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pH 可切换脂质构象变化的分子动力学模拟

Molecular Dynamics Simulation on the Conformational Change of a pH-Switchable Lipid.

作者信息

Zhang Hao, Zhuang Xiaoyan, Wang Yutong, Zhao Zhen, Yan Lijuan, Li Guangyong, Li Jun, Yan Hui

机构信息

State Key Laboratory of Macromolecular Drugs and Large-Scale Preparation, School of Pharmaceutical Sciences and Food Engineering, Liaocheng University, Liaocheng 252059, China.

出版信息

Langmuir. 2025 Jan 14;41(1):420-430. doi: 10.1021/acs.langmuir.4c03704. Epub 2024 Dec 23.

Abstract

pH-sensitive lipids are important components of lipid nanoparticles, which enable the targeted delivery and controlled release of drugs. Understanding the mechanism of pH-triggered drug release at the molecular level is important for the rational design of ionizable lipids. Based on a recently reported pH-switchable lipid, named SL2, molecular dynamics (MD) simulations were employed to explore the microscopic mechanism behind the membrane destabilization induced by the conformational change of pH-switchable lipids. The simulated results showed that, at neutral pH, the neutral SL2 lipids assembled with other components (helper lipids and cholesterol) to form a structurally ordered bilayer structure. At this moment, the two hydrocarbon chains of SL2 were closely aligned and inserted in an orderly manner inside of the membrane. With a decrease in pH, the protonation of the pyridinium ring caused a large degree of molecular structural change. The pyridinium ring preferred to form intramolecular H-bonds with the methoxy groups and intermolecular H-bonds with water, resulting in the flip of the pyridinium ring. Meanwhile, due to the structural flip, the two alkane chains showed a more open state, which perturbed the arrangement of molecules within the membrane. The perturbations caused local collapse of the membrane and the formation of water molecule channels, which contributed to the pH-induced drug release. Our results verified the experimentally proposed mechanism at the molecular level and provided more complementary information, which are expected to have deeper insights into the pH-triggered drug release.

摘要

pH敏感脂质是脂质纳米颗粒的重要组成部分,能够实现药物的靶向递送和控释。在分子水平上理解pH触发药物释放的机制对于可电离脂质的合理设计至关重要。基于最近报道的一种名为SL2的pH可切换脂质,采用分子动力学(MD)模拟来探索pH可切换脂质构象变化引起膜不稳定背后的微观机制。模拟结果表明,在中性pH下,中性的SL2脂质与其他成分(辅助脂质和胆固醇)组装形成结构有序的双层结构。此时,SL2的两条烃链紧密排列并有序地插入膜内。随着pH降低,吡啶鎓环的质子化导致分子结构发生很大变化。吡啶鎓环倾向于与甲氧基形成分子内氢键,并与水形成分子间氢键,导致吡啶鎓环翻转。同时,由于结构翻转,两条烷烃链呈现出更开放的状态,这扰乱了膜内分子的排列。这些扰动导致膜局部塌陷并形成水分子通道,这有助于pH诱导的药物释放。我们的结果在分子水平上验证了实验提出的机制,并提供了更多补充信息,有望对pH触发的药物释放有更深入的了解。

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