Marbofloxacin combined with heavy rare-earth ions makes better candidates for veterinary drugs: crystal structure and bio-activity studies

Chen, Zhi-chuan1; Liu, Rui-xue1,2; Xie, Yan-jie1; Hu, Qin1; Huang, Fu-ping1; Liu, Yan-cheng1; Liang, Hong1

2024-02-27

10.1039/d3dt03343k

DALTON TRANSACTIONS   影响因子和分区

1477-9226

1477-9234

["Marbofloxacin (MB) is a newly developed fluoroquinolone antibiotic used especially as a veterinary drug. It may be regarded as the improved version of enrofloxacin owing to its antibacterial activity, enhanced bioavailability, and pharmacokinetic-pharmacodynamic (PK-PD) properties. In this study, nine heavy rare-earth ions (Y, Gd, Tb, Dy, Ho, Er, Tm, Yb, and Lu) were selected in light of their potential antibacterial activity and satisfactory biosafety to afford the corresponding rare-earth metal complexes of MB: the MB-Ln series. Their chemical structures and coordination patterns were characterized using IR spectroscopy, HRMS, TGA, and X-ray single-crystal diffraction analysis. Our results confirmed that all the MB-Ln complexes yielded the coincident coordination modes with four MB ligands coordinating to the Ln(iii) center. In vitro antibacterial screening on five typical bacteria strains revealed that the MB-Ln complexes exhibited antibacterial activities comparable with MB, as indicated by the MIC/MBC values, in which Escherichia coli and Salmonella typhi were the most sensitive ones to MB-Ln. Furthermore, the MB-Ln complexes were found to be much less toxic in vivo than MB, as suggested by the evaluated LD50 (50% lethal dose) values. All the MB-Ln series complexes fell in the LD50 range of 5000-15 000 mg kg-1, while the LD50 value of MB was only 1294 mg kg-1. Furthermore, MB-Lu, as the selected representative of MB-Ln, could effectively inhibit the activity of DNA gyrase, the same as MB, suggesting the primary antibacterial mechanism of the MB-Ln series. The results demonstrated the good prospects and potential of metal-based veterinary drugs with better drug performance.","Marbofloxacin (MB) combined with heavy rare earth ion makes a series of MB-Ln complexes, who exhibit similar antibacterial activity to MB, but much lower in vivo acute toxicity than MB, suggesting their better medicinal prospect as veterinary drugs."]

SCI ; EI

英语

其他

Guangxi Scientific Research and Technology Development Program[GuiKe/AB20297059] ; Guangxi Key Laboratory of Agricultural Resources Chemistry and Biotechnology[2022KF01]

Chemistry

Chemistry, Inorganic & Nuclear

WOS:001157797600001

ROYAL SOC CHEMISTRY

CHEMISTRY

Web of Science

1.Guangxi Normal Univ, Collaborat Innovat Ctr Guangxi Ethn Med, Sch Chem & Pharmaceut Sci, Minist Educ China,Key Lab Chem & Mol Engn Med Reso, Guilin 541004, Peoples R China
2.Southern Univ Sci & Technol, Dept Chem, Shenzhen 518055, Peoples R China

Chen, Zhi-chuan,Liu, Rui-xue,Xie, Yan-jie,et al. Marbofloxacin combined with heavy rare-earth ions makes better candidates for veterinary drugs: crystal structure and bio-activity studies[J]. DALTON TRANSACTIONS,2024,53(9).

Chen, Zhi-chuan.,Liu, Rui-xue.,Xie, Yan-jie.,Hu, Qin.,Huang, Fu-ping.,...&Liang, Hong.(2024).Marbofloxacin combined with heavy rare-earth ions makes better candidates for veterinary drugs: crystal structure and bio-activity studies.DALTON TRANSACTIONS,53(9).

Chen, Zhi-chuan,et al."Marbofloxacin combined with heavy rare-earth ions makes better candidates for veterinary drugs: crystal structure and bio-activity studies".DALTON TRANSACTIONS 53.9(2024).