scholarly journals Crotamine-like from Southern Pacific rattlesnake (Crotalus oreganus helleri) Venom acts on human leukemia (K-562) cell lines and produces ultrastructural changes on mice adrenal gland

2018 ◽  
Vol 42 (2) ◽  
pp. 116-123
Author(s):  
Elda E. Sánchez ◽  
Roschman González ◽  
Sara Lucena ◽  
Stefanie García ◽  
Héctor J. Finol ◽  
...  
Keyword(s):  
Adrenal Gland ◽  
Cell Lines ◽  
Ultrastructural Changes ◽  
Human Leukemia ◽  
Crotalus Oreganus ◽  
Crotalus Oreganus Helleri

New Mechanistic Insight on the PIM-1 Kinase Inhibitor AZD1208 Using Multidrug Resistant Human Erythroleukemia Cell Lines and Molecular Docking Simulations

2019 ◽  
Vol 19 (11) ◽  
pp. 914-926 ◽  
Author(s):  
Maiara Bernardes Marques ◽  
Michael González-Durruthy ◽  
Bruna Félix da Silva Nornberg ◽  
Bruno Rodrigues Oliveira ◽  
Daniela Volcan Almeida ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Binding Site ◽  
Cell Lines ◽  
Chemotherapeutic Agents ◽  
Atp Binding ◽  
Human Leukemia ◽  
Atp Binding Site ◽  
Mechanistic Insight ◽  
Multiple Drugs

Background:PIM-1 is a kinase which has been related to the oncogenic processes like cell survival, proliferation, and multidrug resistance (MDR). This kinase is known for its ability to phosphorylate the main extrusion pump (ABCB1) related to the MDR phenotype.Objective:In the present work, we tested a new mechanistic insight on the AZD1208 (PIM-1 specific inhibitor) under interaction with chemotherapy agents such as Daunorubicin (DNR) and Vincristine (VCR).Materials and Methods:In order to verify a potential cytotoxic effect based on pharmacological synergism, two MDR cell lines were used: Lucena (resistant to VCR) and FEPS (resistant to DNR), both derived from the K562 non-MDR cell line, by MTT analyses. The activity of Pgp was ascertained by measuring accumulation and the directional flux of Rh123. Furthermore, we performed a molecular docking simulation to delve into the molecular mechanism of PIM-1 alone, and combined with chemotherapeutic agents (VCR and DNR).Results:Our in vitro results have shown that AZD1208 alone decreases cell viability of MDR cells. However, co-exposure of AZD1208 and DNR or VCR reverses this effect. When we analyzed the ABCB1 activity AZD1208 alone was not able to affect the pump extrusion. Differently, co-exposure of AZD1208 and DNR or VCR impaired ABCB1 activity, which could be explained by compensatory expression of abcb1 or other extrusion pumps not analyzed here. Docking analysis showed that AZD1208 is capable of performing hydrophobic interactions with PIM-1 ATP- binding-site residues with stronger interaction-based negative free energy (FEB, kcal/mol) than the ATP itself, mimicking an ATP-competitive inhibitory pattern of interaction. On the same way, VCR and DNR may theoretically interact at the same biophysical environment of AZD1208 and also compete with ATP by the PIM-1 active site. These evidences suggest that AZD1208 may induce pharmacodynamic interaction with VCR and DNR, weakening its cytotoxic potential in the ATP-binding site from PIM-1 observed in the in vitro experiments.Conclusion:Finally, the current results could have a pre-clinical relevance potential in the rational polypharmacology strategies to prevent multiple-drugs resistance in human leukemia cancer therapy.

