测定阳离子两亲性药物与 DNA 的结合模式和 DNA 辅助的荧光共振能量转移放大。
Determination of the cationic amphiphilic drug-DNA binding mode and DNA-assisted fluorescence resonance energy transfer amplification.
机构信息
Department of Chemistry, Aligarh Muslim University, Aligarh 202002, India.
Department of Biochemistry, Aligarh Muslim University, Aligarh 202002, India.
出版信息
Spectrochim Acta A Mol Biomol Spectrosc. 2014 Mar 25;122:553-64. doi: 10.1016/j.saa.2013.11.030. Epub 2013 Nov 16.
Understanding the mechanism of drug-DNA binding is crucial for predicting the potential genotoxicity of drugs. Agarose gel electrophoresis, absorption, steady state fluorescence, and circular dichroism have been used in exploring the interaction of cationic amphiphilic drugs (CADs) such as amitriptyline hydrochloride (AMT), imipramine hydrochloride (IMP), and promethazine hydrochloride (PMT) with calf thymus or pUC19 DNA. Agarose gel electrophoresis assay, along with absorption and steady state fluorescence studies, reveal interaction between the CADs and DNA. A comparative study of the drugs with respect to the effect of urea, iodide induced quenching, and ethidium bromide (EB) exclusion assay reflects binding of CADs to the DNA primarily in an intercalative fashion. Circular dichroism data also support the intercalative mode of binding. Besides quenching, there is fluorescence exchange energy transfer (FRET) in between CADs and EB using DNA as a template.
了解药物-DNA 结合的机制对于预测药物的潜在遗传毒性至关重要。琼脂糖凝胶电泳、吸收、稳态荧光和圆二色性已被用于探索阳离子两亲药物（CADs）如盐酸阿米替林（AMT）、盐酸丙咪嗪（IMP）和盐酸异丙嗪（PMT）与小牛胸腺或 pUC19 DNA 的相互作用。琼脂糖凝胶电泳实验、吸收和稳态荧光研究揭示了 CADs 与 DNA 之间的相互作用。对这些药物的比较研究，包括尿素、碘离子诱导的猝灭和溴化乙锭（EB）排除实验的影响，反映了 CADs 主要以嵌入方式与 DNA 结合。圆二色性数据也支持结合的嵌入模式。除了猝灭之外，CADs 和 EB 之间还存在荧光交换能量转移（FRET），以 DNA 为模板。
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