CN107011413A - Tripeptides CGP with function of blood sugar reduction and application thereof - Google Patents
Tripeptides CGP with function of blood sugar reduction and application thereof Download PDFInfo
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- CN107011413A CN107011413A CN201710399843.7A CN201710399843A CN107011413A CN 107011413 A CN107011413 A CN 107011413A CN 201710399843 A CN201710399843 A CN 201710399843A CN 107011413 A CN107011413 A CN 107011413A
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- tripeptides
- cgp
- alpha
- blood sugar
- function
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/081—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- General Health & Medical Sciences (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses a kind of tripeptides CGP, the amino acid sequence of the tripeptides is:cys‑gly‑pro.The present invention further simultaneously discloses applications of the tripeptides CGP in hypoglycemic drug (particularly preparing the medicine as α Glucosidase inhibitor peptides) is prepared.
Description
Technical field
The invention belongs to biological technical field, more particularly to one can be combined with alpha-glucosidase, suppress its activity
Tripeptides.
Background technology
One of main source of blood glucose is that small intestine is digested and assimilated to carbohydrate, and the carbohydrate such as starch is through α-Portugal
Polyglycoside enzyme resolves into monose, enters blood circulation by intestinal absorption.Therefore alpha-glucosidase is in carbohydrate metabolism
Play an important roll in generation glucose.Alpha-glucosidase restrainer can be by suppressing human small intestine's epitheliochorial brush border
The activity of upper alpha-glucosidase, the generation of delay glucose plays an important roll, current α-grape in reduction postprandial blood sugar
Glycosidase inhibitor is widely used in treating diabetes.
Hypoglycemic medicine common are:
1. alpha-glucosidase restrainer:Acarbose, voglibose and Miglitol etc..
2. Insulin enhancer:Repaglinide, Nateglinide, Glimepiride, gliquidone etc..
3. insulin sensitizer:Melbine, thiazolidinediones etc..
4. insulin and the like:Insulin, insulin lispro, insulin aspart, glulisine etc..
The content of the invention
The technical problem to be solved in the present invention is to provide a kind of tripeptide sequence with function of blood sugar reduction and application thereof.
In order to solve the above-mentioned technical problem, the present invention provides a kind of tripeptides CGP, and the amino acid sequence of the tripeptides is:cys-
gly-pro。
The present invention is also simultaneously there is provided applications of the above-mentioned tripeptides CGP in hypoglycemic drug is prepared.
It is used as the improvement of the tripeptides CGP of present invention application:Prepare the medicine as alpha-glucosaccharase enzyme inhibition peptide.
The tripeptides CGP of the present invention can be used as alpha-glucosaccharase enzyme inhibition peptide.
The tripeptides CGP of the present invention can be by entrusting the synthesis acquisition of Qiang Yao bio tech ltd.
The tripeptide sequence of the present invention has inhibitory activity for alpha-glucosidase, so as to show with function of blood sugar reduction
Characteristic.
The detection method of involved alpha-glucosaccharase enzyme inhibition activity in the present invention:
The 50 certain density polypeptide solutions of μ L (configuration of 0.1mol/L, pH=6.9 phosphate buffer), 100 μ L are taken respectively
10mg/mL alpha-glucosaccharase enzyme solutions (using 0.1mol/L, pH=6.9 phosphate buffers are prepared), add in ELISA Plate, mix
Afterwards, 10min is placed at 25 DEG C.Then the PNPG (p-nitrophenyl-α-D- glucopyranosides) for adding 50 μ L 5mmol/L is molten
Liquid (uses 0.1mol/L, pH=6.9 phosphate buffers are prepared), at 37 DEG C after culture 30min, adds 50 μ L0.67mol/L's
Na2CO3Solution terminating reaction, determines absorbance under 405nm.The system is referred to as sample.
Following 3 systems are set simultaneously:Control, sample blank and control blank.
Control:50 μ L polypeptide solution is substituted with 50 μ L 0.1mol/L, pH=6.9 phosphate buffers.
Sample blank:With 100 μ L 0.1mol/L, pH=6.9 phosphate buffers replace 100 μ L 10mg/mL α-grape
Glucosides enzyme solutions;
Compare blank:Respectively with the 0.1mol/L of respective volume amount, pH=6.9 phosphate buffers replace polypeptide solution and α-
Glucosidase solution, inhibiting rate is calculated as follows.
The tri-peptide molecule of the present invention can suppress the activity of alpha-glucosidase.
The usage and consumption of the alpha-glucosaccharase enzyme inhibition peptide (or referred to as tripeptides CGP) of the present invention are as follows:Orally, every time
2g, 3 times a day.
Embodiment
With reference to specific embodiment, the present invention is described further, but protection scope of the present invention is not limited in
This.
Embodiment 1,
Alpha-glucosaccharase enzyme inhibition activities of the tripeptides CGP under 2.5mg/mL concentration:
Detection method:This tripeptides CGP that will be obtained by chemical synthesis, carries out Activity determination (detection method is ibid).
