Ru(II)/diclofenac-based complexes: DNA, BSA interaction and their anticancer evaluation against lung and breast tumor cells.,Dalton Transactions

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Ru(II)/diclofenac-based complexes: DNA, BSA interaction and their anticancer evaluation against lung and breast tumor cells.
Dalton Transactions ( IF 3.5 ) Pub Date : 2020-08-15 , DOI: 10.1039/d0dt01591a
Katia M Oliveira ₁ , João Honorato ₂ , Guilherme R Gonçalves ₁ , Marcia R Cominetti ₃ , Alzir A Batista ₂ , Rodrigo S Correa ₁

Affiliation

Ruthenium(II) diclofenac-based complexes of the general formula [Ru(dicl)(P–P)(bpy)]PF₆ [dicl = diclofenac, bpy = 2,2′-bipyridine, and P–P = 1,4′-bis(diphenylphosphino)butane (dppb) (1), 1,2′-bis(diphenylphosphino)ethane (dppe) (2), 1,3′-bis(diphenylphosphino)propane (dppp) (3) and 1,1′-bis(diphenylphosphino)ferrocene (dppf) (4)] are synthesized. The complexes (1–4) are characterized by elemental analyses, infrared, NMR, and UV-vis spectroscopy and (3) and (4) are characterized by single crystal X-ray diffraction. The DNA binding of complexes (1–4), studied by circular dichroism (CD) and Hoechst 33 258 staining assay, indicates their binding with the minor grooves. The complexes interact with BSA with binding constants (K_b) in the range of 2.5 × 10³–5.5 × 10⁴ M⁻¹. The complexes exhibit high cytotoxicity against the tumor cell lines A549, MDA-MB-231, and MCF-7 with IC₅₀ values ranging from 0.56 to 15.28 μM. The complexes are more selective for the hormone-dependent MCF-7 breast tumor cell line and complex (1) is the most potent one. The study demonstrates the anticancer activity of ruthenium(II)/diclofenac-based complexes.

中文翻译：

Ru（II）/双氯芬酸基复合物：DNA，BSA相互作用及其对肺和乳腺肿瘤细胞的抗癌评估。

通式[Ru（dicl）（P-P）（bpy）] PF ₆的基于钌（II）双氯芬酸的配合物[dicl =双氯芬酸，bpy = 2,2'-联吡啶，P–P = 1,4 ′-双（二苯基膦基）丁烷（dppb）（1），1,2'-双（二苯基膦基）乙烷（dppe）（2），1,3'-双（二苯基膦基）丙烷（dppp）（3）和1，合成1'-双（二苯基膦基）二茂铁（dppf）（4）]。配合物（1-4）的特征在于元素分析，红外，NMR和UV-vis光谱学，（3）和（4）的特征在于单晶X射线衍射。复合物的DNA结合（1-4），通过圆二色性（CD）和Hoechst 33 258染色分析研究，表明它们与小沟的结合。配合物以2.5×10 ³ –5.5×10 ⁴ M ^-1的结合常数（K _b）与BSA相互作用。该复合物表现出对肿瘤细胞系A549，MDA-MB-231和MCF-7的高细胞毒性，IC ₅₀值为0.56至15.28μM。复合物对激素依赖性MCF-7乳腺癌细胞系具有更高的选择性，复合物（1）是最有效的一种。该研究证明了钌（II）/双氯芬酸基复合物的抗癌活性。

更新日期：2020-09-22

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