CN107011413B - Tripeptide CGP with blood sugar reducing function and application thereof - Google Patents
Tripeptide CGP with blood sugar reducing function and application thereof Download PDFInfo
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- CN107011413B CN107011413B CN201710399843.7A CN201710399843A CN107011413B CN 107011413 B CN107011413 B CN 107011413B CN 201710399843 A CN201710399843 A CN 201710399843A CN 107011413 B CN107011413 B CN 107011413B
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- tripeptide
- cgp
- glucosidase
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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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- 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 tripeptide CGP, the amino acid sequence of which is cys-gly-pro, and the invention also discloses the application of the tripeptide CGP in the preparation of hypoglycemic drugs (especially in the preparation of α -glucosidase inhibitory peptide).
Description
Technical Field
The invention belongs to the technical field of biology, and particularly relates to tripeptide capable of being combined with α -glucosidase and inhibiting the activity of the glucosidase.
Background
One of the main sources of blood sugar is the digestion and absorption of carbohydrates in the small intestine, carbohydrates such as starch are decomposed into monosaccharides by α -glucosidase and absorbed by the small intestine to enter the blood circulation, therefore α -glucosidase plays an important role in the generation of glucose through carbohydrate metabolism, α -glucosidase inhibitor can delay the generation of glucose by inhibiting the activity of α -glucosidase on the chorionic brush border of the epithelium of the small intestine of a human body, and plays an important role in reducing postprandial blood sugar, and α -glucosidase inhibitor is widely applied to the treatment of diabetes at present.
The common drugs for reducing blood sugar are:
① α glucosidase inhibitors, acarbose, voglibose and miglitol.
② insulin promoter such as repaglinide, nateglinide, glimepiride, and gliquidone.
③ insulin sensitizer, such as metformin and thiazolidinediones.
④ insulin and its analogues including insulin, insulin lispro, insulin aspart, and insulin glulisine.
Disclosure of Invention
The invention aims to provide a tripeptide sequence with a blood sugar reducing function and application thereof.
In order to solve the above technical problems, the present invention provides a tripeptide CGP, the amino acid sequence of which is: cys-gly-pro.
The invention also provides the application of the tripeptide CGP in the preparation of hypoglycemic drugs.
As an improvement of the application of the tripeptide CGP, the tripeptide CGP is used for preparing a medicament used as α -glucosidase inhibiting peptide.
The tripeptide CGP of the invention can be used as α -glucosidase inhibition peptide.
The tripeptide CGP of the present invention can be synthesized by trusted blaze biotechnology, Inc.
The tripeptide sequence has an inhibitory activity against α -glucosidase, thereby showing a characteristic of having a hypoglycemic function.
The invention relates to a detection method of α -glucosidase inhibitory activity, which comprises the following steps:
50. mu.L of a polypeptide solution (0.1mol/L, pH 6.9 phosphate buffer) at a given concentration and 100. mu.L of a α -glucosidase solution (0.1mol/L, pH 6.9 phosphate buffer) at 10mg/mL were added to the microplate, mixed well, and then left at 25 ℃ for 10min, 50. mu.L of a 5mmol/L PNPG (p-nitrophenyl- α -D-glucopyranoside) solution (0.1mol/L, pH 6.9 phosphate buffer) was added thereto, and after incubation at 37 ℃ for 30min, 50. mu.L of 0.67mol/L Na was added thereto2CO3The reaction was stopped and absorbance at 405nm was measured. This system is called a sample.
The following 3 systems were set simultaneously: control, sample blank, and control blank.
Comparison: 50. mu.L of the polypeptide solution was replaced with 50. mu.L of 0.1mol/L phosphate buffer pH 6.9.
Sample blank 100. mu.L of 0.1mol/L, pH 6.9 phosphate buffer was used instead of 100. mu.L of 10mg/mL α -glucosidase solution;
control blank the polypeptide solution and α -glucosidase solution were replaced by the corresponding volume amounts of 0.1mol/L phosphate buffer at pH 6.9, respectively, and the inhibition rate was calculated as follows.
