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Balsam pear MC-JJ2163 polypeptide analogs by microwave-enhanced solid-phase synthesis and application thereof

A technology of MC-JJ2163 and analogs, which is applied in the field of MC-JJ2163 polypeptide analogs and their microwave-promoted solid-phase synthesis, can solve the problems of inability to synthesize target polypeptides, loss of the meaning of synthesis, and long synthesis cycle, and achieve easy industrial automation. The effect of low production, production cost and short synthesis cycle

Inactive Publication Date: 2010-07-21
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

[0046] Gly-Ala-Pro-Tyr-Tyr-Ser-Ile-Lys-Lys-Ser-Lys-Thr-(D-Ala)-Met-Lys-His-Met-Ala-Gly-Ala-Ala (SEQ.ID NO : 2) Microwave-promoted solid-phase synthesis

[0047] (1) Swelling of the resin

[0048] 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.

[0049] (2) Microwave promotes removal of Fmoc protecting group

[0050] 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 25...

Embodiment 2~51

[0064] According to the method described in Example 1, the polypeptides of Examples 2-50 were synthesized according to the corresponding sequences, and their respective molecular weights were confirmed by electrospray mass spectrometry (ESI-MS).

Embodiment 2

[0066] Gly-His-Pro-Ala-Tyr-Ser-Ile-Lys-Lys-Ser-Lys-Thr-(D-Ala)-Met-Lys-His-Met-Ala-Gly-Ala-Ala (SEQ.ID NO : 3); Theoretical relative molecular mass 2185.6.ESI-MSm / z: found[M+3H] 3+ 729.5, [M+4H] 4+ 547.4, [M+5H] 5+ 438.1;calu[M+3H] 3+ 729.4, [M+4H] 4+ 547.4, [M+5H] 5+ 438.0;

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PUM

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Abstract

The invention relates to novel high-efficiency blood sugar-reducing balsam pear MC-JJ2163 polypeptide analogs and a microwave-enhanced solid-phase synthesis method thereof. The MC-JJ2163 polypeptide analogs with longer pharmacological action time are obtained by modifying 2, 4, 5, 8 or 9 position of natural balsam pear polypeptides. The chemical synthesis of the balsam pear MC-JJ2163 polypeptide analogs is realized efficiently and quickly through the microwave-enhanced solid-phase synthesis method; coarse products are purified through a preparative high performance liquid phase; and finally the MC-JJ2163 polypeptide analogs are obtained by freeze-drying.

Description

technical field [0001] The invention relates to a MC-JJ2163 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): C07K14/415A61K38/16A61P3/10C07K1/06C07K1/04
Inventor 黄文龙金晶张惠斌钱海王敬杰陈巍陈鑫纪剑峰华杰
Owner CHINA PHARM UNIV
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