具有治疗潜力的新兴肽抗生素。
关键词: ADMET, absorption, distribution, metabolism and excretion – toxicity in pharmacokinetics AMP, antimicrobial peptide AMR, antimicrobial resistance ATCC, ATCC cell collection Antibiotic BAM, β-barrel assembly machinery CC50, cytotoxic concentration to kill 50% of cells CD, circular dichroism CFU, colony forming unit CLSI, clinical and laboratory standards institute CMS, colistin methane sulfonate DMPC, 1,2-dimyristoyl-sn-glycero-3-phosphocholine ESKAPE, acronym encompassing six bacterial pathogens (often carrying antibiotic resistance): Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumonia, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter spp FDA, U. S. Food and Drug Administration HABP, hospital acquired bacterial pneumonia HDP, host-defense peptide HEK293, human embryonic kidney 293 cells HK-2, human kidney 2 cells (proximal tubular cell line) HepG2, human hepatocellular carcinoma cell line Hpg, 4-hydroxy-phenyl glycine ITC, isothermal titration calorimetry KPC, Klebsiella pneumoniae metallo-β-lactamase C resistant LPS, lipopolysaccharide LptA, lipopolysaccharide transport protein A LptC, lipopolysaccharide transport protein C LptD, lipopolysaccharide transport protein D MDR, multidrug-resistant MH-I, Müller-Hinton broth I MH-II, Müller-Hinton broth II (cation adjusted) MIC, minimal inhibitory concentration MRSA, methicilline-resistant S. aureus MSSA, methicilline-sensitive S. aureus MoA, mechanism (mode) of action NDM-1, New Delhi metallo-β-lactamase resistant NOAEL, no adverse effect level ODL, odilorhabdin OMPTA (outer membrane targeting antibiotic) OMPTA, outer membrane targeting antibiotic Omp, outer membrane protein PBMC, peripheral mononuclear blood cell PBP, penicillin-binding protein PBS, phosphate-buffered saline PK, pharmacokinetics POPC, 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine POPG, 2-oleoyl-1-palmitoyl-sn-glycero-3-phospho-(1-glycerol) PrAMPs, polyproline antimicrobial peptides RBC, red blood cell SAR, structure-activity relationship SPR, surface plasmon resonance SPase I, signal peptidase I VABP, ventilator associated bacterial pneumonia VIM-1, beta-lactamase 2 (K. pneumoniae) VISA, vancomycin-intermediate S. aureus VRE, vancomycin-resistant enterococcus WHO, World Health Organization WT, wild type WTA, wall teichoic acid XDR, extremely drug-resistant antimicrobial peptide antimicrobial resistance bid, bis in die (two times a day) i.p., intraperitoneal i.v., intravenous lipopeptide mITT population, minimal intend-to-treat population peptide antibiotic s.c., subcutaneous
来 源:
DOI:10.1016/j.medidd.2020.100078
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