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Pig-derived ACE inhibitory activity polypeptide, pharmaceutical composition or food and application

A technology of active polypeptide and inhibitory activity, applied in blood pressure lowering drugs or food, porcine-derived ACE inhibitory active polypeptide and pharmaceutical composition or food and application, in the field of preparing ACE inhibitor, can solve the problem of short action time and easy blood pressure. Rebound, etc.

Active Publication Date: 2020-12-25
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have shown that ordinary antihypertensive drugs have the characteristics of short action time and easy rebound of blood pressure after drug withdrawal. At the same time, the rapid absorption and excretion of drugs will cause side effects such as cough, kidney damage, and angioneurotic edema. Polypeptide ACE inhibitors only Effective for hypertensive patients, but not for normotensive patients

Method used

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  • Pig-derived ACE inhibitory activity polypeptide, pharmaceutical composition or food and application
  • Pig-derived ACE inhibitory activity polypeptide, pharmaceutical composition or food and application
  • Pig-derived ACE inhibitory activity polypeptide, pharmaceutical composition or food and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1 Screening and Identification of Polypeptide AVATLLKP

[0025] A method combining LC-MS / MS with Shotgun proteomics technology was used. Pig limb bones are used as raw materials, and the pig bone extract is obtained after decoction, ethanol precipitation, acid precipitation, and alkali precipitation. The extract is subjected to LC-MS / MS analysis after centrifugation, ultrafiltration, and desalination. Structure-activity relationship features to screen peptides that have an inhibitory effect on ACE.

[0026] The specific method is as follows:

[0027] Sample preparation: (1) Extraction: fresh pig limb bones were washed, crushed, weighed, added water according to the ratio of material to liquid 1:2 (w / v), extracted under 1.2MPa hot pressure for 1.5h, filtered, repeated extraction once, combined filtrate. (2) Degreasing: the filtrate was cooled at 4°C for 36 hours, and the upper layer of fat was removed. (3) Ethanol precipitation: concentrate in vacuo, add etha...

Embodiment 2

[0033] Example 2 Detection of ACE Inhibitory Activity of Polypeptide AVATLLKP

[0034] principle

[0035] N-[3-(2-furyl)acryloyl]-L-phenylalanyl-glycyl-glycine (FAPGG, λmax=340nm, ε=2270M -1 cm -1 , molecular weight 399.40) can be enzymatically hydrolyzed by ACE into N-[3-(2-furyl)acryloyl]-L-phenylalanyl (FAP, λmax=340nm, ε=1512M -1 cm -1 ) and glycyl-glycine (GG, no absorption at 340nm), so it can be used as the mimic substrate of ACE. The absorbance value of 1mM FAPGG completely converted into FAP and GG is 0.758, and the inhibition rate can be calculated according to the change value of absorbance at 340nm.

[0036] reaction system

[0037] (1) Buffer solution: 0.1M PBS buffer solution (pH 8.2, containing 300mM NaCl)

[0038] (2) Substrate solution: FAPGG solution with a concentration of 1.6 mM was prepared using the above buffer solution.

[0039] (3) Enzyme solution: ACE was prepared into a 0.2 U / mL solution using the above buffer solution.

[0040] (4) Sample solu...

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PUM

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Abstract

The invention relates to a pig-derived ACE inhibitory activity polypeptide, a pharmaceutical composition or food and application, in particular to a pig-derived polypeptide with angiotensin convertingenzyme (ACE) inhibitory activity and a composition or food containing the active polypeptide or acceptable salt thereof. The amino acid sequence of the polypeptide is Ala-Val-Ala-Thr-Leu-Leu-Lys-Pro.The polypeptide AVATLLKP has ACE inhibitory activity and blood pressure lowering activity, and has good application prospects as a health care product and a medicine lead compound for diseases such as hypertension, heart diseases and cardiovascular diseases.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a porcine ACE-inhibiting active polypeptide, a pharmaceutical composition or food and its application, and the application of the active polypeptide AVATLLKP in the preparation of ACE inhibitors, blood pressure-lowering drugs or food. Background technique [0002] Hypertension is a common cardiovascular disease with a high incidence rate, which can seriously damage target organs such as the heart, brain, and kidneys. Treatment and prevention of hypertension are very important issues in the current society. Abnormal activity of renin-angiotensin system is the main cause of hypertension, and angiotensin converting enzyme (ACE) plays an important role in regulating blood pressure and cardiovascular function. ACE can catalyze the conversion of the inactive decapeptide angiotensin I into the octapeptide angiotensin II, which has a strong vasoconstrictive effect, thereby increasi...

Claims

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Application Information

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IPC IPC(8): C07K7/06A61K38/08A61P9/12A23L33/18
CPCA23V2002/00A61K38/00A23L33/18A61P9/12C07K7/06A23V2200/326A23V2250/55
Inventor 靳艳于洋叶明亮徐秀杰
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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