Journal of advanced research · 2021
H2S donating corticosteroids: Design, synthesis and biological evaluation in a murine model of asthma.
СтатьяПоддержка исследования: вне правительства СШАНазвание и аннотация: Перевод в очереди
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Corvino Angela, Citi Valentina, Fiorino Ferdinando, Frecentese Francesco, Magli Elisa, Perissutti Elisa, Santagada Vincenzo, Calderone Vincenzo, Martelli Alma, Gorica Era, Brogi Simone, Colombo Flavia Faganello, Capello Caroline Nunes, Araujo Ferreira Heloisa Helena, Rimoli Maria Grazia, Sodano Federica, Rolando Barbara, Pavese Francesca, Petti Antonio, Muscará Marcelo Nicolás, Caliendo Giuseppe, Severino Beatrice
Аннотация
INTRODUCTION: Hydrogen sulfide (H2S) is a fundamental biological endogenous gas-mediator in the respiratory system. It regulates pivotal patho-physiological processes such as oxidative stress, pulmonary circulation, airway tone and inflammation.
OBJECTIVES: We herein describe the design and synthesis of molecular hybrids obtained by the condensation of several corticosteroids with different hydrogen sulfide releasing moieties.
METHODS: All the molecules are characterized for their ability to release H2S both via amperometric approach and using a fluorescent probe. The chemical stability of the newly synthesized hybrid molecules has been investigated at differing pH values and in human serum.
RESULTS: Prednisone-TBZ hybrid (compound 7) was selected for further evaluations. The obtained results from the in vitro and in vivo studies clearly show evidence in favor of the anti-inflammatory properties of the released H2S.
CONCLUSIONS: The protective effect on airway remodeling makes the hybrid Prednisone-TBZ (compound 7) as a promising therapeutic option in reducing allergic asthma symptoms and exacerbations.
OBJECTIVES: We herein describe the design and synthesis of molecular hybrids obtained by the condensation of several corticosteroids with different hydrogen sulfide releasing moieties.
METHODS: All the molecules are characterized for their ability to release H2S both via amperometric approach and using a fluorescent probe. The chemical stability of the newly synthesized hybrid molecules has been investigated at differing pH values and in human serum.
RESULTS: Prednisone-TBZ hybrid (compound 7) was selected for further evaluations. The obtained results from the in vitro and in vivo studies clearly show evidence in favor of the anti-inflammatory properties of the released H2S.
CONCLUSIONS: The protective effect on airway remodeling makes the hybrid Prednisone-TBZ (compound 7) as a promising therapeutic option in reducing allergic asthma symptoms and exacerbations.