Please use this identifier to cite or link to this item: http://hdl.handle.net/10773/19343
Title: Bis(4-hydroxy-2H-chromen-2-one): Synthesis and effects on leukemic cell lines proliferation and NF-kappa B regulation
Author: Talhi, Oualid
Schnekenburger, Michael
Panning, Jana
Pinto, Diana G. C.
Fernandes, Jose A.
Almeida Paz, Filipe A.
Jacob, Claus
Diederich, Marc
Silva, Artur M. S.
Keywords: K562 CELLS
CURCUMIN
CANCER
DIFFERENTIATION
EXPRESSION
APOPTOSIS
DEATH
INHIBITION
ACTIVATION
PATHWAYS
Issue Date: 2014
Publisher: PERGAMON-ELSEVIER SCIENCE LTD
Abstract: Synthesis of the bis-4-hydroxycoumarin-type compound, 3,3'-[3-(2-hydroxyphenyl)-3-oxopropane-1,1-diyl] bis(4-hydroxy-2H-chromen-2-one), was performed by two alternative pathways, either involving a basic organocatalyzed 1,4-conjugate addition tandem reaction of 4-hydroxycoumarin on chromone-3-carboxylic acid, or a double condensation of 4-hydroxycoumarin on omega-formyl-2'-hydroxyacetophenone. The anti-proliferative effects of the bis-4-hydroxycoumarin-type compound on human K-562 (chronic myeloid leukaemia) and JURKAT (acute T-cell leukaemia) cell lines using trypan blue staining, as well as its involvement in nuclear factor-kappa B (NF-kappa B) regulation analyzed by luciferase reporter gene assay, gene expression analysis and western blots were analysed. This compound inhibited TNF alpha-induced NF-kappa B activation in K-562 (IC50 17.5 mu M) and JURKAT (IC50 19.0 mu M) cell lines, after 8 h of incubation. Interestingly, it exerted mainly cytostatic effects at low doses on both cell lines tested, whereas it decreased JURKAT cell viability starting at 50 mu M from 24 h of treatment. Importantly, it did not affect the viability of peripheral blood mononuclear cells (PBMCs) from healthy donors, even at concentrations above 100 mu M. (C) 2014 Elsevier Ltd. All rights reserved.
Peer review: yes
URI: http://hdl.handle.net/10773/19343
DOI: 10.1016/j.bmc.2014.03.046
ISSN: 0968-0896
Publisher Version: 10.1016/j.bmc.2014.03.046
Appears in Collections:CICECO - Artigos



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