The tripeptide molecule of the invention can inhibit the activity of α -glucosidase.
The α -glucosidase inhibitory peptide (or tripeptide CGP for short) of the present invention is administered orally at 2g each time 3 times a day.
Detailed Description
The invention will be further described with reference to specific examples, but the scope of the invention is not limited thereto.
Examples 1,
α -glucosidase inhibitory activity of tripeptide CGP at a concentration of 2.5 mg/mL:
the detection method comprises the following steps: the tripeptide CGP obtained by the chemical synthesis method is subjected to activity detection (the detection method is the same as the above). The CGP concentration at this time was 2.5 mg/mL.
As a result, the α -glucosidase inhibitory activity at 2.5mg/mL of the tripeptide CGP was 19.3%.
Examples 2,
α -glucosidase inhibitory activity of tripeptide CGP at a concentration of 5.0 mg/mL:
the detection method comprises the following steps: the tripeptide CGP obtained by the chemical synthesis method is subjected to activity detection (the detection method is the same as the above). The concentration of CGP at this time was 5.0 mg/mL.
As a result, the α -glucosidase inhibitory activity at 5.0mg/mL of the tripeptide CGP was 35.9%.
The inhibitory concentration and activity data in example 1 and example 2 show that the activity of the tripeptide CGP has an amount-effect relationship with the concentration, and the tripeptide structure with α -glucosidase inhibitory activity is not reported, and belongs to a novel functional peptide with α -glucosidase inhibitory activity.
Comparative example 1 tripeptide PNR (detection methods same as above)
The α -glucosidase inhibitory activity at 2.5mg/mL of the tripeptide PNR is 1.8%, and the α -glucosidase inhibitory activity at 5.0mg/mL is 2.3%.
Finally, it is also noted that the above-mentioned lists merely illustrate a few specific embodiments of the invention. Obviously, the present invention is not limited to the above examples, and many variations are possible, such as the structure of CGP and its derivative structure obtained by degradation and separation of different protein sources. All modifications which can be derived or suggested by a person skilled in the art from the disclosure of the present invention are to be considered within the scope of the invention.
<110> Zhejiang province academy of agricultural sciences
<120> tripeptide CGP with blood sugar reducing function and application thereof
<160>1
<210>1
<211>3
<212>PRT
<213> Artificial sequence
<220>
<223> tripeptide CGP
<400>1
Cys Gly Pro
Claims (2)
1. The application of tripeptide CGP in preparing hypoglycemic drugs is characterized in that: the amino acid sequence of the tripeptide CGP is as follows: cys-gly-pro.
2. The use of the tripeptide CGP as claimed in claim 1 in the preparation of a hypoglycemic medicament, wherein the tripeptide CGP is used as an α -glucosidase inhibitory peptide.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710399843.7A CN107011413B (en) | 2017-05-31 | 2017-05-31 | Tripeptide CGP with blood sugar reducing function and application thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710399843.7A CN107011413B (en) | 2017-05-31 | 2017-05-31 | Tripeptide CGP with blood sugar reducing function and application thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN107011413A CN107011413A (en) | 2017-08-04 |
| CN107011413B true CN107011413B (en) | 2020-06-16 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710399843.7A Active CN107011413B (en) | 2017-05-31 | 2017-05-31 | Tripeptide CGP with blood sugar reducing function and application thereof |
Country Status (1)
| Country | Link |
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Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109021079B (en) * | 2018-08-31 | 2020-12-22 | 华南理工大学 | Blood sugar reducing sixteen-peptide |
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 |
|---|
| Discovery of a potent peptidic cyclophilin A inhibitor Trp-Gly-Pro;Xiaodong Pang等;《European Journal of Medicinal Chemistry》;20110222;第1701-1705页 * |
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| CN107011413A (en) | 2017-08-04 |
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