氟伐他汀
膜
脂质双层
化学
生物物理学
亲脂性
渗透
分子动力学
细胞膜
生物利用度
辛伐他汀
药理学
生物化学
计算化学
生物
作者
Daniele Belletto,Tânia Cova,Gloria Mazzone,Alberto A. C. C. Pais,Emilia Sicilia
摘要
The chief motivation for the failure of drugs in clinical trials is their low bioavailability caused by the inability to cross the cell membrane. Understanding drug-membrane interactions is crucial for improving therapeutic efficacy. In this work, molecular dynamics simulations were employed to investigate the permeation of simvastatin and fluvastatin across three lipid bilayer models representing normal and cancer cell membranes. Free energy profiles reveal that simvastatin, due to its higher lipophilicity, interacts more strongly with lipid environments, preferentially permeating cancer-like symmetric membranes. Fluvastatin, in contrast, shows less selective behavior across different membrane types, consistent with its charged nature. Statin insertion perturbs membrane structure, increasing area per lipid and decreasing bilayer thickness and lipid order. These findings highlight how membrane composition and asymmetry govern passive drug diffusion and suggest that selective membrane interactions may reflect the differential anticancer potential of statins. The results provide mechanistic insights into structure-permeability relationships and support the strategic use of realistic membrane models in drug discovery and repurposing efforts.
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