Two new families of Cu(II) and Co(II) mononuclear complexes with mixed ligands, [Cu(VanTrpt)(bipy)]ÁMeOH (CuVanTrpt), [Cu(VanSer)(bipy)]Á4H 2 O (CuVanSer), [Cu(VanTyr)(bipy)]ÁH 2 O (CuVanTyr), [Cu(VanThr)(bipy)]Á MeOH (CuVanThr), [Co(VanTrpt)(bipy)(OH 2 )]ÁH 2 OÁMeOH (CoVanTrpt), [Co(VanSer)(bipy)(OH 2 )]ÁMeOH (CoVanSer), [Co(VanTyr)(bipy)(OH 2 )]Á 3H 2 OÁMeOH (CoVanTyr), and [Co(VanThr)(bipy)(OH 2 )] (CoVanThr), (VanX are Schiff base proligands resulted from the condensation of o-vanillin with D,L-tryptophan (VanTrpt), L-serine (VanSer), L-tyrosine (VanTyr), and L-threonine (VanThr), respectively, and bipy is 2,2 0 -bipyridine), have been obtained and characterized on the basis of elemental analysis, magnetic measurements, and spectral data (FT-IR and UV-Vis-Nir spectroscopy). Crystal structures of CuVanTrpt, CuVanSer, and CuVanTyr have been solved by single-crystal X-Ray diffraction. Biological evaluation revealed that they are cytotoxic in HeLa (human carcinoma of the uterine cervix) and LSR-SF-SR (rat sarcoma induced by Rous sarcoma virus strain Schmidt-Ruppin) cells, showing an enhancement of cytotoxicity dependent of concentration and treatment time. The most pronounced cytotoxic effect is expressed by CuVanSer and CoVanSer. Various cytopathological changes of both types of cancer cells were observed after treatment with Cu(II) and Co(II) complexes for 72 h at concentrations of 100 and 200 μg ml À1 . LSR-SF-SR cells were found to be relatively more sensitive to the cytotoxic effect of the complexes investigated as compared to HeLa cells. K E Y W O R D S amino acids, cobalt(II) complexes, copper(II) complexes, cytotoxic activity, Schiff base proligands Desislav Dinev and Daniela C. Culita contributed equally to the manuscript.
Wound debridement is crucial for proper wound care as it promotes fast and efficient wound healing through removal of necrotic tissue. The latter not only impairs new healthy tissue formation but also increases the odour and the wound exudate, allowing bacteria and other harmful foreign invaders to spread and infect the wound. Hydrogel wound dressings are usually applied for promoting autolytic wound debridement but this is slow and not a very efficient process. On the other hand, enzymatic products for wound debridement are either ointments or gels and they are easily washed out when used for treating highly exuding wounds. This study is an attempt to combine enzymatic debridement functionality with the high swelling ability of polyzwitterionic networks and to produce an innovative dressing with debridement functionality for the healing of highly exuding wounds. For this purpose, two polyzwitterionic hydrogels were synthesized, poly(sulfobetaine methacrylate) and poly(carboxybetaine methacrylate) hydrogels, which were loaded with the protease subtilisin DY for imparting debridement functionality. The swelling ability and mechanical properties of zwitterionic polymer (ZP) hydrogels were shown to depend on their different propensities to physical network formation. Poly(carboxybetaine methacrylate) hydrogels demonstrated better capacity for wound exudate absorption as well as for exerting higher enzymatic debridement activity. Both ZP hydrogels were shown to be non‐cytotoxic which confirms their appropriateness for direct contact with injured tissues. Thus, the newly developed ZP hydrogels demonstrate the potential to be used as new dressing materials with enzymatic debridement functionality for highly exuding wounds. © 2019 The Authors. Polymer International published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.
Statins (3-Hydroxy-3-Methylglutaryl-CoA Reductase Inhibitors) have been clinically used for the treatment of dyslipidemia / hypercholesterolemia for almost 40 years. This class of medications represents some of the most frequently prescribed drugs in the world and are the main players in pharmacologic primary and secondary prevention of atherosclerotic cardiovascular disease. Statins have gained much recent attention due to their antitumor effects. This mini review summarizes data about some potential anticancer properties of statins, putative mechanisms of their antitumor activity, and the challenges that have to be overcome in order to facilitate the introduction of these drugs in oncology practice.
The present research is focused on evaluation of complexation ability of Monensic acid (MonH) towards La3+ and Nd3+ ions.Changes in the SRCD spectrum of Monensinate anion were monitored upon addition of lanthanide(III) ions. The antibiotic undergoes formation of one neutral ([Ln(Mon)3(H2O)3]) and two positively charged complex species of composition [Ln(Mon)2(H2O)2]+ and [Ln(Mon) (H2O)]2+, respectively (Ln = La3+, Nd3+). Neutral complexes were isolated as fine powders and were characterized by IR, FAB-MS and ESI-MS. It is assumed that Monensin acts in bidentate coordination mode via monodentate carboxylate moiety and hydroxyl group, both located at the opposite ends of antibiotic molecule.Activity of Monensic acid and [Ln(Mon)3(H2O)3] to decrease visible bacteria growth of B. subtilis, S. Lutea and B. mycoides was evaluated by agar hole diffusion method. Results showed that complexation of lanthanide(III) ions to Monensin enhances the activity of non-coordinated ligand.Antitumor efficacy of compounds was assayed on human triple negative breast cancer and transplantable sarcoma in rat. The cytotoxicity was accessed by MTT test, NR uptake, CV assay and double AO/PI staining. Experimental data revealed that Monensic acid and [Ln(Mon)3(H2O)3] possess concentration- and time-dependent activity, and express promising cytotoxic properties against human and rat permanent cancer cell lines.
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