López M C, Ruiz L M, Craciunescu D, Doadrio A, Osuna A, Alonso C
Chem Biol Interact. 1986 Jul-Aug;59(1):99-111. doi: 10.1016/s0009-2797(86)80057-6.
The nature of the conformational changes produced in DNA by cis-DDP analogs has been studied by physiochemical techniques. The UV spectra showed that the DNA undergoes bathochromic shifts accompanied by hyperchromic effects in reaction with specific analogs (cis-Pt(DDH) (mucobromic)2, cis-Pt(tranilcypromine)2Cl2 and cis-Pt(DDH) Cl2), while a different series of analogs (cis-Pt(DDH) (metafluorobenzoic)2 and cis-Pt(pentamidine)Cl2) induce a significative decrease in the absorbance at 258 nm. Moreover one of these analogs (cis-Pt(pentamidine)Cl2) causes strong stabilization of the double helix to heat denaturation. The CD spectra indicate moreover that cis-Pt(pentamidine)Cl2 modifies the secondary structure of the DNA in a significant way with an increase of the positive band and a decrease of the ellipticity of the negative band. The antitrypanosome activity of cis-Pt(pentamidine)Cl2 is probably due to inhibition of the intracellular parasites division in parasitized cells.
顺铂类似物对DNA产生的构象变化的本质已通过物理化学技术进行了研究。紫外光谱表明，DNA在与特定类似物（顺式-Pt(DDH)(粘溴酸)2、顺式-Pt(反苯环丙胺)2Cl2和顺式-Pt(DDH)Cl2）反应时会发生红移并伴有增色效应，而另一系列类似物（顺式-Pt(DDH)(间氟苯甲酸)2和顺式-Pt(喷他脒)Cl2）会导致258nm处吸光度显著降低。此外，其中一种类似物（顺式-Pt(喷他脒)Cl2）会使双螺旋对热变性具有很强的稳定性。圆二色光谱还表明，顺式-Pt(喷他脒)Cl2以显著方式改变了DNA的二级结构，正带增加，负带椭圆率降低。顺式-Pt(喷他脒)Cl2的抗锥虫活性可能是由于抑制了被寄生细胞内寄生虫的分裂。
