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N1-(2'-四氢呋喃基)-5-氟尿嘧啶和5-氟尿嘧啶对艾氏腹水癌细胞核酸及蛋白质生物合成的影响。

Effect of N1-(2'-tetrahydrofuryl)-5-fluorouracil and 5-fluorouracil on nucleic acid and protein biosyntheses in Ehrlich ascites cells.

作者信息

Fujimoto S, Akao T, Itoh B, Koshizuka I, Koyano K

出版信息

Cancer Res. 1976 Jan;36(1):33-6.

PMID:1248008
Abstract

N1-(2'-Tetrahydrofuryl)-5-fluorouracil (FT-207) is a derivative of 5-fluorouracil (5-FU) and has been accepted as a new chemotherapeutic drug. The inhibitory effects of FT-207 and 5-FU on nucleic acid and protein biosyntheses in Ehrlich ascites cells were compared. Both drugs markedly inhibited the incorporation in vivo of the labeled precursors into nucleic acid and protein. The inhibitory effect of FT-207 on DNA and RNA synthesis lasted for a long period of time. Two hr after administration of 5-FU (250 mug/g body weight), the absolute size of uracil pool of liver increased by at least 50%. However, in an in vitro study, FT-207 at a concentration of 60 mug/ml produced no effect on the incorporation of precursors into DNA and RNA of Ehrlich ascites cells 3 hr incubation. If 5-FU was added to Ehrlich ascites cell suspension simultaneously with [5-3H]uridine, the incorporation of the labeled precursor into RNA increased by 30 to 50%.

摘要

N1-(2'-四氢呋喃基)-5-氟尿嘧啶(FT-207)是5-氟尿嘧啶(5-FU)的衍生物,已被公认为一种新型化疗药物。比较了FT-207和5-FU对艾氏腹水癌细胞核酸和蛋白质生物合成的抑制作用。两种药物均显著抑制体内标记前体掺入核酸和蛋白质。FT-207对DNA和RNA合成的抑制作用持续很长时间。给予5-FU(250微克/克体重)2小时后,肝脏尿嘧啶池的绝对大小至少增加50%。然而,在一项体外研究中,浓度为60微克/毫升的FT-207在孵育3小时后对艾氏腹水癌细胞前体掺入DNA和RNA没有影响。如果在向艾氏腹水细胞悬液中加入[5-3H]尿苷的同时加入5-FU,则标记前体掺入RNA增加30%至50%。

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