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Thessaloníki, Greece

Papazoglou I.,Aristotle University of Thessaloniki | Papadopoulos A.G.,Aristotle University of Thessaloniki | Skoulika S.,University of Ioannina | Lafazanis K.,Aristotle University of Thessaloniki | And 3 more authors.
Polyhedron | Year: 2014

Treatment of a dimethylsulfoxide solution of 2-thioorotic acid (THO) with copper(I) halides unexpectedly results in the formation of the [Cu(L)(DMSO) 2] complex, where L is the tetradentate N2O 2-donor bis(4-carboxylato-6-oxo-pyrimidine-2-yl)sulfide dianion formed in situ by metal-assisted desulfurization of 2-thioorotic acid. The complex features a tetragonally distorted octahedral copper(II) center with two pyrimidine N atoms and two carboxylate O atoms of the ligand, forming a square plane, whereas two O atoms of DMSO solvate molecules occupy the axial positions. The molecular structure, electronic properties and the energetics of the metal-ligand interactions have been studied on the level of density functional calculations. The new compound was evaluated for its in vitro antibacterial activity, DNA degradation activity and for its efficacy as anticancer agent against different cancer and normal human and murine cell lines as well. © 2014 Elsevier Ltd. All rights reserved.

Pontiki E.,Aristotle University of Thessaloniki | Hadjipavlou-Litina D.,Aristotle University of Thessaloniki | Litinas K.,Aristotle University of Thessaloniki | Geromichalos G.,Symeonidion Research Center
Molecules | Year: 2014

Cinnamic acids have been identified as interesting compounds with antioxidant, anti-inflammatory and cytotoxic properties. In the present study, simple cinnamic acids were synthesized by Knoevenagel condensation reactions and evaluated for the above biological activities. Compound 4ii proved to be the most potent LOX inhibitor. Phenylsubstituted acids showed better inhibitory activity against soybean LOX, and it must be noted that compounds 4i and 3i with higher lipophilicity values resulted less active than compounds 2i and 1i. The compounds have shown very good activity in different antioxidant assays. The antitumor properties of these derivatives have been assessed by their 1/IC50 inhibitory values in the proliferation of HT-29, A-549, OAW-42, MDA-MB-231, HeLa and MRC-5 normal cell lines. The compounds presented low antitumor activity considering the IC50 values attained for the cell lines, with the exception of compound 4ii. Molecular docking studies were carried out on cinnamic acid derivative 4ii and were found to be in accordance with our experimental biological results.

Diamantopoulos N.,Theagenion Cancer Hospital | Boutis A.L.,2nd IKA General Hospital Panagia | Koratzis I.,Theagenion Cancer Hospital | Andreadis C.,Theagenion Cancer Hospital | And 3 more authors.
Journal of B.U.ON. | Year: 2010

Purpose: Testicular cancer is the most frequent solid tumor in young male adults and a disease with elusive pathogenesis. The purpose of this study was to determine the role of matrix metalloproteinases and angiogenic factors in the pathogenesis of testicular germ cell tumors (GCTs). Methods: Between 2003 and 2006 we measured the serum levels of matrix metalloproteinase 2 (MMP-2), matrix metalloproteinase 9 (MMP-9), tissue inhibitor of matrix metalloproteinase 2 (TIMP-2), vascular endothelial growth factor A (VEGF-A), basic fibroblast growth factor (bFGF), platelet derived growth factor BB (PDGF-BB) andangiopoietin 2 (Ang-2) in 50patients with testicular GCTs, at baseline, one month after the completion of the second cycle of chemotherapy and one year after the completion of chemotherapy, and in 16 male age-matched controls at baseline. Results: At baseline, mean TIMP-2 value was lower in patients than controls, mean MMP-2/TIMP-2 ratio was higher inpatients than controls and MMP9/TIMP-2 ratio was also higher. Ang-2 value was higher inpatients than controls and bFGF value was also higher. Comparisons of the same parameters were also made among the 3 consecutive serum samples of the patients. All parameters normalized after chemotherapy except Ang-2 which remained elevated. Conclusion: The present study supports the hypothesis that tumor invasion and angiogenesis play a role in testicular GCTs pathogenesis. Also an interesting hypothesis was formed, concerning the role of elevated levels of Ang-2 found in testicular GCTs patients in the pathogenesis of the increased long term cardiovascular morbidity of these patients. Larger prospective studies are needed to confirm our results. © 2010 Zerbinis Medical Publications.

Geromichalos G.D.,Symeonidion Research Center | Papadopoulos T.,Karyo Center | Sahpazidou D.,Symeonidion Research Center | Sinakos Z.,Aristotle University of Thessaloniki
Food and Chemical Toxicology | Year: 2014

Crocin, a main constituent of Crocus sativus L (saffron), has been found to inhibit the growth of K-562 human chronic myelogenous leukemia (CML) cells expressing Bcr-Abl protein tyrosine kinase activity. The aim of our study is to investigate the ability of the bioactive saffron's constituents, crocin (CRC) and safranal (SFR), to inhibit the Bcr-Abl protein activity employing an in silico approach, as well as the in vitro effect of these compounds on K-562 growth and gene expression of Bcr-Abl. In silico molecular docking studies revealed that mostly SFR can be attached to Bcr-Abl protein, positioned inside the protein's binding cavity at the same place with the drug used in the treatment of CML, imatinib mesylate (IM). The predicted polar interactions and hydrophobic contacts constructing a hydrophobic cavity inside the active site, explain the observed inhibitory activity. Cytotoxicity experiments showed that SFR and CRC mediate cytotoxic response to K562 cells. In vitro studies on the expression of Bcr-Abl gene revealed that SFR and in a lesser degree IM inhibited the expression of the gene, while in contrast CRC induced an increase. The ultimate goal was to evaluate the existence of a potential antitumor activity of saffron's constituents SFR and CRC. © 2014 Elsevier Ltd.

Geromichalos G.D.,Symeonidion Research Center | Lamari F.N.,University of Patras | Papandreou M.A.,University of Patras | Trafalis D.T.,National and Kapodistrian University of Athens | And 3 more authors.
Journal of Agricultural and Food Chemistry | Year: 2012

Inhibitors of acetylcholine breakdown by acetylcholinesterase (AChE) constitute the main therapeutic modality for Alzheimer's disease. In the search for natural products with inhibitory action on AChE, this study investigated the activity of saffron extract and its constituents by in vitro enzymatic and molecular docking studies. Saffron has been used in traditional medicine against Alzheimer's disease. Saffron extract showed moderate AChE inhibitory activity (up to 30%), but IC 50 values of crocetin, dimethylcrocetin, and safranal were 96.33, 107.1, and 21.09 μM, respectively. Kinetic analysis showed mixed-type inhibition, which was verified by in silico docking studies. Safranal interacts only with the binding site of the AChE, but crocetin and dimethylcrocetin bind simultaneously to the catalytic and peripheral anionic sites. These results reinforce previous findings about the beneficial action of saffron against Alzheimer's disease and may be of value for the development of novel therapeutic agents based on carotenoid-based dual binding inhibitors. © 2012 American Chemical Society.

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