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首页> 外文期刊>Biochemistry >DNA interactions of monofunctional organometallic ruthenium(II) antitumor complexes in cell-free media.
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DNA interactions of monofunctional organometallic ruthenium(II) antitumor complexes in cell-free media.

机译：在无细胞培养基中单功能有机金属钌（II）抗肿瘤复合物的DNA相互作用。

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摘要

Modifications of natural DNA in a cell-free medium by antitumor monodentate Ru(II) arene compounds of the general formula [(eta(6)-arene)Ru(en)Cl](+) (arene = biphenyl, dihydroanthracene, tetrahydroanthracene, p-cymene, or benzene; en = ethylenediamine) were studied by atomic absorption, melting behavior, transcription mapping, circular and linear dichroism, plasmid unwinding, competitive ethidium displacement, and differential pulse polarography. The results indicate that these complexes bind preferentially to guanine residues in double-helical DNA. The data are consistent with DNA binding of the complexes containing biphenyl, dihydroanthracene, or tetrahydroanthracene ligands that involves combined coordination to G N7 and noncovalent, hydrophobic interactions between the arene ligand and DNA, which may include arene intercalation and minor groove binding. In contrast, the single hydrocarbon rings in the p-cymene and benzene ruthenium complexes cannot interact with double-helical DNA by intercalation. Interestingly, the adducts of the complex containing p-cymene ligand, which has methyl and isopropyl substituents, distort the conformation and thermally destabilize double-helical DNA distinctly more than the adducts of the three multiring ruthenium arene compounds. It has been suggested that the different character of conformational alterations induced in DNA, and the resulting thermal destabilization, may affect differently further downstream different biological effects of this new class of metal-based antitumor compounds. The results point to a unique profile of DNA binding for Ru(II) arene compounds, suggesting that a search for new anticancer compounds based on this class of complexes may also lead to an altered profile of biological activity in comparison with that of metal-based antitumor drugs already used in the clinic or currently on clinical trials.
机译：抗肿瘤的单齿Ru（II）芳烃通式[（eta（6）-arene）Ru（en）Cl]（+）（芳烃=联苯，二氢蒽，四氢蒽，通过原子吸收，熔融行为，转录图谱，圆和线性二色性，质粒解绕，竞争性乙锭置换和微分脉冲极谱法研究了对伞花烃或苯; en =乙二胺）。结果表明，这些复合物优先结合双螺旋DNA中的鸟嘌呤残基。数据与包含联苯，二氢蒽或四氢蒽配体的复合物的DNA结合相一致，这涉及与G N7的联合配位以及芳烃配体和DNA之间的非共价疏水相互作用，其中可能包括芳烃嵌入和较小的凹槽结合。相反，对-异丙苯和苯钌络合物中的单个烃环不能通过嵌入与双螺旋DNA相互作用。有趣的是，具有对甲基苯异丙基取代基的对-甲基异丙基苯配体的复合物的加合物比三个多环钌芳烃化合物的加合物明显扭曲构象并使双螺旋DNA热不稳定。已经提出，在DNA中诱导的构象改变的不同特征，以及由此引起的热不稳定，可能进一步影响这种新型的基于金属的抗肿瘤化合物的下游的不同生物学作用。结果表明与钌（II）芳烃化合物的DNA结合具有独特的特征，这表明与金属基化合物相比，基于此类配合物寻找新的抗癌化合物也可能导致生物学活性的改变临床上已经使用或目前正在临床试验中使用的抗肿瘤药物。

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