The proposed technology is a novel conjugate of vancomycin (Van) and transportan 10 (TP10) and its antimicrobial application.
Vancomycin is an antibiotic with antimicrobial activity against Gram(+) aerobic and anaerobic bacteria. It is often used to treat infections caused by bacteria such as Staphylococcus aureus, Enterococcus spp. and Clostridium difficile. These infections often occur in people after a long hospital stay, chronic illness and a long period of antibiotic use.
Infections located in brain tissue such as bacterial meningitis are particularly dangerous. The efficacy of vancomycin is insufficient due to the increasing number of multidrug-resistant strains of nosocomial bacteria.
A team of researchers from UG and GUMed has invented an antibiotic with improved antibacterial efficacy and that penetrates brain tissue well. These properties were achieved by conjugating vancomycin with transportan 10 (TP10), which has antimicrobial activity and the ability to transport drugs into the cell.
Creation of Van-TP10 conjugates:
-improved pharmacokinetic and pharmacodynamic properties compared to vancomycin alone,
-while maintaining low cellular toxicity.
Van-TP10 conjugates show improved antimicrobial effects and low levels of toxicity against clinical strains of methylcilin-resistant Staphylococcus aureus (MRSA). The new conjugates may prove helpful in the treatment of life-threatening infections, especially those located in the brain, and could therefore be used as drugs in the pharmaceutical industry as an alternative to traditional vancomycin.
