Proapoptotic effects of novel thiazole derivative on human glioma cells.
作者： Nataliya Finiuk , Olha Klyuchivska , Iryna Ivasechko , Volodymyr Hreniukh , Yuriy Ostapiuk
DOI: 10.1097/CAD.0000000000000686
关键词:
摘要: The aim of the present study was to investigate antiproliferative and proapoptotic actions N-(5-benzyl-1,3-thiazol-2-yl)-3,5-dimethyl-1-benzofuran-2-carboxamide derivative (compound 5) in glioma cells comparison with temozolomide (TMZ) doxorubicin (Dox), used as positive controls. activity compound 5, TMZ, Dox on human glioblastoma U251 multiform T98G measured using MTT test. Western blot analysis, fluorescent microscopy, agarose gel retardation assay, flow cytometric DNA comet assay under alkaline conditions were carried out effect 5 cells. This showed ~20 times higher cytotoxicity toward compared effects TMZ approximately two than that Dox. Compound induced apoptosis by PARP1 caspase 3 cleavage mechanisms, also inducing an increase level Bax Bim proteins a decrease phosho-ERK1/2 kinase. associated production hydrogen peroxide formation single-strand breaks. did not intercalate into molecule. Thus, novel thiazole proved be potential antiglioma drug much cytotoxic action Its is induction, reactive oxygen species, breaks without significant intercalation.
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