Dorhout B, Te Velde R J, Ferwerda H, Kingma A W, De Hoog E, Muskiet F A
Central Laboratory for Clinical Chemistry, University Hospital Groningen, The Netherlands.
Int J Cancer. 1995 Apr 10;61(2):214-7. doi: 10.1002/ijc.2910610212.
We studied the in vivo growth-inhibitory effect of the new S-adenosylmethionine decarboxylase inhibitor 4-amidinoindan-1-one 2'-amidinohydrazone (CGP 48664A). L1210-bearing DBA-2 mice were treated with increasing CGP 48664A doses from 1 day after i.p. L1210 cell inoculation. Treatment was continued for 4 days, after which all mice were killed. CGP 48664A caused dose-related exponential decreases of L1210 cell numbers and spermidine and spermine contents. Putrescine contents increased exponentially. Polyamine changes in spleen and liver were less profound. L1210 growth inhibition was not accompanied by changes in cell cycle phase distribution. It is concluded that CGP 48664A is an effective inhibitor of S-adenosylmethionine decarboxylase but that CGP 48664A-induced changes in intracellular polyamine compositions are not necessarily the cause of growth inhibition.
我们研究了新型S-腺苷甲硫氨酸脱羧酶抑制剂4-脒基茚满-1-酮2'-脒基腙（CGP 48664A）的体内生长抑制作用。接种L1210细胞后1天起，给携带L1210的DBA-2小鼠腹腔注射递增剂量的CGP 48664A。持续给药4天，之后处死所有小鼠。CGP 48664A导致L1210细胞数量、亚精胺和精胺含量呈剂量相关的指数下降。腐胺含量呈指数增加。脾脏和肝脏中的多胺变化较小。L1210生长抑制并未伴随细胞周期阶段分布的改变。结论是，CGP 48664A是一种有效的S-腺苷甲硫氨酸脱羧酶抑制剂，但CGP 48664A诱导的细胞内多胺组成变化不一定是生长抑制的原因。
