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一种超分子方法,用于开发具有增强的二肽基肽酶 IV(DPP-IV)抑制活性的新型大豆和羽扇豆肽纳米胶。

A Supramolecular Approach to Develop New Soybean and Lupin Peptide Nanogels with Enhanced Dipeptidyl Peptidase IV (DPP-IV) Inhibitory Activity.

机构信息

Tissue Engineering Unit, Institute for Stem Cell Biology , Regenerative Medicine and Innovative Therapies-ISBReMIT, Fondazione IRCSS Casa Sollievo della Sofferenza , San Giovanni Rotondo ( FG ), Italy.

Center for Nanomedicine and Tissue Engineering (CNTE) , ASST Grande Ospedale Metropolitano Niguarda , Milan , Italy.

出版信息

J Agric Food Chem. 2019 Apr 3;67(13):3615-3623. doi: 10.1021/acs.jafc.8b07264. Epub 2019 Mar 22.

DOI:10.1021/acs.jafc.8b07264
PMID:30879293
Abstract

Soy1 (IAVPTGVA) and Lup1 (LTFPGSAED), two peptides from soybean and lupin protein hydrolysis, have been singled out as dipeptidyl peptidase IV (DPP-IV) activity inhibitors in different model systems. However, their activity is affected by their instability toward intestinal proteases. Here, an innovative strategy based on nanogels was developed in order to increase both their stability and antidiabetic properties through encapsulation into the RADA16 peptide. The nanogel formation was stimulated by a solvent-triggered approach, allowing us to produce stable nanogels ( G' = 1826 Pa, stress-failure ≥50 Pa) with shear-thinning propensity. ThT binding assay, and ATR-FTIR spectroscopy experiments showed that nanogels self-aggregated into stable cross-β structures providing higher resistance against proteases (ex vivo experiments) and increased bioavailability of Soy1 and Lup1 peptides (in situ experiments on Caco-2 cells). Hence, this simple and harmless nanotechnological approach could be a key-step in making innovative nanomaterials for nutraceuticals delivering.

摘要

大豆 1 肽(IAVPTGVA)和羽扇豆 1 肽(LTFPGSAED)是两种来自大豆和羽扇豆蛋白水解物的二肽基肽酶 4(DPP-4)活性抑制剂,在不同的模型系统中被筛选出来。然而,它们的活性受到其对肠道蛋白酶不稳定性的影响。在这里,我们开发了一种基于纳米凝胶的创新策略,通过将其包封到 RADA16 肽中,提高其稳定性和抗糖尿病特性。纳米凝胶的形成是通过溶剂触发的方法刺激的,这使得我们能够生产出具有剪切稀化倾向的稳定纳米凝胶(G'=1826 Pa,应力破坏≥50 Pa)。ThT 结合试验和 ATR-FTIR 光谱实验表明,纳米凝胶自组装成稳定的交叉-β 结构,提供了更高的抗蛋白酶性(离体实验)和提高了大豆 1 肽和羽扇豆 1 肽的生物利用度(Caco-2 细胞的原位实验)。因此,这种简单无害的纳米技术方法可能是开发用于营养输送的创新纳米材料的关键步骤。

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