2,181 research outputs found
Synthesis and characterization of poly-phosphane coinage metals complexes and study on the protein ligation and catalysis
No full textA series of coinage metals centered poly-phosphane complexes has been synthesized and characterized under photophysical, chemical and biochemical aspects also in combination with a protein. Poly-phosphane metal complexes possess many properties in the field of luminescence,[1] catalysis, [2] chemo sensing, [3] and of anticancer activity [4]. In this study phosphane ligands containing the carboxylic functional group in ortho or para position of PPh3 have been used. The introduction of this polar group has the double aim either to make more hydrophilic the complexes and to tune the binding ability of the phosphane. In the case of gold(I) complexes, the poly-phosphine compound have been studied in comparison with the corresponding [bis-triphenylphosphine-gold(I)chloride], where the carboxylic group is absent, to evaluate the influence of its presence in the photopysical properties as well as on the interaction with dihydrofolate reductase, a protein involved in cell proliferation, DNA duplication and many other biological functions [5]. Affinity constants have been estimated through quenching of fluorescence studies and inhibition constants have been evaluated through rate constant determination of the reduction of dihydrofolate (H2F) to tetrahydrofolate (H4F) with reduced nicotinamide adenide dinucleotide phosphate (NADPH) as hydride donor. The tests highlighted a catalytic activity of the gold(I) compounds versus the H2F, which is the substrate of the enzyme. A strong effect of the enzyme on the luminescence properties of the gold(I) complexes have been observed. A coinage metals homolog series have been also evaluated as antiproliferative agent by in vitro MTT tests.
Scheme. Schematic view of a homolog series of coinage metals complexes under study.
References
1. R. Edward, T. Tiekink, J. G. Kang, Coord. Chem. Rev. 2009, 253, 1627-1648
2. David J. Gorin, Benjamin D. Sherry, and F. Dean Toste, Chem. Rev. 2008, 108, 3351–3378
3. X. He, V. W. Yam, Coord. Chem. Rev. 2011, 2111-2123
4. R. Galassi, A.Burini, O. Camille Simon, A. Dolmella, D. Micozzi, S. Vincenzetti, S. Pucciarelli Dalton Trans., 2015, 44, 3043-3056 DOI: 10.1039/C4DT01542H
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Azolate/phosphane Gold(I) compounds in antiproliferative therapy: a new frontier for the azolate gold(I) chemistry
No full textAzolate/phosphane Gold(I) compounds in antiproliferative therapy: a new frontier for the azolate gold(I) chemistry
Azolate gold(I) phosphane compounds have become good candidate for anticancer applications.[1] It was highlighted that azolate gold(I) phosphane compounds were mostly very active in the regards of many panel of cancer cells, in addition to cis-platin resistant cells. Moreover, inhibition studies of pivotal enzymes, such as the seleno dependent ThioredoxinaReductase (TrxR), and an enzyme involved in DNA synthesis such as DeHydroFolateReductase, were carried out highlighting in both cases IC50 ranging from nano- to micromolar scale, respectively.[1][2] In order to study the effectiveness of these new azolate gold(I) phosphane compounds as potential anticancer agents, and to understand in depth the Structure Activity Relationship (SAR) relationship, different cell viability assays (MTT assays) were performed on a human in vitro model of HER2-overexpressing breast cancer: SKBR-3 cells.[3] After this preliminary screening, the most promising and effective compounds were selected to extend the study on A17 cell line, a murine preclinical model of Basal Like Breast Cancer (BLBC).[4] Hence, their efficacy in suppressing BLBC growth in vivo was tested and IHC analysis on explanted tumors were carried on. Overall, in vitro assays demonstrated a remarkable activity for those compounds having the Ph3PAu+ moiety and substituted imidazolate as co-ligands. Concerning the in vivo study the compounds act significantly delaying tumor growth. Accordingly, IHC analysis revealed a remarkable anti-angiogenic activity associated with a lower expression of proliferative markers and a higher level of apoptotic markers in treated tumours in comparison with controls. Moreover, respect to cisplatin these compounds displayed a lower nephrotoxicity, although their liver toxicity was higher. These promising results open the way to further investigations in order to understand the mechanism of action of these new azolate gold (I) posphane complexes.
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[1] R. Galassi et al., Dalton Trans., 2012, (41), pp 5307-5318.
[2] R. Galassi et al., Dalton Trans., 2015, (44), pp 3043-3056.
[3] Fogh, J., Fogh J. M., Orfeo T, J Natl Cancer Inst. , 1977, (59), pp 221-6;
[4] M. Galiè et al., Carcinogenesis , 2005, (11), pp 1868-187
Azolate gold(I) phosphane complexes as innovative therapies for the treatment of HER2-driven breast cancer
No full textGold(I) compounds have been known as cytotoxic agents since 30 years ago1. Lastly, the inhibition activity studies on compounds (such as LAuL’, where L is a phosphane and L’ a co-ligand) led to the individuation of a likely molecular target2, renewing the interest on the field of these metallodrugs. In the design of active gold compounds, the proper hydro / lipophilic balancing provides the lowering of the overall toxicity, maintaining both a good cellular uptake and anticancer properties. Imidazoles and pyrazoles as co-ligands afford to gold(I) phosphane compounds having cytotoxic activity, but enough polarity to be soluble in physiological media. Different azolate gold(I)phosphane complexes have been synthesized. They contain substituents on imidazole or pyrazole ligands such as R = NO2, CF3, CN, Cl, CH2OH) or substituents such as COOH or COONHEt3 in the phosphane moiety. Some of them have been already tested as antitumoral in some panels of cancer cells, resulting active3. In this work we present the study of the cytotoxic effects of several gold(I) compounds and a natural compound on an in vitro model of HER2-overexpressing breast cancer. We tested the effectiveness of these compounds as potential anticancer agents on SKBR-3 cell line, a human breast cancer cell line that overexpresses the HER2 (Neu/ErbB-2) gene product4. These cells display an epithelial morphology in tissue culture and are a useful preclinical model to screen for new therapeutic agents which could overcome the drawback of resistance to HER2-targeted therapies5. In order to screen the cytotoxic activity of these new compounds on SKBR-3 cells we performed different cell viability assays. As conclusion we observed a detrimental effect on the cytotoxicity for those compounds having an ionic structure or highly hydrophilic polar substituents on the azolate or phosphane ligands and a remarkable activity for those compounds having the Ph3PAu+ moiety and substituted imidazolate as co-ligands.
