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Tripeptide with double-target hypoglycemic function and application thereof

A dual-target, hypoglycemic technology, applied in tripeptide components, peptides, metabolic diseases, etc., can solve the problems of poor patient compliance and increase costs, and achieve the effects of reducing hyperglycemia, inhibiting degradation, and promoting insulin secretion.

Pending Publication Date: 2022-04-15
SOUTH CHINA UNIV OF TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the combined use of drugs not only increases the cost, but also has poor patient compliance (Shan Ling; Lu Li; Li Yanbin; Yang Rong, Clinical efficacy of dipeptidyl peptidase 4 inhibitors combined with metformin in the treatment of type 2 diabetes. Practical Medicine and Clinic 2016, 19, (09), 1094-1097.)

Method used

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  • Tripeptide with double-target hypoglycemic function and application thereof
  • Tripeptide with double-target hypoglycemic function and application thereof
  • Tripeptide with double-target hypoglycemic function and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: DPP-IV inhibitory activity of tripeptide 1 (its sequence is as shown in SEQ ID NO.1 IPQ) with dual target hypoglycemic function

[0029] The DPP-IV inhibitory activity assay method is as follows: In a 96-well plate, add 80 μL of sample (tripeptide 1 with dual-target hypoglycemic function, sequence shown in SEQ ID NO.1) and 80 μL of 0.5 mM substrate Gly-Pro -pNA, mix well, place in a microplate reader and incubate at 37°C for 10min, add 40μL of DPP-IV enzyme solution with a concentration of 12.5mU / mL (preheated at 37°C for 3min), shake for 30s, and read at 405nm, Read every 2 minutes for a total of 120 minutes to monitor the release of pNA. The same volume of 100mM pH 8.0 Tris-HCl buffer was used as the control group instead of the sample. The above reagents or samples are prepared or diluted with the Tris-HCl buffer solution. Plot the absorbance value (as the ordinate) versus time (as the abscissa), in the linear range (R 2 >0.995) to obtain the slope of t...

Embodiment 2

[0032] Example 2: DPP-IV inhibitory activity of tripeptide 2 (its sequence is as shown in SEQ ID NO.2 LPQ) with dual-target hypoglycemic function

[0033] The DPP-IV inhibitory activity assay method is as follows: In a 96-well plate, add 80 μL of sample (tripeptide 2 with dual-target hypoglycemic function, sequence shown in SEQ ID NO.2) and 80 μL of 0.5 mM substrate Gly-Pro -pNA, mix well, place in a microplate reader and incubate at 37°C for 10min, add 40μL of 12.5mU / mL DPP-IV enzyme solution (preheated at 37°C for 3min), shake for 30s, and read at 405nm, every Read once every 2 minutes for a total of 120 minutes to monitor the release of pNA. The same volume of 100mM pH 8.0 Tris-HCl buffer was used as the control group instead of the sample. The above reagents or samples are prepared or diluted with the Tris-HCl buffer solution. Plot the absorbance value (as the ordinate) versus time (as the abscissa), in the linear range (R 2 >0.995) to obtain the slope of the curve, and...

Embodiment 3

[0036] Example 3: DPP-IV inhibitory activity of tripeptide 3 (its sequence is VPQ as shown in SEQ ID NO.3) with dual-target hypoglycemic function

[0037] The DPP-IV inhibitory activity assay method is as follows: In a 96-well plate, add 80 μL of sample (tripeptide 3 with dual-target hypoglycemic function, sequence shown in SEQ ID NO.3) and 80 μL of 0.5 mM substrate Gly-Pro -pNA, mix well, place in a microplate reader and incubate at 37°C for 10min, add 40μL of 12.5mU / mL DPP-IV enzyme solution (preheated at 37°C for 3min), shake for 30s, and read at 405nm, every Read once every 2 minutes for a total of 120 minutes to monitor the release of pNA. The same volume of 100mM pH 8.0 Tris-HCl buffer was used as the control group instead of the sample. The above reagents or samples are prepared or diluted with the Tris-HCl buffer solution. Plot the absorbance value (as the ordinate) versus time (as the abscissa), in the linear range (R 2 >0.995) to obtain the slope of the curve, and...

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Abstract

The invention discloses a tripeptide with a double-target hypoglycemic function and application of the tripeptide. The tripeptide of the type has the sequence characteristic of Xaa1-Pro-Xaa2. Wherein Xaa1 comprises one of three amino acids, namely Val, Leu and Ile; and Xaa2 comprises one of two amino acids, namely Asn and Gln. The tripeptide with the double-target hypoglycemic function provided by the invention not only has relatively strong DPP-IV inhibitory activity, but also has relatively strong activity of promoting liver glucose consumption, and the medicine prepared from the tripeptide with the double-target hypoglycemic function can effectively treat and prevent type 2 diabetes mellitus through the two targets.

Description

technical field [0001] The invention relates to the field of medicine and medicine, in particular to the field of prevention and treatment of type 2 diabetes, and in particular to a class of tripeptides with dual-target hypoglycemic functions and applications thereof. Background technique [0002] The incidence of diabetes is increasing year by year, and it has become the third chronic disease that seriously threatens human health. Clinical drugs are often accompanied by side effects such as weight gain, hypoglycemia, and gastrointestinal adverse reactions, and their long-term safety needs to be further confirmed. The active peptide is safe, easy to absorb, and has no side effects. It is an excellent candidate substance for the development of hypoglycemic functional products. [0003] Dipeptidyl peptidase-IV (dipeptidyl peptidase IV, DPP-IV) inhibitor is one of the new targets for the treatment of type 2 diabetes. Endogenous incretin hormones can promote the secretion of i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/083A61K38/06A61P3/10
Inventor 赵谋明王晨阳郑淋胡一心苏国万
Owner SOUTH CHINA UNIV OF TECH
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