scholarly journals Synthesis of New 1-Aryl-2-(3,5-dimethylpyrazol-1-yl)ethanone Oxime Ether Derivatives and Investigation of Their Cytotoxic Effects

Processes ◽  
2021 ◽  
Vol 9 (11) ◽  
pp. 2019
Author(s):  
Mehmet Abdullah Alagöz ◽  
Arzu Karakurt ◽  
Ceylan Hepokur ◽  
Emine Şalva ◽  
Tijen Önkol ◽  
...  

In this study, 12 new 1-aryl-2-(3,5-dimethylpyrazol-1-yl)ethanone oxime ether derivatives were designed and synthesized to investigate their cytotoxic effects. The in vitro cytotoxic activities of the compounds were evaluated against cervix, colon, breast, glioma, neuroblastoma, and lung cancer cell lines, as well as a healthy cell line using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazo-lium bromide (MTT) assays with 5-fluorouracil (5-FU) as the reference compound. Compound 5f (IC50 = 5.13 µM) was found to be more effective than 5-FU (IC50 = 8.34 µM) in the C6 cancer cell line, and it had no cytotoxic effect on the L929 healthy cell line. Flow cytometry was used to investigate the mechanism of action of compound 5f on the cell cycle of the C6 cell line. The analysis showed that cell death was significantly due to apoptosis. These results indicate that compound 5f induces cell cycle arrest, and may be effective in treating glioma.

Medicina ◽  
2019 ◽  
Vol 55 (7) ◽  
pp. 322 ◽  
Author(s):  
Mohammad Firdaus Kamaruddin ◽  
Mohammad Zakir Hossain ◽  
Aied Mohamed Alabsi ◽  
Marina Mohd Bakri

Background and Objectives: The antitumor activities of capsaicin on various types of cancer cell lines have been reported but the effect of capsaicin on oral cancer, which is prevalent among Asians, are very limited. Thus, this study aimed to investigate the effects of capsaicin on ORL-48, an oral cancer cell line of Asian origin. Materials and Methods: Morphological changes of the ORL-48 cells treated with capsaicin were analyzed using fluorescence microscopy. The apoptotic-inducing activity of capsaicin was further confirmed by Annexin V-Fluorescein isothiocyanate / Propidium iodide (V-FITC/PI) staining using flow cytometry. In order to establish the pathway of apoptosis triggered by the compound on ORL-48 cells, caspase activity was determined and the mitochondrial pathway was verified by mitochondrial membrane potential (MMP) assay. Cell cycle analysis was also performed to identify the cell cycle phase of ORL-48 cells being inhibited by the capsaicin compound. Results: Fluorescence microscopy exhibited the presence of apoptotic features in capsaicin-treated ORL-48 cells. Apoptosis of capsaicin-treated ORL-48 cells revealed disruption of the mitochondrial-membrane potential, activation of caspase-3, -7 and -9 through an intrinsic apoptotic pathway and subsequently, apoptotic DNA fragmentation. The cell cycle arrest occurred in the G1-phase, confirming antiproliferative effect of capsaicin in a time-dependent manner. Conclusion: This study demonstrated that capsaicin is cytotoxic against ORL-48 cells and induces apoptosis in ORL-48 cells possibly through mitochondria mediated intrinsic pathway resulting in cell cycle arrest.


ChemInform ◽  
2010 ◽  
Vol 41 (28) ◽  
pp. no-no
Author(s):  
Miguel Angel Martinez-Urbina ◽  
Alejandro Zentella ◽  
Miguel Angel Vilchis-Reyes ◽  
Angel Guzman ◽  
Omar Vargas ◽  
...  

Tumor Biology ◽  
2011 ◽  
Vol 32 (4) ◽  
pp. 801-808 ◽  
Author(s):  
Wei Guo ◽  
Ying-Bo Zou ◽  
Yao-Guang Jiang ◽  
Ru-Wen Wang ◽  
Yun-Ping Zhao ◽  
...  

2020 ◽  
Vol 5 (38) ◽  
pp. 11850-11853
Author(s):  
Anderson Roberto de Souza ◽  
Mona Stefany de Souza Castro ◽  
Thiago Olímpio de Souza ◽  
Rodrigo Cassio Sola Veneziani ◽  
Jairo Kenupp Bastos ◽  
...  

2020 ◽  
Vol 83 (15-16) ◽  
pp. 547-558 ◽  
Author(s):  
Higor Lopes Nunes ◽  
Katiuska Tuttis ◽  
Juliana Mara Serpeloni ◽  
Jessyane Rodrigues do Nascimento ◽  
Claudia Quintino da Rocha ◽  
...  

Sign in / Sign up

Export Citation Format

Share Document