Selenium-containing active polypeptide, preparing method and application thereof

An active polypeptide and an active technology, which is applied in the application field of the polypeptide in the preparation of drugs, can solve the problems of disulfide bond breakage or mismatch, high cost, difficult process, etc., improve the correct folding rate and reduce the dosage , good effect of peptide stability

Active Publication Date: 2013-10-16
SHENZHEN NEPTUNUS PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The ω-MVIIA that has been on the market in the United States is produced by chemical synthesis of peptides. Since the three pairs of cysteines need to be paired correctly to form an active final product, the synthesis steps are many, the process is difficult, and the cost is high.
[0009] In addition, because it has 3 pairs of disulfide bonds, ω-MVIIA will be extremely unstable when encountering reducing conditions such as glutathione, thioredoxin, and protein disulfide bond isomerase in the body, and disulfide bond breaks may occur Or mismatch, resulting in higher-order structure changes, decreased activity or even complete loss, and peptide chains that lose higher-order structures are more likely to be degraded by other proteases in the body

Method used

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  • Selenium-containing active polypeptide, preparing method and application thereof
  • Selenium-containing active polypeptide, preparing method and application thereof
  • Selenium-containing active polypeptide, preparing method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] [Example 1] [Sec 1，16 ] Synthesis of MVIIA (Pseudo-ω-MVIIA Peptide A)

[0052] (1) Solid phase synthesis: According to the pseudo ω-MVIIA peptide [Sec 1，16 ] MVIIA amino acid sequence, using Boc solid-phase chemical synthesis method, using HBTU as coupling reagent and Boc-amino acid (Sigma), MBHA (4-methylbenzhy-drylamine) resin (Advanced Technology & Industrial company) to carry out artificial synthesis. Synthesis of Boc-Sec(MeBzl)-OH: 5g of selenocysteine ​​(Sigma) was added to 20ml of 1M NaOH solution, stirred at 0°C, and 20ml of 0.8M sodium borohydride solution was added at the same time for about 40 minutes. Adjust the pH to 7.0 with glacial acetic acid. Dissolve 1.5g of α-bromoxylene in 20ml of ethanol, add dropwise to the previous reaction solution, and react at 0°C for 2.5 hours. Adjust the pH to 2 with 6M hydrochloric acid to obtain 4-benzyl-L-selenocysteine ​​as a white precipitate. 4-Benzyl-L-selenocysteine ​​4g with K 2 CO 3 Mix 4.5g and dissolve in 30...

Embodiment 2

[0054] [Example 2] Synthetic [Sec 8，20 ], [Sec 15，25 ], [Sec 1，16，8，20 ], [Sec 1，16，15，25 ], [Sec 8，20，15，25 ], [Sec 1，16，8，20，15，25 ] MVIIA (pseudo-omega-MVIIA peptides B, C, D, E, F, G)

[0055] According to the pseudo ω-MVIIA peptide [Sec 8，20 ], [Sec 15，25 ], [Sec 1，16，8，20 ], [Sec 1，16，15，25 ], [Sec 8，20，15，25 ], [Sec 1，16，8，20，15，25 ] MVIIA sequence, prepare the pseudo ω-MVIIA peptide according to the steps of synthesis, bond formation and folding described in Example 1.

Embodiment 3

[0056] [Example 3] Pseudo-ω-MVIIA peptide molecular weight determination

[0057] The quasi-ω-MVIIA peptide was purified and freeze-dried, and the molecular weight was determined by Bruker BIFLEX MALDI-TOF-MS. The results showed that the pseudo ω-MVIIA peptide ([Sec 1，16 ] MVIIA, [Sec 8，20 ] MVIIA, [Sec 15，25 ]MVIIA) has a molecular weight of 2732.61Da, which is consistent with the theoretical molecular weight of 2733.02Da. It suggested that two of the six cysteines constituting ω-MVIIA were replaced by selenocysteine.

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Abstract

The invention relates to a selenocysteine-containing active polypeptide, a synthesizing method and the application thereof in preparing analgesic drugs. The selenocysteine-containing active polypeptide has an SEQ ID NO. 1-8 amino acid sequence, is prepared by a polypeptide solid-phase chemical synthesis method, has stable quality, lower cost, very strong analgesic activity and structure stability and has good development prospect when being used as a non-addiction type analgesic drug.

Description

technical field [0001] The invention relates to a kind of selenium-containing active polypeptide and its preparation method, as well as the application of the polypeptide in medicine preparation. Background technique [0002] Cono snail is a general term for a class of marine animals belonging to the Mollusca family Conidae. As an ocean "snail", it moves slowly and hunts food mainly by the paralysis of venom to conquer the prey. Cono snails have well-evolved venomous organs, the liquid glands behind the radula sac can secrete venom. When necessary, the venom is ejected from the snout, causing the prey to quickly lose the resistance function. [0003] The study of cone snail venom began in the 1950s. In the early 1960s, a study on the toxicity of 37 kinds of cone snail venoms to humans was carried out. In the 1970s, it was found that the lethal component of the venom of the ground cone snail and the weaving cone snail was protein, and was published in 1977. Three pure polyp...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/00C07K1/04C07K1/14A61K38/16A61P25/04A61P29/00
Inventor 吴筱昆王兵朱丹张丽娟赵金华冯汉林于琳徐安龙
Owner SHENZHEN NEPTUNUS PHARM CO LTD
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