It takes two to Tango: Synthesis of cytotoxic quinones containing two redox active centres with potential antitumour activity

2021 ◽  
Author(s):  
Daisy Lima ◽  
Renata G. Almeida ◽  
Guilherme Jardim ◽  
Breno Barbosa ◽  
Augusto Santos ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antitumour Activity ◽  
Fibroblast Cell ◽  
Fibroblast Cell Line ◽  
Redox Active ◽  
New Synthesis ◽  
Murine Fibroblast ◽  
Active Centres

We report a new synthesis of 48 new quinone-based derivatives via click chemistry and their subsequent evaluation against cancer cell lines and the control L929 murine fibroblast cell line. These...

scholarly journals Promising Anticancer Activity of [Bis(1,8-quinolato)palladium (II)] Alone and in Combination

2020 ◽  
Author(s):  
Md. Nur Alam ◽  
Mohammad Moni ◽  
Jun Yu ◽  
Philip Beale ◽  
Peter Turner ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antitumour Activity ◽  
Epigallocatechin Gallate ◽  
Cancer Cell Line ◽  
Resistant Cell ◽  
Colorectal Cancer Cell Line

Abstract Due to similar coordination chemistry of palladium and platinum, a large number of palladium compounds too have been investigated for their anticancer activity. In the present study we describe synthesis, characterization and anticancer activity of palladium complex [Bis(1,8-quinolato)palladium (II)], coded as NH3 against seven different cancer cell lines. NH3 is found to have higher antitumour activity than cisplatin against both parent ovarian A2780 cell line and cisplatin-resistant cell lines. Also, NH3 has the lowest IC50 value against HT-29 colorectal cancer cell line. The higher antitumour activity of NH3 is due to the presence of bulky 8-hydroxy-quinoline ligand thus reducing its reactivity. Proteomic study has identified significantly expressed proteins which have been validated through bioinformatics. NH3 has been found to be less toxic than cisplatin at 2.5 mg/kg and 5 mg/kg dosages on mice models. Binary combinations of NH3 with curcumin and epigallocatechin gallate (EGCG) have demonstrated dose and sequence dependent synergism in ovarian and colorectal cancer models. All of the preclinical studies indicate promising therapeutic potentiality of NH3 [Bis(1,8-quinolato)palladium (II) ] as an anticancer drug.

Reactivity to TGF-β is one step towards transformation in a murine fibroblast cell line

1992 ◽  
Vol 51 (1) ◽  
pp. 139-143
Author(s):  
Michaela Götschl ◽  
Petra Höfler ◽  
Georg Bauer
Keyword(s):  
Cell Line ◽  
Fibroblast Cell ◽  
Fibroblast Cell Line ◽  
Murine Fibroblast ◽  
One Step

Effect of phosphatidylcholine structure on the adenylate cyclase activity of a murine fibroblast cell line

Lipids ◽  
1993 ◽  
Vol 28 (8) ◽  
pp. 727-730 ◽  
Author(s):  
Lido Calorini ◽  
Gabriele Mugnai ◽  
Antonella Mannini ◽  
Salvatore Ruggieri
Keyword(s):  
Adenylate Cyclase ◽  
Cell Line ◽  
Fibroblast Cell ◽  
Cyclase Activity ◽  
Adenylate Cyclase Activity ◽  
Fibroblast Cell Line ◽  
Murine Fibroblast

scholarly journals The oncomir face of microRNA-206: A permanent miR-206 transfection study

2018 ◽  
Vol 243 (12) ◽  
pp. 1014-1023 ◽  
Author(s):  
Dóra Mihály ◽  
Gergő Papp ◽  
Zsolt Mervai ◽  
Andrea Reszegi ◽  
Péter Tátrai ◽  
...  
Keyword(s):  
Soft Tissue ◽  
Cell Line ◽  
Cell Lines ◽  
Target Genes ◽  
Soft Tissue Sarcomas ◽  
Fibroblast Cell ◽  
Fibroblast Cell Line ◽  
Normal Human Fibroblast ◽  
Human Fibroblast Cell ◽  
Normal Human

