Lolamicin is a Gram-negative selective antibiotic targeting the lipoprotein transport system LolCDE complex. It exhibits activity against over 130 multidrug-resistant clinical isolates, improves survival rates in mouse models of septicemia and pneumonia, and protects the gut microbiota.

In the in vitro antibacterial experiments, Lolamicin (1-8 μg/mL, overnight culture) significantly reduced the survival rates of Gram-negative bacteria such as Escherichia coli, Klebsiella pneumoniae, and Enterobacter cloacae by inhibiting the lipoprotein transport system LolCDE [1].
In the drug resistance mutation screening experiments, Lolamicin (8×MIC, 48 hours) induced mutations in the LolC/LolE proteins (e.g., E195K, D264N) in Escherichia coli, Klebsiella pneumoniae, and Enterobacter cloacae, and these mutant strains exhibited significantly reduced susceptibility to Lolamicin [1].
In the confocal microscopy observation experiments, Lolamicin (3×MIC, 1.5 hours) induced cell swelling in wild-type Escherichia coli and Klebsiella pneumoniae, whereas resistant mutant strains such as LolC-N265K and LolE-D264N did not exhibit this phenomenon [1].

Lolamicin (100 mg/kg, intraperitoneal injection, twice daily for 3 days) significantly reduced bacterial load in lung tissues of male CD-1 mice with acute pneumonia models induced by Escherichia coli (AR0349), Klebsiella pneumoniae (AR0040), and Enterobacter cloacae (AR0163) [1].
Lolamicin (200 mg/kg, oral gavage, twice daily for 3 days) reduced bacterial load in lung tissues of male CD-1 mice with acute pneumonia and sepsis models induced by Escherichia coli (AR0349) and improved sepsis survival rate [1].