4-Propargyl-substituted 1H-pyrroles induce apoptosis and autophagy via extracellular signal-regulated signaling pathway in breast cancer

2021-01-01
Atmaca, Harika
Ilhan, Suleyman
Yılmaz, Elif Serel
Zora, Metin
Show full item record
Creative Commons License
This work is licensed under a Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.
48
views
0
downloads
Novel pyrrole derivatives (PDs) with propargyl units (1–7) were investigated for their anticancer activity on breast cancer cells. The MTT assay was used to assess the cell viability. Morphological changes in human breast cancer cells were visualized under a phase-contrast microscope. Apoptosis and autophagy were detected using the DNA fragmentation assay and staining by autophagic vacuoles, respectively. The levels of apoptosis- and autophagy-related proteins such as cytochrome c, Bcl-2, LC3-I/II were investigated by Western blot analysis. The effect of PDs on the ERK1/2 signaling pathway was investigated using specific inhibitors. All the tested PDs were found to be active in the range of 36.7 ± 0.2 to 459.7 ± 4.2 µM. Compounds 3 and 4 showed cytotoxic activity in breast cancer cells, but were found to be safer with lower cytotoxicity on human nontumorigenic epithelial breast cells. Compound 4 induced apoptosis, whereas compound 3 induced autophagy. Both compounds inhibited the ERK signaling pathway in breast cancer cells. The present study revealed that both synthesized PDs induced different programmed cell death types by inhibiting the ERK signaling pathway in two genotypically different breast cancer cells. Therefore, novel PDs might be promising anticancer agents for breast cancer therapy and further structural modifications of PDs may yield promising anticancer agents.
https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85108416939&origin=inward
https://hdl.handle.net/11511/91212
Archiv der Pharmazie
Department of Chemistry, Article

Suggestions

Synthesis and characterization of polymeric magnetic nanoparticles loaded by gemcitabine /
Parsian, Maryam; Gündüz, Ufuk; Tezcaner, Ayşen; Department of Biotechnology (2014)
In this study, different types of magnetic nanoparticles were synthesized for treatment of breast cancer by targeted drug delivery. Polyamidoamine (PAMAM) dendrimer, Chitosan (CS) and Polyhydroxybutyrate (PHB) coated magnetic nanoparticles were prepared and loaded with Gemcitabine. The loading efficiency of drug for various half generations of dendrimer coated magnetic nanoparticles (DcMNPs), Chitosan coated magnetic nanoparticles (CSMNPs) and Polyhydroxybutyrate magnetic nanoparticles (PHB-MNPs) were inves...
Synthesis of novel 6-substituted amino-9-(beta-D-ribofuranosyl)purine analogs and their bioactivities on human epithelial cancer cells
TUNÇBİLEK, MERAL; Kucukdumlu, Asligul; Guven, Ebru Bilget; Altiparmak, Duygu; Atalay, Rengül (2018-02-01)
New nucleoside derivatives with nitrogen substitution at the C-6 position were prepared and screened initially for their in vitro anticancer bioactivity against human epithelial cancer cells (liver Huh7, colon HCT116, breast MCF7) by the NCI-sulforhodamine B assay. N-6-(4-trifluoromethylphenyl) piperazine analog (27) exhibited promising cytotoxic activity. The compound 27 was more cytotoxic (IC50 = 1-4 mu M) than 5-FU, fludarabine on Huh7, HCT116 and MCF7 cell lines. The most potent nucleosides (11, 13, 16,...
2-Amino-2-deoxy-glucose conjugated cobalt ferrite magnetic nanoparticle (2DG-MNP) as a targeting agent for breast cancer cells
Asik, Elif; Aslan, Tugba Nur; Volkan, Mürvet; Güray, Nülüfer Tülün (2016-01-01)
In this study, 2-amino-2-deoxy-glucose (2DG) was conjugated to COOH modified cobalt ferrite magnetic nanoparticles (COOH-MNPs), which were designed to target tumor cells as a potential targetable drug/gene delivery agent for cancer treatment. According to our results, it is apparent that, 2DG labeled MNPs were internalized more efficiently than COOH-MNPs under the same conditions in all cell types (MDA-MB-231 and MCF-7 cancer and MCF-10A normal breast cells) (p < 0.001). Moreover, the highest amount of upta...
Synthesis, anticancer activity, toxicity evaluation and molecular docking studies of novel phenylaminopyrimidine-(thio)urea hybrids as potential kinase inhibitors.
Ture, Asli; Kahraman, Deniz Cansen; Atalay, Rengül; Helvacioglu, Sinem; Charehsaz, Mohammad; KÜÇÜKGÜZEL, İLKAY (2019-02-01)
Thirty-two novel urea/thiourea compounds as potential kinase inhibitor were designed, synthesized and evaluated for their cytotoxic activity on breast (MCF7), colon (HCT116) and liver (Huh7) cancer cell lines. Compounds 10, 19 and 30 possessing anticancer activity with IC50 values of 0.9, 0.8 and 1.6 mu M respectively on Huh7 cells were selected for further studies. These hit compounds were tested against liver carcinoma panel. Real time cell electronic sensing assay was used to evaluate the effects of the ...
Identification of Potential Therapeutic Genes and Pathways in Phytoestrogen Emodin Treated Breast Cancer Cell Lines via Network Biology Approaches
Sakalli-Tecim, Elif; Uyar-Arpaci, Pembegul; Güray, Nülüfer Tülün (2021-02-01)
Phytoestrogens have been investigated for their potential anti-tumorigenic effects in various cancers including breast cancer. Emodin being a phytoestrogen shows anti-carcinogenic properties especially in estrogen receptor positive (ER+) breast cancers. The aim of this study is to identify the molecular mechanism and related biological pathways in both (ER+) MCF-7 and (ER-) MDA-MB-231 breast cancer cell lines upon Emodin treatment via microarray analysis in order to find out therapeutic biomarkers. In both ...
Citation Formats
H. Atmaca, S. Ilhan, E. S. Yılmaz, and M. Zora, “4-Propargyl-substituted 1H-pyrroles induce apoptosis and autophagy via extracellular signal-regulated signaling pathway in breast cancer,” Archiv der Pharmazie, pp. 0–0, 2021, Accessed: 00, 2021. [Online]. Available: https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85108416939&origin=inward.
METU IIS - Integrated Information Service open@metu.edu.tr