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Peptide-dragged mitochondria-targeted electron scavengers as novel and potent anti-inflammatory agents

详细技术说明

None

*Abstract

The inventors have synthesized a series of TEMPO derivatives that contain a hydrophobic hemigramicidin peptide moiety in order to enhance intracellular delivery of the TEMPO (payload). One compound, XJB-5-131, prevented peroxidation of mitochondrial cardiolipin, decreased activation of the pro-apoptotic caspases in ileal mucosal samples from hemorrhaged rats, and significantly prolonged survival.Since many of the inflammatory pathways activated in hemorrhagic shock are also present in sepsis the inventors sought to determine whether XJB-5-131 and XJB-5-131 have protective effects in such circumstance as well.Applications:1) treatment of various acute or chronic medical conditions associated with excessive inflammation, including sepsis, rheumatoid arthritis, and inflammatory bowel disease. Advantages:1) Mechanism of action is novel.2) Compounds are quite potent (activity observed in vitro in the nanomolar range).3) New composition of matter4) New class of anti-inflammatory agents. Stage of DevelopmentPreliminary proof of principle in animalsNon Provisional patent application filed

*Principal Investigation

Name: Mitchell Fink, Professor

Department: Med-Critical Care Medicine

国家/地区

美国