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Article ; Online: A Drug Discovery Approach to a Reveal Novel Antioxidant Natural Source: The Case of Chestnut Burr Biomass.

Trezza, Alfonso / Geminiani, Michela / Cutrera, Giuseppe / Dreassi, Elena / Frusciante, Luisa / Lamponi, Stefania / Spiga, Ottavia / Santucci, Annalisa

International journal of molecular sciences

2024 Volume 25, Issue 5

Abstract: Currently, many environmental and energy-related problems are threatening the future of our planet. In October 2022, the Worldmeter recorded the world population as 7.9 billion people, estimating that there will be an increase of 2 billion by 2057. The ... ...

Abstract	Currently, many environmental and energy-related problems are threatening the future of our planet. In October 2022, the Worldmeter recorded the world population as 7.9 billion people, estimating that there will be an increase of 2 billion by 2057. The rapid growth of the population and the continuous increase in needs are causing worrying conditions, such as pollution, climate change, global warming, waste disposal, and natural resource reduction. Looking for novel and innovative methods to overcome these global troubles is a must for our common welfare. The circular bioeconomy represents a promising strategy to alleviate the current conditions using biomass-like natural wastes to replace commercial products that have a negative effect on our ecological footprint. Applying the circular bioeconomy concept, we propose an integrated in silico and in vitro approach to identify antioxidant bioactive compounds extracted from chestnut burrs (an agroforest waste) and their potential biological targets. Our study provides a novel and robust strategy developed within the circular bioeconomy concept aimed at target and drug discovery for a wide range of diseases. Our study could open new frontiers in the circular bioeconomy related to target and drug discovery, offering new ideas for sustainable scientific research aimed at identifying novel therapeutical strategies.
MeSH term(s)	Humans ; Antioxidants ; Biomass ; Climate Change ; Drug Discovery ; Environmental Pollution
Chemical Substances	Antioxidants
Language	English
Publishing date	2024-02-21
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2019364-6
ISSN	1422-0067 ; 1422-0067 ; 1661-6596
ISSN (online)	1422-0067
ISSN	1422-0067 ; 1661-6596
DOI	10.3390/ijms25052517
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Article ; Online: An update on antibacterial AlkylGuanidino Ureas: Design of new derivatives, synergism with colistin and data analysis of the whole library.

Ardino, Claudia / Sannio, Filomena / Poli, Giulio / Galati, Salvatore / Dreassi, Elena / Botta, Lorenzo / Docquier, Jean-Denis / D'Agostino, Ilaria

European journal of medicinal chemistry

2024 Volume 270, Page(s) 116362

Abstract: Antimicrobial resistance (AMR) represents one of the most challenging global Public Health issues, with an alarmingly increasing rate of attributable mortality. This scenario highlights the urgent need for innovative medicinal strategies showing activity ...

Abstract	Antimicrobial resistance (AMR) represents one of the most challenging global Public Health issues, with an alarmingly increasing rate of attributable mortality. This scenario highlights the urgent need for innovative medicinal strategies showing activity on resistant isolates (especially, carbapenem-resistant Gram-negative bacteria, methicillin-resistant S. aureus, and vancomycin-resistant enterococci) yielding new approaches for the treatment of bacterial infections. We previously reported AlkylGuanidino Ureas (AGUs) with broad-spectrum antibacterial activity and a putative membrane-based mechanism of action. Herein, new tetra- and mono-guanidino derivatives were designed and synthesized to expand the structure-activity relationships (SARs) and, thereby, tested on the same panel of Gram-positive and Gram-negative bacteria. The membrane-active mechanism of selected compounds was then investigated through molecular dynamics (MD) on simulated bacterial membranes. In the end, the newly synthesized series, along with the whole library of compounds (more than 70) developed in the last decade, was tested in combination with subinhibitory concentrations of the last resort antibiotic colistin to assess putative synergistic or additive effects. Moreover, all the AGUs were subjected to cheminformatic and machine learning analyses to gain a deeper knowledge of the key features required for bioactivity.
MeSH term(s)	Anti-Bacterial Agents/pharmacology ; Colistin/pharmacology ; Methicillin-Resistant Staphylococcus aureus ; Gram-Negative Bacteria ; Gram-Positive Bacteria ; Bacteria ; Data Analysis ; Microbial Sensitivity Tests
Chemical Substances	Anti-Bacterial Agents ; Colistin (Z67X93HJG1)
Language	English
Publishing date	2024-03-28
Publishing country	France
Document type	Journal Article
ZDB-ID	188597-2
ISSN	1768-3254 ; 0009-4374 ; 0223-5234
ISSN (online)	1768-3254
ISSN	0009-4374 ; 0223-5234
DOI	10.1016/j.ejmech.2024.116362
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Article ; Online: Tenebrio molitor

