Research Progress on Preparation, Structure-Activity Relationship and Mechanism of Action of Food-Derived Antihypertensive Peptides(食源性降血压肽的制备、构效关系及作用机制研究进展)

Hypertension, as the most prevalent cardiovascular disease worldwide, emerged as one of the major mortality risks threatening human health. Although traditional clinical antihypertensive drugs effectively controlled blood pressure, they required long-term administration and were accompanied by significant side effects. Food-derived antihypertensive peptides, as natural components with prominent biological activities, gained extensive attention due to their considerable potential in lowering blood pressure and preventing cardiovascular diseases. The mechanisms of action of food-derived antihypertensive peptides involved regulating key components of the renin-angiotensin-aldosterone system, such as angiotensin-converting enzyme (ACE), renin, ACE2, and angiotensin receptors, and exerted effects through multiple pathways including the arginine-nitric oxide pathway, calcium ion channels, endothelial function, vascular remodeling, and the sympathetic nervous system, among which ACE inhibition represented the most common antihypertensive mechanism. The antihypertensive properties of food-derived peptides from animal, plant, and microbial sources were extensively explored via in vitro ACE inhibitory activity assays, vascular cell models, and spontaneously hypertensive rat models. The ACE inhibitory activity of peptides was significantly influenced by their structural characteristics, including molecular weight, amino acid sequence, amphiphilicity, and spatial conformation. The study research progress on the preparation of food-derived antihypertensive peptides (including raw material sources and preparation methods), in vitro and in vivo activity evaluation approaches, the structure-activity relationship and their mechanisms of action was systematically summarized. Finally, the challenges faced by food-derived antihypertensive peptides in industrial production and stability enhancement, as well as their future development directions, were elaborated. 〖(高血压作为全球范围内最常见的心血管疾病,已成为威胁人类健康的主要死亡风险因素之一。传统临床降血压药物虽能有效控制血压,但需长期服用且伴随明显副作用；食源性降血压肽作为一种具有显著生物活性的天然成分,因其在降低血压和预防心血管疾病方面展现出的巨大潜力而受到广泛关注。食源性降血压肽的作用机制涉及调控血管紧张素转化酶(angiotensin-converting enzyme, ACE)、肾素、ACE2和血管紧张素受体等肾素-血管紧张素-醛固酮系统关键组分,并且在精氨酸一氧化氮途径、钙离子通道、内皮功能、血管重构和交感神经系统等多途径作用机制发挥作用。其中,抑制ACE是最常见的降血压机制。通过体外ACE抑制活性试验、血管细胞模型和自发性高血压大鼠模型,来自动物、植物和微生物的食源性降血压肽的降血压特性被广泛探索。研究发现,肽的ACE抑制活性受其结构特征影响显著,包括分子质量大小、氨基酸序列、两亲性和空间构象等因素。系统总结了食源性降血压肽的制备(原料来源、制备方法)、体内外活性评价手段、作用机制与构效关系的研究进展,阐述了食源性降血压肽在工业化生产、稳定性提升等方面面临的挑战及未来发展方向。)