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布洛芬与真核细胞膜脂质的相互作用。

Interaction of ibuprofen with eukaryotic membrane lipids.

作者信息

Lygre Henning, Moe Grete, Holmsen Holm

机构信息

Department of Odontology-Dental Pharmacology, University of Bergen, Bergen, Norway.

出版信息

Acta Odontol Scand. 2003 Oct;61(5):303-9. doi: 10.1080/00016350310006555.

Abstract

With the versatility of the molecular mechanism of amphiphilic drugs there is the possibility that ibuprofen could interact with eukaryotic model membrane lipids. Using the Langmuir technique, we first determined the pressure/molecular area isotherms of glycerophospholipids monolayers at 37 degrees C, and, second, using differential scanning calorimetry (DSC), phase transition parameters in liposomes of the same lipids. Ibuprofen interacted in a concentration-independent manner with monolayers of saturated phosphatidylcholines (PC, i.e. markers of the outer membrane leaflet of eukaryotic cells). Ibuprofen was found to interact with liposomes of saturated and unsaturated phosphatidylcholines and -serines (PS, i.e. markers of the inner membrane leaflet of eukaryotic cells), and saturated ethanolamines (PE, i.e. markers of the inner membrane leaflet of eukaryotic cells). A lowering of the lipid melting temperature (Tm) and a change of enthalpy (deltaH) of the gel to liquid-crystalline phase transitions of liposomes were detected.

摘要

鉴于两亲性药物分子机制的多样性,布洛芬有可能与真核模型膜脂相互作用。我们首先使用朗缪尔技术测定了37℃下甘油磷脂单层的压力/分子面积等温线,其次使用差示扫描量热法(DSC)测定了相同脂质脂质体中的相变参数。布洛芬以浓度无关的方式与饱和磷脂酰胆碱(PC,即真核细胞外膜小叶的标志物)单层相互作用。发现布洛芬与饱和和不饱和磷脂酰胆碱以及磷脂酰丝氨酸(PS,即真核细胞内膜小叶的标志物)和饱和乙醇胺(PE,即真核细胞内膜小叶的标志物)的脂质体相互作用。检测到脂质体凝胶到液晶相转变的脂质熔化温度(Tm)降低和焓变(deltaH)变化。

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