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Preparation method of medicine RIP1183 for resisting multi-drug resistance staphylococcia

A technology for RIP1183 and Staphylococcus infection, applied in the biological field, can solve the problems of unfavorable industrial production, low product purity, and poor quality controllability, and achieve the effects of shortening the production cycle, high product purity, and short reaction time

Active Publication Date: 2017-09-22
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are many shortcomings in the previous preparation methods, such as unstable process, low yield, poor quality controllability, low product purity, long production cycle, which is not conducive to industrial production; hydrogen fluoride is used in the preparation process, causing environmental damage serious pollution, etc.

Method used

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  • Preparation method of medicine RIP1183 for resisting multi-drug resistance staphylococcia
  • Preparation method of medicine RIP1183 for resisting multi-drug resistance staphylococcia
  • Preparation method of medicine RIP1183 for resisting multi-drug resistance staphylococcia

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Experimental program
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Effect test

preparation example Construction

[0053] Two, the preparation method of RIP1183

[0054] The method for synthesizing RIP1183 peptide of the solid-phase polypeptide of the present invention comprises the following steps:

[0055] Using any one of Rink Amide MBHA Resin, MBHA Resin, and Rink Amide-AM Resin as the starting material, according to the solid-phase synthesis method, according to the amino acid sequence of RIP1183, connect the corresponding amino acids with Fmoc protection sequentially, during which Remove the Fmoc protecting group in turn, and use one of DIEA / HOBt or DIEA or TBTU / HOAt / HOBt or HBTU / HOBt or HBTU / HOAt or HATU / HOBt or HATU / HOAt or HCTU / HOBt as a condensing agent for peptide grafting After the reaction, the corresponding RIP1183 resin was obtained, and the side chain protection group was removed and the final peptide was cut synchronously to obtain the crude product of RIP1183, which was subjected to C 18 or C 8 The chromatographic column was used for separation and purification to obtai...

Embodiment 1

[0094] Example 1 RIP1183 synthesis process of 1g grade Rink Amide MBHA Resin resin:

[0095] (1) Preparation of Fmoe-Phe-MBHA Resin

[0096] Weigh 1g of Rink Amide MBHA Resin (Gill Biochemical (Shanghai) Co., Ltd.; sample loading: 1.0mmol / g) and pour it into the reaction column, add about 10ml of DMF, soak for 30 minutes (at room temperature) and dry it with a vacuum pump, add the decapping reagent ( 20% piperidine solution in DMF) at 10-50°C for 5-30 minutes, drained with a vacuum pump, re-adding capping reagent at 10-50°C for 10-60 minutes, drained, washed twice with isopropanol, then washed with DMF 2 times, ninhydrin test was positive, drained, added Fmoc-Phe-OH 0.54g, TBTU0.45g, DMF 10ml, HOBt 1ml, DIEA 0.4ml, reacted at room temperature for 2 hours, ninhydrin test was negative, resin Wash twice with isopropanol, twice with DMF, and dry to obtain Fmoc-Phe-MBHA Resin;

[0097] (2) Preparation of Fmoc-Asn(Trt)-Phe-MBHA Resin

[0098] In the Fmoe-Phe-MBHA Resin of step (1...

Embodiment 2

[0114] Example 2 The synthesis process of RIP1183 in pilot scale (taking 20150601 batches as an example)

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Abstract

Disclosed is a preparation method of medicine RIP1183 for resisting multi-drug resistance staphylococcia. Any one of Rink, AmideMBHA Resin, MBHA Resin and Rink Amide-AM Resin is adopted as a starting raw material, on the basis of a solid-phase synthesis method, according to a RIP1183 amino acid sequence, corresponding amino acids with Fmoc protection are connected in sequence, Fmoc protecting groups are removed in sequence in the process, one of DIEA / HOBt or DIEA or TBTU / HOAt / HOBt or HBTU / HOBt or HBTU / HOAt or HATU / HOBt or HATU / HOAt or HCTU / HOBt is adopted as a condensing agent for performing a transpeptidase reaction, aftr corresponding RIP1183 resin is obtained, meanwhile, side chain removal protecting groups and final peptide cut-off are performed, a crude RIP1103 product is obtained, and separation and purification are performed through a C18 or C8 chromatographic column to obtain the needed purified RIP1183 product.

Description

technical field [0001] The invention belongs to the field of biotechnology, and relates to a preparation method of polypeptide RIP1183, an anti-multidrug-resistant staphylococcus infection drug, and is especially suitable for large-scale production. Background technique [0002] RNAIII inhibitory peptide (RNAIII inhibiting pepnde, abbreviated RIP) is an effective inhibitor of the quorum sensing mechanism of staphylococcus discovered in recent years, which can block the signal transduction pathway between staphylococcus cells, thereby inhibiting the formation of biofilm of staphylococcus and preventing staphylococcus Infect. Natural RNAIII inhibitory peptides are produced by coagulase-negative staphylococcus strains, while artificial preparation of such peptides mostly uses solid-state synthesis methods. However, there are many shortcomings in the previous preparation methods, such as unstable process, low yield, poor quality controllability, low product purity, long product...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/31C07K1/06C07K1/04A61P31/04
CPCC07K14/31Y02P20/55
Inventor 罗晓星王增禄李明凯周颖侯征张英起王春娟
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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