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  1. AU="Serena Montalbano"
  2. AU="Morroni, Gianluca"
  3. AU="Choi, Kristal S."
  4. AU="Verma, Smita Rastogi" AU="Verma, Smita Rastogi"
  5. AU="Zhou, Bingfeng"
  6. AU="Kivala, Milan"
  7. AU="Salafia, O S"
  8. AU="Taghavi, Fouad J"
  9. AU="Xiao, Jun-Hua"
  10. AU="Vee Sin Lee, Peter"
  11. AU="Zhu, Yali"
  12. AU="Jiang-Qi Liu"
  13. AU="Moores, Roxanna"

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  1. Artikel ; Online: Antiproliferative Activity and DNA Interaction Studies of a Series of N4,N4-Dimethylated Thiosemicarbazone Derivatives

    Serena Montalbano / Annamaria Buschini / Giorgio Pelosi / Franco Bisceglie

    Molecules, Vol 28, Iss 2778, p

    2023  Band 2778

    Abstract: The exploitation of bioactive natural sources to obtain new anticancer agents with novel modes of action may represent an innovative and successful strategy in the field of medicinal chemistry. Many natural products and their chemical analogues have been ...

    Abstract The exploitation of bioactive natural sources to obtain new anticancer agents with novel modes of action may represent an innovative and successful strategy in the field of medicinal chemistry. Many natural products and their chemical analogues have been proposed as starting molecules to synthesise compounds with increased biological potential. In this work, the design, synthesis, and characterisation of a new series of N4,N4-dimethylated thiosemicarbazone Cu(II), Ni(II), and Pt(II) complexes are reported and investigated for their in vitro toxicological profile against a leukaemia cell line (U937). The antiproliferative activity was studied by MTS assay to determine the GI 50 value for each compound after 24 h of treatment, while the genotoxic potential was investigated to determine if the complexes could cause DNA damage. In addition, the interaction between the synthesised molecules and DNA was explored by means of spectroscopic techniques, showing that for Pt and Ni derivatives a single mode of action can be postulated, while the Cu analogue behaves differently.
    Schlagwörter thiosemicarbazone metal complexes ; U937 cell line ; antiproliferative activity ; DNA damage ; DNA interaction ; Organic chemistry ; QD241-441
    Thema/Rubrik (Code) 540
    Sprache Englisch
    Erscheinungsdatum 2023-03-01T00:00:00Z
    Verlag MDPI AG
    Dokumenttyp Artikel ; Online
    Datenquelle BASE - Bielefeld Academic Search Engine (Lebenswissenschaftliche Auswahl)

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  2. Artikel ; Online: A Key Silencing Histone Mark on Chromatin Is Lost When Colorectal Adenocarcinoma Cells Are Depleted of Methionine by Methionine γ-Lyase

    Samanta Raboni / Serena Montalbano / Stephanie Stransky / Benjamin A. Garcia / Annamaria Buschini / Stefano Bettati / Simone Sidoli / Andrea Mozzarelli

    Frontiers in Molecular Biosciences, Vol

    2021  Band 8

    Abstract: Methionine is an essential amino acid used, beyond protein synthesis, for polyamine formation and DNA/RNA/protein methylation. Cancer cells require particularly high methionine supply for their homeostasis. A successful approach for decreasing methionine ...

    Abstract Methionine is an essential amino acid used, beyond protein synthesis, for polyamine formation and DNA/RNA/protein methylation. Cancer cells require particularly high methionine supply for their homeostasis. A successful approach for decreasing methionine concentration is based on the systemic delivery of methionine γ-lyase (MGL), with in vitro and in vivo studies demonstrating its efficacy in cancer therapy. However, the mechanisms explaining how cancer cells suffer from the absence of methionine more significantly than non-malignant cells are still unclear. We analyzed the outcome of the human colorectal adenocarcinoma cancer cell line HT29 to the exposure of MGL for up to 72 h by monitoring cell viability, proteome expression, histone post-translational modifications, and presence of spurious transcription. The rationale of this study was to verify whether reduced methionine supply would affect chromatin decondensation by changing the levels of histone methylation and therefore increasing genomic instability. MGL treatment showed a time-dependent cytotoxic effect on HT29 cancer cells, with an IC50 of 30 µg/ml, while Hs27 normal cells were less affected, with an IC50 of >460 µg/ml. Although the levels of total histone methylation were not altered, a loss of the silencing histone mark H3K9me2 was observed, as well as a decrease in H4K20me3. Since H3K9me2/3 decorate repetitive DNA elements, we proved by qRT-PCR that MGL treatment leads to an increased expression of major satellite units. Our data indicate that selected histone methylation marks may play major roles in the mechanism of methionine starvation in cancer cells, proving that MGL treatment directly impacts chromatin homeostasis.
    Schlagwörter methionine ; cancer therapy ; histone methylation ; mass spectrometry ; enzyme-based therapy ; Biology (General) ; QH301-705.5
    Thema/Rubrik (Code) 570
    Sprache Englisch
    Erscheinungsdatum 2021-10-01T00:00:00Z
    Verlag Frontiers Media S.A.
    Dokumenttyp Artikel ; Online
    Datenquelle BASE - Bielefeld Academic Search Engine (Lebenswissenschaftliche Auswahl)

