Document Detail


Synthesis, characterization, antitumoral and osteogenic activities of quercetin vanadyl(IV) complexes.
MedLine Citation:
PMID:  16821038     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The development of new vanadium derivatives with organic ligands, which improve the beneficial actions (insulin-mimetic, antitumoral) and decrease the toxic effects, is of great interest. A good candidate for the generation of a new vanadium compound is the flavonoid quercetin because of its own anticarcinogenic effect. The complex [VO(Quer)(2)EtOH]( n ) (QuerVO) has been synthesized and characterized by means of different spectroscopic techniques (UV-vis, Fourier transform IR, electron paramagnetic resonance) and its magnetic and stability properties. The inhibitory effect on bovine alkaline phosphatase (ALP) activity has been tested for the free ligand, the complex as well as for the vanadyl(IV) (comparative purposes). The biological activity of the complex on the proliferation of two osteoblast-like cells in culture, a normal one (MC3T3E1) and a tumoral one (UMR106), has been compared with that of the vanadyl(IV) cation and quercetin. The differentiation osteoblast markers ALP specific activity and collagen synthesis have been also tested. In addition, the effect of QuerVO on the activation of the extracellular regulated kinase (ERK) pathway is reported. The bone antitumoral effect of quercetin alone was established with the cell proliferation assays (it inhibits the proliferation of the tumoral cells and does not exert any effect on the normal osteoblasts). Moreover, the complex exerts osteogenic effects since it stimulates the type I collagen production and is a weak inhibitory agent upon ALP activity. Finally, QuerVO stimulated the ERK phosphorylation in a dose-response manner and this activation seems to be involved as one of the possible mechanisms for the biological effects of the complex.
Authors:
Evelina G Ferrer; María V Salinas; María J Correa; Luciana Naso; Daniel A Barrio; Susana B Etcheverry; Luis Lezama; Teófilo Rojo; Patricia A M Williams
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Publication Detail:
Type:  Historical Article; Journal Article; Research Support, Non-U.S. Gov't     Date:  2006-07-05
Journal Detail:
Title:  Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry     Volume:  11     ISSN:  0949-8257     ISO Abbreviation:  J. Biol. Inorg. Chem.     Publication Date:  2006 Sep 
Date Detail:
Created Date:  2006-07-21     Completed Date:  2006-09-27     Revised Date:  2009-11-19    
Medline Journal Info:
Nlm Unique ID:  9616326     Medline TA:  J Biol Inorg Chem     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  791-801     Citation Subset:  IM    
Affiliation:
CEQUINOR (Centro de Química Inorgánica), Facultad de Ciencias Exactas, Universidad Nacional de La Plata, 47 y 115, 1900 La Plata, Argentina.
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MeSH Terms
Descriptor/Qualifier:
3T3-L1 Cells
Alkaline Phosphatase / metabolism
Animals
Antineoplastic Agents / chemical synthesis*,  chemistry,  pharmacology*
Blotting, Western
Cell Proliferation
Electron Spin Resonance Spectroscopy
Extracellular Signal-Regulated MAP Kinases / metabolism
History, 20th Century
Intestines / enzymology
Mice
Osteogenesis / drug effects*
Quercetin / chemistry*
Spectrophotometry, Ultraviolet
Spectroscopy, Fourier Transform Infrared
Vanadium / chemistry*
Chemical
Reg. No./Substance:
0/Antineoplastic Agents; 117-39-5/Quercetin; 7440-62-2/Vanadium; EC 2.7.11.24/Extracellular Signal-Regulated MAP Kinases; EC 3.1.3.1/Alkaline Phosphatase

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