食源性血糖调节活性肽的研究进展

Research Progress on Food Derived Blood Glucose Regulating Peptides

糖尿病已成为全球最严重的慢性疾病之一,亟需新型的预防、干预、调控手段。食物蛋白源小肽与参与血糖调节的受体、酶、生物分子,以及葡萄糖转运体相互作用,干预并调控血糖水平。它具有组织亲和力和特异性高、副作用低的优势,是一种前景广阔的糖尿病应对方案。本文综述了食源性血糖调节活性肽的作用机制、动植物食物来源、结构特征、制备和活性评价手段、构效关系研究方法,以及产业化推广的诸多挑战,包括DPP-IV抑制肽、α-葡萄糖苷酶抑制肽、α-淀粉酶抑制肽的序列特征,多种生物信息学技术(电子模拟、分子对接、定量构效关系等)联用分析降糖机制与活性位点。为未来研究提供了思路:a.从细胞通路、代谢组学角度明确机理,保障并强化体内功效;b.通过细胞和动物实验结合临床试验评估消化稳定性、生物利用度和安全性;c.采用新型载体技术,提高肽基活性物质的溶解度、稳定性和渗透性。本文期望为促进降糖功能食品的产业化应用提供理论和科学参考。

Diabetes mellitus has become one of the most serious chronic diseases all over the world,which need to be to prevented,intervened,regulated by innovative means.Food derived small peptides can regulate blood glucose by acting with receptors,enzymes,biological molecules and glucose transporters.They show high tissue affinities,significant specificities,with low side effects,which are promising strategies for diabetes mellitus.This survey summarizes the mechanisms,food protein sources,preparation and activity evaluation procedures,structure-activity relationships and challenges during commercial development of food derived blood glucose regulating peptides.Specifically,it includes the sequence characteristics of DPP-IV inhibitory peptide,α-glucosidase inhibitory peptides andα-amylase inhibitory peptides.Besides,the active sites are also discussed from different perspectives of sequence alignment:bioinformatics technologies such as in silico analysis,molecular structure alignment/docking,and quantitative structure activity relationship analysis.It may provide ideas for future research:a.Exploring the mechanism from the aspect of cell pathways and metabonomic to improve in vivo efficacy.b.Combining cell/animal experiments with clinical trials to evaluate digestive stability,bioav-ailability and safety.c.Innovative carriers to improve the solubility,stability and permeability of peptides.Supports for promoting the industrial application of diabetes functional foods are expected.