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Microwave irradiation solid phase synthesis of balsam pear hypoglycemic MC-JJ0108 polypeptide analogue and application thereof

A MC-JJ0108, solid-phase synthesis technology, applied in the fields of peptides, drug combinations, peptide preparation methods, etc., can solve the problems of inability to synthesize target peptides, loss of synthetic significance, long synthesis cycle, etc., to achieve easy industrial automation production, The effect of low production cost and short synthesis cycle

Inactive Publication Date: 2011-04-06
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Using the traditional solid-phase method to synthesize long peptides, the yield is often very low and the impurities are more difficult to purify, thus losing the meaning of synthesis from a practical point of view
Secondly, the synthesis cycle is long. In the case of no difficult peptide sequence in the middle, it usually takes nearly a week to complete the synthesis cycle of 30 peptides. If there is a difficult peptide sequence, it is often impossible to synthesize the target peptide.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Microwave-promoted solid-phase synthesis of Ala-Pro-Ala-Ala-Ile-Ser-Lys-Ala-Ser (SEQ.ID NO: 2)

[0027] (1) Swelling of the resin

[0028] Weigh 50mg of Fmoc-rink amide-MBHA Resin (substitution amount 0.4mmol / g), swell with 7mL DCM for 30min, filter to remove DCM, then swell with 10mL NMP for 30min, and finally rinse with NMP, DCM, and NMP 7mL respectively.

[0029] (2) Microwave promotes removal of Fmoc protecting group

[0030] Put the swollen resin into the reactor, add 7mL of 25% piperidine / NMP (V / V) solution containing 0.1M HOBT, react in the microwave reactor for 1min, the microwave power is 15W, and the reaction temperature is controlled at 50°C Within the time period, use an air compressor to compress the air to cool, and filter the solution after the reaction; add 7 mL of 25% piperidine / NMP (V / V) solution containing 0.1M HOBT and react in a microwave reactor for another 4 minutes, and the microwave power is 25W , the reaction temperature was controlled at 50°...

Embodiment 2

[0045] Ala-Pro-Ala-Cys-Ile-Ser-Lys-Ala-Ser (SEQ.ID NO: 3); Theoretical relative molecular mass 847.0

[0046] ESI-MSm / z: found[M+3H] 3+ 283.4, [M+4H] 4+ 212.7, [M+5H] 5+ 170.3;calu[M+3H] 3+ 283.3, [M+4H] 4+ 212.7, [M+5H] 5+ 170.4

Embodiment 3

[0048] Ala-Pro-Ala-Gly-Ile-Ser-Lys-Ala-Ser (SEQ.ID NO: 4); Theoretical relative molecular mass 800.9

[0049] ESI-MSm / z: found[M+3H] 3+ 268.1, [M+4H] 4+ 201.1, [M+5H] 5+ 161.2;calu[M+3H] 3+ 268.0, [M+4H] 4+ 201.2, [M+5H] 5+ 161.2

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PUM

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Abstract

The invention relates to a novel efficient hypoglycemic balsam pear MC-JJ0108 polypeptide analogue and a microwave irradiation solid phase synthesis method thereof. Locus 1,3,4,7 or 8 of natural balsam pear polypeptide is modified so as to obtain the MC-JJ0108 polypeptide analogue with longer pharmacological action time; and chemical synthesis is realized efficiently and rapidly by a microwave irradiation solid phase synthesis method. A crude product is subject to high-performance liquid purification and is freeze-dried so as to obtain the MC-JJ0108 polypeptide analogue.

Description

technical field [0001] The invention relates to a MC-JJ0108 polypeptide analog and a microwave-promoted solid-phase synthesis method thereof. Background technique [0002] Diabetes is an important disease that endangers human health today. At present, about 5%-7% of people in the world suffer from diabetes. It is considered to be the third largest killer of human disability and death after cardiovascular and cerebrovascular diseases and malignant tumors. . [0003] Diabetes is divided into type I and type II. Type I diabetes is an autoimmune disease that requires insulin injections for survival. Type II diabetes accounts for about 95% of the total number of diabetic patients. Type II diabetes is caused by metabolic disorders of islet cells, insufficient insulin secretion, or insulin resistance, which is a metabolic disease caused by insulin resistance mainly accompanied by relatively insufficient insulin secretion, or relatively insufficient insulin secretion accompanied b...

Claims

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Application Information

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IPC IPC(8): C07K7/06C07K1/20C07K1/08C07K1/06C07K1/04A61K38/08A61P3/10
Inventor 黄文龙金晶钱海张惠斌王敬杰陈巍杜阔
Owner CHINA PHARM UNIV
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