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.

H2S donating corticosteroids: Design, synthesis and biological evaluation in a murine model of asthma / Corvino, A.; Citi, V.; Fiorino, F.; Frecentese, F.; Magli, E.; Perissutti, E.; Santagada, V.; Calderone, V.; Martelli, A.; Gorica, E.; Brogi, S.; Colombo, F. F.; Capello, C. N.; Araujo Ferreira, H. H.; Rimoli, M. G.; Sodano, F.; Rolando, B.; Pavese, F.; Petti, A.; Muscara, M. N.; Caliendo, G.; Severino, B.. - In: JOURNAL OF ADVANCED RESEARCH. - ISSN 2090-1232. - 35:(2022), pp. 267-277. [10.1016/j.jare.2021.05.008]

H2S donating corticosteroids: Design, synthesis and biological evaluation in a murine model of asthma

Corvino A.;Fiorino F.;Frecentese F.;Magli E.;Perissutti E.;Santagada V.;Rimoli M. G.;Sodano F.;Caliendo G.;Severino B.
2022

Abstract

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.
2022
H2S donating corticosteroids: Design, synthesis and biological evaluation in a murine model of asthma / Corvino, A.; Citi, V.; Fiorino, F.; Frecentese, F.; Magli, E.; Perissutti, E.; Santagada, V.; Calderone, V.; Martelli, A.; Gorica, E.; Brogi, S.; Colombo, F. F.; Capello, C. N.; Araujo Ferreira, H. H.; Rimoli, M. G.; Sodano, F.; Rolando, B.; Pavese, F.; Petti, A.; Muscara, M. N.; Caliendo, G.; Severino, B.. - In: JOURNAL OF ADVANCED RESEARCH. - ISSN 2090-1232. - 35:(2022), pp. 267-277. [10.1016/j.jare.2021.05.008]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/880655
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