A New Calcium(II)-Based Substitute for Enrofloxacin with Improved Medicinal Potential

Enrofloxacin (EFX) reacting with Ca(II) afforded a new complex, [Ca(EFX)(2)(H(2)O)(4)] (EFX-Ca), which was structurally characterized both in solid and solution chemistry. E. coli and S. typhi were tested to be the most sensitive strains for EFX-Ca. The LD(50) value of EFX-Ca in mice was 7736 mg/kg,...

Descripción completa

Detalles Bibliográficos
Autores principales: Yan, Hou-Tian, Liu, Rui-Xue, Yang, Qi-Zhen, Liu, Yan-Cheng, Li, Hong-Chang, Guo, Rui-Feng, Wu, Lin-Hua, Liu, Li-Min, Liang, Hong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8878047/
https://www.ncbi.nlm.nih.gov/pubmed/35213984
http://dx.doi.org/10.3390/pharmaceutics14020249
Descripción
Sumario:Enrofloxacin (EFX) reacting with Ca(II) afforded a new complex, [Ca(EFX)(2)(H(2)O)(4)] (EFX-Ca), which was structurally characterized both in solid and solution chemistry. E. coli and S. typhi were tested to be the most sensitive strains for EFX-Ca. The LD(50) value of EFX-Ca in mice was 7736 mg/kg, implying the coordination of EFX to Ca(II) effectively reduced its acute toxicity. EFX-Ca also decreased the plasma-binding rate and enhanced the drug distribution in rats along with longer elimination half-life. EFX-Ca also showed similar low in vivo acute toxicity and higher anti-inflammation induced by H(2)O(2) or CuSO(4) in zebrafish, with reactive oxygen species (ROS)-related elimination. The therapeutic effects of EFX-Ca on two types (AA and 817) of E. coli-infected broilers were also better than those of EFX, with cure rates of 78% and 88%, respectively. EFX-Ca showed promise as a bio-safe metal-based veterinary drug with good efficacy and lower toxicity.

Ejemplares similares