Institute of Theoretical and Experimental Biophysics, Russian Academy of Sciences, Institutskaya 3, Pushchino, Moscow Region, 142290, Russia; Mari State University, pl. Lenina 1, Yoshkar-Ola, Mari El, 424001, Russia.
Institute of Cell Biophysics, Russian Academy of Sciences, Institutskaya 3, Pushchino, Moscow Region, 142290, Russia.
Chem Biol Interact. 2019 Feb 1;299:8-14. doi: 10.1016/j.cbi.2018.11.017. Epub 2018 Nov 26.
Bedaquiline (BDQ) is a new drug from the family of diarylquinolines, which has a potent bactericidal activity against Mycobacterium tuberculosis. This paper has examined the interaction of BDQ with model membranes (liposomes and BLM) and rat erythrocytes. It was shown that BDQ (1-10 mol%) changed the thermotropic phase behavior of DMPC liposomes, leading to the lateral phase separation in the lipid bilayer and the formation of membrane microdomains. BDQ (10-50 μM) was also demonstrated to cause permeabilization of lecithin liposomes loaded with the fluorescent dye sulforhodamine B. At the same time, it did not alter the ionic conductivity of BLM. A dynamic light scattering study showed that BDQ led to the emergence of two populations of light-scattering particles in the suspension of lecithin liposomes, suggesting that an aggregation of the vesicles took place. In rat erythrocytes, BDQ was found to induce changes in their size and shape, as well as aggregation and lysis of the cells.
贝达喹啉（BDQ）是一种新型二芳基喹啉类药物，对结核分枝杆菌具有很强的杀菌活性。本文研究了 BDQ 与模型膜（脂质体和 BLM）和大鼠红细胞的相互作用。结果表明，BDQ（1-10μmol%）改变了 DMPC 脂质体的热致相行为，导致脂质双层中的横向相分离和膜微区的形成。BDQ（10-50μM）还导致负载荧光染料 sulforhodamine B 的卵磷脂脂质体的通透性增加。同时，它不会改变 BLM 的离子电导率。动态光散射研究表明，BDQ 导致卵磷脂脂质体悬浮液中出现两种光散射粒子群体，表明囊泡发生了聚集。在大鼠红细胞中，BDQ 被发现诱导其大小和形状的变化，以及细胞的聚集和裂解。
