Deka Smriti Rekha, Yadav Santosh, Kumar Dheeresh, Garg Sumit, Mahato Manohar, Sharma Ashwani Kumar
Nucleic Acids Research Laboratory, CSIR-Institute of Genomics Integrative Biology, Mall Road, Delhi, 110 007, India.
Nucleic Acids Research Laboratory, CSIR-Institute of Genomics Integrative Biology, Mall Road, Delhi, 110 007, India; Academy of Scientific and Innovative Research, New Delhi, India.
Colloids Surf B Biointerfaces. 2017 Jul 1;155:332-340. doi: 10.1016/j.colsurfb.2017.04.036. Epub 2017 Apr 20.
In the recent studies, it has been demonstrated that incorporation of unnatural amino acid, α,β-dehydrophenylalanine, in small peptides results in stable self-assembled nanostructures with different sizes and shapes. Here, we have replaced the natural amino acid, phenylalanine, from our earlier reported work on self-assembled peptide, Boc-Pro-Phe-Gly-OMe, with a constrained dehydro amino acid, α,β-dehydrophenylalanine, to study its influence on self-assembled nanostructures. Dehydrotripeptide, Boc-Pro-ΔPhe-Gly-OMe, self-assembled into nanostructures in aqueous solutions and formed hydrophobic matrix with improved encapsulation efficiency of hydrophobic molecules. The hydrodynamic size of peptide nanostructures from DLS study was found to be ∼257nm. The morphology and size of the loaded nanoparticles were also determined by TEM. To improve aqueous dispersibility the projected nanostructures for efficient use in drug delivery, self-assembled dehydropeptide nano carriers were further stabilized with Vitamin-E-TPGS. The final complex drug nanoparticles provided controlled drug release. These findings demonstrated that incorporation of constrained dehydro amino acids in peptides have the potential to construct stable nanostructures for development of nano materials with controlled drug release.
在最近的研究中,已证明在小肽中掺入非天然氨基酸α,β-脱氢苯丙氨酸会产生具有不同尺寸和形状的稳定自组装纳米结构。在此,我们用一种受限的脱氢氨基酸α,β-脱氢苯丙氨酸取代了我们先前报道的自组装肽Boc-Pro-Phe-Gly-OMe中的天然氨基酸苯丙氨酸,以研究其对自组装纳米结构的影响。脱氢三肽Boc-Pro-ΔPhe-Gly-OMe在水溶液中自组装成纳米结构,并形成了具有更高疏水分子包封效率的疏水基质。通过动态光散射研究发现肽纳米结构的流体力学尺寸约为257nm。负载纳米颗粒的形态和尺寸也通过透射电子显微镜确定。为了提高用于药物递送的自组装纳米结构的水分散性,用维生素E-TPGS进一步稳定了自组装脱氢肽纳米载体。最终的复合药物纳米颗粒实现了药物的可控释放。这些发现表明,在肽中掺入受限的脱氢氨基酸有可能构建稳定的纳米结构,用于开发具有可控药物释放功能的纳米材料。