Anti-microbial efficacy, mechanisms and druggability evaluation of the natural flavonoids.
J Appl Microbiol
; 133(3): 1975-1988, 2022 Sep.
Article
em En
| MEDLINE
| ID: mdl-35801665
ABSTRACT
AIMS:
This study was conducted to evaluate 35 natural flavonoids for their in vitro susceptibility against E. coli (ATCC 25922), Ps. aeruginosa (ATCC 27853), B. subtilis (ATCC 530) and Staph. aureus (ATCC 6538) in search of a potential broad-spectrum antibiotic. METHODS ANDRESULTS:
Glabridin, a natural isoflavonoid isolated from Glycyrrhiza glabra L., was identified to be highly active with a MIC of 8-16 µg ml-1 against Staph. aureus, B. subtilis and E. coli. By the results of the docking simulation, we located the potential targets of glabridin as DNA gyrase and dihydrofolate reductase (DHFR). The subsequent DNA gyrase inhibition assays (glabridin IC50 = 0.8516 µmol L-1 , ciprofloxacin IC50 = 0.04697 µmol L-1 ), DHFR inhibition assays (glabridin inhibition ratio = 29%, methotrexate inhibition ratio = 45% under 100 µmol L-1 treatment) and TUNEL confirmed that glabridin acted as DNA gyrase inhibitor and DHFR mild inhibitor, exerting bactericidal activity by blocking bacterial nucleic acid synthesis. CCK-8 and in silico calculations were also conducted to verify the low cytotoxicity and acceptable druggability of glabridin.CONCLUSION:
These findings suggest that glabridin represents the prototypical member of an exciting structural class of natural antimicrobial agents. SIGNIFICANCE AND IMPACT OF THE STUDY This study reports a novel mechanism of bactericidal activity of glabridin against Staph. aureus.Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Flavonoides
/
Glycyrrhiza
Tipo de estudo:
Prognostic_studies
Idioma:
En
Revista:
J Appl Microbiol
Assunto da revista:
MICROBIOLOGIA
Ano de publicação:
2022
Tipo de documento:
Article
País de afiliação:
China