Department of Chemistry, Shantou University, Shantou, 515063, China.
Analyst. 2010 Oct;135(10):2653-60. doi: 10.1039/c0an00386g. Epub 2010 Aug 11.
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.
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。