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Peptides as well as pharmaceutical composition and application thereof

A composition and drug technology, applied in the field of peptides or their pharmaceutically acceptable salts, preparation of pharmaceutical compositions, and new peptides, can solve problems such as difficult folding, cost and production bottlenecks, and limited production

Active Publication Date: 2017-05-10
唐琼瑶 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This structure limits its yield during chemical synthesis and biosynthesis due to difficulty in folding into the correct conformation
Although there are recent patents for directing the synthesis of full-length GsMTx-4 polypeptides in yeast, cost and yield are still bottlenecks in drug development

Method used

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  • Peptides as well as pharmaceutical composition and application thereof
  • Peptides as well as pharmaceutical composition and application thereof
  • Peptides as well as pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0056] 1. Experimental animals, instruments and reagents

[0057] Adult Sprague-Dawley male rats (more than 8 weeks old), weighing 180g-220g, were purchased from Shandong Jinan Pengyue Experimental Animal Breeding Co., Ltd.

[0058] Carrageenan (Carrageenan, abbreviated as Carr) is a product of the U.S. sigma company, and 1% carrageenan is prepared respectively (0.1g carrageenan is dissolved in 10ml 0.9% normal saline solution, and is divided into 10 EP tubes) and 2% carrageenan (0.2g carrageenan dissolved in 10ml 0.9% normal saline solution, distributed to 10 EP tubes), stored at -20°C, taken out half an hour before use and placed on ice.

[0059] GsMTx-4 was purchased from alomone labs in the United States. All peptides from SEQ ID No.1 to SEQ ID No.8 were prepared into 5mM or 10mM mother solutions with high-temperature sterilized deionized water (DD water), and distributed in EP tubes. Store at -80°C and dilute with saline to the concentration required for the experiment w...

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Abstract

The invention provides a group of peptides as well as a pharmaceutical composition and application thereof. The peptides are as shown in sequence tables; the peptides have amino acid sequences with an analgesic effect, or are pharmacologically acceptable salts of the peptides. A ring is formed by two cysteines at the head end and the tail end of each peptide. A pharmacophore (a structural domain) which has abirritation in the GsMTx-4 peptide is determined by comparing multiple inhibitor cystein knot (ICK)-containing peptide sequences such as GsMTx-4 and GsMTX-2 and carrying out behavior test on a rat pain model.

Description

technical field [0001] The invention belongs to the technical field of biomedicine and relates to a group of novel peptides, in particular to peptides with analgesic effect or their pharmaceutically acceptable salts used in medicine. In addition, the present invention also relates to the use of the group of peptides in the preparation of pharmaceutical compositions. Background technique [0002] In 2000, Dr. Frederick Sachs of York State University successfully isolated the polypeptide GsMTx-4 from the venom of a Chilean tarantula (Chileantarantula) (Sachs F, et a., J Gen Physiol.115, Po583-598, 2000). The report pointed out that this is a polypeptide that has a specific inhibitory effect on mechanosensitive ion channels. GsMTx-4 was found to prevent congestive heart failure caused by cellular swelling, especially in the lungs, liver, and legs (Sachs F. et al., JGP 2000). There are also reports that GsMTx-4 can inhibit atrial fibrillation in rabbits without affecting other...

Claims

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Application Information

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IPC IPC(8): C07K7/06C07K7/08A61K38/08A61K38/10A61P29/00
CPCA61K38/00C07K7/06C07K7/08
Inventor 唐琼瑶张赭唐明希董平柯少溪冯验军杜项荣李辉张飞飞
Owner 唐琼瑶
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