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G-四链体DNA是抗肿瘤药物研究开发的重要靶点,选择性识别并稳定G-四链体DNA的化合物是潜在的抗肿瘤药物.文章利用紫外可见吸收滴定,荧光滴定,CD光谱以及荧光共振能量转移熔点实验(FRET-melting)研究了三个基于邻菲罗啉的新型衍生物(A,B和C)与人端粒G-四链体DNA的相互作用.结果表明三个化合物通过末端堆积方式与G-四链体DNA相互作用,结合常数(K)约为106 mol-1.L.当浓度为3μmol.L-1时,化合物A,B和C分别使G-四链体DNA熔点温度增加(ΔTm)16.2,10.5和10.9℃.而且在10倍过量双螺旋DNA存在下均能选择性识别并稳定G-四链体结构.
G-quadruplex DNA is an important target for research and development of anticancer drugs, and compounds that selectively recognize and stabilize G-quadruplex DNA are potential anticancer drugs.Using UV-Vis absorption titration, fluorescence titration, CD spectroscopy and Fluorescence resonance energy transfer melting point experiments (FRET-melting) The interaction of three novel phenanthroline-based derivatives (A, B and C) with human telomere G-quadruplex DNA was studied. The results show that three compounds The binding constant (K) was about 106 mol- 1.L by end-stacking interaction with G-quadruplex DNA.Compounds A, B and C, respectively, caused the G- quadruplex The melting temperature of the bulk DNA increased (ΔTm) by 16.2, 10.5 and 10.9 ° C, and the G-quadruplex structure was selectively recognized and stabilized in the presence of 10-fold excess of duplex DNA.