AVX 13616 shows the potent in vivo antibacterial activity of Avexa’s lead antibacterial candidate; particularly against drug-resistant Staphylococcus pathogens. IC50 value: 2-4 ug/ml (MICs) Target: antibacterial agent AVX13616 was as active as mupirocin i
Oritavancin is a novel semisynthetic glycopeptide antibiotics. On August 6, 2014, the FDA approved oritavancin for treatment of skin infections. Oritavancin possesses potent and rapid bactericidal activity in vitro against a broad spectrum of both resistant and susceptible Gram-positive bacteria, including Staphylococcus aureus, MRSA, enterococci, and streptococci.
Kocurin is a thiazolyl peptide originally isolated fromK. palustrisand has antibiotic activity.1It is active against methicillin-resistantS. aureus(MRSA; MIC = 0.25 μg/ml), as well asB. subtilisandE. faeciumin a solid agar test when used at a concentration of 8 μg/ml. Kocurin is also active againstE. faecium,E. faecalis,S. epidermidis, and clinical isolates of vancomycin-resistant enterococci (MICs = 0.004-1.025 μg/ml).2In vivo, kocurin (2.5, 5, and 10 mg/ml) increases survival in a mouse model ofE. faecium-induced septicemia. It decreases the number of colony forming units (CFUs) in a mouse model of MRSA lung infection.
1.Martin, J., da S. Sousa, T., Crespo, G., et al.Kocurin, the true structure of PM181104, an anti-methicillin-resistant Staphylococcus aureus (MRSA) thiazolyl peptide from the marine-derived bacterium Kocuria palustrisMar. Drugs11(2)387-398(2013) 2.Mahajan, G., Thomas, B., Parab, R., et al.In vitro and in vivo activities of antibiotic PM181104Antimicrob. Agents Chemother.57(11)5315-5319(2013)
Platencin is a natural, broad spectrum Gram-positive antibiotic isolated from S. platensis, which is also the source of platensimycin . Platencin inhibits two key enzymes in bacterial fatty acid synthesis, β-ketoacyl-ACP synthases II and III (FabF and FabH, respectively), unlike platensimycin which only targets FabF. The IC50 values for platencin against FabF and FabH are 1.95 and 3.91 μg/ml, respectively. It does not exhibit cross-resistance to antibiotic resistant bacterial strains, including methicillin-resistant S. aureus, vancomycin-intermediate S. aureus, and vancomycin-resistant Enterococci. For these reasons, platencin has potential applications in fighting antibiotic resistant bacteria.
Glyasperin C acts as a partial estrogen antagonist, it shows tyrosinase inhibitory activity (IC (50) = 0.13 +/- 0.01 microg/mL), it could be a promising candidate in the design of skin-whitening agents. Glyasperin C shows potent anti-vancomycin-resistant