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绿茶提取物-生物膜相互作用研究:其两种主要成分(-)-表没食子儿茶素没食子酸酯和(-)-表没食子儿茶素的作用。

Green tea extract-biomembrane interaction study: The role of its two major components, (-)-epigallocatechin gallate and (-)-epigallocatechin.

机构信息

LEPABE - Laboratory for Process Engineering, Environment, Biotechnology and Energy, Faculty of Engineering, University of Porto, Rua Dr. Roberto Frias, 4200-465 Porto, Portugal.

出版信息

Biochim Biophys Acta Biomembr. 2021 Jan 1;1863(1):183476. doi: 10.1016/j.bbamem.2020.183476. Epub 2020 Sep 15.

Abstract

The interaction of antioxidants with biological membranes is closely related with their efficacy to inhibit the lipid peroxidation, the cause of several pathologies including cancer, neurodegenerative and cardiovascular disorders. Despite being pointed as a promising antioxidant agent by some authors, the anti-lipid peroxidation of green tea extract (GTE) has not aroused consensus among the scientific community. Since the interaction of drugs with biological membranes plays a key role on their therapeutic activity, this study aims to evaluate the interaction of GTE with liposomes as in vitro biomembrane models composed of 1,2-dimyristoyl-sn-glycero-3-phosphocholine phospholipids in the absence and presence of cholesterol (CHOL) (15 mol%). The affinity of GTE and its main components (-)-epigallocatechin gallate (EGCG) and (-)-epigallocatechin (EGC) to the lipid bilayer, their membrane location as well as their effect on the membrane fluidity was investigated by diverse biophysical techniques. Derivative spectrophotometry results proved that GTE has high affinity to the membrane by establishing hydrophobic interactions with the non-polar region of phospholipids and electrostatic interactions with the polar phospholipid heads. Fluorescence and dynamic light scattering data confirm that GTE is located in both hydrophobic and hydrophilic regions of the lipid membrane, therefore affecting the structure of the biomembrane by increasing its fluidity. However, the increased stiffness and organization of the lipid bilayer caused by CHOL significantly affected the interaction of GTE with the membrane. Moreover, the obtained findings suggest a direct contribution of EGCG and EGC on the GTE-membrane interaction.

摘要

抗氧化剂与生物膜的相互作用与其抑制脂质过氧化的功效密切相关,脂质过氧化是包括癌症、神经退行性和心血管疾病在内的几种病理学的原因。尽管一些作者指出绿茶提取物 (GTE) 是一种有前途的抗氧化剂,但 GTE 的抗脂质过氧化作用在科学界尚未达成共识。由于药物与生物膜的相互作用对其治疗活性起着关键作用,因此本研究旨在评估 GTE 与脂质体的相互作用,脂质体作为由 1,2-二肉豆蔻酰-sn-甘油-3-磷酸胆碱磷脂组成的体外生物膜模型,在不存在和存在胆固醇 (CHOL)(15 mol%)的情况下。通过多种生物物理技术研究了 GTE 及其主要成分 (-)-表没食子儿茶素没食子酸酯 (EGCG) 和 (-)-表儿茶素 (EGC) 与脂质双层的亲和力、它们在膜中的位置以及它们对膜流动性的影响。导数分光光度法结果证明,GTE 通过与磷脂的非极性区域建立疏水性相互作用以及与极性磷脂头部建立静电相互作用,对膜具有高亲和力。荧光和动态光散射数据证实 GTE 位于脂质膜的疏水区和亲水区,因此通过增加其流动性来影响生物膜的结构。然而,CHOL 引起的脂质双层的刚性和组织增加显著影响了 GTE 与膜的相互作用。此外,获得的发现表明 EGCG 和 EGC 直接参与了 GTE 与膜的相互作用。

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