Now CGP concentration is 2.5mg/mL.
As a result:Alpha-glucosaccharase enzyme inhibition activities of the tripeptides CGP in 2.5mg/mL is 19.3%.
Embodiment 2,
Alpha-glucosaccharase enzyme inhibition activities of the tripeptides CGP under 5.0mg/mL concentration:
Detection method:This tripeptides CGP that will be obtained by chemical synthesis, carries out Activity determination (detection method is ibid).
Now CGP concentration is 5.0mg/mL.
As a result:Alpha-glucosaccharase enzyme inhibition activities of the tripeptides CGP in 5.0mg/mL is 35.9%.
By the inhibition concentration and activity data in embodiment 1 and embodiment 2, illustrate this tripeptides CGP activity and concentration
There is dose-effect relationship, there is this tripeptides structure alpha-glucosaccharase enzyme inhibition activity to have no report, belonging to new has phlorose
Glycosides enzyme inhibition activity Functional Polypeptides.
Comparative example 1, tripeptides PNR (detection method is ibid)
Alpha-glucosaccharase enzyme inhibition activities of the tripeptides PNR in 2.5mg/mL is 1.8%, α-grape in 5.0mg/mL
Glucoside inhibiting activity is 2.3%.
Finally, in addition it is also necessary to it is noted that listed above is only several specific embodiments of the invention.Obviously, this hair
It is bright to be not limited to above example, can also have many deformations, such as the separating obtained CGP structures of different proteins source degraded and
Its derivatization structure.All changes that one of ordinary skill in the art directly can export or associate from present disclosure
Shape, is considered as protection scope of the present invention.
<110>Zhejiang Academy of Agricultural Science
<120>Tripeptides CGP with function of blood sugar reduction and application thereof
<160> 1
<210> 1
<211> 3
<212> PRT
<213>Artificial sequence
<220>
<223>Tripeptides CGP
<400> 1
Cys Gly Pro
Claims (3)
1. tripeptides CGP, it is characterized in that:The amino acid sequence of the tripeptides is:cys-gly-pro.
2. applications of the tripeptides CGP as claimed in claim 1 in hypoglycemic drug is prepared.
3. applications of the tripeptides CGP according to claim 2 in hypoglycemic drug is prepared, it is characterized in that:Prepare as α-
The medicine of Glucosidase inhibitor peptide.
Priority Applications (1)
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CN201710399843.7A CN107011413B (en) | 2017-05-31 | 2017-05-31 | Tripeptide CGP with blood sugar reducing function and application thereof |
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CN201710399843.7A CN107011413B (en) | 2017-05-31 | 2017-05-31 | Tripeptide CGP with blood sugar reducing function and application thereof |
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CN107011413A true CN107011413A (en) | 2017-08-04 |
CN107011413B CN107011413B (en) | 2020-06-16 |
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CN201710399843.7A Active CN107011413B (en) | 2017-05-31 | 2017-05-31 | Tripeptide CGP with blood sugar reducing function and application thereof |
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN109021079A (en) * | 2018-08-31 | 2018-12-18 | 华南理工大学 | A kind of hypoglycemic ten hexapeptide |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1798837A (en) * | 2003-03-31 | 2006-07-05 | 独立行政法人产业技术综合研究所 | Thioredoxin modification |
JP2008161185A (en) * | 2006-12-04 | 2008-07-17 | Locomogene Inc | Decomposition promotion technology of misfolded protein with endoplasmic reticulum reductase |
CN103965287A (en) * | 2014-05-07 | 2014-08-06 | 吉林大学 | Deuterohemin-beta-Ala-His-Lys(DhHP-3), and preparation method and application thereof |
CN103992372A (en) * | 2014-06-05 | 2014-08-20 | 浙江省农业科学院 | Dipeptide GT with function of decreasing blood glucose and application thereof |
-
2017
- 2017-05-31 CN CN201710399843.7A patent/CN107011413B/en active Active
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1798837A (en) * | 2003-03-31 | 2006-07-05 | 独立行政法人产业技术综合研究所 | Thioredoxin modification |
JP2008161185A (en) * | 2006-12-04 | 2008-07-17 | Locomogene Inc | Decomposition promotion technology of misfolded protein with endoplasmic reticulum reductase |
CN103965287A (en) * | 2014-05-07 | 2014-08-06 | 吉林大学 | Deuterohemin-beta-Ala-His-Lys(DhHP-3), and preparation method and application thereof |
CN103992372A (en) * | 2014-06-05 | 2014-08-20 | 浙江省农业科学院 | Dipeptide GT with function of decreasing blood glucose and application thereof |
Non-Patent Citations (1)
Title |
---|
XIAODONG PANG等: "Discovery of a potent peptidic cyclophilin A inhibitor Trp-Gly-Pro", 《EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY》 * |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN109021079A (en) * | 2018-08-31 | 2018-12-18 | 华南理工大学 | A kind of hypoglycemic ten hexapeptide |
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CN107011413B (en) | 2020-06-16 |
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