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Anti-hypertension active peptide Orn-Hyp-Pro, application thereof, and medicinal composition

An antihypertensive, active peptide technology, applied in the field of biomedicine, can solve the problems of low bioavailability, high cost, constraints and the like

Inactive Publication Date: 2017-11-10
YANCHENG INST OF HEALTH SCI
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  • 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

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  • Anti-hypertension active peptide Orn-Hyp-Pro, application thereof, and medicinal composition
  • Anti-hypertension active peptide Orn-Hyp-Pro, application thereof, and medicinal composition
  • Anti-hypertension active peptide Orn-Hyp-Pro, application thereof, and medicinal composition

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Synthesis of Orn-Hyp-Pro tripeptide. The antihypertensive active peptide of the present invention is artificially chemically synthesized, and the specific operation is as follows:

[0021] The polypeptide of the present invention is synthesized by a liquid-phase polypeptide synthesis method, and a certain amount of (2S)-2,5-bis[(tert-butoxycarbonyl)amino]valeric acid (Boc-Orn(Boc)-OH) and hydroxysuccinyl Put the imine (Hosu) into a round bottom flask, add tetrahydrofuran (THF) to dissolve until clear, continue to add dicyclohexylcarbodiimide (DCC), stir gently, and react overnight.

[0022] Further, the above reaction solution was vacuum filtered, 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, the obtained oil was (2S)-2,5-bis[(tert-butoxycarbonyl)amino]pentyl succinimide (Boc-...

Embodiment 2

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

[0031]Hippuryl-L-histidyl-L-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...

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 rat blood pressure before gavage, then 1.0mg / kg body weight dose carries out sample (active tripeptide of embodiment 1, Orn-Hyp-Pro) gavage, blank control group gavage equal volume normal saline (Saline), The blood pressure of the drug control group ...

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Abstract

The invention relates to an anti-hypertension active peptide Orn-Hyp-Pro, an application thereof, and a medicinal composition. The amino acid sequence of the active peptide is ornithyl-hydroxyprolyl-proline, and the active peptide has a structure represented by formula I. The angiotensin converting enzyme (ACE) activity inhibition concentration IC50 of the active peptide is 326.72 [mu]mol / L, the blood pressure of a congenital hypertension rat which is intragastrically administrated according to a dosage of 1.0 mg / kg body weight decreases to a lowest point of 195 mmHg from 212 mmHg 2 h later, and the drug effect lasting time is 2 h.

Description

technical field [0001] The invention belongs to the field of biomedicine, and more specifically relates to an antihypertensive active peptide Orn-Hyp-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 w...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/09A61K38/06A61P9/12A23L33/18
CPCC07K5/0815A23L33/18A23V2002/00A61K38/00A23V2200/326A23V2250/55
Inventor 钱炳俊霍江华韦朝华俞黎黎丁凤云张云蝶龚婷
Owner YANCHENG INST OF HEALTH SCI