Established Human Cell Lines as Models to Study Anti-leukemic Effects of Flavonoids

Sak, Katrin; Everaus, Hele

doi:10.2174/1389202917666160803165447

Cited by 29 publications

(30 citation statements)

References 281 publications

(575 reference statements)

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“…Normal cells were chosen to represent the different routes of exposure by which this kind of chemicals can come in contact and/or enter human bodies: epidermal contact (Hs27), inhalation (HFL1) and ingestion (CRL1790). In addition, we used a tumoral cell line (U937), since it is a good cell model used worldwide to identify cytotoxicity and genotoxic activity of drugs 40 . Looking at the results (Table 2 and Figure S10 ) it can be seen that only L5 has a good cytotoxicity profile, while, unfortunately, all the copper complexes showed important cytotoxicity in the micromolar range, and cannot be further evaluated.…”

Section: Discussionmentioning

confidence: 99%

Thiosemicarbazone scaffold for the design of antifungal and antiaflatoxigenic agents: evaluation of ligands and related copper complexes

Rogolino¹,

Gatti²,

Carcelli³

et al. 2017

Sci Rep

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The issue of food contamination by aflatoxins presently constitutes a social emergency, since they represent a severe risk for human and animal health. On the other hand, the use of pesticides has to be contained, since this generates long term residues in food and in the environment. Here we present the synthesis of a series of chelating ligands based on the thiosemicarbazone scaffold, to be evaluated for their antifungal and antiaflatoxigenic effects. Starting from molecules of natural origin of known antifungal properties, we introduced the thio- group and then the corresponding copper complexes were synthesised. Some molecules highlighted aflatoxin inhibition in the range 67–92% at 100 μM. The most active compounds were evaluated for their cytotoxic effects on human cells. While all the copper complexes showed high cytotoxicity in the micromolar range, one of the ligand has no effect on cell proliferation. This hit was chosen for further analysis of mutagenicity and genotoxicity on bacteria, plants and human cells. Analysis of the data underlined the importance of the safety profile evaluation for hit compounds to be developed as crop-protective agents and at the same time that the thiosemicarbazone scaffold represents a good starting point for the development of aflatoxigenic inhibitors.

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Section: Discussionmentioning

confidence: 99%

Thiosemicarbazone scaffold for the design of antifungal and antiaflatoxigenic agents: evaluation of ligands and related copper complexes

Rogolino¹,

Gatti²,

Carcelli³

et al. 2017

Sci Rep

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“…Jurkat cells are good model for studying acute T‐cell leukemia. MOLT‐4 T‐cells have also been isolated from a patient with T‐cell acute lymphoblastic leukemia . As a control we used PTK7‐negative U266 cell line .…”

Section: Introductionmentioning

confidence: 99%

DNA Aptamers in the Detection of Leukemia Cells by the Thickness Shear Mode Acoustics Method

et al. 2019

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By using the thickness shear mode acoustics method (TSM) and single-molecule force spectroscopy (SMFS) we studied the interactions between DNA aptamers (sgc8c) specific to the protein tyrosine kinase 7 (PTK7), which is localized in the membranes of leukemia lymphoblastics (MOLT-4), and lymphocyte (Jurkat) cell lines, as well with PTK7-negative U266 myeloid leukemia cells. The TSM method allowed the development of a highly sensitive, label-free biosensor for the detection leukemia cells with a limit of detection of (195 � 20) cells/mL. SMFS approved the high selectivity of the sgc8c aptamers to the PTK7 receptors at the cell surface and allowed determining the binding probability of the aptamers to the PTK7 receptors at different cell lines.

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“…Myeloid cells are capable of differentiation, but in CML there is uncontrolled proliferation ( 10 ).Although treatment with tyrosine kinase inhibitors has led to significant improvements in CML outcomes, drug resistance may be seen as a major problem with their use. Various studies have been conducted to overcome drug resistance ( 11 , 12 , 13 , 14 ).…”

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confidence: 99%

Cytotoxic Effects of Some Flavonoids and Imatinib on the K562 Chronic Myeloid Leukemia Cell Line: Data Analysis Using the Combination Index Method

et al. 2019

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Background:Flavonoids are natural compounds with antioxidant, anticarcinogenic, and anti-inflammatory effects.Aims:To determine the cytotoxic effects of flavonoids and drug resistance related to P-gp on K562 human chronic myeloid leukemia cells. We also aimed to evaluate the therapeutic potential of imatinib and flavonoid combinations.Study Design:Cell culture study.Methods:In this study, K562 cells were treated with apigenin, luteolin, 5-desmethyl sinensetin and the anticancer drug imatinib mesylate. The effect of flavonoids on K562 cell proliferation was detected using the 3-(4,5-dimethylthiazolyl)2,5‑diphenyl‑tetrazolium bromide assay. Concentrations of apigenin, luteolin, and 5-desmethyl sinensetin ranging from 25 to 200 μM and of imatinib from 5 to 50 μM administered for 72 h were studied. Apoptosis/necrosis and P-gp activity were measured using flow cytometry. The combined effects of different concentrations of flavonoids with imatinib were evaluated according to combination index values calculated using CompuSyn software.Results:In our study, the IC50 values for apigenin, luteolin, and 5-desmethyl sinensetin were found to be 140 μM, 100 μM, and >200 μM, respectively. Luteolin (100 μM) had the highest cytotoxic activity of these flavonoids. These results were statistically significant (p<0.05). Among the flavonoids studied, the combination of luteolin and imatinib was the most effective and is therefore recommended for its cytotoxic activity in the K562 cell line. After 72 h of incubation at their respective IC50 concentrations, all flavonoids were associated with an apoptosis rate of approximately 50%. P-glycoprotein activity was increased in all groups. Combination treatment may provide better outcomes in terms of cytotoxicity and thus reduce the dosages of imatinib used.Conclusion:The combination of some flavonoids and imatinib mesylate may increase the cytotoxic effect; However, the antagonistic effect should be considered in combined use on k562 cells.

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Established Human Cell Lines as Models to Study Anti-leukemic Effects of Flavonoids

Cited by 29 publications

References 281 publications

Thiosemicarbazone scaffold for the design of antifungal and antiaflatoxigenic agents: evaluation of ligands and related copper complexes

Thiosemicarbazone scaffold for the design of antifungal and antiaflatoxigenic agents: evaluation of ligands and related copper complexes

DNA Aptamers in the Detection of Leukemia Cells by the Thickness Shear Mode Acoustics Method

Cytotoxic Effects of Some Flavonoids and Imatinib on the K562 Chronic Myeloid Leukemia Cell Line: Data Analysis Using the Combination Index Method

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