PMID: 9545568May 16, 1998Paper

The aminosterol antibiotic squalamine permeabilizes large unilamellar phospholipid vesicles

Biochimica Et Biophysica Acta
B S SelinskyA E Shinnar

Abstract

The ability of the shark antimicrobial aminosterol squalamine to induce the leakage of polar fluorescent dyes from large unilamellar phospholipid vesicles (LUVs) has been measured. Micromolar squalamine causes leakage of carboxyfluorescein (CF) from vesicles prepared from the anionic phospholipids phosphatidylglycerol (PG), phosphatidylserine (PS), and cardiolipin. Binding analyses based on the leakage data show that squalamine has its highest affinity to phosphatidylglycerol membranes, followed by phosphatidylserine and cardiolipin membranes. Squalamine will also induce the leakage of CF from phosphatidylcholine (PC) LUVs at low phospholipid concentrations. At high phospholipid concentrations, the leakage of CF from PC LUVs deviates from a simple dose-response relationship, and it appears that some of the squalamine can no longer cause leakage. Fluorescent dye leakage generated by squalamine is graded, suggesting the formation of a discrete membrane pore rather than a generalized disruption of vesicular membranes. By using fluorescently labeled dextrans of different molecular weight, material with molecular weight </=4000 g/mol is released from vesicles by squalamine, but material with molecular weight >/=10,000 is retained. N...Continue Reading

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Citations

Feb 22, 2002·Steroids·Youheng ShuBarry S Selinsky
Jul 11, 2000·British Journal of Haematology·K L Talks, A L Harris
Sep 21, 2011·Proceedings of the National Academy of Sciences of the United States of America·Michael ZasloffGerard C L Wong
Jul 5, 2005·Expert Opinion on Investigational Drugs·H T Zhang, A L Harris
Nov 10, 2004·Biochimica Et Biophysica Acta·Toshihiro HoudaiMichio Murata
Aug 10, 2007·Expert Opinion on Investigational Drugs·Chanaz Salmi, Jean M Brunel
Jun 13, 2009·Pharmaceutical Development and Technology·S M SammetaS Narasimha Murthy
Nov 4, 2000·Expert Opinion on Investigational Drugs·P B Savage, C Li
Jun 24, 2000·Bioorganic & Medicinal Chemistry Letters·S KhabnadidehI H Gilbert
Jul 6, 2000·Bioscience, Biotechnology, and Biochemistry·S MachidaY Yu
Jan 28, 2017·Proceedings of the National Academy of Sciences of the United States of America·André Pineda, Jacqueline Burré
Sep 9, 2021·The Journal of Antibiotics·Shinichi Nishimura

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