4.7 Article

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

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PHARMACEUTICS
卷 14, 期 2, 页码 -

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MDPI
DOI: 10.3390/pharmaceutics14020249

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enrofloxacin; calcium(II) complex; veterinary drug; antibacterial activity; animal chemotherapy

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A new complex, EFX-Ca, was synthesized by reacting enrofloxacin with Ca(II). The study showed that EFX-Ca had lower toxicity and better therapeutic effects in bacteria and zebrafish.
Enrofloxacin (EFX) reacting with Ca(II) afforded a new complex, [Ca(EFX)(2)(H2O)(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 LD50 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 H2O2 or CuSO4 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.

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