Sequestration of bacterial lipopolysaccharide by bis(Args) gemini compounds

Sunil David, Lourdes Pérez, M. Rosa Infante

Research output: Contribution to journalArticle

25 Scopus citations

Abstract

Gemini compounds of the type Nα,Nω-bis(Nα-lauroyl arginine)α,ω-alkylenediamides or bis(Args) bind bacterial lipopolysaccharide and neutralize endotoxic activity in in vitro tumor necrosis factor-α and nitric oxide release assays. Sequestration of lipopolysaccharide results in protection in a murine model of endotoxemia. However, the bis(Args) compounds are cytotoxic by virtue of being highly membrane-active. The development of less surface-active analogues may yield potentially therapeutically useful compounds for the treatment of Gram-negative sepsis.

Original languageEnglish (US)
Pages (from-to)357-360
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume12
Issue number3
DOIs
StatePublished - Feb 11 2002

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