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首页> 外文期刊>Chemotherapy: International Journal of Experimental and Clinical Chemotherapy >Cytotoxic effects of diazenes on tumor cells in vitro.
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Cytotoxic effects of diazenes on tumor cells in vitro.

机译：二氮嗪对体外肿瘤细胞的细胞毒性作用。

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BACKGROUND: We have shown previously that diazenecarboxamides (diazenes) were cytotoxic for several tumor cell lines. Their target seems to be the intracellular glutathione (GSH). To improve the solubility and biological activity of these drugs, new compounds have been synthesized. In the present study we examined the cytotoxic effect of six new diazenes: BR-25, UP-39, UP-11, JK-1024, RL-514 and RL-625. METHODS: The cytotoxicity of diazenes was tested on nine human tumor cell lines: laryngeal carcinoma HEp2 cells, cervical carcinoma HeLa cells, mammary carcinoma MCF-7 cells, breast adenocarcinoma SK-BR-3 cells, and glioblastoma A1235 cells and their four drug-resistant cell lines. Cytotoxicity was determined using the colorimetric MTT assay. The intracellular GSH content (following the treatment with diazenes) was examined spectrophotometrically in human cervical carcinoma cells by the procedure developed by Tietze. RESULTS: Results show that diazene UP-39 was mostly efficient, significantly reducing the cell survival of all nine cell lines examined, including four drug-resistant cell lines. Diazenes UP-11, RL-514 and BR-25 given in the highest concentrations decreased the survival of some examined cell lines, but to less than 50%. Diazenes RL-625 and JK-1024 had no influence on the cell survival. None of the examined diazenes significantly influenced the intracellular level of GSH. CONCLUSION: Our results suggest that diazene UP-39 may be a promising new drug for the treatment of tumors and encourage further research on this compound. Copyright 2002 S. Karger AG, Basel
机译：背景：我们先前已经证明，重氮羧酰胺（二氮烯）对几种肿瘤细胞系具有细胞毒性。他们的目标似乎是细胞内谷胱甘肽（GSH）。为了提高这些药物的溶解度和生物活性，已经合成了新化合物。在本研究中，我们检查了六种新的二氮烯的细胞毒性作用：BR-25，UP-39，UP-11，JK-1024，RL-514和RL-625。方法：在9种人类肿瘤细胞系上检测了二氮烯的细胞毒性：喉癌HEp2细胞，宫颈癌HeLa细胞，乳腺癌MCF-7细胞，乳腺腺癌SK-BR-3细胞和胶质母细胞瘤A1235细胞及其四种药物抗性细胞系。使用比色MTT测定法测定细胞毒性。通过Tietze开发的方法，用分光光度法检查了人宫颈癌细胞中的细胞内GSH含量（用二氮烯治疗后）。结果：结果表明，重氮UP-39最有效，显着降低了所有9种细胞株（包括4种耐药细胞株）的细胞存活率。浓度最高的Diazenes UP-11，RL-514和BR-25降低了某些受检细胞系的存活率，但低于50％。 Diazenes RL-625和JK-1024对细胞存活没有影响。所检查的二氮烯均未显着影响细胞内GSH水平。结论：我们的结果表明，重氮UP-39可能是一种有望用于治疗肿瘤的新药，并鼓励对该化合物的进一步研究。版权所有2002 S. Karger AG，巴塞尔

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