33 research outputs found

    Novel 1,3,4-thiadiazole-chalcone hybrids containing catechol moiety: synthesis, antioxidant activity, cytotoxicity and DNA interaction studies

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    Hybrid compounds that combine the 1,3,4-thiadiazole-containing catechol moiety with a chalcone motif were synthesized and examined for their antioxidant activity, cytotoxicity, and DNA-binding activity. A series of thirteen compounds showed strong antioxidant and cytotoxic effects on human acute promyelocytic leukemia HL-60 cells. Several compounds exerted good cytotoxic activities on cervical adenocarcinoma HeLa cells. The treatment of HeLa cells with IC50 and double IC50 concentrations of the compounds 5a, 5c, 5f, and 5m induced a statistically significant increase in the percentage of cells within a subG1 cell cycle phase. The examined compounds caused G2/M cell cycle arrest in HeLa cells. Each of these compounds triggered apoptosis in HeLa cells through activation of caspase-3, the main effector caspase, caspase-8, which is involved in the extrinsic apoptotic pathway, and caspase-9, which is involved in the intrinsic apoptotic pathway. All of the examined compounds decreased the expression levels of MMP2 in HeLa cells and levels of protumorigenic miR-133b. Compounds 5a and 5m lowered the expression level of oncogenic miR-21 in HeLa cells. In addition, compounds 5a, 5f, and 5m decreased the expression levels of oncogenic miR-155 while the treatment of HeLa cells with compounds 5a, 5c, and 5f increased expression of tumor-suppressive miR-206. Observed effects of these compounds on expression levels of four examined miRNAs suggest their prominent cancer-suppressive activity. An investigation by absorption and fluorescence spectroscopy showed more efficient calf thymus DNA binding activity of the compound 5m in comparison to other tested compounds. Results of a pUC19 plasmid cleavage study and comet assay showed DNA damaging activities of compounds 5a and 5c.Related to published version:[https://imagine.imgge.bg.ac.rs/handle/123456789/1168]This is the peer reviewed version of the paper: Jakovljević, K., Joksović, M. D., Matić, I., Petrović, N., Stanojković, T., Sladić, D., Vujčić, M., Janović, B., Joksović, L., Trifunović, S., & Marković, V. (2018). Novel 1,3,4-thiadiazole-chalcone hybrids containing catechol moiety: Synthesis, antioxidant activity, cytotoxicity and DNA interaction studies. Medchemcomm, 9(10), 1679ā€“1697. [https://doi.org/10.1039/c8md00316e

    Sorption of textile dyes from textile wastewater by chitosan-based hydrogel

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    With the excessive risks that are present in today's environment, it is of great importance to treat wastewaters before their discharge in water streams. One of the everyday challenges is design of a low-cost and environmentally friendly sorbent such as hydrogel based on chitosan, itaconic and methacrylic acid that can remove wide range of textile dyes. In the present study, this hydrogel has been utilized for investigation of removal of three different azo dyes from simulated textile wastewater: C.I. Basic Blue 9, C.I. Basic Red 1 and C.I. Acid Orange 7. It was found that pH value of the solution had significant effect on dye sorption. Removal of basic dyes was successful at higher pH values, while sorption of acid dye was possible only at low pH value of solution. Simulated textile wastewater is a complex system with various salts, acids and polymers present beside dyes. Regardless of these components, excellent sorption capacity was achieved (more than 80% of dyes were removed), which makes this hydrogel attractive for use under real conditions

    PO-129 In vitro radiosensitivity and repair kinetics of PBMCs from prostate cancer patients and healthy donors evaluated by comet assay

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    A high cellular radiosensitivity is connected with a risk for development of severe side effects after radiotherapy. In this study we have attempted to find a correlation between the initial radiosensitivity of in vitro irradiated peripheral blood mononuclear cells (PBMC) of prostate cancer patients and the adverse side effects of radiotherapy

    Cu(II), Mn(II) and Zn(II) complexes of hydrazones with a quaternary ammonium moiety: synthesis, experimental and theoretical characterization and cytotoxic activity

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    In this paper, Cu(II), Mn(II) and Zn(II) complexes with N,N,N-trimethyl-2-oxo-2-(2-(1-(thiazol-2-yl)ethylidene)hydrazinyl)ethan-1-aminium chloride (HL1Cl) were synthesized and characterized by single-crystal X-ray diffraction, IR spectroscopy, elemental analysis and DFT calculations. In all three complexes, a ligand (L1) is coordinated in a deprotonated formally neutral zwitterionic form via NNO donor set atoms. Cu(II) and Zn(II) form mononuclear penta-coordinated complexes [CuL1(N3)(CH3OH)]BF4 and [ZnL1(N3)2], respectively, while Mn(II) forms a binuclear [Mn2L12(Ī¼-1,1-N3)2(N3)2]Ā·2CH3OH complex, with unusual distorted trigonal-prismatic geometry around the metal centers. The antimicrobial activity of these complexes was tested against a panel of Gram-negative and Gram-positive bacteria, two yeasts and one fungal strain. The binuclear Mn(II) complex showed antifungal activity of similar intensity to amphotericin B. Based on the results of the brine shrimp test and DPPH radical scavenging activity, the most active Cu(II) and Mn(II) complexes were selected for evaluation of cytotoxic activity against five malignant cancer cell lines (HeLa, A375, MCF7, PC-3 and A549) and one normal cell line HaCaT. Both complexes showed significant activity. It should be pointed out that the activity of the Mn(II) complex against the MCF7 breast cancer cell line is only slightly weaker than that of cisplatin, but with selectivity to the tumor cell line in comparison to normal HaCaT cells, which is non-existent in the case of cisplatin.Related crystallographic data (CCDC 2110386): []Related crystallographic data (CCDC 2110387): []Related crystallographic data (CCDC 2110388): [

    Supporting information for: "Cu(II), Mn(II) and Zn(II) complexes of hydrazones with a quaternary ammonium moiety: synthesis, experimental and theoretical characterization and cytotoxic activity"

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    In this paper, Cu(II), Mn(II) and Zn(II) complexes with N,N,N-trimethyl-2-oxo-2-(2-(1-(thiazol-2-yl)ethylidene)hydrazinyl)ethan-1-aminium chloride (HL1Cl) were synthesized and characterized by single-crystal X-ray diffraction, IR spectroscopy, elemental analysis and DFT calculations. In all three complexes, a ligand (L1) is coordinated in a deprotonated formally neutral zwitterionic form via NNO donor set atoms. Cu(II) and Zn(II) form mononuclear penta-coordinated complexes [CuL1(N3)(CH3OH)]BF4 and [ZnL1(N3)2], respectively, while Mn(II) forms a binuclear [Mn2L12(Ī¼-1,1-N3)2(N3)2]Ā·2CH3OH complex, with unusual distorted trigonal-prismatic geometry around the metal centers. The antimicrobial activity of these complexes was tested against a panel of Gram-negative and Gram-positive bacteria, two yeasts and one fungal strain. The binuclear Mn(II) complex showed antifungal activity of similar intensity to amphotericin B. Based on the results of the brine shrimp test and DPPH radical scavenging activity, the most active Cu(II) and Mn(II) complexes were selected for evaluation of cytotoxic activity against five malignant cancer cell lines (HeLa, A375, MCF7, PC-3 and A549) and one normal cell line HaCaT. Both complexes showed significant activity. It should be pointed out that the activity of the Mn(II) complex against the MCF7 breast cancer cell line is only slightly weaker than that of cisplatin, but with selectivity to the tumor cell line in comparison to normal HaCaT cells, which is non-existent in the case of cisplatin.The supporting information for: Stevanović, Nevena, Zlatar, Matija, Novaković, Irena, Pevec, Andrej, Radanović, DuÅ”anka, Matić, Ivana Z., Đorđić Crnogorac, Marija, Stanojković, Tatjana, Vujčić, Miroslava, Gruden, Maja, Sladić, DuÅ”an, Anđelković, Katarina, Turel, Iztok, Čobeljić, Božidar, "Cu(II), Mn(II) and Zn(II) complexes of hydrazones with a quaternary ammonium moiety: synthesis, experimental and theoretical characterization and cytotoxic activity" in Dalton Transactions, 51, no. 1 (2022):185-196, [https://doi.org/10.1039/D1DT03169D]Published article: [https://cherry.chem.bg.ac.rs/handle/123456789/4857]Related crystallographic data (CCDC 2110386): [https://cherry.chem.bg.ac.rs/handle/123456789/4859]Related crystallographic data (CCDC 2110387): [https://cherry.chem.bg.ac.rs/handle/123456789/4860]Related crystallographic data (CCDC 2110388): [https://cherry.chem.bg.ac.rs/handle/123456789/4861

    PO-410 Cytotoxicity and genotoxicity of new gadolinium, iron oxide, cobalt ferrite and graphene oxide nanoparticles on some tumour cell lines in vitro

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    Nanoparticles (NPs) are increasingly used in cancer therapy as delivery agents and in the diagnosis of malignant diseases as contrast agents for magnetic resonance imaging (MRI). The aim of this work was in vitro assessments of Gd-NPs, Fe- NPs, CoFe-NPs and Graphene Oxide-NPs cytotoxicity and genotoxicity on some tumour and normal human cell lines.Abstracts of the 25th Biennial Congress of the European Association for Cancer Research, Amsterdam, The Netherlands, 30 June ā€“ 3 July 201
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