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

Autor: Federica Sodano, Ferdinando Fiorino, Elisa Perissutti, Francesco Frecentese, Valentina Citi, Antonio Petti, Caroline Nunes Capello, Flavia Faganello Colombo, Era Gorica, Francesca Pavese, Vincenzo Calderone, Giuseppe Caliendo, Vincenzo Santagada, Marcelo Nicolas Muscará, Maria Grazia Rimoli, Elisa Magli, Alma Martelli, Heloisa Helena Araujo Ferreira, Angela Corvino, Barbara Rolando, Beatrice Severino, Simone Brogi
Přispěvatelé: 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.
Rok vydání: 2021
Předmět:
0301 basic medicine
Medicine (General)
Science (General)
Hydrogen sulfide
Anti-Inflammatory Agents
Pharmaceutical Science
Endogeny
Hybrids
Pharmacology
medicine.disease_cause
Adrenal Cortex Hormone
chemistry.chemical_compound
Q1-390
Mice
0302 clinical medicine
Adrenal Cortex Hormones
Multidisciplinary
S releasing compound
Steroidal anti-inflammatory drug
H2S releasing compounds
Steroidal anti-inflammatory drugs
Anti-Inflammatory Agent
030220 oncology & carcinogenesis
medicine.symptom
Human
Asthma
H
2
S releasing compounds
Lung diseases
Inflammation
03 medical and health sciences
R5-920
In vivo
medicine
Molecule
Animals
Humans
ComputingMethodologies_COMPUTERGRAPHICS
Animal
medicine.disease
ANTI-INFLAMATÓRIOS
In vitro
Hybrid
Disease Models
Animal
030104 developmental biology
chemistry
Lung disease
Oxidative stress
Zdroj: Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual)
Universidade de São Paulo (USP)
instacron:USP
Journal of Advanced Research, Vol 35, Iss, Pp 267-277 (2022)
Journal of Advanced Research
Popis: Graphical abstract
Highlights • Hydrogen sulfide is a fundamental endogenous gas-mediator in the respiratory system. • Design and synthesis of SAIDs-hydrogen sulfide donors hybrids are described. • Hydrogen sulfide release and chemical stability at differing pH were investigated. • Prednisone-TBZ hybrid (compound 7) was selected for further evaluations. • Prednisone-TBZ is a promising therapeutic option in allergic asthma treatment.
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.
Databáze: OpenAIRE
Externí odkaz: