Abstract：
Yamanashi et al., conducted a study on the absorption of cholesterol and β-sitosterol, as well as the inhibitory effect of ezetimibe (EZE). They used CaCo-2 cells to simulate the intestines and investigated how different mixed micelles, acting as carriers, were absorbed into these cells through the Niemann-Pick C1-like 1 (NPC1L1) protein. The study focused on the impact of micelle shape, size, and zeta potential on absorption and the inhibitory effect of EZE. I utilized small-angle X-ray scattering and a zeta potential measuring device to measure these characteristics. The findings revealed a two-step mechanism: NPC1L1 selectively bound micelles based on their shape and size, and once bound, the absorption was regulated by the molecular structure of the micelle components. EZE\'s inhibitory effect changed with micelle composition, influencing micelle size and shape. EZE initially acted on the micelle\'s shape and size, and then NPC1L1 selectively bound micelles based on their shape and size, allowing EZE to directly inhibit absorption by interacting with NPC1L1. This groundbreaking discovery challenges existing concepts and holds significant implications for researchers in drug development, as well as physicians and pharmacists.
摘要：
山梨等人。,对胆固醇和β-谷甾醇的吸收进行了研究，以及依泽替米贝（EZE）的抑制作用。他们使用CaCo-2细胞模拟肠道，并研究了不同的混合胶束，作为承运人，通过Niemann-PickC1样1（NPC1L1）蛋白吸收到这些细胞中。研究重点是胶束形状的影响,尺寸,和zeta电位对EZE的吸收和抑制作用。我利用小角度X射线散射和zeta电位测量装置来测量这些特性。研究结果揭示了两步机制：NPC1L1根据胶束的形状和大小选择性结合胶束，一旦被束缚，吸收受胶束组分的分子结构调节。EZE的抑制作用随胶束组成而变化，影响胶束的大小和形状。EZE最初作用于胶束的形状和大小，然后NPC1L1根据胶束的形状和大小选择性结合胶束，允许EZE通过与NPC1L1相互作用直接抑制吸收。这一开创性的发现挑战了现有的概念，并对药物开发的研究人员具有重要意义。以及医生和药剂师。
