Yazar "Korkmaz C.G." seçeneğine göre listele

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    Antimicrobial and cytotoxic studies of new 2-substitue-1H-benzimidazole derivatives [Yeni 2-sübstitüe-1H-benzimidazol türevi bileşikler üzerinde antimikrobiyal ve sitotoksik çali{dotless}şmalar]
    (University of Istanbul, 2011) Sarikaya G.; Alpan A.S.; Taşli H.; Sevin G.; Korkmaz C.G.; Güneş H.S.
    We synthesized a series of 2-substituted-1H-benzimidazole derivatives (1-9) of which six of them were original and elucidated their structures by spectral analyses. We also evaluated the in-vitro antimicrobial activities of the synthesized compounds and detected potent inhibitory action in some of the compounds. Moreover, 2-(1H-benzimidazole-2-yl)phenol intermediates, bearing o-hydroxyphenyl substituent on 1H-benzimidazole ring possess equal or similar results compared to the standard compound, Ceftazidime. The synthesized compounds didn't show any significant antifungal activity on Candida albicans. All nine 1H-benzimidazole derivatives were tested for their cytotoxicity through WST-1 colorimetric assay-based in vitro tests on the mammalian LNCaP cell line. Compounds 7 and 8 were found to have IC50 values of 0,09 ± 0,01 µM and 0,03 ± 0,02 µM, respectively. It is noteworthy that the values obtained with these two compounds were highly comparable to that of Doxorubicine 0,053 ± 0,003 µM, the reference drug used in our study.
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    Doxycycline down-regulates matrix metalloproteinase expression and inhibits NF-?b signalling in LPS-induced PC3 cells
    (Via Medica, 2016) Ogut D.; Reel B.; Korkmaz C.G.; Arun M.Z.; Micili S.C.; Ergur B.U.
    Introduction. Matrix metalloproteinase enzymes (MMPs) play important role in inflammation, malignant cell proliferation, invasion and angiogenesis by mediating extracellular matrix degradation. Doxycycline, a synthetic tetracycline, behaves as a MMP inhibitor at a subantimicrobial dose and inhibits tumor cell proliferation, invasion and angiogenesis. The aberrant activity of nuclear factor kappa B (NF-?B) causes activation of MMPs and thereby proliferation and invasion of cancer cells. The aim of this study was to investigate the effects of doxycycline on the expression of MMPs in lipopolysaccharide (LPS)-induced PC3 human prostate cancer cells and the possible role of NF-?B signaling. Material and methods. PC3 cells were incubated with LPS (0.5 µg/mL) for 24 h in the presence or absence of doxycycline (5 µg/mL). The effects of LPS and doxycycline on the expressions of MMP-2, MMP-8, MMP-9, MMP-10, NF-?B/p65, I?B-?, p-I?B-?, IKK-ß were examined by Western blotting and immunohistochemistry in PC3 cells. Furthermore, relative proteinase activities of MMP-2 and MMP-9 were determined by gelatin zymography. Results. LPS increased expression and activity of MMP-9 and expression of MMP-8, MMP-10, NF-?B/p65, p-I?B-?, IKK-ß and doxycycline down-regulated its effects with the exception of MMP-10 expression. The expression of MMP-2 and I?B-a was affected by neither LPS nor doxycycline. Conclusions. Our findings indicate that doxycycline inhibits the expression of various MMPs and NF-?B signaling may play a role in the regulation of MMPs expression in LPS-induced PC3 human prostate cancer cells. ©Polish Society for Histochemistry and Cytochemistry.