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Mycophenolic acid-xenopus laevis glucagon like peptide-1 conjugated peptide and application thereof

A technology of glucagon and Xenopus laevis, applied in the direction of glucagon, hormone peptides, specific peptides, etc., can solve the problems of short half-life and limited application of GLP-1

Inactive Publication Date: 2018-05-04
XUZHOU NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, dipeptidyl peptidase (dipeptidyl-peptidase, DPP-IV) and neutral endopeptidase (neutralendopeptidase, NEP) in the human body will rapidly degrade GLP-1, resulting in a very short half-life of GLP-1 in vivo (1 ~ 2min ), which limits its clinical application

Method used

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  • Mycophenolic acid-xenopus laevis glucagon like peptide-1 conjugated peptide and application thereof
  • Mycophenolic acid-xenopus laevis glucagon like peptide-1 conjugated peptide and application thereof
  • Mycophenolic acid-xenopus laevis glucagon like peptide-1 conjugated peptide and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034]

[0035] (1) Swelling of the resin

[0036]Weigh 0.262g (0.1mmol) of Rink Amide MBHA resin with a loading capacity of 0.382mmol / g, put it into a 25mL reactor, wash the resin once with 7mL of DCM and methanol alternately, and wash the resin twice with 7mL of DCM, The resin was then swollen with 7 mL of DCM for 1 h, and finally the resin was washed 3 times with 7 mL of DMF.

[0037] (2) Removal of resin Fmoc protecting group

[0038] Transfer the swollen resin to a peptide synthesizer, add 7mL 20% piperidine / DMF to react at room temperature for 5min, filter off the deprotection solution, wash the resin once with 7mL DMF, then add 7mL 20%piperidine / DMF to deprotect and wash the resin for 15min, Finally, the resin was washed 4 times with 7 mL of DMF, 1.5 min each time, to obtain the Rink resin from which the Fmoc protecting group was removed.

[0039] (3) Synthesis of Fmoc-Lys-Rink amide-MBHA Resin

[0040] Weigh Fmoc-Lys(Boc)-OH (0.4mmol), dissolve it with 3mL 10% DM...

Embodiment 2～6

[0050] According to the method described in Example 1, the XenGLP-1 derivatives of Examples 2-6 were synthesized according to the corresponding sequences and side chains, and their respective molecular weights were confirmed by ESI-MS.

Embodiment 2

[0052]

[0053] The theoretical relative molecular mass is 4129.2. ESI-MS m / z:calu[M+3H] 3+ 1377.4,[M+4H] 4+ 1033.3;found[M+3H] 3+ 1377.8,[M+4H] 4+ 1033.6.

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Abstract

The invention relates to a mycophenolic acid-xenopus laevis glucagon like peptide-1 (XenGLP-1) conjugated peptide and application thereof. The preparation method comprises the following steps: performing structural modification on side chains of XenGLP-1, and introducing mycophenolic acid small-molecule derivatives with a high binding rate of serum protein, thereby obtaining the XenGLP-1 conjugated peptide with high hypoglycemic activity and long pharmacological action time. The XenGLP-1 conjugated peptide disclosed by the invention has the effect of obviously improving the biological activity, and has excellent effects of reducing blood glucose and losing weight for a long time.

Description

technical field [0001] The invention relates to a class of Xenopus glucagon-like peptide-1 (XenGLP-1) derivatives and applications thereof Background technique [0002] Diabetes mellitus (Diabetes Mellitus) is a metabolic disease characterized by hyperglycemia due to defects in insulin secretion or insulin action. According to the International Diabetes Federation (IDF), there are currently 387 million diabetics worldwide. The number of people with diabetes is expected to increase by 55% to 600 million by 2035. Among them, type 2 diabetes accounts for 85% to 95%, which is the main type of diabetes. The main pathogenesis of type 2 diabetes involves islet β cell dysfunction and peripheral insulin resistance. [0003] Glucagon-Like Peptide-1 (GLP-1) is an incretin hormone secreted by the human body and transcribed from the proglucagon gene. It is secreted by intestinal L cells, and its synthetic secretion is induced by feeding stimulation. GLP-1 activates intracellular aden...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/605A61K38/26A61P3/04A61P3/10
CPCA61K38/00C07K14/605
Inventor 费颖颖韩京傅俊杰周凤张莹
Owner XUZHOU NORMAL UNIVERSITY
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