Gorneva G A, Bergol'ts V V, Mladenova I P, Smirnova Z S, Nikolaeva T G
Eksp Onkol. 1989;11(1):63-5.
A comparative study was carried out with two alkylating agents IMB-MM and IMB-97 which are di-(2-halogenoethyl) hydrazides of amino acid derivatives. They have been found to exert a high activity towards wide spectrum of experimental tumours. Both agents caused inhibition of incorporation of 3H-thymidine into DNA of melanoma B16, marrow, intestinal mucosa, spleen and liver cells of mice with tumours. A maximal inhibition of DNA synthesis in all tissues was observed 24 h after the single doses of drugs. However 96 h later this effect was removed excluding the tumour cells. The cytofluorimetric study have shown that IMB-MM, like sarcolysine, caused an accumulation of tumour cells in G2/M phase of cell cycle, while IMB-97 increased accumulation of S-phase cells. The difference in phase sensitivity of tumour cells towards IMB-MM and IMB-97 is due to the differences in aminoacid carriers of di-(2-halogenethyl) hydrazide groups.
对两种烷基化剂IMB-MM和IMB-97进行了一项比较研究,它们是氨基酸衍生物的二(2-卤代乙基)酰肼。已发现它们对多种实验性肿瘤具有高活性。两种药剂均导致3H-胸腺嘧啶核苷掺入患有肿瘤的小鼠的黑色素瘤B16、骨髓、肠粘膜、脾脏和肝细胞的DNA受到抑制。单次给药后24小时观察到所有组织中DNA合成的最大抑制。然而,96小时后,除肿瘤细胞外,这种效应消失。细胞荧光分析表明,IMB-MM与溶肉瘤素一样,导致肿瘤细胞在细胞周期的G2/M期积累,而IMB-97增加了S期细胞的积累。肿瘤细胞对IMB-MM和IMB-97的相敏感性差异是由于二(2-卤代乙基)酰肼基团的氨基酸载体不同。