Kunxian YANG , Jiashu CHEN , Bingbing ZHAI , Weiming CHEN , Huanglan YANG , Yufen XIAO , Juping WANG , Wenjie MEI
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引用次数: 0
摘要
目的合成铜(II)卟啉配合物并研究其与c-myc - g -四重体DNA的相互作用。方法采用常规加热法合成5-对羟基苯基- 10,15,20 -三(对甲氧基苯基)铜(II)卟啉配合物[p-HTMOPPCu (II)]。采用紫外(UV)滴定法、荧光滴定法、荧光共振能量转移(FRET)熔点法和竞争法研究了p-HTMOPPCu (II)与c-myc g -四重体DNA的相互作用。结果紫外吸收光谱和荧光光谱结果表明,p-HTMOPPCu (II)配合物与c-myc - g -四重体DNA结合较好;FRET熔点试验和竞争熔点试验表明,p-HTMOPPCu (II)可以选择性地结合和稳定c-myc g -四重体DNA。结论- htmoppcu (II)可结合并稳定c-myc g -四重体DNA,有望发展成为一类靶向c-myc g -四重体DNA的小分子抑制剂,用于临床治疗肿瘤。
Synthesis of copper (II) porphyrin complexes and their interaction with c-myc G-quadruplex DNA
Objective
To synthesize copper (II) porphyrin complexes and study their interactions with c-myc G-quadruplex DNA.
Methods
The 5-p-hydroxyphenyl-10, 15, 20-tris (p-methoxyphenyl) copper (II) porphyrin complex [p-HTMOPPCu (II)] was synthesized by the conventional heating method. Ultraviolet (UV) titration, fluorescence titration, fluorescence resonance energy transfer (FRET) melting point and competitive assays were used to study the interactions between p-HTMOPPCu (II) and c-myc G-quadruplex DNA.
Results
The UV absorption spectrum and fluorescence spectroscopy results indicated that the complex of p-HTMOPPCu (II) bound better with c-myc G-quadruplex DNA; the FRET melting point assay, and competitive melting point assay demonstrated that p-HTMOPPCu (II) could selectively bind and stabilize c-myc G-quadruplex DNA.
Conclusion
p-HTMOPPCu (II) can bind and stabilize c-myc G-quadruplex DNA and will potentially be developed into a class of small molecule inhibitors targeting c-myc G-quadruplex DNA for clinical applications in the treatment of tumors.