Dube Taru, Mandal Saurabh, Panda Jiban Jyoti
Institute of Nano Science and Technology, Habitat Centre, Phase-10, Sector-64, Mohali, Punjab, 160062, India.
Amino Acids. 2017 May;49(5):975-993. doi: 10.1007/s00726-017-2403-8. Epub 2017 Mar 10.
Surging reports of peptide-based nanosystems and their growing potency in terms of biological utility demand for the search of newer and simpler peptide-based systems that could serve as smart templates for the development of self-assembled nanostructures. Use of simple amino acids as monomeric building blocks for synthesizing ensembles of nanostructures have gained momentum in this direction with some reports focusing on the development of nanosystems from single or modified single amino acids. In this work, we have demonstrated self-assembly and nanoparticle formation ability of a single amino acid derivative, N-alpha-(9-fluorenylmethyloxycarbonyl)-N(in)-tert-butyloxycarbonyl-L-tryptophan [Fmoc-Trp(Boc)-OH]. The nanoparticles formed by the amino acid were found to be stable to various environmental perturbations like temperature, salts and showed responsiveness to pH change. These were capable of loading and releasing different bioactive molecules and were biocompatible. These systems demonstrated high cellular uptake and doxorubicin-loaded nanoparticles were found to be more efficient in killing glioma cells as compared to the drug alone. Thus, their simple amino acid-based origin along with the ability to ferry bioactive molecules to various cells, endows them the suitability for future applications in the field of drug delivery.
基于肽的纳米系统的报道激增，其在生物效用方面的效力不断提高，这就需要寻找更新颖、更简单的基于肽的系统，这些系统可以作为自组装纳米结构开发的智能模板。使用简单氨基酸作为合成纳米结构集合体的单体构建块在这一方向上已获得发展势头，一些报道聚焦于从单一或修饰的单一氨基酸开发纳米系统。在这项工作中，我们展示了一种单一氨基酸衍生物N-α-（9-芴甲氧羰基）-N-（内）-叔丁氧羰基-L-色氨酸[Fmoc-Trp（Boc）-OH]的自组装和纳米颗粒形成能力。发现由该氨基酸形成的纳米颗粒对温度、盐等各种环境扰动具有稳定性，并对pH变化有响应。它们能够负载和释放不同的生物活性分子，并且具有生物相容性。这些系统表现出高细胞摄取率，并且与单独的药物相比，负载阿霉素的纳米颗粒在杀死胶质瘤细胞方面更有效。因此，它们基于简单氨基酸的起源以及将生物活性分子转运到各种细胞的能力，使它们适合未来在药物递送领域的应用。
