Papers by Nina Rembialkowska
Acta Crystallographica Section C: Structural Chemistry, Sep 23, 2022
Derivatives of pyrido[3,4-d]pyridazine, namely, 1-hydroxy-5-methyl-7-phenylpyrido[3,4-d]pyridazin... more Derivatives of pyrido[3,4-d]pyridazine, namely, 1-hydroxy-5-methyl-7-phenylpyrido[3,4-d]pyridazin-4(3H)-one dimethylformamide monosolvate, C14H11N3O2·C3H7NO (2), ethyl [1-(2-ethoxy-2-oxoethoxy)-5-methyl-4-oxo-7-phenyl-3,4-dihydropyrido[3,4-d]pyridazin-3-yl]acetate, C18H17N3O4 (3), and ethyl [(5-methyl-4-oxo-7-phenyl-3,4-dihydropyrido[3,4-d]pyridazin-1-yl)oxy]acetate, C22H23N3O6 (4), were synthesized with the aim of discovering new potential biologically active agents. The properties of all three derivatives were characterized by 1H NMR, 13C NMR and FT–IR spectroscopic analysis. All the crystals were obtained by a solvent diffusion method from dimethylformamide (DMF) or dimethyl sulfoxide (DMSO) and characterized by single-crystal X-ray diffraction. The collected X-ray data revealed that the crystals of 2 and 4 belong to the triclinic space group P\overline{1}, whereas the crystal of 3 belongs to the monoclinic space group P21/c. The presented derivatives crystallized with one molecule in the asymmetric unit, but only compound 2 crystallized as a solvate with DMF. Structure analysis showed that the molecule of 2 exists as its amide–imidic acid tautomer and that O-alkylation occurred before N-alkylation during the synthesis of the mono- and disubstituted derivatives, i.e. 3 and 4, respectively. The molecular geometries of the 5-methyl-7-phenylpyrido[3,4-d]pyridazine core within the studied derivatives differ in the mutual orientation of the rings. The interplanar angles between the heterocyclic ring and the bound aromatic ring are 1.71 (7), 18.16 (3) and 3.1 (1)° for 2, 3 and 4, respectively. The potential cytotoxicity of these compounds was evaluated against one normal (HaCat) and four human cancer cell lines (A549, DU145, MDA-MB-231 and SKOV-3).
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Pharmaceuticals, Jan 13, 2022
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Bioelectrochemistry, Oct 1, 2023
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Bioelectrochemistry, Jun 1, 2022
Electroporation is a phenomenon of transient or irreversible permeabilization of the cell membran... more Electroporation is a phenomenon of transient or irreversible permeabilization of the cell membrane after pulsed electric field treatment. Fluorescent probes are frequently used to assess the extent of permeabilization, however, as an alternative, a D-luciferin oxidation-based method can be used. In this work, we have used sequences of a microsecond (1.3 kV/cm × 100 µs) and nanosecond (12.5 kV/cm × 100 ns) pulses to trigger various levels of cell permeabilization and assessed the differences in the response using a conventional fluorescent probe (YO-PRO-1 (YP)) and D-luciferin oxidation methodology. The nanosecond pulses (n = 5-100) have been delivered with 1 kHz repetition frequency, and the results were compared with 1 MHz protocols. Additionally, the effects of extracellular Ca2+ have been assessed. Various concentrations of CaCl2 (2, 5, and 10 mM) have been used, and it was shown that the bioluminescence of the cells after electroporation depends on extracellular calcium concentration. It was shown that the changes in bioluminescence signal could be used as a marker of cell membrane permeabilization on par with YP assay when calcium is added and thus, effectively employed for analysis of electroporation phenomenon in vitro both for nanosecond and microsecond pulses.
