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    Wyświetlanie 1-3 z 3
    Tytuł:
    PEGYLATED GEMCITABINE AND METHOTREXATE: IN VITRO CYTOTOXICITY ANALYSIS AND IN VIVO DRUG RELEASE PROFILING TO ASSESS THEIR ENHANCED BLOOD CIRCULATION
    Autorzy:
    Ahmed, Mahmood
    Powiązania:
    https://bibliotekanauki.pl/articles/895274.pdf
    Data publikacji:
    2019-08-30
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    drug delivery
    anti-proliferation
    Pegylation
    spheroids
    Opis:
    In the present study, four new pegylated drugs were synthesized to investigate the anticancer activity. All the compounds were characterized on the basis of FTIR and 1HNMR. The new compounds were evaluated against HCT116 cell line by CellTiter-Glo® 3D cell viability assay. The sustained release pattern of newly synthesized compounds were also evaluated, slow released lasts for 240 h which was confirmed by in vivo and in vitro drug release profile. The sustained and controlled release behavior of pegylated drugs over the extended period of time showed a linear profile and this release pattern was not limited to diffusion process instead supporting chemically controlled release pattern which was dependent only on how fast the compound hydrolyzed. The newly designed pegylated drugs showed almost same killing effect against the cancer cells as the free drugs. The compounds with lower cLogP value showed more antiproliferative (lower IC50) effect due their higher cell permeability.
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2019, 76, 4; 653-659
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    CAMPTOTHECIN INHIBITS MIGRATION, INVASION AND CLONOGENIC PROPERTY OF LIVER CANCER CELLS BY MODULATING MICRORNA EXPRESSION
    Autorzy:
    Liu, Zhenzhong
    Wu, Song
    Li, Xiaoqian
    Powiązania:
    https://bibliotekanauki.pl/articles/895460.pdf
    Data publikacji:
    2020-04-29
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    Hepatocellular Carcinoma
    cell proliferation
    cell cycle
    Camptothecin
    miRNA
    Opis:
    Camptothecin (CPT), an alkaloid natural product, extracted from Camptotheca acuminata bark, has been reported to have potential antitumor activity in diverse cancers. MicroRNAs (MiRNAs) are a class of short, non-coding RNAs that plays a crucial role in the normal physiology by attenuating translation. Here, we showed that the CPT modulates the expression of miRNAs in hepatocellular carcinoma cells (HCC). Microarray analysis reveals that CPT modulates the expression of as many as 39 miRNAs in HCC cells (Huh7), 27 miRNAs were downregulated whereas 12 miRNAs were upregulated. miR-16 is the key miRNA upregulated by CPT and targets key prosurvival proteins (MMP-2, MMP-9 and cyclin D1). Our results demonstrate that CPT is inhibiting cell viability of HCC cells significantly when compared with the untreated cells. Wound healing and colony formation assay confirm inhibition of cell migration and clonogenic property of Huh7 cells respectively, upon the dose-dependent treatment of CPT. Furthermore, the Boyden chamber assay analysis revealed a significant inhibition of number of invasive cells in CPT treated cells with comparison to untreated Huh7 cells. Mechanistically, CPT upregulates miR-16 expression which targets MMP-2, MMP-9, cyclin D1 downregulation and subsequently upregulates the expression of E-cadherin, TIMP1, p21, and p27, thereby inhibits cell migration, invasion and clonogenic property of HCC cells. In summary, CPT treatment in Huh7 cells decreases cell viability and upregulates miR-16 expression, which results in inhibition of cell migration, invasion and clonogenic property of cells, by decreasing MMP-2, MMP-9, cyclin D1 and increasing the expression of cell cycle-regulated proteins p21 and p27.
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2020, 77, 2; 295-304
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Synthesis, immunosuppressive properties, mechanism of action and X-ray analysis of a new class of isoxazole derivatives
    Autorzy:
    Bąchor, Urszula
    Ryng, Stanisław
    Mączyński, Marcin
    Artym, Jolanta
    Kocięba, Maja
    Zaczyńska, Ewa
    Kochanowska, Iwona
    Tykarska, Ewa
    Zimecki, Michał
    Powiązania:
    https://bibliotekanauki.pl/articles/895268.pdf
    Data publikacji:
    2019-04-30
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    apoptosis
    proliferation
    isoxazoles
    Passerini three-component reaction
    Jurkat cells
    Opis:
    In the search for potential therapeutics, isoxazole derivatives are still objects of interest. Previously described immunoregulatory properties of 5-amino-3-methyl-4-isoxazolecarboxylic acid (AC) benzylamides prompted us to synthesize a new class of compounds of immunotropic activity. A series of new compounds containing the isoxazole moiety were synthesized using Passerini three-component reaction. The effects on phytohemagglutinin A (PHA)-induced proliferation of human peripheral blood mononuclear cells (PBMC), production of tumor necrosis factor alpha (TNF α) in human whole blood cultures stimulated with lipopolysaccharide (LPS) and two-way mixed lymphocyte reaction (MLR) of PBMC, were investigated. Also, the effect of 1-(cyclohexylcarbamoyl)cyclohexyl 5-amino-3-methylisoxazole-4-carboxylate (PUB1) on the expression of signaling molecules associated with cell apoptosis in Jurkat cells was also determined. The results showed that the compounds inhibited to various degree mitogen-induced PBMC proliferation in a dose-dependent manner and TNF α production at 10 μg/ml. PUB1 compound, selected on the basis of its strongest antiproliferative activity, was also shown to inhibit MLR. The molecular data suggest that immunosuppressive action of PUB1 depended on induction of Fas and elevation of caspase 8 expression. In summary, we revealed immunosuppressive properties of a new class of isoxazoles and established the mechanism of action of a representative PUB1 compound.
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2019, 76, 2; 251-263
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
      Wyświetlanie 1-3 z 3

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