Unlock instant, AI-driven research and patent intelligence for your innovation.

Antihypertensive active peptide GABA-The-Pro as well as application and pharmaceutical compositions

An antihypertensive, active peptide technology, applied in the field of biomedicine, can solve the problems of restriction, low repeatability and high cost

Inactive Publication Date: 2017-11-03
YANCHENG INST OF HEALTH SCI
View PDF6 Cites 6 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this preparation method has high cost, low reproducibility, and low bioavailability, and there is an urgent need to develop a new alternative production technology
These studies are all based on the peptide information contained in the protein. Although as the molecular weight of the peptide increases, its structure will vary widely and its activity will become more potential. However, due to the molecular sieve effect of the intestinal mucosa and its rich peptidase, the In order to use natural protein active resources to develop ACEI peptide small molecule substances

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Antihypertensive active peptide GABA-The-Pro as well as application and pharmaceutical compositions
  • Antihypertensive active peptide GABA-The-Pro as well as application and pharmaceutical compositions
  • Antihypertensive active peptide GABA-The-Pro as well as application and pharmaceutical compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Synthesis of GABA-The-Pro tripeptide. The antihypertensive active peptide of the present invention can be artificially chemically synthesized, and the specific operations are as follows:

[0021] The polypeptide of the present invention is synthesized by a liquid-phase polypeptide synthesis method, and a certain amount of N-tert-butoxycarbonyl theanine methyl ester (Boc-The-OH) and proline methyl ester hydrochloride (H-Pro-Ome.HCl ) into a round bottom flask, add dimethylformamide (DMF) to dissolve until clear, continue to add nitrogen methylmorpholine (NMM) and dicyclohexylcarbodiimide (DCC), stir gently, and react overnight .

[0022] Further, the above reaction solution was subjected to vacuum filtration, and ethyl acrylate (EA) and H 2 O for chromatography. Absorb the upper liquid, using NaHCO 3 / H 2 Wash twice with O, then wash with citric acid / H 2 Washed twice with O, washed twice with saturated NaCl solution, Na 2 SO 4 After drying, evaporated to dryness ...

Embodiment 2

[0030] Angiotensin-converting enzyme (ACE) activity inhibition test in vitro.

[0031]Hippuryl histidyl leucine (hippuryl-L-histidyl-L-leucine, HHL) is rapidly decomposed under the catalysis of ACE enzyme to produce hippuric acid (Hippuric Acid, HA) and dipeptide histidyl-leucine (HL), adding After ACE enzyme inhibitor, the activity of ACE enzyme is inhibited, and the production of HA and HL is reduced. In this embodiment, ACE is extracted from rabbit lung, and the enzyme activity is 0.76mU / mL. It is developed by DAB and measured by spectrophotometer. The amount of HA produced and the activity of ACE enzyme were analyzed. Ethyl acetate extracts hippuric acid in the reactant, then reacts with a pyridine solution (DAB chromogen) containing p-dimethylaminobenzaldehyde in acetic anhydride to generate an orange-yellow compound, and directly measures its OD value at 459nm colorimetrically, The inhibition rate of ACE enzyme inhibitors to ACE enzyme was evaluated according to the fol...

Embodiment 3

[0038] In vivo antihypertensive test in congenitally hypertensive rats (SHR).

[0039] Using SoftronBP-98A intelligent non-invasive blood pressure instrument for rats, the systolic blood pressure (SBP) of the rats was determined by the tail method.

[0040] In the awake state of SHR rats (spontaneously hypertensive rats), first put the rats in a rat bag, keep a constant temperature, and use the Softron BP-98A rat intelligent non-invasive blood pressure instrument to measure the tail vein blood pressure. Systolic blood pressure (SBP) in rats. One week before the experiment, the blood pressure of the rats was measured every other day, and the experimental records were started after the rats got used to it stably. First measure the blood pressure of rats before gavage, then 1.5mg / kg body weight dose carries out sample (the active tripeptide that embodiment 1 makes, GABA-The-Pro) gavage, blank control group gavage equal volume normal saline (Saline ), the antihypertensive drug c...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to an antihypertensive active peptide GABA-The-Pro as well as application and pharmaceutical compositions. The amino acid sequence of the active peptide is: gamma-aminobutyric acid-theanine-proline with a structure shown as formula I. The invention provides a novel active peptide, and the active peptide of inhibiting angiotensin converting enzyme (ACE) activity of IC50 is 207.64 mu mol / L, a mouse with congenital hypertension is gavaged with the dosage / weight of 1.5 mg / kg antihypertensive active peptide GABA-The-Pro, after 2.5 hours, the blood pressure drops from 187mmHg to the lowest point of 166mmHg, and sustained duration of pesticide effect is 3.5 hours. The formula I is shown in the description.

Description

technical field [0001] The invention belongs to the field of biomedicine, and more specifically relates to an antihypertensive active peptide GABA-The-Pro and its application, and an antihypertensive pharmaceutical composition. Background technique [0002] The "China Cardiovascular Disease Report 2015" pointed out that the prevalence of cardiovascular disease in my country is in a stage of continuous increase. It has become a consensus that hypertension is the main risk factor for cardiovascular disease, and it is the driving factor for the continuous increase in the prevalence of cardiovascular disease in my country. According to statistics from the Ministry of Health in 2014, the prevalence rate of hypertension in my country is 25.5%, reaching 27.9% in some provinces, and the number of hypertensive patients nationwide is estimated to reach 270 million. [0003] At present, many antihypertensive drugs are considered to be the first-line therapeutic drugs in clinic, among ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C07K5/027A61K38/06A61P9/12A23L33/18
CPCC07K5/0205A23L33/18A61K38/00
Inventor 钱炳俊温尧林霍江华丁凤云
Owner YANCHENG INST OF HEALTH SCI