Tianjin Key Laboratory of Radiation Medicine and Molecular Nuclear Medicine, Institute of Radiation Medicine, Chinese Academy of Medical Science & Peking Union Medical College , Tianjin 300192, P. R. China.
ACS Appl Mater Interfaces. 2014 Apr 23;6(8):5558-65. doi: 10.1021/am406007g. Epub 2014 Apr 2.
D-peptides, which consist of D-amino acids and can resist the hydrolysis catalyzed by endogenous peptidases, are one of the promising candidates for construction of peptide materials with enhanced biostability in vivo. In this paper, we report on a self-assembling supramolecular nanostructure of D-amino acid-based peptide Nap-G(D)F(D)F(D)YGRGD (D-fiber, (D)F meant D-phenylalanine, (D)Y meant D-tyrosine), which were used as carriers for 10-hydroxycamptothecin (HCPT). Transmission electron microscopy observations demonstrated the filamentous morphology of the HCPT-loaded peptides (d-fiber-HCPT). The better selectivity and antitumor activity of D-fiber-HCPT than L-fiber-HCPT were found in the in vitro and in vivo antitumor studies. These results highlight that this model D-fiber system holds great promise as vehicles of hydrophobic drugs for cancer therapy.
D-肽由 D-氨基酸组成，可以抵抗内源性肽酶催化的水解，是构建体内生物稳定性增强的肽材料的有前途的候选物之一。在本文中，我们报告了基于 D-氨基酸的肽 Nap-G(D)F(D)F(D)YGRGD（D-纤维，（D）F 表示 D-苯丙氨酸，（D）Y 表示 D-酪氨酸）的自组装超分子纳米结构，该肽用作 10-羟基喜树碱（HCPT）的载体。透射电子显微镜观察证明了负载 HCPT 的肽（d-纤维-HCPT）的纤维状形态。在体外和体内抗肿瘤研究中发现，D-纤维-HCPT 的选择性和抗肿瘤活性优于 L-纤维-HCPT。这些结果表明，该模型 D-纤维系统作为用于癌症治疗的疏水性药物载体具有很大的潜力。
