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Öğe Effective anticancer agents based-on two Pillar[5]arene derivatives for pancreas cancer cell lines: synthesis, apoptotic effect, caspase pathway(Springer, 2023) Karaselek, Mehmet Ali; Kuccukturk, Serkan; Duran, Tugce; Kursunlu, Ahmed Nuri; Ozmen, Mustafa; Bozdag, Ceren; Alkan, SelmanThis study aimed to evaluate the possible anticancer effects of two different pillar[5]arene derivatives (5Q-[P5] and 10Q-P[5]) on two different pancreatic cancer cell lines in vitro. For this purpose, changes in the expression of major genes that play a role in apoptosis and caspase pathways were investigated. Panc-1 and BxPC-3 cell lines were used in the study and the cytotoxic dose of pillar[5]arenes was determined by the MTT method. Changes in gene expression after pillar[5]arenes treatment were evaluated by real-time polymerase chain reaction (qPCR). Apoptosis was studied by flow cytometry. As a result of analysis, it was determined that proapoptotic genes and genes involved in major caspase activation were upregulated and antiapoptotic genes were down-regulated in Panc-1 cell line treated with pillar[5]arenes. Flow cytometric apoptosis analysis also showed an increased apoptosis rate in this cell line. On the contrary, although MTT analysis showed cytotoxic effect in BxPC-3 cell line treated with two pillar[5]arene derivatives, the apoptosis pathway was not active. This suggested that it may activate different death pathways for BxPC-3 cell line. Thus, it was first determined that the pillar[5]arene derivatives reduced cancer cell proliferation on pancreatic cancer cells.Öğe Impacts of potential anticancer agents based on pillar[5]arene for head and neck squamous cell carcinoma cells(Springer, 2023) Kuccukturk, Serkan; Karaselek, Mehmet Ali; Duran, Tugce; Kursunlu, Ahmed Nuri; Ozmen, MustafaPurposeThis study was conducted to investigate impacts of potential anticancer (associated with apoptosis and caspase pathways) of two newly synthesized derivatives of pillar[5]arene, named as d-Q-P5 and p-Q-P5, on Squamous cell carcinomas of the head and neck (HNSCC) cells.Materials and methodsThe MTT method was used to determine the IC50 doses of the derivatives on HNSCC cells, and the changes in gene expression were analyzed by real-time polymerase chain reaction (qPCR). The apoptosis change was confirmed by flow cytometry analysis.ResultsThe results showed that the d-Q-P5 and p-Q-P5 effectively inhibited the proliferation of the cells by upregulating proapoptotic genes (Bax, Bad, p53, Bak, and Apaf-1) and genes involved in the caspase pathway (Casp2, Casp3, and Casp9), while downregulating the antiapoptotic gene (Bcl-2).ConclusionsThis study is the first to demonstrate the potential anticancer effects of these two agents on HNSCC cells by positively regulating apoptosis gene expression.Öğe Synthesis and evaluation of anticancer effect of a novel molecule based-on pillar[5]arene including multi quinoline units(Springer Birkhauser, 2020) Gunes, Canan Eroglu; Karaselek, Mehmet Ali; Kursunlu, Ahmed Nuri; Ozmen, Mustafa; Kurar, ErcanIn this study, pillar[5]arene containing ten terminal alkynyl-functional group was prepared and carried out an optimization procedure for target molecule with using 5-hydroxyquinoline molecule known with biological activity. The novel molecule was named as iso-QP[5] and characterized by FT-IR, melting point, NMR, elemental analysis, and mass spectroscopy. The aim was to evaluate the anticancer effects of iso-QP[5] on MCF7 human breast cancer cells. The IC50 dose of iso-QP[5] in MCF7 cells was found to be 25 mu M for 24 h using XTT assay. Expressions of eight genes for apoptosis were determined by qPCR. The results showed a significant increase in the expression of BAX, CASP3, CASP9, CYCS, and P53 genes after treatment with iso-QP[5] in MCF7 cells. However, iso-QP[5] treatment significantly decreased expression of BCL2 and CASP8 genes. It is concluded that novel molecule iso-QP[5] caused apoptosis by regulating genes that are important in apoptosis in human breast cancer cells.