248602-44-0Relevant articles and documents
Modular Design of Membrane-Active Antibiotics: From Macromolecular Antimicrobials to Small Scorpionlike Peptidomimetics
Wang, Minghui,Feng, Xiaoqian,Gao, Ruixuan,Sang, Peng,Pan, Xin,Wei, Lulu,Lu, Chao,Wu, Chuanbin,Cai, Jianfeng
, p. 9894 - 9905 (2021)
Infections caused by multidrug-resistant bacteria have emerged in recent decades, leading to escalating interest in host defense peptides (HDPs) to reverse this dangerous trend. Inspired by the modular design in bioengineering, herein we report a new class of small amphiphilic scorpionlike peptidomimetics based on this strategy. These HDP mimics show potent antimicrobial activity against both Gram-positive and Gram-negative bacteria without drug resistance but with a high therapeutic index. The membrane-compromising action mode was suggested to be their potential bactericidal mechanism. Pharmacodynamic experiments were conducted using a murine abscess model of methicillin-resistantStaphylococcus aureus(MRSA) infections. The lead compound 12 showed impressive in vivo therapeutic efficacy with ～99.998% (4.7log) reduction in skin MRSA burden, a significantly higher bactericidal efficiency than ciprofloxacin, and good biocompatibility. These results highlight the potential of these HDP mimics as novel antibiotic therapeutics.
Lipopeptide stabilized microbubbles as diagnostic/therapeutic agents
-
, (2008/06/13)
Novel membrane-forming amphiphilic lipopeptides comprising one or more peptide moieties containing 2-50 aminoacyl residues and one or more hydrocarbon chains containing 5-50 carbon atoms. Such lipopeptides may be used in the formation of stabilized gas microbubble dispersions suitable for use as diagnostic and/or therapeutic agents, for example as ultrasound contrast agents.
