Zhou Ying, Bielec Krzysztof, Pasitsuparoad Pakorn, Hołyst Robert
Institute of Physical Chemistry, Polish Academy of Sciences, Kasprzaka 44/52, 01-224 Warsaw, Poland.
Analyst. 2020 Oct 21;145(20):6600-6606. doi: 10.1039/d0an01108h. Epub 2020 Aug 12.
Anthracyclines are one of the most studied anticancer drugs approved for medical treatment. The equilibrium constant (K) of the reaction between these drugs with DNA in both in vitro and in vivo experiments lacks consensus. The K values vary from 10 up to 10 M, which suggest a 1000-fold error in determining the effective concentration needed to form the drug-DNA complex. Until 2014, only one study by García [J. Phys. Chem. B, 2014, 118, 1288-1295] showed that the binding of anthracycline representative doxorubicin occurs in two reactions. We support this result by brightness analysis at a single molecular level for the four most common anthracyclines: doxorubicin, daunorubicin, epirubicin, and idarubicin.
蒽环类药物是经批准用于医学治疗的研究最多的抗癌药物之一。在体外和体内实验中，这些药物与DNA反应的平衡常数（K）尚无定论。K值从10到10 M不等，这表明在确定形成药物-DNA复合物所需的有效浓度时存在1000倍的误差。直到2014年，只有加西亚的一项研究[《物理化学杂志B》，2014年，118卷，1288 - 1295页]表明，蒽环类代表性药物阿霉素的结合发生在两个反应中。我们通过对四种最常见的蒽环类药物：阿霉素、柔红霉素、表柔比星和伊达比星进行单分子水平的亮度分析来支持这一结果。
