Products/Services Used | Details | Operation |
---|---|---|
Plasmid DNA Preparation | … HindIII sites, were purchased from GenScript. The larvae of G… solution (10 μL) was injected into the right posterior proleg at … CFU/mL, strain 42) was injected into the right posterior proleg. … | Get A Quote |
The wide spread of metallo-β-lactamase (MBL)-expressing bacteria has greatly threatened human health, and there is an urgent need for inhibitors against MBLs. Herein, we present a cephalosporin-tripodalamine conjugate (DPASC) as a potent MBL inhibitor with a block-release design. The cephalosporin tag blocks the ligand binding site to reduce toxicity and is cleaved by MBLs to release active ligands to inhibit MBLs . The screening of MBL-expressing pathogenic strains with 16 μg/mL DPASC showed a decrease of the minimum inhibitory concentration of meropenem (MEM) by 16 to 512-fold, and its toxicity was minimal to human HepG2 cells, with an IC exceeding 512 μg/mL. An infection model with Galleria mellonell... More