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[二价铂抗肿瘤化合物与DNA复合物的光学性质]

[Optical properties of DNA complexes with antitumor compounds of bivalent platinum].

作者信息

Akimenko N M, Balcarová Z, Kleinwächter V, Evdokimov Iu M

出版信息

Antibiotiki. 1984 Oct;29(10):743-8.

PMID:6508249
Abstract

The optical properties of the DNA complexes with the compounds of bivalent platinum were studied. The compounds differed by the nature of the anionic and neutral ligands and their spatial arrangement about the platinum atom. It was shown that the same as cis-[Pt (NH3)2Cl2] the platinum compounds with the biological activity, i.e. [Pt (en) Cl2], cis-[PtNH3 (Bz) Cl2] and cis-[Pt (NH3)2NO2Cl] induced at low values of r (a ratio of the number of the platinum moles added to the number of the DNA nucleotide moles in the solution) an increase in the amplitude of the positive band in the spectrum of the circular dichroism (CD) of the linear DNA and a marked decrease in the amplitude of the negative band in the spectrum of the CD of the liquid crystalline microphase of DNA formed in the presence of polyethyleneglycol. By the character of the action on the CD spectrum of the linear and condensed DNA [Pt (tetrameen)Cl2] which had no selective antimitotic effect might be referred to the above platinum compounds. Trans-[Pt (NH3)2NO2Cl], [PtNH3PyCl2], cis-[Pt (NH3)2(NO2)2] and [Pt (NH3)3Cl]Cl having no biological activity either induced only a decrease in the amplitude of the positive band in the CD spectrum of the linear DNA or had no effect on the CD spectrum. The effect of these compounds on the CD spectrum of the liquid crystalline microphase of DNA was slightly pronounced or not observed.

摘要

研究了二价铂化合物与DNA复合物的光学性质。这些化合物在阴离子和中性配体的性质以及它们围绕铂原子的空间排列上有所不同。结果表明,与顺式-[Pt(NH₃)₂Cl₂]一样,具有生物活性的铂化合物,即[Pt(en)Cl₂]、顺式-[PtNH₃(Bz)Cl₂]和顺式-[Pt(NH₃)₂NO₂Cl],在低r值(溶液中添加的铂摩尔数与DNA核苷酸摩尔数之比)时,会导致线性DNA圆二色性(CD)光谱中正带的振幅增加,以及在聚乙二醇存在下形成的DNA液晶微相CD光谱中负带的振幅显著降低。根据对线性和凝聚态DNA的CD光谱的作用特点,没有选择性抗有丝分裂作用的[Pt(tetrameen)Cl₂]可能属于上述铂化合物。没有生物活性的反式-[Pt(NH₃)₂NO₂Cl]、[PtNH₃PyCl₂]、顺式-[Pt(NH₃)₂(NO₂)₂]和[Pt(NH₃)₃Cl]Cl要么只导致线性DNA的CD光谱中正向带的振幅降低,要么对CD光谱没有影响。这些化合物对DNA液晶微相CD光谱的影响不明显或未观察到。

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