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The mechanisms of action of water-soluble aminohexanoic and malonic adducts of fullerene C60 with hexamethonium on model lipid membranes.
Biochimica et Biophysica Acta (BBA) - Biomembranes ( IF 3.4 ) Pub Date : 2020-08-05 , DOI: 10.1016/j.bbamem.2020.183433
S S Efimova 1 , D A Khaleneva 1 , E V Litasova 2 , L B Piotrovskiy 2 , O S Ostroumova 1
Affiliation  

In an attempt to understand the possibility of applications of the fullerene-based systems for transporting various polar compounds like hexamethonium through the blood–brain barrier, we studied the influence of a series of derivatives of fullerene C60 in the form of salts with hexamethonium bis-anion, namely the adducts of fullerenols with 6-aminohexanoic acid (IEM-2197), and two bis-adduct malonic acid derivatives of fullerene with addents bound in two hemispheres (IEM-2143) and in equatorial positions (IEM-2144), on model membranes. We showed that IEM-2197 induced the disintegration of the bilayers composed of DOPC at the concentrations more than 2 mg/ml. IEM-2144 and IEM-2143-induced ion-permeable pores at concentrations of 0.3 and 0.02 mg/ml, respectively; herewith, IEM-2143 was characterized by the greater efficiency than IEM-2144. IEM-2197 did not significantly affect the phase behavior of DPPC, while the melting temperature significantly decreased with addition of IEM-2144 and IEM-2143. The increase in the half-width of the main transition peaks by more than 2.0 °C in the presence of IEM-2144 and IEM-2143 was observed, along with the pronounced peak deconvolution. We proposed that the immersion of IEM-2144 and IEM-2143 into the polar region of the DOPC or DPPC bilayers led to an increase in the relative mobility of tails and formation of ion-permeable defects. IEM-2197 demonstrated the more pronounced effects on the melting and ion permeability of PG- and PS-containing bilayers compared to PC-enriched membranes. These results indicated that IEM-2197 preferentially interacts with the negatively charged lipids compared to neutral species.



中文翻译:

富勒烯C60与六甲铵的水溶性氨基己酸和丙二酸加合物在模型脂质膜上的作用机理。

为了理解以富勒烯为基础的系统通过血脑屏障转运六甲铵等多种极性化合物的可能性,我们研究了一系列富勒烯C 60衍生物与六甲双胍盐形成的盐的影响。-阴离子,即富勒烯醇与6-氨基己酸(IEM-2197)和两个-富勒烯的丙二酸丙二酸衍生物,其添加剂结合在模型膜上的两个半球(IEM-2143)和赤道位置(IEM-2144)中。我们表明,IEM-2197可以诱导浓度大于2 mg / ml的由DOPC组成的双层的崩解。IEM-2144和IEM-2143诱导的离子渗透孔的浓度分别为0.3和0.02 mg / ml;因此,IEM-2143的效率要高于IEM-2144。IEM-2197不会显着影响DPPC的相行为,而熔融温度随着添加IEM-2144和IEM-2143而显着降低。在存在IEM-2144和IEM-2143的情况下,观察到主跃迁峰的半峰宽增加了2.0°C以上,同时还有明显的峰去卷积。我们提出将IEM-2144和IEM-2143浸入DOPC或DPPC双层的极性区域中会导致尾部的相对迁移率增加,并形成离子可渗透缺陷。与富含PC的膜相比,IEM-2197对含PG和PS的双层的熔融和离子渗透性具有更明显的影响。这些结果表明,与中性物种相比,IEM-2197优先与带负电荷的脂质相互作用。

更新日期:2020-08-18
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