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Balsam pear hypoglycemic MC-JJ0104 polypeptide analogue by microwave-accelerated solid-phase synthesis and application thereof

A MC-JJ0104, solid-phase synthesis technology, applied in the direction of medical preparations, peptides, drug combinations, etc. The effect of automatic production, low production cost and short synthesis cycle

Inactive Publication Date: 2010-09-15
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 10 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

[0025] Microwave-promoted solid-phase synthesis of Gly-Pro-Ala-Ala-Tyr-Ile-Ser-Ala-Ala-Ser (SEQ.ID NO: 2)

[0026] (1) Swelling of the resin

[0027] Weigh 50mg of Fmoc-Ala 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.

[0028] (2) Microwave promotes removal of Fmoc protecting group

[0029] 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°C, and c...

Embodiment 2

[0044] Gly-Pro-(D-Ala)-Ala-Tyr-Ile-Ser-Ala-Ala-Ser (SEQ.ID NO: 3); Theoretical relative molecular mass 907.0ESI-MSm / z: found[M+3H] 3+ 303.5, [M+4H] 4+ 227.6, [M+5H] 5+ 182.2;calu[M+3H] 3+ 303.3, [M+4H] 4+ 227.7, [M+5H] 5+ 182.4

Embodiment 3

[0046] Gly-Pro-Ala-(D-Ala)-Tyr-Ile-Ser-Ala-Ala-Ser (SEQ.ID NO: 4); Theoretical relative molecular mass 907.0ESI-MSm / z: found[M+3H] 3+ 303.3, [M+4H] 4+ 227.5, [M+5H] 5+ 182.4;calu[M+3H] 3+ 303.3, [M+4H] 4+ 227.7, [M+5H] 5+ 182.4

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PUM

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Abstract

The invention relates to a novel high-efficiency hypoglycemic balsam pear MC-JJ0104 polypeptide analogue and a microwave-accelerated solid-phase synthesis method. The MC-JJ0104 polypeptide analogue with longer pharmacological action time is obtained by modifying the 3, 4, 8 or 9 locus of a natural balsam pear polypeptide. The chemical synthesis of the polypeptide analogue is efficiently and quickly realized by the microwave-accelerated solid-phase synthesis method. The crude product is purified by a preparative scale high-efficiency liquid phase, and the MC-JJ0104 polypeptide analogue is finally obtained through freeze-drying.

Description

technical field [0001] The invention relates to a MC-JJ0104 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
CPCY02P20/55
Inventor 黄文龙金晶钱海张惠斌王敬杰陈巍朱孝云华杰杜阔
Owner CHINA PHARM UNIV
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