Brai, Annalaura / Poggialini, Federica / Vagaggini, Chiara / Pasqualini, Claudia / Simoni, Sauro / Francardi, Valeria / Dreassi, Elena

International journal of molecular sciences

2023 Volume 24, Issue 3

Abstract: The progression of drugs into clinical phases requires proper toxicity assessment in animals and the correct identification of possible metabolites. Accordingly, different animal models are used to preliminarily evaluate toxicity and biotransformations. ... ...

Abstract	The progression of drugs into clinical phases requires proper toxicity assessment in animals and the correct identification of possible metabolites. Accordingly, different animal models are used to preliminarily evaluate toxicity and biotransformations. Rodents are the most common models used to preliminarily evaluate the safety of drugs; however, their use is subject to ethical consideration and elevated costs, and strictly regulated by national legislations. Herein, we developed a novel, cheap and convenient toxicity model using
MeSH term(s)	Animals ; Mice ; Rats ; Coleoptera ; Tenebrio/metabolism
Language	English
Publishing date	2023-01-24
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2019364-6
ISSN	1422-0067 ; 1422-0067 ; 1661-6596
ISSN (online)	1422-0067
ISSN	1422-0067 ; 1661-6596
DOI	10.3390/ijms24032296
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Article ; Online: Progress towards Adjuvant Development: Focus on Antiviral Therapy.

Brai, Annalaura / Poggialini, Federica / Pasqualini, Claudia / Trivisani, Claudia Immacolata / Vagaggini, Chiara / Dreassi, Elena

International journal of molecular sciences

2023 Volume 24, Issue 11

Abstract: In recent decades, vaccines have been extraordinary resources to prevent pathogen diffusion and cancer. Even if they can be formed by a single antigen, the addition of one or more adjuvants represents the key to enhance the response of the immune signal ... ...

Abstract	In recent decades, vaccines have been extraordinary resources to prevent pathogen diffusion and cancer. Even if they can be formed by a single antigen, the addition of one or more adjuvants represents the key to enhance the response of the immune signal to the antigen, thus accelerating and increasing the duration and the potency of the protective effect. Their use is of particular importance for vulnerable populations, such as the elderly or immunocompromised people. Despite their importance, only in the last forty years has the search for novel adjuvants increased, with the discovery of novel classes of immune potentiators and immunomodulators. Due to the complexity of the cascades involved in immune signal activation, their mechanism of action remains poorly understood, even if significant discovery has been recently made thanks to recombinant technology and metabolomics. This review focuses on the classes of adjuvants under research, recent mechanism of action studies, as well as nanodelivery systems and novel classes of adjuvants that can be chemically manipulated to create novel small molecule adjuvants.
MeSH term(s)	Humans ; Aged ; Adjuvants, Immunologic/pharmacology ; Vaccines ; Immunologic Factors ; Adjuvants, Pharmaceutic ; Antiviral Agents/pharmacology
Chemical Substances	Adjuvants, Immunologic ; Vaccines ; Immunologic Factors ; Adjuvants, Pharmaceutic ; Antiviral Agents
Language	English
Publishing date	2023-05-25
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	2019364-6
ISSN	1422-0067 ; 1422-0067 ; 1661-6596
ISSN (online)	1422-0067
ISSN	1422-0067 ; 1661-6596
DOI	10.3390/ijms24119225
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Article ; Online: DEAD-Box Helicase DDX3X as a Host Target against Emerging Viruses: New Insights for Medicinal Chemical Approaches.

