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

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

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Published in:Pharmaceutics 2022-01, Vol.14 (2), p.249
Main Authors: 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
Format: Article
Language:English
Subjects:
animal chemotherapy
Animal diseases
antibacterial activity
Antimicrobial agents
Aqueous solutions
Bacteria
calcium(II) complex
Crystal structure
Drug resistance
enrofloxacin
Ligands
Pharmacokinetics
R&D
Research & development
Toxicity
veterinary drug
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Summary:Enrofloxacin (EFX) reacting with Ca(II) afforded a new complex, [Ca(EFX) (H O) ] (EFX-Ca), which was structurally characterized both in solid and solution chemistry. and were tested to be the most sensitive strains for EFX-Ca. The LD 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 O or CuSO in zebrafish, with reactive oxygen species (ROS)-related elimination. The therapeutic effects of EFX-Ca on two types (AA and 817) of -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.
ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics14020249