1) Benoît Bertrand, and Angela Casini. Dalton Trans., 2014, 43, 4209. DOI: 10.1039/c3dt52524d
2) a) Peter J. Barnard, Susan J. Berners-Price. Coord. Chem. Rev. 2007, 251, 1889–1902. DOI:10.1016/j.ccr.2007.04.006. b) A. Bindoli, M. P. Rigobello, G. Scutari, C. Gabbiani, A. Casini, L. Messori, Coord. Chem. Rev., 2009, 253, 1692–1707. DOI: 10.1016/j.ccr.2009.02.026.
3) a) R. Galassi, A. Burini, S. Ricci, M. Pellei, M. P. Rigobello, A. Citta, A. Dolmella, V. Gandin, C Marzano. Dalton Trans., 2012, 41, 5307. DOI: 10.1039/c2dt11781a b)
4) Fogh J, Fogh JM, Orfeo T, 1977, One hundred and twenty-seven cultured human tumor cell lines producing tumors in nude mice. J Natl Cancer Inst. , 59(1):221-6. DOI: 10.1016/j.bmcl.2013.11.058.
5) Saturnino C, Sirignano E, Botta A, Sinicropi MS, Caruso A, Pisano A, Lappano R, Maggiolini M, Longo P, 2014, New titanocene derivatives with high antiproliferative activity against breast cancer cells. Bioorg Med Chem Lett., 1;24(1):136-40. DOI: 10.1016/j.bmcl.2013.11.058
Martina Drijverová and her literary works for children (author´s portrait)
No full textThis thesis Martina Drijverova and her literatur for children (the author´s portrait) is engaged in work of writer and screenwriter Martina Drijeverová. She is an excellent writer of literature for children. In the first part of this work her story writing is mentioned and the second part deals with her fairy-tale writing. The other author´s work written for children is in the third part. The conclusion of this thesis appreciates the author´s credit in literature for chidlren. Analysis of some books are available. The supplementary part is composed of autor´s biography and her photograph, some book covers, list of the autor´s work {--} televiews, radio plays and serials, audio tapes and CDs, stage plays, books written in Braille
HERStory Makers 2022: Martina Čagalj
No full textMartina Čagalj is a PhD candidate at the University of Split studying seaweeds as a potential source of bioactive compounds. She took part in HERStory Makers 2022.What is HERStory Makers?HERStory Makers is a social media competition for female-identifying early career researchers to share their research, their career journeys, and to inspire the next generation. Winners are selected by public vote. HERStory Makers is also part of EXPLORATHON, Scotland's contribution to European Researchers' Night.In 2022-23, EXPLORATHON was supported by the Engineering & Physical Sciences Research Council [grant number EP/X020894/1].Author contributions to contentMartina Čagalj conceived, planned, and recorded the video content. Kirsty Ross edited the video content to insert HERStory Maker credits, add subtitles, and maintain video length below Twitter/X limit of 2 mins and 20 secs, prior to scheduling the social media posts.</p
The role of data science in software development
No full textauthor: Martina WeberMasterarbeit Universität Innsbruck 201
The role of data science in software development
No full textauthor: Martina WeberMasterarbeit Universität Innsbruck 201
The role of data science in software development
No full textauthor: Martina WeberMasterarbeit Universität Innsbruck 201
Man kann nicht nicht vergleichen. Sprachvergleich und Sprachreflexion in einer integrierten Mehrsprachigkeitsdidaktik mit Englisch als Brückensprache
No full textPlurilinguism and plurilingual didactics have gained an important position in scientific discussion, even though interlingual and integrated approaches to teaching practice are still lacking. After a short description of various approaches, all based on language comparison and metalingual reflection, the author suggests adopting English as a bridge-language in plurilingual didactics, independent of the language family and languages studied. On the basis of various learner profiles, the author illustrates the benefit of using English as an element of language comparison and reflection in the learning process of other languages
Author Correction: Gluten consumption and inflammation affect the development of celiac disease in at-risk children
No full textThe original version of this Article contained an error in the spelling of the authors Renata Auricchio, Ilaria Calabrese, Martina Galatola, Donatella Cielo, Fortunata Carbone, Marianna Mancuso, Giuseppe Matarese, Riccardo Troncone, Salvatore Auricchio & Luigi Greco which were incorrectly given as Auricchio Renata, Calabrese Ilaria, Galatola Martina, Cielo Donatella, Carbone Fortunata, Mancuso Marianna, Matarese Giuseppe, Troncone Riccardo, Auricchio Salvatore & Greco Luigi. The original article has been corrected
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