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CN-121991163-A - Peptide APRP with antihypertensive and antioxidant activities and preparation method and application thereof

CN121991163ACN 121991163 ACN121991163 ACN 121991163ACN-121991163-A

Abstract

The invention discloses a peptide APRP with antihypertensive and antioxidant activities, and a preparation method and application thereof, belonging to the fields of food science and biotechnology. The invention screens out a short peptide APRP (with a sequence of Ala-Pro-Arg-Pro) with potential antihypertensive activity, the peptide APRP has obvious ACE inhibitory activity, the half inhibitory concentration (IC 50 ) is 0.2892mM, and the inhibition rate in an HK-2 cell model is as high as 72.85% at a concentration of 1 nM. Molecular docking results show that APRP is stably combined with ACE active centers through hydrogen bonds, salt bridges and hydrophobic interactions, and the conversion of angiotensin I is effectively blocked. The polypeptide APRP also has antioxidant activity, the DPPH free radical scavenging capacity reaches 9.14%, and the hydroxyl free radical scavenging rate reaches 5.1%. The invention provides a new candidate molecule for natural treatment with both hypertension and antioxidant properties.

Inventors

  • DU MING
  • FU BAIFENG
  • CHENG SHUZHEN
  • WANG SHAOYUN
  • CHANG ZHIHUI
  • WANG ZHENYU
  • WU CHAO
  • MA XIAOYU

Assignees

  • 大连工业大学

Dates

Publication Date
20260508
Application Date
20260130

Claims (10)

  1. 1. A polypeptide, wherein the amino acid sequence of the polypeptide is APRP or Ala-Pro-Arg-Pro.
  2. 2. A product comprising the polypeptide of claim 1, wherein the product comprises a food product, a pharmaceutical product, a commodity product, or a health product.
  3. 3. The product of claim 2, wherein the pharmaceutical product further comprises a pharmaceutically acceptable carrier and/or a pharmaceutically acceptable adjuvant.
  4. 4. The product of claim 3, wherein the pharmaceutically acceptable carrier comprises microcapsules, microspheres, nanoparticles, and/or liposomes, and the pharmaceutically acceptable adjuvant comprises excipients and/or additives.
  5. 5. The product of claim 4, wherein the pharmaceutical product comprises an oral formulation, an injectable formulation, or a sustained release formulation.
  6. 6. The product of claim 5, wherein the daily chemical product comprises a skin care product or a cosmetic product.
  7. 7. Use of the polypeptide of claim 1 for the preparation of a product that contributes to antioxidant properties.
  8. 8. The product of claim 7, wherein the product comprises a health product, a daily chemical product, or a pharmaceutical product.
  9. 9. Use of the polypeptide of claim 1 for the preparation of a medicament for reducing blood pressure.
  10. 10. The use of claim 9, wherein the pharmaceutical product comprises an oral pharmaceutical product or a topical pharmaceutical product.

Description

Peptide APRP with antihypertensive and antioxidant activities and preparation method and application thereof Technical Field The invention relates to the fields of food science and biotechnology, in particular to peptide APRP with antihypertensive and antioxidant activities, a preparation method and application thereof. Background Hypertension and oxidative stress are two key pathophysiological factors which seriously threaten human health, are interrelated and mutually promoted, and are important causes of occurrence and development of chronic diseases such as cardiovascular and cerebrovascular diseases, metabolic syndrome and the like. In the current disease prevention and health management field, the development of functional components with dual effects of blood pressure reduction and antioxidation has become an urgent need for research hotspots and industrial development. At present, substances with relevant biological activities existing in markets and scientific researches generally have certain limitations. In terms of blood pressure reduction, although the main stream drugs such as angiotensin converting enzyme inhibitors and the like have definite curative effects, the long-term use of the main stream drugs can possibly be accompanied with side effects, and the main stream drugs belong to the category of drugs and are not suitable for daily health care. The activity intensity, stability and specificity of antihypertensive peptides derived from food-borne proteins are often uneven. While common synthetic antioxidants present potential safety concerns in terms of antioxidant activity, natural antioxidants such as vitamins C, E and the like, their bioavailability and stability in complex systems present challenges. More importantly, most of the existing products tend to be single in function, or only aim at blood pressure regulation, or only focus on antioxidation, and difficult to cooperatively cope with complex health conditions such as hypertension aggravated by oxidative stress. Therefore, there is a need in the art for a novel functional factor that has significant activity, clear mechanism and easy industrial preparation, and can act on two key targets of blood pressure regulation and oxidative damage alleviation simultaneously. Disclosure of Invention [ Technical problem ] The invention aims to overcome the defects of the prior art, provide a novel peptide with high-efficiency antihypertensive and antioxidant dual activities, and solve the key technical bottleneck in large-scale preparation and application. Hypertension and oxidative stress often promote each other in disease progression, forming a vicious circle. However, most products in the market and research, such as chemical antihypertensives or single antioxidants, often target only a single target, and lack synergistic intervention capability. Food-borne antihypertensive peptides generally have weak antioxidant activity, and conventional antioxidants lack a clear mechanism for lowering blood pressure. The characteristic of this separation of functions limits its comprehensive application in the prevention and management of cardiovascular diseases exacerbated by oxidative stress, etc. Technical scheme The invention provides a novel active peptide APRP, which has unique sequence, and is proved to be capable of inhibiting the activity of angiotensin converting enzyme efficiently by in vitro activity verification and cell model evaluation, thereby playing a role in reducing blood pressure, and meanwhile, the peptide segment has strong free radical scavenging capability and reducing power and can effectively reduce oxidative stress damage. The synergistic effect of the two activities provides a better solution for preventing and assisting in managing hypertension and complications thereof. According to the technical scheme provided by the invention, the problems of difficulty in finding active peptide and indistinct efficacy and mechanism in the background technology are directly solved by providing ACE inhibitory peptide with brand new sequence, high efficiency and definite mechanism, and safe and effective candidate substances are provided for developing novel antihypertensive drugs and functional foods, so that the ACE inhibitory peptide has a good application prospect. The invention provides a polypeptide, and the amino acid sequence of the polypeptide is APRP or Ala-Pro-Arg-Pro. The invention provides products containing said polypeptides. In one embodiment, the product comprises a food product, a pharmaceutical product, a commodity product, or a health product. In one embodiment, the pharmaceutical product further comprises a pharmaceutically acceptable carrier and/or a pharmaceutically acceptable adjuvant. In one embodiment, the pharmaceutically acceptable carrier comprises microcapsules, microspheres, nanoparticles, and/or liposomes. In one embodiment, the pharmaceutical excipients comprise excipients and/or additives. In one embodi