Khomenko A K, Semeniĭ V Ia, Gridina N Ia, Diachok F I, Kudriavets Iu I
Eksp Onkol. 1986;8(3):61-4.
The inhibitory effect of difluoromethylornithine (DFMO) synthesized by the authors on the activity of the ornithine decarboxylase (ODC) and proliferation of microbial and mammalian cells in vitro was studied. The in vivo growth of ascite plasmocytoma of solid melanoma B-16 cells in mice was also effectively inhibited by DFMO. But the antiproliferative activity of DFMO in solid tumours was substantially lower. Such a decrease in the antitumour activity may be associated with polyamines released from necrotic areas of solid tumours. As the tumour cells "catch" the vitally important metabolites, their effect inside solid tumours is turned against the tumour cells themselves. The second reason of the decrease in the DFMO activity is adsorption of polyamines on the erythrocyte surface.
研究了作者合成的二氟甲基鸟氨酸(DFMO)对鸟氨酸脱羧酶(ODC)活性以及微生物和哺乳动物细胞体外增殖的抑制作用。DFMO还能有效抑制小鼠体内实体黑色素瘤B - 16细胞腹水浆细胞瘤的生长。但DFMO在实体瘤中的抗增殖活性明显较低。这种抗肿瘤活性的降低可能与实体瘤坏死区域释放的多胺有关。由于肿瘤细胞“捕获”了至关重要的代谢物,它们在实体瘤内的作用反而对肿瘤细胞自身不利。DFMO活性降低的第二个原因是多胺在红细胞表面的吸附。