Effects of carboplatin in combination with other anticancer agents on human leukemia cell lines

1993 ◽  
Vol 17 (2) ◽  
pp. 113-119 ◽  
Author(s):  
Yasuhiko Kano ◽  
Miyuki Akutsu ◽  
Kenichi Suzuki ◽  
Minoru Yoshida
Keyword(s):  
Cell Lines ◽  
Anticancer Agents ◽  
Leukemia Cell ◽  
Human Leukemia ◽  
Human Leukemia Cell ◽  
Leukemia Cell Lines

Antitumor and apoptotic effects of new-generation platinum compounds on human leukemia cell lines HL-60 and K562

Biologia ◽  
2021 ◽  
Author(s):  
Neslihan Tekin Karacaer ◽  
Barış Kerimoğlu ◽  
Talat Baran ◽  
Mehtap Tarhan ◽  
Ayfer Menteş ◽  
...  
Keyword(s):  
Cell Lines ◽  
Leukemia Cell ◽  
Human Leukemia ◽  
Platinum Compounds ◽  
Human Leukemia Cell ◽  
Leukemia Cell Lines ◽  
New Generation ◽  
Apoptotic Effects

Evaluation of theIn VitroAntiproliferative Properties of Four Novel Anthracyclines YM1, 3, 4 and 6 in Human Leukemia Cell Lines

1992 ◽  
Vol 4 (5) ◽  
pp. 306-311 ◽  
Author(s):  
X.R. Jiang ◽  
A.C. Newland ◽  
M.G. Macey ◽  
G.C. Jenkins ◽  
T. Miki ◽  
...  
Keyword(s):  
Cell Lines ◽  
Leukemia Cell ◽  
Human Leukemia ◽  
Human Leukemia Cell ◽  
Leukemia Cell Lines

Effect of sodium dichloroacetate on apoptotic gene expression in human leukemia cell lines

2019 ◽  
Vol 71 (2) ◽  
pp. 248-256 ◽  
Author(s):  
Jagoda Abramek ◽  
Jacek Bogucki ◽  
Marta Ziaja-Sołtys ◽  
Andrzej Stępniewski ◽  
Anna Bogucka-Kocka
Keyword(s):  
Gene Expression ◽  
Cell Lines ◽  
Leukemia Cell ◽  
Human Leukemia ◽  
Human Leukemia Cell ◽  
Apoptotic Gene ◽  
Leukemia Cell Lines

scholarly journals Interaction of Arylidenechromanone/Flavanone Derivatives with Biological Macromolecules Studied as Human Serum Albumin Binding, Cytotoxic Effect, Biocompatibility Towards Red Blood Cells

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3172 ◽  
Author(s):  
Angelika A. Adamus-Grabicka ◽  
Magdalena Markowicz-Piasecka ◽  
Michał B. Ponczek ◽  
Joachim Kusz ◽  
Magdalena Małecka ◽  
...  
Keyword(s):  
Human Serum Albumin ◽  
Serum Albumin ◽  
Red Blood Cells ◽  
Human Serum ◽  
Cell Line ◽  
Cell Lines ◽  
Blood Cells ◽  
Cytotoxic Effect ◽  
Human Leukemia ◽  
Ic50 Values

The aim of this study was to determine the cytotoxic effect of 3-arylidenechromanone (1) and 3arylideneflavanone (2) on HL-60 and NALM-6 cell lines (two human leukemia cell lines) and a WM-115 melanoma cell line. Both compounds exhibited high cytotoxic activity with higher cytotoxicity exerted by compound 2, for which IC50 values below 10 µM were found for each cell line. For compound 1, the IC50 values were higher than 10 µM for HL-60 and WM-115 cell lines, but IC50 < 10 µM was found for the NALM-6 cell line. Both compounds, at the concentrations close to IC50 (concentration range: 5–24 µM/L for compound 1 and 6–10 µM/L for compound 2), are not toxic towards red blood cells. The synthesized compounds were characterized using spectroscopic methods 1H- and 13C-NMR, IR, MS, elemental analysis, and X-ray diffraction. The lipophilicity of both synthesized compounds was determined using an RP-TLC method and the logP values found were compared with the theoretical ones taken from the Molinspiration Cheminformatics (miLogP) software package. The mode of binding of both compounds to human serum albumin was assessed using molecular docking methods.

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