Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 2 de 2
Filtrar
Mais filtros











Base de dados
Intervalo de ano de publicação
1.
ChemMedChem ; 13(20): 2229-2239, 2018 10 22.
Artigo em Inglês | MEDLINE | ID: mdl-30157309

RESUMO

As a growing public health concern, the worldwide spread of antimicrobial resistance urges the development of new therapies. Antibacterial photodynamic therapy (a-PDT) may be an alternative to conventional antibiotic therapy. Herein we report the synthesis and characterization of seven original reactive oxygen species (ROS)-producing ruthenium(II) polypyridyl complexes. These are part of a collection of 17 derivatives varying in terms of the nature of the substituent(s), molecular symmetry, electrical charge, and counterions. They were characterized by considering 1) their physical properties (absorption coefficient at irradiation wavelength, 1 O2 generation quantum yield, luminescence) and 2) their antibacterial activity in a series of photodynamic assays using Gram-positive and Gram-negative bacteria of clinical relevance. The results unveiled some structure-activity relationships: one derivative that combines multiple beneficial features for a-PDT was effective against all the bacteria considered, regardless of their Gram status, species, or antibiotic resistance profile. This systematic study could guide the design of next-generation ruthenium-based complexes for enhanced antibacterial photodynamic strategies.


Assuntos
Antibacterianos/farmacologia , Complexos de Coordenação/farmacologia , Fenantrolinas/farmacologia , Fármacos Fotossensibilizantes/farmacologia , Rutênio/química , Antibacterianos/síntese química , Antibacterianos/efeitos da radiação , Antibacterianos/toxicidade , Complexos de Coordenação/síntese química , Complexos de Coordenação/efeitos da radiação , Complexos de Coordenação/toxicidade , Escherichia coli/efeitos dos fármacos , Ligantes , Luz , Luminescência , Medições Luminescentes , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Estrutura Molecular , Fenantrolinas/síntese química , Fenantrolinas/efeitos da radiação , Fenantrolinas/toxicidade , Fármacos Fotossensibilizantes/síntese química , Fármacos Fotossensibilizantes/efeitos da radiação , Fármacos Fotossensibilizantes/toxicidade , Pseudomonas aeruginosa/efeitos dos fármacos , Oxigênio Singlete/metabolismo , Relação Estrutura-Atividade
2.
Biosci Rep ; 37(6)2017 Dec 22.
Artigo em Inglês | MEDLINE | ID: mdl-29046368

RESUMO

The pathophysiology of obstructive pulmonary diseases, such as cystic fibrosis (CF), leads to the development of chronic infections in the respiratory tract. Thus, the symptomatic management of the disease requires, in particular, repetitive antibiotherapy. Besides these antibacterial treatments, certain pathologies, such as CF or chronic obstructive pulmonary disease (COPD), require the intake of many drugs. This simultaneous absorption may lead to undesirable drug interactions. For example, Orkambi® (lumacaftor/Ivacaftor, Vertex), a pharmacological drug employed to treat F508del patients, cannot be used with antibiotics such as rifampicin or rifabutin (rifamycin family) which are necessary to treat Mycobacteriaceae. As far as gene therapy is concerned, bacteria and/or biofilm in the airways present an additional barrier for gene transfer. Thus, aerosol administration of nanoparticles have to overcome many obstacles before allowing cellular penetration of therapeutic compounds. This review focusses on the development of aerosol formulations adapted to the respiratory tract and its multiple barriers. Then, formulations that are currently used in clinical applications are summarized depending on the active molecule delivered. Finally, we focus on new therapeutic approaches to reduce possible drug interactions by transferring the antibacterial activity to the nanocarrier while ensuring the transfection efficiency.


Assuntos
Antibacterianos/administração & dosagem , Terapia Genética/métodos , Pneumopatias Obstrutivas/terapia , Nanocápsulas/administração & dosagem , Transfecção/métodos , Aerossóis , Interações Medicamentosas , Humanos , Pneumopatias Obstrutivas/tratamento farmacológico , Pneumopatias Obstrutivas/microbiologia
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA