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    Wyświetlanie 1-7 z 7
    Tytuł:
    Antiproliferative activity of new benzimidazole derivatives
    Autorzy:
    Błaszczak-Świątkiewicz, Katarzyna
    Olszewska, Paulina
    Mikiciuk-Olasik, Elżbieta
    Powiązania:
    https://bibliotekanauki.pl/articles/1039545.pdf
    Data publikacji:
    2013
    Wydawca:
    Polskie Towarzystwo Biochemiczne
    Tematy:
    anticancer activity
    ntiproliferation
    apoptosis
    benzmidazole
    hypoxia
    nitrobenzimidazole
    Opis:
    A series of new benzimidazole derivatives were synthesized and tested in vitro for possible anticancer activity. Their effect of proliferation into selected tumor cell lines at normoxia and hypoxia conditions was determined by WST-1 test. Additionally, apoptosis test (caspase 3/7 assay) was used to check the mode caused by the agents of cell death. Four of the examined compounds (7, 8, 13, 11) showed a very good antiproliferative effect and three of them were specific for hypoxia conditions (8, 14, 11). Compound 8 was the most cytotoxic against human lung adenocarcinoma A549 cells at hypoxic conditions. Hypoxia/ normoxia cytotoxic coefficient of compound 14 (4.75) is close to hypoxia/normoxia cytotoxic coefficient of tirapazamine (5.59) - a reference compound in our experiments and this parameter locates it between mitomycin C and 2-nitroimidazole (misonidazole). Screening test of caspase-dependent apoptosis proved that exposure to A549 cells of compounds 7-8 and 13-14 for 48 h promote apoptotic cell death. These results supplement our earlier study of the activity of new potentialy cytotoxic heterocyclic compounds against selected tumor cells.
    Źródło:
    Acta Biochimica Polonica; 2013, 60, 3; 427-433
    0001-527X
    Pojawia się w:
    Acta Biochimica Polonica
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    STUDIES TOWARDS HEMOCOMPATIBILITY OF POLYAMINE CONJUGATES WITH BICYCLIC SYSTEMS
    Autorzy:
    Szumilak, Marta
    Markowicz-Piasecka, Magdalena
    Mikiciuk-Olasik, Elzbieta
    Stanczak, Andrzej
    Sikora, Joanna
    Powiązania:
    https://bibliotekanauki.pl/articles/895466.pdf
    Data publikacji:
    2018-08-31
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    coagulation
    biocompatibility
    fibrinolysis
    erythrotoxicity
    polyamine conjugates
    Opis:
    Assessing hemocompatibility of anticancer drug candidate is very important task due to the fact that coagulation disorders are often correlated with malignancy or induced by chemotherapy. The aim of this study was to examine the influence of some polyamine conjugates with bicyclic systems on the process of coagulation and fibrinolysis. In addition their effect on the healthy human erythrocytes (RBCs) was assessed. Prothrombin Time (PT), Activated Partial Tromboplastin Time (APTT), clot formation and lysis test (CL-test) were performed to evaluate the influence of some polyamine conjugates on plasma hemostasis. The effects of tested compounds on RBCs were assessed using hemolysis assays and microscopy studies. APTT and PT examination revealed that all tested compounds apart from the highest concentrations of compounds 3 and 5 did not exert significant effects on intrinsic and extrinsic coagulation pathways. Despite their substantial influence on the kinetic parameters of the process of clot formation and fibrinolysis, the examined compounds, over the entire concentration range, did not alter the overall potential of clot formation and lysis (CLAUC) suggesting that they might be regarded as biocompatible concerning plasma hemostasis. At potential therapeutic concentrations (constituting IC50 value for MCF-7 cells) tested polyamine conjugates showed no adverse effects on the membranes of RBCs. Promising antiproliferative activity of representative polyamine conjugates together with their hemocompatibility make them good anticancer drug candidates for further preclinical evaluation.
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2018, 75, 4; 861-874
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    New benzimidazole derivatives with potential cytotoxic activity - study of their stability by RP-HPLC
    Autorzy:
    Błaszczak-Świątkiewicz, Katarzyna
    Mirowski, Marek
    Kaplińska, Katarzyna
    Kruszyński, Rafał
    Trzęsowska-Kruszyńska, Agata
    Mikiciuk-Olasik, Elżbieta
    Powiązania:
    https://bibliotekanauki.pl/articles/1039749.pdf
    Data publikacji:
    2012
    Wydawca:
    Polskie Towarzystwo Biochemiczne
    Tematy:
    benzimidazole
    hypoxia
    RP-HPLC
    nitrobenzimidazole
    anti-cancer drugs
    Opis:
    Obtained benzimidazole derivatives, our next synthesized heterocyclic compounds, belong to a new group of chemical bondings with potential anticancer properties (Błaszczak-Świątkiewicz & Mikiciuk-Olasik, 2006, J Liguid Chrom Rel Tech 29: 2367-2385; Błaszczak-Świątkiewicz & Mikiciuk-Olasik, 2008, Wiad Chem 62: 11-12, in Polish; Błaszczak-Świątkiewicz & Mikiciuk-Olasik, 2011, J Liguid Chrom Rel Tech 34: 1901-1912). We used HPLC analysis to determine stability of these compounds in 0.2% DMSO (dimethyl sulfoxide). Optimisation of the chromatographic system and validation of the established analytical method were performed. Reversed phases (RP-18) and a 1:1 mixture of acetate buffer (pH 4.5) and acetonitrile as a mobile phase were used for all the analysed compounds at a flow rate 1.0 mL/min. The eluted compounds were monitored using a UV detector, the wavelength was specific for compounds 6 and 9 and compounds 7 and 10. The retention time was specific for all four compounds. The used method was found to have linearity in the concentration range of (0.1 mg/mL-0.1 μg/mL) with a correlation coefficient not less than r2=0.9995. Statistical validation of the method proved it to be a simple, highly precise and accurate way to determine the stability of benzimidazole derivatives in 0.2% DMSO. The recoveries of all four compounds examined were in the range 99.24-100.00%. The developed HPLC analysis revealed that the compounds studied remain homogeneous in 0.2% DMSO for up to 96 h and that the analysed N-oxide benzimidazole derivatives do not disintegrate into their analogues - benzimidazole derivatives. Compounds 8, 6 and 9 exhibit the best cytotoxic properties under normoxic conditions when tested against cells of human malignant melanoma WM 115.
    Źródło:
    Acta Biochimica Polonica; 2012, 59, 2; 279-288
    0001-527X
    Pojawia się w:
    Acta Biochimica Polonica
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
      Wyświetlanie 1-7 z 7

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