A New Calcium(II)-Based Substitute for Enrofloxacin with Improved Medicinal Potential
Enrofloxacin (EFX) reacting with Ca(II) afforded a new complex, [Ca(EFX)<sub>2</sub>(H<sub>2</sub>O)<sub>4</sub>] (EFX-Ca), which was structurally characterized both in solid and solution chemistry. <i>E. coli</i> and <i>S. typhi</i> were t...
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| Format: | Article |
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MDPI AG
2022-01-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/2/249 |
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| author | Hou-Tian Yan Rui-Xue Liu Qi-Zhen Yang Yan-Cheng Liu Hong-Chang Li Rui-Feng Guo Lin-Hua Wu Li-Min Liu Hong Liang |
| author_facet | Hou-Tian Yan Rui-Xue Liu Qi-Zhen Yang Yan-Cheng Liu Hong-Chang Li Rui-Feng Guo Lin-Hua Wu Li-Min Liu Hong Liang |
| author_sort | Hou-Tian Yan |
| collection | DOAJ |
| description | Enrofloxacin (EFX) reacting with Ca(II) afforded a new complex, [Ca(EFX)<sub>2</sub>(H<sub>2</sub>O)<sub>4</sub>] (EFX-Ca), which was structurally characterized both in solid and solution chemistry. <i>E. coli</i> and <i>S. typhi</i> were tested to be the most sensitive strains for EFX-Ca. The LD<sub>50</sub> 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<sub>2</sub>O<sub>2</sub> or CuSO<sub>4</sub> in zebrafish, with reactive oxygen species (ROS)-related elimination. The therapeutic effects of EFX-Ca on two types (AA and 817) of <i>E. coli</i>-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. |
| first_indexed | 2024-03-09T21:14:49Z |
| format | Article |
| id | doaj.art-3b1965195f7847dbae2b5438ea7b8610 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T21:14:49Z |
| publishDate | 2022-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-3b1965195f7847dbae2b5438ea7b86102023-11-23T21:36:10ZengMDPI AGPharmaceutics1999-49232022-01-0114224910.3390/pharmaceutics14020249A New Calcium(II)-Based Substitute for Enrofloxacin with Improved Medicinal PotentialHou-Tian Yan0Rui-Xue Liu1Qi-Zhen Yang2Yan-Cheng Liu3Hong-Chang Li4Rui-Feng Guo5Lin-Hua Wu6Li-Min Liu7Hong Liang8School of Chemistry & Pharmaceutical Sciences, State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, Guangxi Normal University, Guilin 541004, ChinaSchool of Chemistry & Pharmaceutical Sciences, State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, Guangxi Normal University, Guilin 541004, ChinaSchool of Chemistry & Pharmaceutical Sciences, State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, Guangxi Normal University, Guilin 541004, ChinaSchool of Chemistry & Pharmaceutical Sciences, State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, Guangxi Normal University, Guilin 541004, ChinaSchool of Chemistry & Pharmaceutical Sciences, State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, Guangxi Normal University, Guilin 541004, ChinaSchool of Chemistry & Pharmaceutical Sciences, State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, Guangxi Normal University, Guilin 541004, ChinaCollege of Pharmacy, Guangxi Medical University, Nanning 530021, ChinaCollege of Pharmacy, Guangxi Medical University, Nanning 530021, ChinaSchool of Chemistry & Pharmaceutical Sciences, State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, Guangxi Normal University, Guilin 541004, ChinaEnrofloxacin (EFX) reacting with Ca(II) afforded a new complex, [Ca(EFX)<sub>2</sub>(H<sub>2</sub>O)<sub>4</sub>] (EFX-Ca), which was structurally characterized both in solid and solution chemistry. <i>E. coli</i> and <i>S. typhi</i> were tested to be the most sensitive strains for EFX-Ca. The LD<sub>50</sub> 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<sub>2</sub>O<sub>2</sub> or CuSO<sub>4</sub> in zebrafish, with reactive oxygen species (ROS)-related elimination. The therapeutic effects of EFX-Ca on two types (AA and 817) of <i>E. coli</i>-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.https://www.mdpi.com/1999-4923/14/2/249enrofloxacincalcium(II) complexveterinary drugantibacterial activityanimal chemotherapy |
| spellingShingle | Hou-Tian Yan Rui-Xue Liu Qi-Zhen Yang Yan-Cheng Liu Hong-Chang Li Rui-Feng Guo Lin-Hua Wu Li-Min Liu Hong Liang A New Calcium(II)-Based Substitute for Enrofloxacin with Improved Medicinal Potential Pharmaceutics enrofloxacin calcium(II) complex veterinary drug antibacterial activity animal chemotherapy |
| title | A New Calcium(II)-Based Substitute for Enrofloxacin with Improved Medicinal Potential |
| title_full | A New Calcium(II)-Based Substitute for Enrofloxacin with Improved Medicinal Potential |
| title_fullStr | A New Calcium(II)-Based Substitute for Enrofloxacin with Improved Medicinal Potential |
| title_full_unstemmed | A New Calcium(II)-Based Substitute for Enrofloxacin with Improved Medicinal Potential |
| title_short | A New Calcium(II)-Based Substitute for Enrofloxacin with Improved Medicinal Potential |
| title_sort | new calcium ii based substitute for enrofloxacin with improved medicinal potential |
| topic | enrofloxacin calcium(II) complex veterinary drug antibacterial activity animal chemotherapy |
| url | https://www.mdpi.com/1999-4923/14/2/249 |
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