Brai, Annalaura / Trivisani, Claudia Immacolata / Poggialini, Federica / Pasqualini, Claudia / Vagaggini, Chiara / Dreassi, Elena

Journal of medicinal chemistry

2022 Volume 65, Issue 15, Page(s) 10195–10216

Abstract: In recent years, globalization, global warming, and population aging have contributed to the spread of emerging viruses, such as coronaviruses (COVs), West Nile (WNV), Dengue (DENV), and Zika (ZIKV). The number of reported infections is increasing, and ... ...

Abstract	In recent years, globalization, global warming, and population aging have contributed to the spread of emerging viruses, such as coronaviruses (COVs), West Nile (WNV), Dengue (DENV), and Zika (ZIKV). The number of reported infections is increasing, and considering the high viral mutation rate, it is conceivable that it will increase significantly in the coming years. The risk caused by viruses is now more evident due to the COVID-19 pandemic, which highlighted the need to find new broad-spectrum antiviral agents able to tackle the present pandemic and future epidemics. DDX3X helicase is a host factor required for viral replication. Selective inhibitors have been identified and developed into broad-spectrum antivirals active against emerging pathogens, including SARS-CoV-2 and most importantly against drug-resistant strains. This perspective describes the inhibitors identified in the last years, highlighting their therapeutic potential as innovative broad-spectrum antivirals.
MeSH term(s)	Antiviral Agents/pharmacology ; Antiviral Agents/therapeutic use ; COVID-19 ; DEAD-box RNA Helicases ; Humans ; Pandemics ; SARS-CoV-2 ; Virus Replication ; Viruses ; Zika Virus ; Zika Virus Infection
Chemical Substances	Antiviral Agents ; DDX3X protein, human (EC 3.6.1.-) ; DEAD-box RNA Helicases (EC 3.6.4.13)
Language	English
Publishing date	2022-07-28
Publishing country	United States
Document type	Journal Article ; Review
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.2c00755
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Zs.B 151: Show issues			Location: Je nach Verfügbarkeit (siehe Angabe bei Bestand) bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular ab Jg. 2022: Lesesaal (EG)
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Article: Sweet Cherry Extract as Permeation Enhancer of Tyrosine Kinase Inhibitors: A Promising Prospective for Future Oral Anticancer Therapies.

Poggialini, Federica / Vagaggini, Chiara / Brai, Annalaura / Pasqualini, Claudia / Carbone, Anna / Musumeci, Francesca / Schenone, Silvia / Dreassi, Elena

Pharmaceuticals (Basel, Switzerland)

2023 Volume 16, Issue 11

Abstract: Although patients would rather oral therapies to injections, the gastrointestinal tract's low permeability makes this method limiting for most compounds, including anticancer drugs. Due to their low bioavailability, oral antitumor therapies suffer from ... ...

Abstract	Although patients would rather oral therapies to injections, the gastrointestinal tract's low permeability makes this method limiting for most compounds, including anticancer drugs. Due to their low bioavailability, oral antitumor therapies suffer from significant variability in pharmacokinetics and efficacy. The improvement of their pharmacokinetic profiles can be achieved by a new approach: the use of natural extracts enriched with polyphenolic compounds that act as intestinal permeability enhancers. Here, we propose a safe sweet cherry extract capable of enhancing oral absorption. The extract was characterized by the HPLC-UV/MS method, evaluated for in vitro antioxidant activity, safety on the Caco-2 cell line, and as a potential permeation enhancer. The sweet cherry extract showed a high antioxidant capacity (ABTS and DPPH assays were 211.74 and 48.65 µmol of Trolox equivalent/g dried extract, respectively), high content of polyphenols (8.44 mg of gallic acid per gram of dry extract), and anthocyanins (1.80 mg of cyanidin-3-glucoside equivalent per g of dry extract), reassuring safety profile (cell viability never lower than 98%), and a significant and fully reversible ability to alter the integrity of the Caco-2 monolayer (+81.5% of Lucifer yellow permeability after 2 h). Furthermore, the ability of the sweet cherry extract to improve the permeability (P
Language	English
Publishing date	2023-10-27
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2193542-7
ISSN	1424-8247
ISSN	1424-8247
DOI	10.3390/ph16111527
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Article ; Online: Development and validation of derivatization-based LC-MS/MS method for quantification of short-chain fatty acids in human, rat, and mouse plasma.

