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新型S-腺苷甲硫氨酸脱羧酶抑制剂双脒腙对人红白血病K562细胞的抗肿瘤作用

Antitumor effect of methylglyoxal bis(butylamidinohydrazone), a new inhibitor of S-adenosylmethionine decarboxylase, against human erythroid leukemia K 562 cells.

作者信息

Hibasami H, Tsukada T, Maekawa S, Nakashima K

出版信息

Cancer Lett. 1986 Jan;30(1):17-23. doi: 10.1016/0304-3835(86)90127-8.

DOI:10.1016/0304-3835(86)90127-8
PMID:3455877
Abstract

Methylglyoxal bis(butylamidinohydrazone) (MGBB) inhibited S-adenosylmethionine decarboxylase (SAMDC) activity competitively with S-adenosylmethionine (SAM) showing the Ki value of 1.8 X 10(-5) M. MGBB showed less SAMDC-stabilizing effect in rat liver in vivo than did methylglyoxal bis-(guanylhydrazone) (MGBG). MGBB inhibited the growth of human erythroid leukemia K 562 cells. Putrescine, spermidine and spermine concentrations in MGBB-treated cells were depressed to 56%, 58% and 88% of the values of control cells, respectively. [35S]Methionine incorporation into trichloroacetic acid-insoluble fraction was decreased in the inhibitor-treated cells.

摘要

甲基乙二醛双（丁基脒腙）（MGBB）对S-腺苷甲硫氨酸脱羧酶（SAMDC）活性的抑制作用与S-腺苷甲硫氨酸（SAM）存在竞争性，其Ki值为1.8×10⁻⁵M。与甲基乙二醛双（胍腙）（MGBG）相比，MGBB在大鼠肝脏体内对SAMDC的稳定作用较小。MGBB抑制人红白血病K 562细胞的生长。经MGBB处理的细胞中，腐胺、亚精胺和精胺的浓度分别降至对照细胞值的56%、58%和88%。在经抑制剂处理的细胞中，[³⁵S]甲硫氨酸掺入三氯乙酸不溶部分的量减少。

相似文献

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Antitumor effect of methylglyoxal bis(butylamidinohydrazone), a new inhibitor of S-adenosylmethionine decarboxylase, against human erythroid leukemia K 562 cells.新型S-腺苷甲硫氨酸脱羧酶抑制剂双脒腙对人红白血病K562细胞的抗肿瘤作用
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