Department of Chemistry, Lehigh University, Bethlehem, Pennsylvania 18015, USA.
Bioconjug Chem. 2012 Mar 21;23(3):336-9. doi: 10.1021/bc200669e. Epub 2012 Mar 6.
PEGylated phospholipids are commonly used to increase the blood-circulation time of liposomes by providing a steric barrier around them. This paper documents a fundamentally new property of these lipids-an ability to stimulate the release of cholesterol from phospholipid membranes. Evidence for such stimulation has been obtained by measuring the transport of dehydroergosterol (DHE), a fluorescent simulant of cholesterol, from donor liposomes made from 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC), 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000 (DSPE-PEG(2000)), and DHE to acceptor liposomes made from POPC, 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoglycerol (POPG), and cholesterol. The potential of PEGylated lipids to serve as novel cholesterol-lowering agents is briefly discussed.
聚乙二醇化磷脂通常用于通过在脂质体周围提供空间位阻来增加脂质体的血液循环时间。本文记录了这些脂质的一个全新特性——能够刺激胆固醇从磷脂膜中释放。通过测量从由 1-棕榈酰基-2-油酰基-sn-甘油-3-磷酸胆碱 (POPC)、1,2-二硬脂酰基-sn-甘油-3-磷酸乙醇胺-N-[甲氧基（聚乙二醇）-2000] (DSPE-PEG(2000)) 和 DHE 制成的供体脂质体向由 POPC、1-棕榈酰基-2-油酰基-sn-甘油-3-磷酸甘油 (POPG) 和胆固醇制成的受体脂质体运输脱氢麦角甾醇 (DHE)，可以获得这种刺激的证据。简要讨论了聚乙二醇化脂质作为新型降胆固醇药物的潜力。