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  3. Artikel ; Online: Mechanistic insights on the mode of action of an antiproliferative thiosemicarbazone-nickel complex revealed by an integrated chemogenomic profiling study

    Enrico Baruffini / Roberta Ruotolo / Franco Bisceglie / Serena Montalbano / Simone Ottonello / Giorgio Pelosi / Annamaria Buschini / Tiziana Lodi

    Scientific Reports, Vol 10, Iss 1, Pp 1-

    2020  Band 14

    Abstract: Abstract Thiosemicarbazones (TSC) and their metal complexes display diverse biological activities and are active against multiple pathological conditions ranging from microbial infections to abnormal cell proliferation. Ribonucleotide reductase (RNR) is ... ...

    Abstract Abstract Thiosemicarbazones (TSC) and their metal complexes display diverse biological activities and are active against multiple pathological conditions ranging from microbial infections to abnormal cell proliferation. Ribonucleotide reductase (RNR) is considered one of the main targets of TSCs, yet, the existence of additional targets, differently responsible for the multifaceted activities of TSCs and their metal complexes has been proposed. To set the basis for a more comprehensive delineation of their mode of action, we chemogenomically profiled the cellular effects of bis(citronellalthiosemicarbazonato)nickel(II) [Ni(S-tcitr)2] using the unicellular eukaryote Saccharomyces cerevisiae as a model organism. Two complementary genomic phenotyping screens led to the identification of 269 sensitive and 56 tolerant deletion mutant strains and of 14 genes that when overexpressed make yeast cells resistant to an otherwise lethal concentration of Ni(S-tcitr)2. Chromatin remodeling, cytoskeleton organization, mitochondrial function and iron metabolism were identified as lead cellular processes responsible for Ni(S-tcitr)2 toxicity. The latter process, and particularly glutaredoxin-mediated iron loading of RNR, was found to be affected by Ni(S-tcitr)2. Given the multiple pathways regulated by glutaredoxins, targeting of these proteins by Ni(S-tcitr)2 can negatively affect various core cellular processes that may critically contribute to Ni(S-tcitr)2 cytotoxicity.
    Schlagwörter Medicine ; R ; Science ; Q
    Thema/Rubrik (Code) 570
    Sprache Englisch
    Erscheinungsdatum 2020-06-01T00:00:00Z
    Verlag Nature Portfolio
    Dokumenttyp Artikel ; Online
    Datenquelle BASE - Bielefeld Academic Search Engine (Lebenswissenschaftliche Auswahl)

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  4. Artikel ; Online: The AFLATOX ® Project

    Serena Montalbano / Francesca Degola / Jennifer Bartoli / Franco Bisceglie / Annamaria Buschini / Mauro Carcelli / Donatella Feretti / Serena Galati / Laura Marchi / Nicolò Orsoni / Giorgio Pelosi / Marianna Pioli / Francesco M. Restivo / Dominga Rogolino / Mirco Scaccaglia / Olga Serra / Giorgio Spadola / Gaia C. V. Viola / Ilaria Zerbini /
    Claudia Zani

    International Journal of Molecular Sciences, Vol 22, Iss 4520, p

    Approaching the Development of New Generation, Natural-Based Compounds for the Containment of the Mycotoxigenic Phytopathogen Aspergillus flavus and Aflatoxin Contamination

    2021  Band 4520

    Abstract: The control of the fungal contamination on crops is considered a priority by the sanitary authorities of an increasing number of countries, and this is also due to the fact that the geographic areas interested in mycotoxin outbreaks are widening. Among ... ...

