Effect of benzocaine and propranolol on phospholipid-based bilayers,Physical Chemistry Chemical Physics

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Effect of benzocaine and propranolol on phospholipid-based bilayers
Physical Chemistry Chemical Physics ( IF 2.9 ) Pub Date : 2017-10-31 00:00:00 , DOI: 10.1039/c7cp06077g
G. Mangiapia _{1,

2,

3,

4} , M. Gvaramia _{1,

2,

3,

4,

5} , L. Kuhrts _{1,

2,

3,

4} , J. Teixeira _{6,

7,

8,

9} , A. Koutsioubas _{1,

2,

3,

4} , O. Soltwedel _{3,

4,

10,

11} , H. Frielinghaus _{1,

2,

3,

4}

Affiliation

Cell membranes play a fundamental role in protecting the cell from its surroundings, in addition to hosting many proteins with fundamental biological tasks. A study of drug/lipid interactions is a necessary and important step in fully clarifying the role and action mechanism of active ingredients, and shedding light on possible complications caused by drug overdosage. In this paper, the influence of benzocaine and propranolol drugs on the structure of L-α-phosphatidylcholine-based membranes has been investigated by means of neutron reflectivity, grazing incidence small angle neutron scattering, and small/ultra-small angle neutron scattering. Investigations allowed discovering a stiffening of the membranes and the formation of stalks, caused by the presence of benzocaine. On the other hand, disordered bilayers (lamellar powders) and highly curved structures were found in the presence of propranolol. The results obtained may be rationalized in terms of the molecular structures of drugs and may serve as a starting point for explaining the toxic behavior in long-term and overdosage scenarios.

中文翻译：

苯佐卡因和普萘洛尔对磷脂双分子层的影响

细胞膜除了可以承载许多具有基本生物学任务的蛋白质外，在保护细胞免受周围环境影响方面也起着基本作用。药物/脂质相互作用的研究是充分阐明活性成分的作用和作用机制，并阐明由药物过量引起的可能并发症的必要且重要的步骤。本文研究了苯佐卡因和普萘洛尔药物对L结构的影响已经通过中子反射率，掠入射小角中子散射和小/超小角中子散射研究了基于-α-磷脂酰胆碱的膜。研究允许发现由于苯佐卡因的存在而引起的膜变硬和茎的形成。另一方面，在普萘洛尔的存在下，发现了无序的双层结构（层状粉末）和高度弯曲的结构。获得的结果可以根据药物的分子结构进行合理化，并且可以作为解释长期和过量使用情况下的毒性行为的起点。

更新日期：2017-11-28

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