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4-氨基-3-乙酰基喹啉对小鼠白血病细胞系L1210的细胞毒性及凋亡诱导作用

Cytotoxicity and induction of apoptosis by 4-amino-3-acetylquinoline in murine leukemia cell line L1210.

作者信息

Repický Andrej, Jantová Sona, Theiszová Marica, Milata Viktor

机构信息

Department of Biochemistry and Microbiology, Slovak University of Technology, Radlinského 9, Bratislava, Slovak Republic.

出版信息

Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2005 Dec;149(2):345-7. doi: 10.5507/bp.2005.055.

Abstract

Nitrogen heterocyclic compounds are used in the pharmaceutical industry, in medicine and in agriculture for their biological activity. 4-Amino-3-acetylquinoline, a new synthetically prepared quinoline derivative, was the most effective compound in our primary cytotoxic screening. In this study, we evaluated cytotoxic/antiproliferative activity of quinoline using murine leukemia cell line L1210. Its ability to induce apoptosis was studied, too. Quinoline derivative acted cytotoxically on tumor cell line L1210, the IC(100) value were 50 microg/ml (for 24 h), 25 microg/ml (for 48 h) and 10 microg/ml (for 72 h). The IC(50) values was found to be less than 4 microg/ml, a limit put forward by the National Cancer Institute (NCI) for classification of he compound as a potential anticancer drug. The cytotoxic concentrations of 4-amino-3-acetyl quinoline induced morphological changes of L1210 cells and the apoptotic DNA fragmentation.

摘要

氮杂环化合物因其生物活性而被用于制药工业、医学和农业领域。4-氨基-3-乙酰基喹啉是一种新合成的喹啉衍生物,在我们最初的细胞毒性筛选中是最有效的化合物。在本研究中,我们使用小鼠白血病细胞系L1210评估了喹啉的细胞毒性/抗增殖活性。我们还研究了其诱导细胞凋亡的能力。喹啉衍生物对肿瘤细胞系L1210具有细胞毒性,IC(100)值分别为50微克/毫升(24小时)、25微克/毫升(48小时)和10微克/毫升(72小时)。发现IC(50)值小于4微克/毫升,这是美国国立癌症研究所(NCI)将该化合物归类为潜在抗癌药物所提出的一个界限。4-氨基-3-乙酰基喹啉的细胞毒性浓度诱导了L1210细胞的形态变化和凋亡性DNA片段化。

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