Vagaggini, Chiara / Brai, Annalaura / Bonente, Denise / Lombardi, Jessica / Poggialini, Federica / Pasqualini, Claudia / Barone, Virginia / Nicoletti, Claudio / Bertelli, Eugenio / Dreassi, Elena

Journal of pharmaceutical and biomedical analysis

2023 Volume 235, Page(s) 115599

Abstract: Short-chain fatty acids (SCFAs), the end products of gut microbial fermentation of dietary fibers and non-digestible polysaccharides, act as a link between the microbiome, immune system, and inflammatory processes. The importance of accurately ... ...

Abstract	Short-chain fatty acids (SCFAs), the end products of gut microbial fermentation of dietary fibers and non-digestible polysaccharides, act as a link between the microbiome, immune system, and inflammatory processes. The importance of accurately quantifying SCFAs in plasma has recently emerged to understand their biological role. In this work, a sensitive and reproducible LC-MS/MS method is reported for SCFAs quantification in three different matrices such as human, rat and mouse plasma via derivatization, using as derivatizing agent O-benzylhydroxylamine (O-BHA), coupled with liquid-liquid extraction. First, the instrumental parameters of the mass spectrometer and then the chromatographic conditions were optimized using previously SCFAs derivatives synthetized and used as standards. After that, the best conditions for derivatization and extraction from plasma were studied and a series of determinations were performed on human, rat, and mouse plasma aliquots to validate the overall method (derivatization, extraction, and LC-MS/MS determination). The method showed good performance in terms of recovery (> 80%), precision (RSD <14%), accuracy (RE < ± 10%) and sensitivity (LOQ of 0.01 µM for acetic, butyric, propionic and isobutyric acid) in all plasma samples. The method thus developed and validated was applied to the quantification of major SCFAs in adult and aged mice, germ-free mice and in germ-free recipient mice subjected to fecal transplant from adult and aged donors. Results highlighted how plasma concentrations of SCFAs are correlated with age further highlighting the importance of developing a method that is reliable for the quantification of SCFAs to study their biological role.
MeSH term(s)	Mice ; Rats ; Humans ; Animals ; Aged ; Chromatography, Liquid/methods ; Tandem Mass Spectrometry/methods ; Feces/chemistry ; Fatty Acids, Volatile/analysis ; Gastrointestinal Microbiome
Chemical Substances	Fatty Acids, Volatile
Language	English
Publishing date	2023-07-23
Publishing country	England
Document type	Journal Article
ZDB-ID	604917-5
ISSN	1873-264X ; 0731-7085
ISSN (online)	1873-264X
ISSN	0731-7085
DOI	10.1016/j.jpba.2023.115599
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Article ; Online: Identification of Novel Non-Nucleoside Inhibitors of Zika Virus NS5 Protein Targeting MTase Activity.

Fiorucci, Diego / Meaccini, Micaela / Poli, Giulio / Stincarelli, Maria Alfreda / Vagaggini, Chiara / Giannecchini, Simone / Sutto-Ortiz, Priscila / Canard, Bruno / Decroly, Etienne / Dreassi, Elena / Brai, Annalaura / Botta, Maurizio

International journal of molecular sciences

2024 Volume 25, Issue 4

Abstract: Zika virus (ZIKV) is a positive-sense single-stranded virus member of ... ...

Abstract	Zika virus (ZIKV) is a positive-sense single-stranded virus member of the
MeSH term(s)	Humans ; Zika Virus/metabolism ; Zika Virus Infection/drug therapy ; Models, Molecular ; Antiviral Agents/chemistry ; Viral Nonstructural Proteins/metabolism
Chemical Substances	Antiviral Agents ; Viral Nonstructural Proteins
Language	English
Publishing date	2024-02-19
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2019364-6
ISSN	1422-0067 ; 1422-0067 ; 1661-6596
ISSN (online)	1422-0067
ISSN	1422-0067 ; 1661-6596
DOI	10.3390/ijms25042437
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Article ; Online: Serendipitous Identification of Azine Anticancer Agents Using a Privileged Scaffold Morphing Strategy.