    Abstract The control of the fungal contamination on crops is considered a priority by the sanitary authorities of an increasing number of countries, and this is also due to the fact that the geographic areas interested in mycotoxin outbreaks are widening. Among the different pre- and post-harvest strategies that may be applied to prevent fungal and/or aflatoxin contamination, fungicides still play a prominent role; however, despite of countless efforts, to date the problem of food and feed contamination remains unsolved, since the essential factors that affect aflatoxins production are various and hardly to handle as a whole. In this scenario, the exploitation of bioactive natural sources to obtain new agents presenting novel mechanisms of action may represent a successful strategy to minimize, at the same time, aflatoxin contamination and the use of toxic pesticides. The Aflatox ® Project was aimed at the development of new-generation inhibitors of aflatoxigenic Aspergillus spp. proliferation and toxin production, through the modification of naturally occurring molecules: a panel of 177 compounds, belonging to the thiosemicarbazones class, have been synthesized and screened for their antifungal and anti-aflatoxigenic potential. The most effective compounds, selected as the best candidates as aflatoxin containment agents, were also evaluated in terms of cytotoxicity, genotoxicity and epi-genotoxicity to exclude potential harmful effect on the human health, the plants on which fungi grow and the whole ecosystem.
    Schlagwörter aflatoxins ; Aspergillus flavus ; antiaflatoxigenic molecules ; antifungals ; antimycotoxigenic molecules ; new generation fungicides ; Biology (General) ; QH301-705.5 ; Chemistry ; QD1-999
    Thema/Rubrik (Code) 333
    Sprache Englisch
    Erscheinungsdatum 2021-04-01T00:00:00Z
    Verlag MDPI AG
    Dokumenttyp Artikel ; Online
    Datenquelle BASE - Bielefeld Academic Search Engine (Lebenswissenschaftliche Auswahl)

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  5. Artikel: Investigation of antibacterial activity of new classes of essential oils derivatives

    Bassanetti, Irene / Annamaria Buschini / Dominga Rogolino / Giovanni Tosi / Giuliano Leonardi / Laura Fiorentini / Mauro Carcelli / Paola Massi / Paolo Pelagatti / Serena Montalbano

    Food control. 2017 Mar., v. 73

    2017  

    Abstract: Essential oils (EOs) have deserved much attention in the past decades for their antimicrobial activity, since many of them have demonstrated efficacy against food-borne pathogenic and spoilage microorganisms. Moreover, they have potential application in ... ...

    Abstract Essential oils (EOs) have deserved much attention in the past decades for their antimicrobial activity, since many of them have demonstrated efficacy against food-borne pathogenic and spoilage microorganisms. Moreover, they have potential application in animal nutrition as multifunctional feed supplements, avoiding or diminishing the use of antibiotics in livestock. However, low solubility and bioavailability as well as volatility and marked aromatic note are important limitations in food and feed applications. In this study we present the synthesis, characterization and evaluation of the antibacterial activity of new thymol, carvacrol and menthol derivatives. The new compounds have been designed to overcome the limitations of the precursors, such as poor water solubility and volatility, still maintaining a good antimicrobial profile. We evaluated the activity of the synthetized compounds against pathogens causing important foodborne diseases, i.e. Clostridium perfringens, Salmonella typhimurium, Salmonella enteritidis and Escherichia coli. The low MICs and MBCs values for some of the studied compounds, combined with water solubility and negligible cytotoxicity towards HT-29 human cells, confirmed the potential use for EOs derivatives in the food industry.
    Schlagwörter animal nutrition ; antibacterial properties ; antibiotics ; bioavailability ; carvacrol ; Clostridium perfringens ; cytotoxicity ; Escherichia coli ; essential oils ; feed supplements ; food industry ; foodborne illness ; human cell lines ; livestock ; menthol ; minimum inhibitory concentration ; Salmonella Enteritidis ; Salmonella Typhimurium ; spoilage microorganisms ; thymol ; water solubility
    Sprache Englisch
    Erscheinungsverlauf 2017-03
    Umfang p. 606-612.
    Erscheinungsort Elsevier Ltd
    Dokumenttyp Artikel
    ZDB-ID 1027805-9
    ISSN 0956-7135
    ISSN 0956-7135
    DOI 10.1016/j.foodcont.2016.09.010
    Datenquelle NAL Katalog (AGRICOLA)

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  6. Artikel ; Online: Thiosemicarbazone scaffold for the design of antifungal and antiaflatoxigenic agents

    Dominga Rogolino / Anna Gatti / Mauro Carcelli / Giorgio Pelosi / Franco Bisceglie / Francesco Maria Restivo / Francesca Degola / Annamaria Buschini / Serena Montalbano / Donatella Feretti / Claudia Zani

    Scientific Reports, Vol 7, Iss 1, Pp 1-

    evaluation of ligands and related copper complexes

    2017  Band 12

    Abstract: Abstract The issue of food contamination by aflatoxins presently constitutes a social emergency, since they represent a severe risk for human and animal health. On the other hand, the use of pesticides has to be contained, since this generates long term ... ...

