Please use this identifier to cite or link to this item: http://hdl.handle.net/10553/74264
Title: Evaluation of synthetic chalcones on cell viability of human leukemia cell lines
Authors: Saavedra Díaz, Ester Gloria 
Loro Ferrer, Juan Francisco 
Estévez Rosas, Francisco Jesús 
Del Rosario García, Henoc 
Quintana Aguiar, José Martín 
Brouard Martín,Ignacio 
UNESCO Clasification: 32 Ciencias médicas
3209 Farmacología
320713 Oncología
Keywords: Synthetic chalcones
Leukemia
Issue Date: 2015
Journal: Basic and Clinical Pharmacology and Toxicology 
Conference: 36 Congreso de la Sociedad Española de Farmacología (SEF) 
Abstract: P-glycoprotein is a member of the ATP-binding cassette transporter family which is involved in the multidrug resistance of cancer cells to several anti-cancer drugs. To synthesize and to determine the effects of selected chalcones on viability of human leukemia cell lines and in particular P-glycoproteinoverexpressing K-562/ADR cells. Chalcones were synthesized by a Claisen–Schmidt condensation of 2- hydroxyacetophenones and benzaldehydes and their structures were determined by spectroscopic analyses. HL-60, U-937, MOLT-3, K-562 and K-562/ADR cells were grown in RPMI 1640 medium and cytotoxicity was analyzed by colorimetric MTT assay. Cell cycle phase distribution and reactive oxygen species were determined by flow cytometry. The evaluation of apoptosis was carried out by fluorescent microscopy, flow cytometry and DNA fragmentation. Caspase activity was determined using colorimetric substrates, processing of caspases and release of mitochondrial proteins by Western blot. We evaluated the antiproliferative activity of seventeen synthetic chalcones against human leukemia cell lines and found that 20-hydroxy-60 -benzyloxy-4-bromochalcone was the most potent, showing IC50 values of approximately 5 mM, including the multidrug resistant K-562/ADR. This compound induced apoptosis in a concentration- and time-dependent manner and blocked cell cycle progression at the S phase. Cell death was found to be associated with the release of mitochondrial pro-apoptotic proteins, the cleavage and activation of caspases and an increase of intracellular reactive oxygen species generation. The selected chalcone effectively induces cell death in leukemia cells that overexpress P-glycoprotein and could be a potential candidate for developing novel anti-cancer agents.
URI: http://hdl.handle.net/10553/74264
ISSN: 1742-7835
Source: Basic & Clinical Pharmacology & Toxicology [ISSN 1742-7835], v. 117 (sup. 2), p. 42, Abstract C029, (Diciembre 2015)
Appears in Collections:Póster de congreso
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