Over the last years, we have been focused on chloramphenicol conjugates that combine in their structure chloramphenicol base with natural polyamines, spermine, spermidine and putrescine, and their modifications. Conjugate , with spermidine (SPD) as a natural polyamine linked to chloramphenicol base, showed the best antibacterial and anticancer properties. Using as a prototype, we here explored the influence of the antibacterial and anticancer activity of additional benzyl groups on N1 amino moiety together with modifications of the alkyl length of the aminobutyl fragment of SPD. Our data demonstrate that the novel modifications did not further improve the antibacterial activity of the prototype. However, one of the novel conjugates () showed anticancer activity without affecting bacterial growth, thus emerging as a promising anticancer agent, with no adverse effects on bacterial microflora when taken orally.
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http://dx.doi.org/10.3390/antibiotics8010009 | DOI Listing |
Poult Sci
January 2025
Avian Disease Research Center, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, PR China; Institute of Veterinary Medicine and Immunology, Sichuan Agricultural University, Chengdu 611130, PR China; Key Laboratory of Animal Disease and Human Health of Sichuan Province, Sichuan Agricultural University, Chengdu 611130, PR China; Engineering Research Center of Southwest Animal Disease Prevention and Control Technology, Ministry of Education, PR China. Electronic address:
Escherichia coli (E. coli) is a significant pathogen responsible for intestinal infections and foodborne diseases. The rise of antibiotic resistance poses a significant challenge to global public health.
View Article and Find Full Text PDFMikrochim Acta
January 2025
School of Science, Xihua University, Chengdu, 610039, People's Republic of China.
A dual-mode detection platform utilizing colorimetric and Raman was developed based on the exponential amplification reaction (EXPAR) strategy and a "core-satellite" structure constructed by bimetallic nanozymes to detect chloramphenicol (CAP). Initially, DNA-gated metal-organic frameworks (MOFs) incorporating cascaded amplification were used to be nanocarriers for the colorimetric and Raman reporter molecules (3,3',5,5'-tetramethylbiphenyl; TMB). Subsequently, assembled DNA served as gatekeepers to create a stimulus-responsive DNA-gated MOF (TMB@DNA/MOF).
View Article and Find Full Text PDFBiochimie
February 2025
China and Portugal Joint Research Center, Shaanxi International Cooperation Demonstration Base, Shaanxi University of Technology, Hanzhong, 723000, Shaanxi, China; Centre of Molecular and Environmental Biology, Department of Biology, University of Minho, Campus de Gualtar, 4710-057, Braga, Portugal; Department of Biomedical Sciences, Ontario Veterinary College, University of Guelph, N1G 2W1, Guelph, Ontario, Canada. Electronic address:
Small molecule drugs often exhibit short half-lives, requiring frequent administrations to maintain therapeutic concentrations over an extended period. To address this issue, the fragment crystallizable (Fc) region of IgG, known to prolong the half-life of antibodies via its interaction with the Fc neonatal receptor, was harnessed as a carrier protein to extend the half-life of a small molecule drug, florfenicol. Florfenicol, was chemically coupled to a recombinant Fc protein expressed using the eukaryotic expression system in HEK293 cells.
View Article and Find Full Text PDFBMC Microbiol
September 2024
Institute of Microbiology, Faculty of Veterinary Science, University of Veterinary and Animal Sciences, Lahore, Pakistan.
Semin Ophthalmol
February 2025
Corneoplastic Unit, Queen Victoria Hospital NHS Foundation Trust, East Grinstead, UK.
Purpose: Topical chloramphenicol is one of the most ubiquitous antibiotics used in ophthalmology and oculoplastic surgery globally. It shows broad-spectrum activity against a variety of different pathogenic organisms, is well tolerated on the ocular surface and displays excellent topical pharmacokinetics. Chloramphenicol has been available for purchase over the counter in the United Kingdom since 2005.
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