    Abstract Abstract The issue of food contamination by aflatoxins presently constitutes a social emergency, since they represent a severe risk for human and animal health. On the other hand, the use of pesticides has to be contained, since this generates long term residues in food and in the environment. Here we present the synthesis of a series of chelating ligands based on the thiosemicarbazone scaffold, to be evaluated for their antifungal and antiaflatoxigenic effects. Starting from molecules of natural origin of known antifungal properties, we introduced the thio- group and then the corresponding copper complexes were synthesised. Some molecules highlighted aflatoxin inhibition in the range 67–92% at 100 μM. The most active compounds were evaluated for their cytotoxic effects on human cells. While all the copper complexes showed high cytotoxicity in the micromolar range, one of the ligand has no effect on cell proliferation. This hit was chosen for further analysis of mutagenicity and genotoxicity on bacteria, plants and human cells. Analysis of the data underlined the importance of the safety profile evaluation for hit compounds to be developed as crop-protective agents and at the same time that the thiosemicarbazone scaffold represents a good starting point for the development of aflatoxigenic inhibitors.
    Schlagwörter Medicine ; R ; Science ; Q
    Thema/Rubrik (Code) 540
    Sprache Englisch
    Erscheinungsdatum 2017-09-01T00:00:00Z
    Verlag Nature Publishing Group
    Dokumenttyp Artikel ; Online
    Datenquelle BASE - Bielefeld Academic Search Engine (Lebenswissenschaftliche Auswahl)

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  7. Artikel: A battery of assays as an integrated approach to evaluate fungal and mycotoxin inhibition properties and cytotoxic/genotoxic side-effects for the prioritization in the screening of thiosemicarbazone derivatives

    Zani, Claudia / Annamaria Buschini / Dominga Rogolino / Donatella Feretti / Elisabetta Ceretti / Francesca Degola / Francesco Maria Restivo / Franco Bisceglie / Gaia V.C. Viola / Giorgio Pelosi / Marianna Pioli / Mauro Carcelli / Serena Galati / Serena Montalbano

    Food and chemical toxicology. 2017,

    2017  

    Abstract: Aflatoxins represent a serious problem for a food economy based on cereal cultivations used to fodder animal and for human nutrition. The aims of our work are two-fold: first, to perform an evaluation of the activity of newly synthesized ... ...

    Abstract Aflatoxins represent a serious problem for a food economy based on cereal cultivations used to fodder animal and for human nutrition. The aims of our work are two-fold: first, to perform an evaluation of the activity of newly synthesized thiosemicarbazone compounds as antifungal and anti-mycotoxin agents and, second, to conduct studies on the toxic and genotoxic hazard potentials with a battery of tests with different endpoints. In this paper we report an initial study on two molecules: S-4-isopropenylcyclohexen-1-carbaldehydethiosemicarbazone and its metal complex, bis(S-4-isopropenylcyclohexen-1-carbaldehydethiosemicarbazonato)nickel (II). The outcome of the assays on fungi growth and aflatoxin production inhibition show that both molecules possess good antifungal activities, without inducing mutagenic effects on bacteria. From the assays to ascertain that the compounds have no adverse effects on human cells, we have found that they are cytotoxic and, in the case of the nickel compound, they also present genotoxic effects.
    Schlagwörter adverse effects ; aflatoxins ; antifungal properties ; bacteria ; cytotoxicity ; forage ; fungi ; human nutrition ; humans ; mutagens ; nickel ; prioritization ; screening ; toxicology
    Sprache Englisch
    Umfang p. .
    Erscheinungsort Elsevier Ltd
    Dokumenttyp Artikel
    Anmerkung Pre-press version
    ZDB-ID 782617-5
    ISSN 1873-6351 ; 0278-6915
    ISSN (online) 1873-6351
    ISSN 0278-6915
    DOI 10.1016/j.fct.2017.05.008
    Datenquelle NAL Katalog (AGRICOLA)

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