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Design and synthesis of INF195, a new NLRP3 Inflammasome Inhibitor with ex vivo cardioprotective effect

Abstract
Data di Pubblicazione:
2024
Abstract:
The NLRP3 inflammasome, a cytosolic multi protein complex involved in inflammatory processes, is emerging in the myocardial ischemia-reperfusion injury (IRI) framework, being engaged in both cell survival and damage [1-3]. In the search for novel NLRP3 inhibitors, we designed a series of compounds with the help of molecular docking techniques. The activity of the compounds was evaluated in vitro in human macrophages. One compound, INF195, was selected to investigate the cardioprotective properties [4]. We measured infarct size (IS) in isolated mouse hearts exposed to 30-minute global ischemia and then one-hour reperfusion, either in the absence or presence of different doses of INF195 (5, 10 or 20 µM). We also evaluated the production of the markers of NLRP3 activation, caspase-1 and IL-1β, measuring their concentrations in cardiac tissue homogenates. The results infer that heart pre-treatment with low doses of INF195, 5 and 10 µM, considerably reduce IS and IL-1β production, suggesting therefore that the activation of NLRP3 expressed in myocardial cells plays a role in IRI. Moreover, INF195 at low doses significantly reduced the infarcted area (the infusion at 5µM reduced IS from 64.8±1.9% to 38.1±1.3%). Overall, INF195 showed a promising cardioprotective effect worth of further studies.
Tipologia CRIS:
04F-Poster
Elenco autori:
Francesca Boccato, Simone Gastaldi, Magalì Giordano, Elisabetta Marini, Francesca Spyrakis, Pasquale Pagliaro, Claudia Penna, Massimo Bertinaria
Autori di Ateneo:
BERTINARIA Massimo
MARINI Elisabetta
PAGLIARO Pasquale
PENNA Claudia
SPYRAKIS Francesca
Link alla scheda completa:
https://iris.unito.it/handle/2318/1982150
Link al Full Text:
https://iris.unito.it/retrieve/handle/2318/1982150/1309848/Poster%20INF195_GIFC_2024%20def.pdf
https://iris.unito.it/retrieve/handle/2318/1982150/1309849/Boccato%20F_GIFC_2024.pdf
Titolo del libro:
Book of Abstract
Progetto:
Brain penetrant and gut-directed NLRP3 inhibitors in protection of physiological barriers.... - Finanziamento dell’Unione Europea – NextGenerationEU – missione 4, componente 2, investimento 1.1.
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Aree Di Ricerca

Settori (5)


PE5_18 - Medicinal chemistry - (2022)

MEDICINA, SALUTE e BENESSERE - Chimica e Salute

PIANETA TERRA, AMBIENTE, CLIMA, ENERGIA e SOSTENIBILITA' - Chimica e Ambiente

SCIENZE DELLA VITA e FARMACOLOGIA - Chimica Analitica e Farmaceutica

SCIENZE MATEMATICHE, CHIMICHE, FISICHE - Materiali Avanzati
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