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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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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: 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: A Facile Access to Green Fluorescent Albumin Derivatives.

Saletti, Mario / Paolino, Marco / Venditti, Jacopo / Bonechi, Claudia / Giuliani, Germano / Lamponi, Stefania / Tassone, Giusy / Boccia, Antonella / Botta, Chiara / Blancafort, Lluís / Poggialini, Federica / Vagaggini, Chiara / Cappelli, Andrea

Chembiochem : a European journal of chemical biology

2024 Volume 25, Issue 8, Page(s) e202300862

Abstract: A Morita-Baylis-Hillman Adduct (MBHA) derivative bearing a triphenylamine moiety was found to react with human serum albumin (HSA) shifting its emission from the blue to the green-yellow thus leading to green fluorescent albumin (GFA) derivatives and ... ...

Abstract	A Morita-Baylis-Hillman Adduct (MBHA) derivative bearing a triphenylamine moiety was found to react with human serum albumin (HSA) shifting its emission from the blue to the green-yellow thus leading to green fluorescent albumin (GFA) derivatives and enlarging the platform of probes for aggregation-induced fluorescent-based detection techniques. A possible interaction of MBHA derivative 7 with a lipophilic pocket within the HSA structure was suggested by docking studies. DLS experiments showed that the reaction with HSA induce a conformational change of the protein contributing to the aggregation process of GFA derivatives. The results of investigations on the biological properties suggested that GFA retained the ability of binding drug molecules such as warfarin and diazepam. Finally, cytotoxicity evaluation studies suggested that, although the MBHA derivative 7 at 0.1 μg/mL affected the percentage of cell viability in comparison to the negative control, it cannot be considered cytotoxic, whereas at all the other concentrations≥0.5 μg/mL resulted cytotoxic at different extent.
MeSH term(s)	Humans ; Antineoplastic Agents/chemistry ; Proteins/metabolism ; Serum Albumin, Human/chemistry ; Protein Binding ; Spectrometry, Fluorescence ; Molecular Docking Simulation
Chemical Substances	Antineoplastic Agents ; Proteins ; Serum Albumin, Human (ZIF514RVZR)
Language	English
Publishing date	2024-03-13
Publishing country	Germany
Document type	Journal Article
ZDB-ID	2020469-3
ISSN	1439-7633 ; 1439-4227
ISSN (online)	1439-7633
ISSN	1439-4227
DOI	10.1002/cbic.202300862
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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
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Article ; Online: Early investigation of a novel SI306 theranostic prodrug for glioblastoma treatment.

Vagaggini, Chiara / Petroni, Debora / D'Agostino, Ilaria / Poggialini, Federica / Cavallini, Chiara / Cianciusi, Annarita / Salis, Annalisa / D'Antona, Lucia / Francesconi, Valeria / Manetti, Fabrizio / Damonte, Gianluca / Musumeci, Francesca / Menichetti, Luca / Dreassi, Elena / Carbone, Anna / Schenone, Silvia

Drug development research

2024 Volume 85, Issue 1, Page(s) e22158

Abstract: Glioblastoma multiforme (GBM) is one of the most aggressive malignancies with a high recurrence rate and poor prognosis. Theranostic, combining therapeutic and diagnostic approaches, arises as a successful strategy to improve patient outcomes through ... ...

Abstract	Glioblastoma multiforme (GBM) is one of the most aggressive malignancies with a high recurrence rate and poor prognosis. Theranostic, combining therapeutic and diagnostic approaches, arises as a successful strategy to improve patient outcomes through personalized medicine. Src is a non-receptor tyrosine kinase (nRTK) whose involvement in GBM has been extensively demonstrated. Our previous research highlighted the effectiveness of the pyrazolo[3,4-d]pyrimidine SI306 and its more soluble prodrug CMP1 as Src inhibitors both in in vitro and in vivo GBM models. In this scenario, we decided to develop a theranostic prodrug of SI306, ProSI-DOTA(
MeSH term(s)	Humans ; Precision Medicine ; Glioblastoma/diagnostic imaging ; Glioblastoma/drug therapy ; Blood-Brain Barrier ; Cell Line ; Prodrugs/pharmacology
Chemical Substances	Prodrugs
Language	English
Publishing date	2024-02-13
Publishing country	United States
Document type	Journal Article
ZDB-ID	604587-x
ISSN	1098-2299 ; 0272-4391
ISSN (online)	1098-2299
ISSN	0272-4391
DOI	10.1002/ddr.22158
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Article: Biological Evaluation and In Vitro Characterization of ADME Profile of In-House Pyrazolo[3,4-

Poggialini, Federica / Vagaggini, Chiara / Brai, Annalaura / Pasqualini, Claudia / Crespan, Emmanuele / Maga, Giovanni / Perini, Cecilia / Cabella, Noemi / Botta, Lorenzo / Musumeci, Francesca / Frosini, Maria / Schenone, Silvia / Dreassi, Elena

Pharmaceutics

2023 Volume 15, Issue 2

Abstract: The therapeutic use of tyrosine kinase inhibitors (TKIs) represents one of the successful strategies for the treatment of glioblastoma (GBM). Pyrazolo[3,4- ...

Abstract	The therapeutic use of tyrosine kinase inhibitors (TKIs) represents one of the successful strategies for the treatment of glioblastoma (GBM). Pyrazolo[3,4-
Language	English
Publishing date	2023-01-30
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2527217-2
ISSN	1999-4923
ISSN	1999-4923
DOI	10.3390/pharmaceutics15020453
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