Bioactive peptides (BPs) are widely used in the food industry, pharmaceutical industry, cosmetics industry, and feed industry due to their excellent biological activity, selectivity, and low toxicity. Despite the continuous emergence of articles on the functional research of BPs and the commercialization of BPs, there is a lack of a systematic review of functional evaluation methods for BPs. This article centers on BPs, systematically summarizing their major preparation methods and global regulatory frameworks. It delves into an analysis of their biological functions and the relationship between structure and function, in addition to outlining the in vivo degradation pathways of BPs and providing suggestions for improving their stability. Notably, for the first time, we have reviewed the functional evaluation systems applicable to BPs. This article proposes a comprehensive evaluation system for BPs, covering various aspects from computer simulation prediction to clinical application evaluation. It comprehensively explores the application value of computer technology, chemical analysis, in vitro cell models, animal models, and clinical evaluation in the functional evaluation of BPs and points out the limitations faced by each evaluation model. In addition, for the first time, the introduction of organoid and microfluidic technology into the functional evaluation model of the food industry has been proposed. This integrated bottom-up evaluation framework establishes a multidisciplinary paradigm for BP functional assessment, synergizing computational prediction, organoid-microfluidic validation, and clinical translation. It provides both methodological advancements for rational experimental design and actionable strategies to accelerate the development of BP-derived therapeutics and functional products, ultimately bridging the gap between academic discovery and industrial application.
Keywords: bioactive peptides; biological activity; computer simulation; function evaluation; organoids; preparation methods.