Lug-15 is a rapid bactericide exhibiting strong antibacterial activity against various Gram-positive and Gram-negative bacteria, including drug-resistant strains. It swiftly eradicates bacteria primarily by disrupting bacterial cell membranes and has a very low tendency to induce resistance. Lug-15 shows low hemolytic toxicity and demonstrates significant efficacy in various infection models. It can be used for research on combating multidrug-resistant infections.

Lug-15 exhibits strong antibacterial activity against both Gram-positive and Gram-negative bacteria. The MIC values are as follows: Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA) at 3.13 μg/mL, Enterococcus faecium at 6.25 μg/mL, and Pseudomonas aeruginosa, Acinetobacter baumannii, and Escherichia coli at 12.5 μg/mL. At 2× MIC for 0-12 hours, Lug-15 reduces colony-forming units of Staphylococcus aureus and Enterococcus faecium, and decreases Escherichia coli counts from 10^5.5 CFU/mL to zero within 4 hours. At 0.5-4× MIC for 0.5-1 hour, it compromises the integrity of the bacterial outer/inner membranes in Staphylococcus aureus and Escherichia coli, inducing irreversible membrane damage in Escherichia coli. Additionally, at 0.5-4× MIC for 4 hours, Lug-15 significantly reduces intracellular ATP levels and enhances ROS levels in Staphylococcus aureus in a concentration-dependent manner. Lug-15 is highly challenging to induce resistance in Staphylococcus aureus upon 21 passages at 0.5× MIC. At 6.25-200 μg/mL for 1 hour, its hemolysis rate on rat erythrocytes at effective antibacterial concentrations is below 10%. Moreover, it demonstrates good stability in mammalian serum and retains its antibacterial activity in complex physiological environments over 0-48 hours.

Lug-15 (1 mg/mL, eye drops, multiple applications) is effective in treating methicillin-resistant Staphylococcus aureus (MRSA) or Pseudomonas aeruginosa eye infections in mice. Additionally, Lug-15 (5-15 mg/kg, administered intraperitoneally or topically as a hydrogel, in single or 2-4 doses) shows significant efficacy in mouse models of MRSA infection in the thighs, lungs, and wounds.