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含N,S型配体的新型η-对异丙基苯钌(II)配合物的抗癌和抗菌性能、其结构及理论表征

Anticancer and antimicrobial properties of novel η--cymene ruthenium(ii) complexes containing a N,S-type ligand, their structural and theoretical characterization.

作者信息

Namiecińska Ewelina, Sadowska Beata, Więckowska-Szakiel Marzena, Dołęga Anna, Pasternak Beata, Grazul Magdalena, Budzisz Elzbieta

机构信息

Department of Cosmetic Raw Materials Chemistry, Medical University of Lodz Muszynskiego 1 90-151 Lodz Poland

Department of Immunology and Infectious Biology, Institute of Microbiology, Biotechnology and Immunology, Faculty of Biology and Environmental Protection, University of Lodz Banacha 12/16 90-237 Lodz Poland.

出版信息

RSC Adv. 2019 Nov 27;9(66):38629-38645. doi: 10.1039/c9ra08736b. eCollection 2019 Nov 25.

Abstract

Ruthenium(ii) complexes are lately of great scientific interest due to their chemotherapeutic potential as anticancer and antimicrobial agents. Here we present the synthesis of new pyrazole carbothioamide derivatives and their four arene-ruthenium complexes. The title compounds were characterized with the application of IR, NMR, mass spectrometry, elemental analysis and X-ray diffraction. Additionally, for new complexes DFT calculations were done. Their antimicrobial activity (MIC, MBC/MFC) was examined against , , , , and . Their cytotoxic effects, using the MTT assay, against three cancer cell lines: HL-60, NALM-6, WM-115 and normal human foreskin fibroblasts (HFF-1) were also investigated. The influence of the new arene-ruthenium(ii) complexes on the DNA structure was also tested. From our results, compound 2d showed higher cytotoxicity against melanoma cell line WM-115 than cisplatin. Strong biostatic and biocidal activity of the tested complexes against Gram-positive bacteria, including , and was demonstrated. The new arene-ruthenium(ii) compounds could not only inhibit proliferation of cancer cells, but also protect patients against malignant wound infections.

摘要

钌(II)配合物因其作为抗癌和抗菌剂的化疗潜力,近来受到了极大的科学关注。在此,我们展示了新型吡唑碳硫酰胺衍生物及其四种芳烃钌配合物的合成。通过红外光谱、核磁共振、质谱、元素分析和X射线衍射对标题化合物进行了表征。此外,对新配合物进行了密度泛函理论计算。检测了它们对金黄色葡萄球菌、表皮葡萄球菌、枯草芽孢杆菌、大肠杆菌、铜绿假单胞菌和白色念珠菌的抗菌活性(最低抑菌浓度、最低杀菌/杀真菌浓度)。还使用MTT法研究了它们对三种癌细胞系:HL-60、NALM-6、WM-115和正常人包皮成纤维细胞(HFF-1)的细胞毒性作用。还测试了新型芳烃钌(II)配合物对DNA结构的影响。从我们的结果来看,化合物2d对黑色素瘤细胞系WM-115的细胞毒性高于顺铂。已证明测试的配合物对革兰氏阳性菌,包括金黄色葡萄球菌、表皮葡萄球菌和枯草芽孢杆菌具有很强的抑菌和杀菌活性。新型芳烃钌(II)化合物不仅可以抑制癌细胞的增殖,还可以保护患者免受恶性伤口感染。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/785a/9075995/184e7265f87f/c9ra08736b-s1.jpg

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