MiR-206 is a remarkable miRNA because it functions as a suppressor miRNA in rhabdomyosarcoma while at the same time, as previously showed, it can act as an oncomiRNA in SMARCB1 immunonegative soft tissue sarcomas. The aim of this study was to investigate the effect of miR-206 on its several target genes in various human tumorous and normal cell lines. In the current work, we created miR-206-overexpressing cell lines (HT-1080, Caco2, iASC, and SS-iASC) using permanent transfection. mRNA expression of the target genes of miR-206 (SMARCB1, ACTL6A, CCND1, POLA1, NOTCH3, MET, and G6PD) and SMARCB1 protein expression were examined with quantitative real-time polymerase chain reaction, immunoblotting, immunocytochemistry, and flow cytometry. MiRNA inhibition was used to validate our results. We found a diverse silencing effect of miR-206 on its target genes. While an overall tendency of downregulation was noted, expression profiles of individual cell lines showed large variability. Only CCND1 and MET were consistently downregulated. MiR-206 had an antiproliferative effect on a normal human fibroblast cell line. A strong silencing effect of SMARCB1 in miR-206 transfected SS-iASC was most likely caused by the synergic influence of the SS18-SSX1 fusion protein and miR-206. In the same cell line, a moderate decrease of SMARCB1 protein expression could be observed with immunocytochemistry and flow cytometry. In the most comprehensive analysis of miR-206 effects so far, a modest but significant downregulation of miR-206 targets on the mRNA level was confirmed across all cell lines. However, the variability of the effect shows that the action of this miRNA is largely cell context-dependent. Our results also support the conception that the oncomiR effect of miR-206 on SMARCB1 plays an important but not exclusive role in SMARCB1 immunonegative soft tissue sarcomas so it can be considered important in planning the targeted therapy of these tumors in the future. Impact statement Mir-206 is a very unique microRNA because it can act as a suppressor miRNA or as an oncomiRNA depending on the tumor tissue. In SMARCB1 negative soft tissue sarcomas miR-206 is overexpressed, so thus in epithelioid and synovial sarcomas it functions as an oncomiRNA. MiR-206 has diverse silencing effects on its target genes. We found that the action of miR-206 is largely cell context dependent. The oncomiR role of miR-206 is crucial but not exclusive in SMARCB1 negative soft tissue sarcomas and miR-206 has an antiproliferative effect on a normal human fibroblast cell line. Expressions of miR-206 targets observed in tumors can only be reproduced in the corresponding tumorous cell lines. This is the first study which examined the permanent effect of miR-206 on its target genes in normal, tumor, and genetically engineered cell lines.

scholarly journals Cytotoxicity of Quillaja saponaria Saponins towards Lung Cells Is Higher for Cholesterol-Rich Cells

Biophysica ◽  
2021 ◽  
Vol 1 (2) ◽  
pp. 126-136
Author(s):  
Natalia Kozińska ◽  
Katarzyna Tokarska ◽  
Michał Chudy ◽  
Kamil Wojciechowski
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Herbal Medicines ◽  
Fibroblast Cell ◽  
Cholesterol Content ◽  
Lung Cells ◽  
Fibroblast Cell Line ◽  
Quillaja Saponaria ◽  
Macro Scale ◽  
Saponin Fraction

The purpose of the study was to compare cytotoxicity of two Quillaja saponaria bark saponin (QBS) mixtures against two lung cell lines: normal MRC-5 fibroblast cell line and tumor A-549 epithelial cells of lungs’ alveoli. The study, performed both at a macro-scale and in a dedicated microfluidic device, showed that QBS was more toxic to the cell line more abundant in cholesterol (MRC-5). The QBS mixture with higher saponin fraction was found to be more cytotoxic towards both cell lines. The results may help to better understand the cytotoxicity of saponin-rich herbal medicines towards normal and tumor cells depending on their cholesterol content.

ANTITUMOR EFFECT OF SUNITINIB AND BORTEZOMIB ON BREAST CANCER CELL LINE IN VITRO

2017 ◽  
Vol 63 (1) ◽  
pp. 141-145
Author(s):  
Yuliya Khochenkova ◽  
Eliso Solomko ◽  
Oksana Ryabaya ◽  
Yevgeniya Stepanova ◽  
Dmitriy Khochenkov
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Antitumor Effect ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Actual Problem

The discovery for effective combinations of anticancer drugs for treatment for breast cancer is the actual problem in the experimental chemotherapy. In this paper we conducted a study of antitumor effect of the combination of sunitinib and bortezomib against MDA-MB-231 and SKBR-3 breast cancer cell lines in vitro. We found that bortezomib in non-toxic concentrations can potentiate the antitumor activity of sunitinib. MDA-MB-231 cell line has showed great sensitivity to the combination of bortezomib and sunitinib in vitro. Bortezomib and sunitinib caused reduced expression of receptor tyrosine kinases VEGFR1, VEGFR2, PDGFRa, PDGFRß and c-Kit on HER2- and HER2+ breast cancer cell lines

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