当前位置: X-MOL 学术BBA Biomembr. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Evaluation of the effects in cellular membrane models of antitrypanosomal poly-thymolformaldehyde (PTF) using Langmuir monolayers
Biochimica et Biophysica Acta (BBA) - Biomembranes ( IF 3.4 ) Pub Date : 2020-10-29 , DOI: 10.1016/j.bbamem.2020.183500
Giovana A. Parolin , Giulia E.G. Gonçalves , Thais A. Costa-Silva , Andre G. Tempone , Luciano Caseli , João Henrique G. Lago , Laura O. Péres

The polymerization of bioactive compounds may be interesting because the supramolecular structures formed can boost biological action on microorganism membranes. In the present work, poly-thymolformaldehyde (PTF) activity, prepared by condensation of thymol and formaldehyde, was evaluated against trypomastigote forms of Trypanosoma cruzi and related with the physicochemical changes provided by the incorporation of the compound in protozoan cell membrane models. PTF exhibited an EC50 value of 23.4 μg/mL and no toxicity against mammalian cells (CC50 > 200 μg/mL). To understand the molecular action of PTF as an antiprotozoal candidate, this compound was incorporated in Langmuir monolayers of dipalmitoylphosphatidylglycerol (DPPG) as a model for parasite cell membranes. PTF shifted DPPG surface pressure-area isotherms to higher areas, indicating its incorporation in the lipid films. Additionally, it changed the thermodynamic, compressional, structural, and morphological properties of the floating monolayers, decreasing the collapse pressure, reducing the surface elasticity, and segregating molecules at the interface, forming domains with different reflectivities. Infrared spectroscopy showed that the lipid films with PTF presented an increased rate of gauche/all-trans conformers for the methylene groups from the acyl chains, indicating molecular disorder. Therefore, these results show that PTF alters the physicochemical properties of DPPG monolayers as a model for protozoa cell membranes, which can enhance the comprehension of the parasitic action of PTF against T. cruzi.



中文翻译:

使用Langmuir单层膜评估抗胰锥虫聚百里酚甲醛(PTF)在细胞膜模型中的作用

生物活性化合物的聚合可能是令人感兴趣的,因为形成的超分子结构可以增强对微生物膜的生物学作用。在本工作中,针对百里香锥虫的锥虫病形式评价了通过百里香酚和甲醛缩合制备的聚百里酚甲醛(PTF)活性,并与在原生动物细胞膜模型中掺入该化合物所提供的物理化学变化有关。PTF的EC 50值为23.4μg/ mL,对哺乳动物细胞无毒性(CC 50 > 200μg/ mL)。为了理解PTF作为抗原生动物候选物的分子作用,将该化合物掺入二棕榈酰磷脂酰甘油(DPPG)的Langmuir单层中,作为寄生虫细胞膜的模型。PTF将DPPG的表面压力-面积等温线转移到更高的区域,表明它已结合到脂质膜中。此外,它改变了浮动单层的热力学,压缩,结构和形态特性,降低了压塌压力,降低了表面弹性,并使分子在界面处隔离,从而形成了具有不同反射率的畴。红外光谱表明,PTF脂质膜呈现率增加笨拙/全部反式酰基链中亚甲基的构象异构体,表明分子无序。因此,这些结果表明,PTF改变了DPPG单层的物理化学性质,作为原生动物细胞膜的模型,这可以增强对PTF对克氏锥虫的寄生作用的理解。

更新日期:2020-10-30
down
wechat
bug