Lammi Carmen, Bollati Carlotta, Gelain Fabrizio, Arnoldi Anna, Pugliese Raffaele
Department of Pharmaceutical Sciences, University of Milan, >Milan, Italy.
Tissue Engineering Unit, Institute for Stem Cell Biology, Regenerative Medicine and Innovative Therapies-ISBReMIT, Fondazione IRCSS Casa Sollievo della Sofferenza, >San Giovanni Rotondo, Italy.
Front Chem. 2019 Jan 24;6:670. doi: 10.3389/fchem.2018.00670. eCollection 2018.
Although there is an increasing interest for bioactive food protein hydrolysates as valuable ingredients for functional food and dietary supplement formulations, their potential applications are hampered by their insufficient stability in physiological conditions. In this study, an innovative strategy based on nanomaterials was developed in order to increase the hempseed hydrolysate stability and the anti-diabetic properties, through their encapsulation into ionic self-complementary RADA16 peptide based-hydrogels. Atomic force microscope (AFM) morphological analysis indicated that the new nanomaterials were composed of a nanofibril network, whose increased diameter in respect to native RADA16 suggests the presence of transient non-covalent interactions among the RADA16 supramolecular assemblies and the embedded hempseed peptides. Structural analysis by FT-IR spectroscopy indicated typical β-sheet signatures. The RADA16-hempseed protein hydrolysate hydrogel was shown to act as a novel dipeptidyl peptidase IV (DPPIV) inhibitor in different biological assays. Finally, this nanoformulation was used as a drug delivery system of the anti-diabetic drug sitagliptin, helping to reduce its dosage and eventually associated side-effects.
尽管生物活性食品蛋白水解物作为功能性食品和膳食补充剂配方的宝贵成分越来越受到关注，但其在生理条件下稳定性不足限制了其潜在应用。在本研究中，开发了一种基于纳米材料的创新策略，通过将大麻籽水解物封装到基于离子自互补RADA16肽的水凝胶中，提高其稳定性和抗糖尿病特性。原子力显微镜（AFM）形态分析表明，新的纳米材料由纳米纤维网络组成，相对于天然RADA16，其直径增加表明RADA16超分子聚集体与嵌入的大麻籽肽之间存在瞬时非共价相互作用。傅里叶变换红外光谱（FT-IR）的结构分析表明具有典型的β-折叠特征。在不同的生物学试验中，RADA16-大麻籽蛋白水解物水凝胶被证明可作为一种新型的二肽基肽酶IV（DPPIV）抑制剂。最后，这种纳米制剂被用作抗糖尿病药物西他列汀的药物递送系统，有助于减少其剂量并最终减少相关副作用。
