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2-(4-氟苯基氨基)-5-(2,4-二羟基苯基)-1,3,4-噻二唑对二棕榈酰磷脂酰胆碱脂质多层膜的分子组织和结构性质的影响

Effect of 2-(4-fluorophenylamino)-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole on the molecular organisation and structural properties of the DPPC lipid multibilayers.

作者信息

Kamiński Daniel M, Matwijczuk Arkadiusz, Pociecha Damian, Górecka Ewa, Niewiadomy Andrzej, Dmowska Mirosława, Gagoś Mariusz

机构信息

Department of Chemistry, University of Life Sciences, Lublin, Poland.

出版信息

Biochim Biophys Acta. 2012 Nov;1818(11):2850-9. doi: 10.1016/j.bbamem.2012.07.013. Epub 2012 Jul 24.

Abstract

Interactions and complex formation between lipids and biologically active compounds are crucial for better understanding of molecular mechanisms occurring in living cells. In this paper a molecular organisation and complex formation of 2-(4-fluorophenylamino)-5-(2,4-dihydroxybenzeno)-1,3,4-thiadiazole (FABT) in DPPC multibilayers are reported. The simplified pseudo binary phase diagram of this system was created based on the X-ray diffraction study and fourier transform infrared spectroscopic data. The detailed analysis of the refraction effect indicates a much higher concentration of FABT in the polar zones during phase transition. Both the lipid and the complex ripple after cooling. It was found that FABT occupied not only the hydrophilic zones of the lipid membranes but also partly occupied the central part of the non polar zone. The infrared spectroscopy study reveals that FABT strongly interact with hydrophilic (especially PO(2)(-)) and hydrophobic (especially "kink" vibrations of CH(2) group). The interactions of FABT molecules with these groups are responsible for changes of lipid multibilayers observed in X-ray diffraction study.

摘要

脂质与生物活性化合物之间的相互作用及复合物形成对于更好地理解活细胞中发生的分子机制至关重要。本文报道了2-(4-氟苯氨基)-5-(2,4-二羟基苯)-1,3,4-噻二唑(FABT)在二棕榈酰磷脂酰胆碱(DPPC)多层膜中的分子组织及复合物形成。基于X射线衍射研究和傅里叶变换红外光谱数据构建了该系统的简化伪二元相图。对折射效应的详细分析表明,在相变过程中FABT在极性区域的浓度要高得多。冷却后脂质和复合物都会出现波纹。研究发现,FABT不仅占据脂质膜的亲水区域,还部分占据非极性区域的中心部分。红外光谱研究表明,FABT与亲水基团(特别是PO(2)(-))和疏水基团(特别是CH(2)基团的“扭结”振动)强烈相互作用。FABT分子与这些基团的相互作用导致了X射线衍射研究中观察到的脂质多层膜的变化。

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