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喹唑啉CB 3717和CB 3703对艾氏腹水癌细胞及宿主小鼠某些器官中叶酸保留和代谢的抑制作用。

Quinazoline CB 3717 and CB 3703 inhibition of folate retention and metabolism in Ehrlich ascites carcinoma cells and some organs of the host-mouse.

作者信息

Sikora F, Grzelakowska-Sztabert B

出版信息

Cancer Lett. 1984 Jul;23(3):289-95. doi: 10.1016/0304-3835(84)90096-x.

Abstract

Disturbances in folate metabolism in Ehrlich ascites carcinoma-bearing mice caused by 2 quinazoline-antifolates are described. They are manifested by diminished retention in tumour cells and the host-liver of injected radioactive folate and by a decreased extent of its conversion to coenzymatic, polyglutamate forms. Kidney retention of folate was also affected by either quinazoline, showing a severalfold decrease in mice treated with CB 3703, and a 2-fold increase in those treated with CB 3717. Kidney folylpolyglutamate content was also greatly reduced.

摘要

描述了由2种喹唑啉抗叶酸剂引起的荷艾氏腹水癌小鼠叶酸代谢紊乱。其表现为肿瘤细胞和宿主肝脏中注射的放射性叶酸保留减少,以及其转化为辅酶形式的多聚谷氨酸形式的程度降低。喹唑啉对肾脏中叶酸的保留也有影响,在用CB 3703处理的小鼠中叶酸保留减少了几倍,而在用CB 3717处理的小鼠中则增加了2倍。肾脏中叶酸多聚谷氨酸的含量也大大降低。

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