Suppr超能文献

DNA 作为抗癌化合物筛选的靶标,直接通过共振光散射技术。

DNA as a target for anticancer compounds screening directly by resonance light scattering technique.

机构信息

Department of Chemistry, Shantou University, Shantou, 515063, China.

出版信息

Analyst. 2010 Oct;135(10):2653-60. doi: 10.1039/c0an00386g. Epub 2010 Aug 11.

Abstract

Anticancer drugs which selectively interact with DNA can change DNA's conformation and inhibit the duplication or transcription of DNA. An instrument-based assay for directly screening DNA-targeted anticancer drugs using resonance light scattering (RLS) technique with a common spectrofluorometer was proposed. To monitor the proposed screening method, the interactions between three anticarcinogens (Adriamycin (ADM), Bleomycin A (BLMA), Actinomycin D (ACTD)) and DNA were studied. The sequence of binding constants for the three anticarcinogens obtained from RLS spectra is: K(RLS) (ACTD, 9.43 × 10(5) L mol(-1)) > K(RLS) (ADM, 6.67 × 10(5) L mol(-1)) > K(RLS) (BLMA, 8.88 × 10(3) L mol(-1)) and of binding numbers is: N(RLS) (ACTD, 3.36 mmol g(-1)) < N(RLS) (ADM, 3.81 mmol g(-1)) < N(RLS) (BLMA, 57.44 mmol g(-1)). From the results we got the sequence of combination intensity between these three drugs and DNA as follows: ACTD-DNA > ADM-DNA > BLMA-DNA, which was completely consistent with drug activity. The conclusion indicated that the present method was direct, rapid, reliable and was another important innovation of the application of RLS technique.

摘要

抗癌药物与 DNA 选择性相互作用可以改变 DNA 的构象,并抑制 DNA 的复制或转录。本文提出了一种基于仪器的方法,使用带有普通分光光度计的共振光散射(RLS)技术直接筛选靶向 DNA 的抗癌药物。为了监测所提出的筛选方法,研究了三种抗癌剂(阿霉素(ADM)、博来霉素 A(BLMA)、放线菌素 D(ACTD))与 DNA 之间的相互作用。从 RLS 光谱中获得的三种抗癌剂的结合常数顺序为:K(RLS)(ACTD,9.43×10^5 L mol^-1)> K(RLS)(ADM,6.67×10^5 L mol^-1)> K(RLS)(BLMA,8.88×10^3 L mol^-1),结合数顺序为:N(RLS)(ACTD,3.36 mmol g^-1)< N(RLS)(ADM,3.81 mmol g^-1)< N(RLS)(BLMA,57.44 mmol g^-1)。结果表明,这三种药物与 DNA 的结合强度顺序为:ACTD-DNA > ADM-DNA > BLMA-DNA,与药物活性完全一致。结论表明,该方法直接、快速、可靠,是 RLS 技术应用的又一重要创新。

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