Suppr超能文献

1-甲基-7H-茚并[1,2-b]喹啉-7-(4-二甲氨基)苯甲醛三氟甲磺酸酯的细胞毒性活性和 DNA 结合特性。

Cytotoxic activities and DNA binding properties of 1-methyl-7H-indeno[1,2-b]quinolinium-7-(4-dimethylamino) benzylidene triflate.

机构信息

College of Pharmaceutical Sciences, Soochow University, Suzhou, China.

出版信息

DNA Cell Biol. 2012 Jun;31(6):1046-53. doi: 10.1089/dna.2011.1432. Epub 2012 Jan 25.

Abstract

The interaction of calf thymus DNA (ct-DNA) with a novel synthesized pyrazolo[1,5-a]indole compound 1-methyl-7H-indeno[1,2-b]quinolinium-7-(4-dimethylamino) benzylidene triflate (MIDBT) was extensively studied by various spectroscopic techniques, viscosity measurements, and gel electrophoresis. The UV-visible observation implied that the compound interacted with ct-DNA by two binding modes, intercalating into the DNA base pairs and attaching to the helix exterior of DNA. The results of the fluorescent quenching and viscosity measurements showed that MIDBT could intercalate into DNA base pairs deeply in a classical intercalative mode. Circular dichroism results showed that the binding of MIDBT shifted ct-DNA conformation from B to A at low concentrations. In the gel electrophoresis, the compound was found to promote the cleavage of plasmid pBR 322 DNA effectively. Furthermore, cytotoxic studies of this compound against eleven selected tumor cell lines have been done. The values of 50% cytotoxic concentration (IC(50)) were in the range of 1.09-18.84 μM, exhibiting the potent cytotoxic properties.

摘要

通过各种光谱技术、粘度测量和凝胶电泳,广泛研究了小牛胸腺 DNA(ct-DNA)与新型合成的吡唑并[1,5-a]吲哚化合物 1-甲基-7H-茚并[1,2-b]喹啉-7-(4-二甲氨基)苄叉三氟甲磺酸酯(MIDBT)的相互作用。紫外-可见观察表明,该化合物通过两种结合模式与 ct-DNA 相互作用,即嵌入 DNA 碱基对和附着在 DNA 螺旋外。荧光猝灭和粘度测量的结果表明,MIDBT 可以以经典的嵌入模式深入嵌入 DNA 碱基对。圆二色性结果表明,在低浓度下,MIDBT 的结合将 ct-DNA 构象从 B 型转变为 A 型。在凝胶电泳中,发现该化合物能有效地促进质粒 pBR 322 DNA 的断裂。此外,还对该化合物对 11 种选定的肿瘤细胞系的细胞毒性进行了研究。50%细胞毒性浓度(IC(50))值在 1.09-18.84 μM 范围内,表现出很强的细胞毒性。

相似文献

本文引用的文献

3
Investigation on the toxic interaction of toluidine blue with calf thymus DNA.丁香胺与小牛胸腺 DNA 毒性相互作用的研究。
J Hazard Mater. 2010 Mar 15;175(1-3):274-8. doi: 10.1016/j.jhazmat.2009.09.160. Epub 2009 Oct 7.

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验