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两种改良甾体烷基化剂诱导的细胞遗传学和抗肿瘤作用的比较研究。

A comparative study on cytogenetic and antineoplastic effects induced by two modified steroidal alkylating agents.

作者信息

Papageorgiou A, Tsavdaridis D, Geromichalos G D, Camoutsis C, Karaberis E, Mourelatos D, Chrysogelou E, Houvartas S, Kotsis A

机构信息

Laboratory of Experimental Chemotherapy, Theagenion Anticancer Institute, Thessaloniki, Greece.

出版信息

Cancer Detect Prev. 2001;25(4):369-74.

PMID:11531014
Abstract

We investigated the effects of two newly synthesized steroidal derivatives of nitrogen mustard on sister chromatid exchange rates and on human lymphocyte proliferation kinetics. The compound 33-hydroxy-5alpha,22alpha-spirostan- 12-one-p-(N,N-bis(2-chloroethyl)amino)phenylacetate(1) was, on a molar basis, less effective in inducing sister chromatid exchange and suppressing cell proliferation rate indices than compound 3beta-hydroxy-12alpha-aza-C-homo-5alpha,22alpha-spirostan-12-one-p-(N,N-bis(2-chloroethyl)amino)phenylacetate(2). A correlation was observed between the magnitude of the sister chromatid exchange response and the depression of cell proliferation index. We also studied the effects of the aforementioned compounds on Lewis lung carcinoma. The order of the percent inhibition of tumor growth achieved by the compounds coincides with the order of the cytogenetic effects they induce.

摘要

我们研究了两种新合成的氮芥甾体衍生物对姐妹染色单体交换率和人淋巴细胞增殖动力学的影响。在摩尔基础上,化合物33 - 羟基 - 5α,22α - 螺旋甾烷 - 12 - 酮 - p -(N,N - 双(2 - 氯乙基)氨基)苯乙酸酯(1)在诱导姐妹染色单体交换和抑制细胞增殖率指标方面比化合物3β - 羟基 - 12α - 氮杂 - C - 高 - 5α,22α - 螺旋甾烷 - 12 - 酮 - p -(N,N - 双(2 - 氯乙基)氨基)苯乙酸酯(2)效果更差。观察到姐妹染色单体交换反应的程度与细胞增殖指数的降低之间存在相关性。我们还研究了上述化合物对刘易斯肺癌的影响。这些化合物实现的肿瘤生长抑制百分比顺序与它们诱导的细胞遗传学效应顺序一致。

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