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Polypeptide and application thereof in preparation of ACE inhibitor or blood pressure reducing product

An inhibitor and blood pressure lowering technology, applied in the field of biomedicine, can solve problems such as unsuitable for industrial application and complex structure

Active Publication Date: 2021-04-23
JIANGSU VOCATIONAL COLLEGE OF MEDICINE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Judging from the prior art, most of the polypeptide structures that use proline as the antihypertensive peptide have activity are relatively complex and not suitable for industrial application

Method used

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  • Polypeptide and application thereof in preparation of ACE inhibitor or blood pressure reducing product
  • Polypeptide and application thereof in preparation of ACE inhibitor or blood pressure reducing product
  • Polypeptide and application thereof in preparation of ACE inhibitor or blood pressure reducing product

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 Molecular docking analysis of the combination of polypeptide compound Sar-bAla-Pro and ACE

[0032] First, the structure of the polypeptide compound Sar-bAla-Pro was generated by chemdraw software

[0033] And the crystal structure of human ACE (1o86.pdb) was extracted from the protein database. Then, the ACE protein (including its cofactors chloride and zinc) in PDBQT format was extracted using the AutoDock tool software (v1.5.6), and Gasteiger charges were assigned and polar hydrogen bonds were added.

[0034] Subsequently, molecular docking simulations were performed using AutoDock Vina software (v1.1.2) to predict the binding affinity and conformation of compounds to ACE. ACE was set to rigid throughout the simulation. Scoring uses a weighted sum of steric and hydrophobic interactions, as well as hydrogen bonds. When running molecular docking, the exhaustiveness parameter was set to 32 and the coordinates were set to X:40.69, Y:32.80, and Z:47.29. Th...

Embodiment 2

[0037] Synthesis of embodiment 2 polypeptide compound Sar-bAla-Pro

[0038] The polypeptide compound Sar-bAla-Pro of the present invention is artificially synthesized, and the specific operation is as follows:

[0039] First, Fmoc-β-alanine was added to the proline dichloro resin, and TBTU (O-benzotriazole-N,N,N',N'-tetramethyluronium tetrafluoroboric acid and DIEA (N,N-diisopropylethylamine) for coupling, the coupling time is 60 minutes, and wash 3 times with piperidine / dimethylformamide with a volume ratio of 20% to remove the terminal Fmoc, and then use hexahydropyridine Carry out deprotection, and after deprotection, wash 6 times with piperidine / dimethylformamide whose volume ratio is 20%, and obtain an intermediate product after drying;

[0040] Add the intermediate product to Fmoc-sarcosine, TBTU and DIEA for coupling, the coupling time is 60 minutes, and wash 3 times with piperidine / dimethylformamide with a volume ratio of 20%, and deprotect with hexahydropyridine Aft...

Embodiment 3

[0043] ACE inhibitory activity detection of the polypeptide compound Sar-bAla-Pro of embodiment 3

[0044] 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 3.19mU / 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 evalu...

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Abstract

The invention discloses a polypeptide and an application thereof in preparation of an ACE inhibitor or an antihypertensive product. The amino acid sequence of the polypeptide is Sar-bAla-Pro and the structure is shown in the general formula (I) in the specification. The polypeptide is artificially synthesized from rare amino acids Sar and bAla and conventional amino acids Pro, is of a single-chain linear structure, is white powder, is slightly soluble in water, has the molecular weight of 257.14 Da and the tPSA value of 98.74, shows relatively good hydrophobicity, can resist further hydrolysis of in-vivo protease, has relatively good ACE inhibition activity, and can be used as a lead compound serving as an effective component of medicines and functional foods for treating cardiovascular diseases such as hypertension and has good potential and application value.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to a class of polypeptide and its application in the preparation of ACE inhibitors or blood pressure lowering products. Background technique [0002] The "China Cardiovascular Disease Report 2019" pointed out that the prevalence of cardiovascular disease in my country is on the rise. 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. The 2015 National Hypertension Survey showed that the prevalence of hypertension in my country was 27.9%, and the number of hypertensive patients nationwide was estimated to reach 245 million. In 2017, 2.54 million people in my country died of high systolic blood pressure. If all hypertensive patients were treated and their blood pressure was controlled, 803,000 cardiovascular events per year would be r...

Claims

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Application Information

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IPC IPC(8): C07D207/16A61P9/12A61K31/401
CPCC07D207/16A61P9/12Y02P20/55
Inventor 俞黎黎钱炳俊田冲冲温尧林胡君杨烨戴丽
Owner JIANGSU VOCATIONAL COLLEGE OF MEDICINE
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