Ceragenins (cationic steroid compounds), a novel class of antimicrobial agents.
Ceragenins are a group of cholic acid derivatives that have been chemically modified to make them cationic amphiphiles. Several of these derivatives exhibit antimicrobial activity against a broad range of bacteria. These compounds have advantages over cationic amphipathic peptides in that they are resistant to proteolysis and they incorporate stably into membranes. Although some forms of ceragenins are effective against both Gram-negative and Gram-positive bacteria, they are generally more potent against Gram-positive bacteria. Surprisingly, it is not the cell wall, but the high content of phosphatidylethanolamine in most Gram-negative bacteria that endow them with resistance. Ceragenins have the unusual property of forming complexes with phospholipids. Factors contributing to the mechanism of action of these agents are discussed. The ceragenins are a class of agents with many properties to make them favorable for application as antiinfective agents.
Epand
Richard M
RM
Department of Biochemistry and Biomedical Sciences, McMaster University, Hamilton, Ontario, Canada. epand@mcmaster.ca
Epand
Raquel F
RF
Savage
Paul B
PB
D000818:Animals; D000890:Anti-Infective Agents / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects* / Q000254:growth & development; D002793:Cholic Acids / Q000737:chemistry / Q000494:pharmacology*; D024881:Drug Resistance, Bacterial; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013256:Steroids / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013501:Surface-Active Agents / Q000737:chemistry / Q000494:pharmacology*
D000890:Anti-Infective Agents; D002793:Cholic Acids; D013256:Steroids; D013501:Surface-Active Agents; C521528:ceragenin CSA-13; C521527:ceragenin CSA-8