis-inhibitory effect than did other fluorinated pyrimidines, partly due to its pharmacokinetic properties characterized by maintaining of higher and long-lasting blood levels of 5-FU and partly due the inhibitory effects derived from gamma-hydroxybutyric acid and gamma-butyrolactone, UFT-specific metabolites.
术后口服尿嘧啶和替加氟可抑制裸鼠体内人乳腺癌细胞微转移的进展。
DOI：
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发表时间：
1997
期刊：
Clinical cancer research : an official journal of the American Association for Cancer Research.
影响因子：
--
作者：
Kurebayashi,J;Nukatsuka,M;Fujioka,A;Saito,H;Takeda,S;Unemi,N;Fukumori,H;Kurosumi,M;Sonoo,H;Dickson,RB
通讯作者：
Dickson,RB
影响因子：
56.9
作者：
Jan Thompson;Anderson Kd;JM DiPietro;J. Zwiebel;M. Zametta;W. Anderson;T. Maciag
通讯作者：
Jan Thompson;Anderson Kd;JM DiPietro;J. Zwiebel;M. Zametta;W. Anderson;T. Maciag
影响因子：
3.1
作者：
NGUYEN, M;SHING, Y;FOLKMAN, J
通讯作者：
FOLKMAN, J