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本文考察了阳离子环肽处理后Caco-2细胞膜表面的微观形态变化,研究了细胞膜形态变化与亲水性大分子药物胰岛素跨膜渗透性的关系。采用原子力显微镜轻敲模式,在大气条件下对Caco-2细胞膜进行实时观察,发现阳离子环肽TD-34(ACSSKKSKHCG)作用于Caco-2细胞膜后,细胞膜表面失去原有的平整性和光滑性,细胞膜表面粗糙度较未处理组提高近一倍,胰岛素跨Caco-2细胞膜表观渗透系数增大,为原来的2.5倍。研究表明,原子力显微镜可用于阳离子环肽作用后细胞膜表面微观形态变化的实时观测,阳离子环肽通过增加Caco-2细胞膜流动性促进了胰岛素通过胞吞途径的跨膜吸收。
In this paper, we investigated the morphological changes of Caco-2 cell surface after cationic cyclic peptide treatment, and studied the relationship between the morphological changes of the cell membrane and the transmembrane permeability of hydrophilic macromolecular drugs. Atomic force microscopy (AFM) tapping mode was used to observe the Caco-2 cell membrane under atmospheric conditions. It was found that the cationic cyclopeptide TD-34 (ACSSKKSKHCG) lost its original flatness and smoothness on the surface of Caco- The surface roughness of cell membrane nearly doubled compared with untreated group, and the apparent permeability coefficient of insulin across Caco-2 cell membrane increased by 2.5 times. Studies have shown that atomic force microscopy can be used for real-time observation of the microscopic morphological changes of the cell membrane surface after the action of the cationic cyclic peptide, and the cationic cyclic peptide can promote the transmembrane absorption of insulin through the endocytosis pathway by increasing the fluidity of the Caco-2 cell membrane.