Supramolecular surfactants: amphiphilic polymers designed to disrupt lipid membranes.
Simple polyesters derived from poly(ethylene glycol)s and alpha, omega-dicarboxylic acids exhibit a broad range of activity in disrupting phospholipid membranes. This activity has been analyzed by measuring the release of liposome-encapsulated 5(6)-carboxy-fluorescein (CF). Comparison with an analogous monomeric surfactant, and with Triton X-100, demonstrates that macromolecular activity is a sensitive function of the size of the hydrophobic and hydrophilic segments within each repeat unit, and that high disrupting power is possible. In vitro studies with the human immunodeficiency virus type-1 have revealed that those polyesters which exhibit the highest membrane disrupting power also provide significant protection for human CD4+ lymphocytes against HIV-1. The potential for adjusting and utilizing these "supramolecular surfactants" in medicine is briefly discussed.
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Department of Chemistry, Lehigh University, Bethlehem, Pennsylvania 18015.
Jayasuriya
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Fabianowski
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D015497:HIV-1 / Q000187:drug effects; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D008051:Lipid Bilayers; D010743:Phospholipids; D011108:Polymers / Q000138:chemical synthesis / Q000494:pharmacology*; D013501:Surface-Active Agents / Q000138:chemical synthesis / Q000494:pharmacology*
D008051:Lipid Bilayers; D010743:Phospholipids; D011108:Polymers; D013501:Surface-Active Agents