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首页> 外文期刊>DNA and Cell Biology >Interaction of Calf Thymus DNA with the Antiviral Drug Lamivudine
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Interaction of Calf Thymus DNA with the Antiviral Drug Lamivudine

机译:小牛胸腺DNA与抗病毒药物拉米夫定的相互作用

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One approach to accelerate the availability of new cancer drugs is to test drugs approved for other conditions as anticancer agents. In recent years, some researchers have shown that antiviral drugs, such as ritonavir, saquinavir, and nelfinavir, inhibit the growth of over 60 cancer cell lines derived from nine different tumor types. This article studied the anticancer potential of an antiviral drug, lamivudine (LA). The interaction of LA and calf thymus DNA (CT-DNA) was studied using emission, absorption, circular dichroism (CD), and viscosity techniques. The binding constants evaluated from fluorescence data at different temperatures revealed that fluorescence enhancement is a static process that involves complex-DNA formation in the ground state. Further, the enthalpy and entropy of the reaction between the drug and CT-DNA showed Delta H < 0 (-126.38 +/- 0.61 kJ mol(-1)) and Delta S < 0 (-352.17 +/- 2.1 J mol(-)1 K(-1)); therefore, van der Waals interactions or hydrogen bonds are the main forces in the binding of LA to CT-DNA. The values of K(f) clearly underscore the high affinity of LA to DNA. In addition, detectable changes in the CD spectrum of CT-DNA in the presence of LA indicated conformational changes. All these results showed that groove binding is the binding mode of this drug and CT-DNA.
机译:加快新癌症药物可用性的一种方法是测试已获准在其他条件下用作抗癌药的药物。近年来,一些研究人员表明,抗病毒药物(如ritonavir,saquinavir和nelfinavir)可抑制60多种源自9种不同肿瘤类型的癌细胞的生长。本文研究了抗病毒药拉米夫定(LA)的抗癌潜力。使用发射,吸收,圆二色性(CD)和粘度技术研究了LA与小牛胸腺DNA(CT-DNA)的相互作用。从不同温度下的荧光数据评估的结合常数表明,荧光增强是一个静态过程,涉及在基态形成复杂的DNA。此外,药物与CT-DNA之间反应的焓和熵显示Delta H <0(-126.38 +/- 0.61 kJ mol(-1))和Delta S <0(-352.17 +/- 2.1 J mol( -)1 K(-1));因此,范德华相互作用或氢键是LA与CT-DNA结合的主要作用力。 K(f)的值显然强调了LA对DNA的高亲和力。另外,在存在LA的情况下,CT-DNA的CD光谱的可检测变化指示构象变化。所有这些结果表明,凹槽结合是该药物与CT-DNA的结合方式。

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