Albumin as a functional carrier solubilizing and facilitating fusidic acid transmembrane delivery into Gram-negative bacteria.
Int J Biol Macromol
; 277(Pt 1): 134019, 2024 Oct.
Article
in En
| MEDLINE
| ID: mdl-39059524
ABSTRACT
Reversing the bacterial resistance is of great significance and importance. Fusidic acid (FA) is commonly effective against Gram-positive bacterial infections, but most Gram-negative bacteria have intrinsic resistance to FA, primarily due to the strong cell membrane-FA interactions, which highly inhibit the intracellular transport of FA. Herein, we use albumin (bovine serum albumin, BSA) as a bifunctional carrier to solubilize FA and facilitate its transmembrane delivery into Gram-negative bacterial cells. The water solubility of FA is significantly enhanced from 11.87 to 442.20 µg/mL by 5 mg/mL BSA after forming FA-BSA complex. Furthermore, FA-BSA (200 µg/mL) causes 99.96 % viability loss to the model pathogen E. coli upon incubation for 3 h, while free FA or BSA alone shows little activity. Elongation of E. coli cells after treated by FA-BSA is demonstrated by SEM, and the transmembrane transport of FA-BSA is demonstrated by CLSM. Interestingly, increasing the BSA amount substantially reduce the antibacterial activity of FA-BSA, implying an albumin-based transmembrane delivery mechanism may exist. This is the first report regarding successfully reversing the intrinsic resistance of Gram-negative bacteria to FA in the form of FA-BSA. The ready availability of albumin and the simple preparation allows FA-BSA to have great potentials for clinical use.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Solubility
/
Serum Albumin, Bovine
/
Escherichia coli
/
Fusidic Acid
Limits:
Animals
Language:
En
Journal:
Int J Biol Macromol
Year:
2024
Document type:
Article
Affiliation country:
Country of publication: