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细胞穿透肽(cell-penetrating peptide,CPP)作为一种潜在的药物输送高效转运载体一直得到研究者的广泛关注。本文中采用4种肿瘤细胞系(MCF-7、MDA-MB-231、C6和B16F10)分别摄取异硫氰酸荧光素(fluorescein isothiocyanate,FITC)标记的CPP,观察到CPP入胞,并具有时间和浓度的依赖性,同时发现了C6细胞对CPP的胞吐作用,其胞吐动力学符合零级方程;在低温(4℃)和内吞抑制剂存在条件下探讨了CPP入胞的机制。低温条件对CPP的入胞未产生抑制作用;肝素钠作为细胞表面硫酸糖蛋白受体抑制剂对CPP的入胞有较强抑制作用,肝素组对CPP的摄取只达到对照组的3%～10%;而氯丙嗪、氯喹和N-乙酰基-N-异丙基阿米洛利[5-(N-ethyl-N-isopropyl)-amiloride,EIPA]对CPP的入胞影响不大。本研究表明,CPP穿透细胞没有选择性,即缺乏细胞特异性,但CPP的摄取量与细胞种类有关。硫酸蛋白聚糖的吸附介导在CPP穿透细胞中发挥了重要作用。
Cell-penetrating peptide (CPP), as a potential drug delivery efficient transporter, has received much attention from researchers. In this study, four tumor cell lines (MCF-7, MDA-MB-231, C6 and B16F10) were respectively used to inoculate CPCs labeled with fluorescein isothiocyanate (FITC) And the dependence of concentration on CPP. At the same time, the exocytosis of CPP was found in C6 cells. The exocytosis kinetics was in accordance with zero-order equation. The mechanism of CPP entry was discussed in the presence of low temperature (4 ℃) and endocytosis inhibitor. Low temperature had no inhibitory effect on CPP entry; heparin as a cell surface inhibitor of sulfated glucagon had a strong inhibitory effect on CPP entry, CPP uptake in heparin group only reached 3% -10% of control group %. However, chlorpromazine, chloroquine and N-ethyl-N-isopropyl-amiloride (EIPA) had little effect on CPP entry. This study shows that CPP penetrates cells with no selectivity, ie lack of cell specificity, but CPP uptake depends on cell type. Adsorption mediated by proteoglycan plays an important role in CPP penetration into cells.