Resistance modulatory and efflux-inhibitory activities of capsaicinoids and capsinoids.
Bioorg Chem
; 82: 378-384, 2019 02.
Article
en En
| MEDLINE
| ID: mdl-30428416
ABSTRACT
Capsaicinoids are reported to have a bunch of promising pharmacological activities, among them antibacterial effects against various strains of bacteria. In this study the effect on efflux pumps of mycobacteria was investigated. The importance of efflux pumps, and the inhibition of these, is rising due to their involvement in antibiotic resistance development. In order to draw structure and activity relationships we tested natural and synthetical capsaicinoids as well as synthetical capsinoids. In an accumulation assay these compounds were evaluated for their ability to accumulate ethidium bromide into mycobacterial cells, a well-known substrate for efflux pumps. Capsaicin and dihydrocapsaicin, the two most abundant capsaicinoids in Capsicum species, proved to be superior efflux pump inhibitors compared to the standard verapamil. A dilution series showed dose dependency of both compounds. The compound class of less pungent capsinoids qualified for further investigation as antibacterials against Mycobacterium smegmatis.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Ésteres
/
Ácidos Grasos
/
Amidas
/
Guayacol
/
Antibacterianos
Idioma:
En
Año:
2019
Tipo del documento:
Article