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International Journal of Molecular Sciences, Oct 26, 2022
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World Scientific News, 2019
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Bioelectrochemistry, Dec 1, 2022
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Bioelectrochemistry, Apr 1, 2023
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Anticancer Research, Jul 1, 2019
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Photodiagnosis and Photodynamic Therapy, Mar 1, 2017
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in Vivo, 2019
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Slovenian Veterinary Research, Dec 28, 2017
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Frontiers in Oncology, Sep 14, 2022
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Medicinal Chemistry, Nov 18, 2019
Background: Hydrazine-hydrazones represent a group of bioactive compounds that display antibacter... more Background: Hydrazine-hydrazones represent a group of bioactive compounds that display antibacterial, anti-inflammatory, antiviral or anticancer activities. Methods: The group of new derivatives was evaluated by the viability assay in human cancer and normal cells. Results: The dimethylpyridine hydrazones showed potent inhibition of cell proliferation of breast, colon cancer cells, human melanoma and glioblastoma. Compound 12 inhibited proliferation of cancer cells exhibiting a drug-resistant phenotype (MCF-7/DX and LoVoDX) at low millimolar concentrations. Whereas, antimelanoma activity was revealed by Compounds 2, 4, 7 and 12. Conclusion: The present results highlighted newly synthetized hydrazine derivatives an excellent base for the design of new anticancer agents and resistance inhibitors.
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Pharmaceuticals
Breast cancer ranks among the top three most common malignant neoplasms in Poland. The use of cal... more Breast cancer ranks among the top three most common malignant neoplasms in Poland. The use of calcium ion-assisted electroporation is an alternative approach to the classic treatment of this disease. The studies conducted in recent years confirm the effectiveness of electroporation with calcium ions. Electroporation is a method that uses short electrical pulses to create transitional pores in the cell membrane to allow the penetration of certain drugs. The aim of this study was to investigate the antitumor effects of electroporation alone and calcium ion-assisted electroporation on human mammary adenocarcinoma cells that are sensitive (MCF-7/WT) and resistant to doxorubicin (MCF-7/DOX). The cell viability was assessed using independent tests: MTT and SRB. The type of cell death after the applied therapy was determined by TUNEL and flow cytometry (FACS) methods. The expression of Cav3.1 and Cav3.2 proteins of T-type voltage-gated calcium channels was assessed by immunocytochemistry, ...
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Applied Sciences
Electrochemotherapy (ECT) with bleomycin has been effectively used in recent years to treat vario... more Electrochemotherapy (ECT) with bleomycin has been effectively used in recent years to treat various skin tumors. Microsecond electric pulses significantly improve bleomycin (BLM) delivery and its anticancer potential. Up to now, we can determine electric field distribution in the targeted tissue, however, the distribution of the injected drug is still not well known. In this study, we propose the combination of indocyanine green (ICG) with bleomycin as a practical approach for ECT, enabling drug distribution control and detection. Normal skeletal muscle (L6) and fibrosarcoma (WEHI-164) cells were used for the viability evaluation by MTT assay after 24 and 72 h. Cells were exposed to the ESOPE protocol alone and in combination with drugs. Additionally, visualization of the uptake of ICG and ICG + BLM supported by electroporation was performed by confocal microscopy. The mast cell tumor (MCTs) was diagnosed in the feline case. The mixture of ICG + BLM was injected into the tumor, and ...
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International Journal of Molecular Sciences
Cancer is one of the greatest challenges in modern medicine today. Difficult and long-term treatm... more Cancer is one of the greatest challenges in modern medicine today. Difficult and long-term treatment, the many side effects of the drugs used and the growing resistance to treatment of neoplastic cells necessitate new approaches to therapy. A very promising targeted therapy is based on direct impact only on cancer cells. As a continuation of our research on new biologically active molecules, we report herein the design, synthesis and anticancer evaluation of a new series of N-Mannich-base-type hybrid compounds containing morfoline or different substituted piperazines moieties, a 1,3,4-oxadiazole ring and a 4,6-dimethylpyridine core. All compounds were tested for their potential cytotoxicity against five human cancer cell lines, A375, C32, SNB-19, MCF-7/WT and MCF-7/DX. Two of the active N-Mannich bases (compounds 5 and 6) were further evaluated for growth inhibition effects in melanoma (A375 and C32), and normal (HaCaT) cell lines using clonogenic assay and a population doubling tim...
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Biochimica et Biophysica Acta (BBA) - Biomembranes
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Photodiagnosis and Photodynamic Therapy, 2017
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Neoplasma, 2016
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Papers by Nina Rembialkowska