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他莫昔芬与二硬脂酰磷脂酰胆碱多层囊泡的相互作用:傅里叶变换红外光谱和差示扫描量热法研究

Interactions of tamoxifen with distearoyl phosphatidylcholine multilamellar vesicles: FTIR and DSC studies.

作者信息

Bilge Duygu, Sahin Ipek, Kazanci Nadide, Severcan Feride

机构信息

Department of Physics, Faculty of Science, Ege University, 35100 İzmir, Turkey.

Department of Physics, Faculty of Science, Ege University, 35100 İzmir, Turkey.

出版信息

Spectrochim Acta A Mol Biomol Spectrosc. 2014 Sep 15;130:250-6. doi: 10.1016/j.saa.2014.04.027. Epub 2014 Apr 18.

DOI:10.1016/j.saa.2014.04.027
PMID:24792199
Abstract

Interactions of a non-steroidal antiestrogen drug, tamoxifen (TAM), with distearoyl-sn-glycero-3-phosphatidylcholine (DSPC) multilamellar liposomes (MLVs) were investigated as a function of drug concentration (1-15 mol%) by using two noninvasive techniques, namely Fourier transform infrared (FTIR) spectroscopy and differential scanning calorimetry (DSC). FTIR spectroscopy results show that increasing TAM concentrations (except 1 mol%) increased the wavenumbers of the CH2 stretching modes, implying an disordering effect for DSPC MLVs both in the gel and liquid crystalline phases. The bandwidth values of the CH2 stretchings except for 1 mol% increased when TAM concentrations increased for DSPC liposomes, indicating an increase in the dynamics of liposomes. The CO stretching and PO2- antisymmetric double bond stretching bands were analyzed to study interactions of TAM with head groups of lipids. As the concentrations of TAM increased, dehydration occurred around these functional groups in the polar part of the lipids. The DSC studies on thermal properties of DSPC lipids indicate that TAM eliminated the pre transition, shifted the main phase transition to lower temperatures and broadened the phase transition curve of the liposomes.

摘要

通过使用傅里叶变换红外(FTIR)光谱和差示扫描量热法(DSC)这两种非侵入性技术,研究了非甾体类抗雌激素药物他莫昔芬(TAM)与二硬脂酰-sn-甘油-3-磷脂酰胆碱(DSPC)多层脂质体(MLV)之间的相互作用,并将其作为药物浓度(1-15摩尔%)的函数进行研究。FTIR光谱结果表明,增加TAM浓度(1摩尔%除外)会增加CH2伸缩振动模式的波数,这意味着DSPC MLV在凝胶相和液晶相中均具有无序化作用。对于DSPC脂质体,当TAM浓度增加时,除1摩尔%外,CH2伸缩振动的带宽值增加,表明脂质体动力学增加。分析了CO伸缩振动和PO2-反对称双键伸缩振动带,以研究TAM与脂质头部基团的相互作用。随着TAM浓度的增加,脂质极性部分的这些官能团周围发生脱水。对DSPC脂质热性质的DSC研究表明,TAM消除了预转变,将主相变温度降低,并拓宽了脂质体的相变曲线。

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