Cesarini, Silvia / Vicenti, Ilaria / Poggialini, Federica / Filippi, Silvia / Mancin, Eleonora / Fiaschi, Lia / De Marchi, Elisa / Giammarino, Federica / Vagaggini, Chiara / Bizzarri, Bruno Mattia / Saladino, Raffaele / Dreassi, Elena / Zazzi, Maurizio / Botta, Lorenzo

Molecules (Basel, Switzerland)

2024 Volume 29, Issue 7

Abstract: The use of privileged scaffolds as a starting point for the construction of libraries of bioactive compounds is a widely used strategy in drug discovery and development. Scaffold decoration, morphing and hopping are additional techniques that enable the ... ...

Abstract	The use of privileged scaffolds as a starting point for the construction of libraries of bioactive compounds is a widely used strategy in drug discovery and development. Scaffold decoration, morphing and hopping are additional techniques that enable the modification of the chosen privileged framework and better explore the chemical space around it. In this study, two series of highly functionalized pyrimidine and pyridine derivatives were synthesized using a scaffold morphing approach consisting of triazine compounds obtained previously as antiviral agents. Newly synthesized azines were evaluated against lymphoma, hepatocarcinoma, and colon epithelial carcinoma cells, showing in five cases acceptable to good anticancer activity associated with low cytotoxicity on healthy fibroblasts. Finally, ADME in vitro studies were conducted on the best derivatives of the two series showing good passive permeability and resistance to metabolic degradation.
MeSH term(s)	Humans ; Antineoplastic Agents/pharmacology ; Antiviral Agents/pharmacology ; Azo Compounds ; Carcinoma, Hepatocellular ; Liver Neoplasms
Chemical Substances	Antineoplastic Agents ; Antiviral Agents ; Azo Compounds
Language	English
Publishing date	2024-03-24
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	1413402-0
ISSN	1420-3049 ; 1431-5165 ; 1420-3049
ISSN (online)	1420-3049
ISSN	1431-5165 ; 1420-3049
DOI	10.3390/molecules29071452
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Article ; Online: Proteins from Tenebrio molitor: An interesting functional ingredient and a source of ACE inhibitory peptides

Brai, Annalaura / Immacolata Trivisani, Claudia / Vagaggini, Chiara / Stella, Roberto / Angeletti, Roberto / Iovenitti, Giulia / Francardi, Valeria / Dreassi, Elena

Food Chemistry. 2022 Nov., v. 393 p.133409-

2022

Abstract: The angiotensin-converting enzyme (ACE) inhibitory potential of the main protein fractions from Tenebrio molitor larvae (TML) was examined to evaluate their use as a novel antihypertensive functional food. Both fractions contained YAN tripeptide, ... ...

Abstract	The angiotensin-converting enzyme (ACE) inhibitory potential of the main protein fractions from Tenebrio molitor larvae (TML) was examined to evaluate their use as a novel antihypertensive functional food. Both fractions contained YAN tripeptide, previously reported as responsible for ACE inhibition. Although YAN has been synthesized and was used as a standard for LC-MS/MS quantification and IC₅₀ against ACE was determined, low yields of YAN from TML did not explain adequately the activity of the whole protein fraction. LC-HRMS/MS investigation led to the identification of other three peptides, which were evaluated in silico, synthesized and tested against ACE. Among them, tetrapeptide NIKY showed the most promising activity (52 µM), highlighting once more the potential of TML and paving the way for exploitation in novel foods.
Keywords	Tenebrio molitor ; computer simulation ; food chemistry ; functional foods ; ingredients ; peptidyl-dipeptidase A ; tripeptides ; Edible insects ; ACE inhibition ; Active peptides ; Sustainable proteins
Language	English
Dates of publication	2022-11
Publishing place	Elsevier Ltd
Document type	Article ; Online
ZDB-ID	243123-3
ISSN	1873-7072 ; 0308-8146
ISSN (online)	1873-7072
ISSN	0308-8146
DOI	10.1016/j.foodchem.2022.133409
Database	NAL-Catalogue (AGRICOLA)

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