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Anti-thrombocyte tetratitanate-NB06 and its application

An anti-platelet, peptide compound technology, applied in the field of medicine and biology, can solve problems such as no reports, and achieve the effect of improving anti-platelet aggregation activity and stability

Inactive Publication Date: 2007-10-03
牛勃
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The new tetrapeptide sequence structure involved in the present invention has not been reported so far

Method used

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  • Anti-thrombocyte tetratitanate-NB06 and its application
  • Anti-thrombocyte tetratitanate-NB06 and its application
  • Anti-thrombocyte tetratitanate-NB06 and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] : The solid-phase synthesis of NB06

[0021] Weigh 76mg of Rink Amide MBHA resin (0.55mM / g load), swell with dichloromethane in the polypeptide reaction bottle for 1 hour, remove the dichloromethane by suction filtration; add 5 ml of 20% pyridine / dimethylformamide , shake and mix at room temperature for 10 minutes to remove the Fmoe protective group; remove the deprotection solution by suction filtration, and repeat the deprotection once; weigh 5 times excess Fmoc-protected tryptophan and dissolve it in 1ml (or 0.5ml) of 2M DIEA , add a 5-fold excess of 0.5M HBTU / HoBT, mix well, and activate at room temperature for 10 minutes; transfer the activated protected amino acid to the reactor, oscillate and mix well, and react at room temperature for 60 minutes, then remove the liquid under negative pressure; add dichloromethane 4ml, shake and mix for 30 seconds, remove the washing liquid under negative pressure, and repeat the washing for 7 times; take a small amount of peptid...

Embodiment 2

[0022] : Solid phase synthesis of peptide-resin cleavage

[0023] Take the peptide-resin obtained in Example 1, add 2 ml of lysis solution (95% trifluoroacetic acid, 2.5% water, 2.5% triisopropylsilane), stir and react at room temperature for two hours; then suck out the cutting solution and use A small amount of TFA was used to wash the resin in the reaction bottle, and the TFA was filtered out and incorporated into the cutting solution; the filtered cutting solution was sucked dry under negative pressure, and precipitated with ice ether, separated and dissolved in 1ml of water.

Embodiment 3

[0024] : Purification of NB06

[0025] Take a small amount of dissolved cleavage product, carry out high-pressure liquid chromatography, determine the retention time of the product, and separate the product. The conditions for reverse-phase high-pressure liquid phase purification are: C8 column (3.9 × 150mm, waters company), mobile phase A: 0.1% TFA / H 2 O, B: 0.1% TFA / acetonitrile, gradient elution, flow rate 1ml / mm, monitoring the absorption peak at 214nm. The result is shown in Figure 1: there are two main elution peaks, respectively the elution peak (recorded as P1) of 17.422 minutes and the elution peak (recorded as P2) of 17.712 minutes; Wherein P1 is the target compound, and its peak area is about 40% of the total area. The eluted peak of P1 was collected and vacuum freeze-dried to obtain purified NB06.

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PUM

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Abstract

This invention relates to a new thrombocyte anti-aggregation tetrapeptide - NB06, its amino acid sequence is omega - aminocaprylic acid - glycine - aspartic acid - tryptophyl amine peptide. The amidated carboxyl terminal could enlarge top space of 'V' type peptide, thereby enhance biology activity of object compound, along with it advance its ability of resisting hydrolization, establish good foundation for its using in preparing drugs for thrombocyte anti-aggregation and cerebrovascular disease treatment.

Description

Technical field: [0001] The invention relates to a novel linear tetrapeptide compound with anti-platelet aggregation effect in the field of medical biotechnology. Background technique: [0002] Thrombosis, tumor metastasis and bone destruction and absorption have seriously affected human health for a long time. In recent years, with the continuous improvement of the theory of cell-cell interaction—the theory of cell adhesion, the adhesion and transport between cells and between cells and extracellular matrix are considered to be the main link in the occurrence of the above diseases. Further studies have found that the combination of a tripeptide sequence RGD (Arg-Gly-Asp) and its corresponding ligand is an essential part of cell interaction, and research on blocking this link will have a significant impact on the pathogenesis and clinical treatment of the above diseases. It has important theoretical and practical significance. [0003] The RGD sequence on the fibrinogen α ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/10A61K38/07A61P9/00A61P7/02
Inventor 牛勃王国亮罗佳王建华冯倩佳李乐意李乐工韩锐
Owner 牛勃
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