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Micromolecule active peptide of stichopus japonicus source, and efficient screening method thereof

A technology of small molecule active peptides and small molecule peptides, applied in the fields of peptides, sexual diseases, food ingredients, etc., can solve the problems that hinder the widespread use of non-professional users, take a long time, and have many influencing factors, and achieve efficient, fast and universal applicability. Effect

Active Publication Date: 2019-02-12
DALIAN SHENLAN PEPTIDE TECH R & D CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the general problem is that these screening methods are cumbersome and complicated, with many influencing factors, require professional or experienced personnel to operate, take a long time and have poor general applicability
[0004] With the construction of the peptide database, the discovery of a large number of active peptides, the study of peptide properties and structure-activity relationships, computer-aided activity screening and drug design have become inevitable. Patent 201711431033.1 uses different online databases to efficiently inhibit ACE activity after multiple rounds of screening. Inhibiting peptides, this invention also uses molecular docking to dock with ACE during the screening process. Although highly active peptides can be obtained, this step is more complicated. Molecular docking involves more knowledge, requires a lot of professional background knowledge, and affects There are many factors that seriously hinder the widespread use of non-professional users

Method used

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  • Micromolecule active peptide of stichopus japonicus source, and efficient screening method thereof
  • Micromolecule active peptide of stichopus japonicus source, and efficient screening method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0034] The small molecule active peptides derived from sea cucumbers, the small molecule active peptides include two highly active small molecule peptides derived from sea cucumbers, the amino acid sequences of which are Lys-Phe-Pro-Pro-Pro-Met and Phe-Asp-Gly- Pro-Glu-Gly-Pro-Arg.

[0035] The active peptide sequence can be used as the core to be adjusted or modified accordingly.

[0036] The application after said corresponding adjustment or modification includes carrying out further drug design to two small molecule active peptides:

[0037] When Lys-Phe-Pro-Pro-Pro-Met is used for anti-breast cancer drug design, Phe can be included in Glu, Arg, Thr, Gly, Ser, Cys, Met, Asp, Leu, Pro, Gln, Ala, Lys, His Any substitution of any of the amino acids at positions 3, 4, 5, and 6 can be replaced by Val when designing antihypertensive drugs;

[0038]When Phe-Asp-Gly-Pro-Glu-Gly-Pro-Arg is used for anti-breast cancer drug design, Pro at the 4th position can be replaced by any of C...

Embodiment 2

[0041] High-efficiency screening method for small-molecule active peptides derived from sea cucumbers described in Example 1: Step 1. Preparation of sea cucumber enzymatically hydrolyzed oligopeptides

[0042] Fresh sea cucumber 5Kg adds water 10L homogenate and is placed in the enzymolysis tank, then adds the compound protease preparation of 15g, the mass ratio of compound protease is: neutral protease: papain: flavor protease=2:3:3, at 50 The enzymatic hydrolysis was carried out at ℃ for 4 hours, and the pH value of the enzyme reaction was controlled at 8.5. After the enzymatic hydrolysis, the temperature was raised to 90 ℃ to inactivate the enzyme for 10 minutes to obtain the japonicus protein enzymatic hydrolyzate. The proteolysis solution was centrifuged at 8000 rpm for 10 minutes to remove particulate matter, and then separated by ultrafiltration membrane separation technology with a molecular weight cut-off of 3000 Da, and the membrane liquid was spray-dried to obtain sm...

Embodiment 3

[0061] The steps of the high-efficiency screening method for the small molecule active peptides of sea cucumber origin described in this embodiment are all the same as in Example 2, the difference is: the mass ratio of the composite protease is: neutral protease: papain: flavor Protease=3:4:4.

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Abstract

The invention discloses a micromolecule active peptide of a stichopus japonicus source, and an efficient screening method thereof, and belongs to the field of the marine organism micromolecule activepeptide. The micromolecule active peptide comprises high-activity micromolecule peptide of two stichopus japonicus sources and has an amino acid sequence of Lys-Phe-Pro-Pro-Pro-Met and Phe-Asp-Gly-Pro-Glu-Gly-Pro-Arg. An enzymolysis technology is used for obtaining a stichopus japonicus enzymolysis oligopeptide product, an efficient liquid phase chromatography-tandem mass spectrum is adopted to analyze and authenticate the amino acid sequence of a peptide fragment contained in the oligopeptide, finally, a plurality of online databases are used for carrying out comprehensive activity screeningon authenticated 88 peptide fragments, and two high-activity micromolecule peptides are obtained. The high throughput analysis and authentication and high efficiency activity screening of a great quantity of micromolecule peptide products are realized. The method is simple, quick, high in operability and easy in implementation, the screening success probability of the active peptide is greatly improved, the method is suitable for the early-stage screening of a great quantity of active peptides, and the obtained peptide can be used for developing functional food, health care food and biologicalmedicine products with the functions of resisting breast cancer and lowering high blood pressure, and has a wide application prospect.

Description

technical field [0001] The invention belongs to the field of small-molecule active peptides of marine organisms, and in particular relates to small-molecule active peptides derived from sea cucumber enzymolysis and a high-efficiency screening method thereof. Background technique [0002] Cancer and hypertension are two major diseases with a high incidence rate, which seriously threaten human health. The main treatment methods for cancer are surgery and chemotherapy. However, in many cases, some cancer drugs not only cannot effectively treat patients, but also There are also many side effects, and it may also cause multi-drug resistance. A class of drugs for the treatment of hypertension are chemically synthesized ACE inhibitors such as captopril, lisinopril, etc., but these drugs can cause certain side effects, including cough, rash, and angioedema, so the development effect is good and Efficient therapeutic drugs without toxic and side effects are imperative. Small-molecu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C12P21/06A61K38/08A61P9/12A61P35/00A61P15/14A23L33/18
CPCA23V2002/00A61K38/00A23L33/18A61P9/12A61P15/14A61P35/00C07K7/06C12P21/06A23V2200/308A23V2200/326A23V2250/55
Inventor 包卫洋左爱华王祖哲马普孙天利
Owner DALIAN SHENLAN PEPTIDE TECH R & D CO LTD