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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
Database	MEDical Literature Analysis and Retrieval System OnLINE

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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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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
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Zs.A 1850: Show issues

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Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
Jg. 1995 - 2021: Lesesall (1.OG)
ab Jg. 2022: Lesesaal (EG)

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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: A novel bioresponsive self-immolative spacer based on aza-quinone methide reactivity for the controlled release of thiols, phenols, amines, sulfonamides or amides.

Ermini, Elena / Brai, Annalaura / Cini, Elena / Finetti, Federica / Giannini, Giuseppe / Padula, Daniele / Paradisi, Lucrezia / Poggialini, Federica / Trabalzini, Lorenza / Tolu, Paola / Taddei, Maurizio

Chemical science

2024 Volume 15, Issue 16, Page(s) 6168–6177

Abstract: A stimuli-sensitive linker is one of the indispensable components of prodrugs for cancer therapy as it covalently binds the drug and releases it upon external stimulation at the tumour site. Quinone methide elimination has been widely used as the key ... ...

Abstract	A stimuli-sensitive linker is one of the indispensable components of prodrugs for cancer therapy as it covalently binds the drug and releases it upon external stimulation at the tumour site. Quinone methide elimination has been widely used as the key transformation to release drugs based on their nucleofugacity. The usual approach is to bind the drug to the linker as a carbamate and release it as a free amine after a self-immolative 1,6-elimination. Although this approach is very efficient, it is limited to amines (as carbamates), alcohols or phenols (as carbonates) or other acidic functional groups. We report here a self-immolative spacer capable of directly linking and releasing amines, phenols, thiols, sulfonamides and carboxyamides after a reductive stimulus. The spacer is based on the structure of (5-nitro-2-pyrrolyl)methanol (NPYM-OH), which was used for the direct alkylation of the functional groups mentioned above. The spacer is metabolically stable and has three indispensable sites for bioconjugation: the bioresponsive trigger, the conjugated 1,6 self-immolative system and a third arm suitable for conjugation with a carrier or other modifiers. Release was achieved by selective reduction of the nitro group over Fe/Pd nanoparticles (NPs) in a micellar aqueous environment (H
Language	English
Publishing date	2024-04-02
Publishing country	England
Document type	Journal Article
ZDB-ID	2559110-1
ISSN	2041-6539 ; 2041-6520
ISSN (online)	2041-6539
ISSN	2041-6520
DOI	10.1039/d4sc01576b
Database	MEDical Literature Analysis and Retrieval System OnLINE

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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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Article ; Online: Viral Envelope Membrane: A Special Entry Pathway and a Promising Drug Target.

Palombi, Nastasja / Brai, Annalaura / Gerace, Martina / Di Maria, Salvatore / Orofino, Francesco / Corelli, Federico

Current medicinal chemistry

2021 Volume 28, Issue 34, Page(s) 6957–6976

Abstract: Enveloped viruses belong to a large class of pathogens responsible for multiple serious diseases. Their spread into new territories has been the cause of major epidemics throughout human history, including the Spanish flu in 1918 and the latest COVID-19 ... ...

Abstract	Enveloped viruses belong to a large class of pathogens responsible for multiple serious diseases. Their spread into new territories has been the cause of major epidemics throughout human history, including the Spanish flu in 1918 and the latest COVID-19 pandemic. Thanks to their outer membrane, consisting essentially of host lipids, enveloped viruses are more resistant to enzymes and are also less susceptible to host immune defenses than their naked counterparts. Therefore, the development of effective approaches to combat enveloped virus infections represents a major challenge for antiviral therapy in the current century. This review focuses on the characteristics of enveloped viruses, their importance in the entry phase, drugs targeting envelope membrane- mediated entry, and those specifically designed to target the envelope. The broad- -spectrum antiviral activity of these compounds can be attributed to their ability to affect the envelope, an essential structural feature common to several viruses. This makes this class of compounds agents of great interest when no specific drugs or vaccines are available to block viral infections.
MeSH term(s)	Antiviral Agents/pharmacology ; COVID-19 ; Humans ; Influenza Pandemic, 1918-1919 ; Pandemics ; Pharmaceutical Preparations ; SARS-CoV-2 ; Viral Envelope ; Virus Internalization
Chemical Substances	Antiviral Agents ; Pharmaceutical Preparations
Language	English
Publishing date	2021-02-18
Publishing country	United Arab Emirates
Document type	Journal Article ; Review
ZDB-ID	1319315-6
ISSN	1875-533X ; 0929-8673
ISSN (online)	1875-533X
ISSN	0929-8673
DOI	10.2174/0929867328666210218182203
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Zs.A 4432: Show issues

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Jg. 1995 - 2021: Lesesall (2.OG)
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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 Volume 393, Page(s) 133409

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 IC
MeSH term(s)	Angiotensin-Converting Enzyme Inhibitors/pharmacology ; Animals ; Chromatography, Liquid ; Peptides/pharmacology ; Peptidyl-Dipeptidase A ; Tandem Mass Spectrometry ; Tenebrio
Chemical Substances	Angiotensin-Converting Enzyme Inhibitors ; Peptides ; Peptidyl-Dipeptidase A (EC 3.4.15.1)
Language	English
Publishing date	2022-06-09
Publishing country	England
Document type	Journal Article
ZDB-ID	243123-3
ISSN	1873-7072 ; 0308-8146
ISSN (online)	1873-7072
ISSN	0308-8146
DOI	10.1016/j.foodchem.2022.133409
Database	MEDical Literature Analysis and Retrieval System OnLINE

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