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Neuropeptide and synthesis method and application thereof

A synthesis method and neuropeptide technology, applied in the field of neuropeptides and their synthesis, can solve problems such as body load, toxic injury, temporary cure, etc., and achieve the effect of facilitating degradation, changing activity and state, and improving social memory defects

Active Publication Date: 2017-06-13
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Currently, the drugs for the treatment of nervous system diseases currently on the market are basically inhibitors of certain receptors. Although these drugs can relieve or treat the disease to a certain extent, they often have the following disadvantages: 1. It has normal physiological functions, and drug inhibition will affect its normal function; 2. Because the target receptors are often not only expressed in a specific area, or there are multiple target receptors, inhibitor drugs will have certain effects. Side effects, serious ones may even lead to the death of the patient; 3. Inhibitor drugs are exogenous small molecules, and removing these molecules will bring a certain load to the body, or even toxic damage; 4. Treat the symptoms but not the root cause, many drugs can only Temporary relief of the condition, must be administered frequently over a long period of time

Method used

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  • Neuropeptide and synthesis method and application thereof
  • Neuropeptide and synthesis method and application thereof
  • Neuropeptide and synthesis method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0043] Embodiment 1 The synthesis of polypeptide (TAT-PBD) of the present invention

[0044] The specific sequence of the polypeptide is: tyrosine-glycine-arginine-lysine-lysine-arginine-arginine-glutamine--arginine-arginine-arginine-histamine Acid-Serine-Threonine-Threonine-Arginine-Valine (YGRKKRRQRRRHSTTRV)

[0045] 1. Main raw materials: Cl resin, amino acid, DIEA (N,N-diisopropylethylamine), DIC (N,N-diisopropylcarbodiimide), HOBT (1-hydroxybenzotriazole) , DMF (dimethylformamide), Piperidine (piperidine), trifluoroacetic acid, ethanedithiol, phenol, thioanisole, methanol, and water.

[0046] 2. Synthesis idea:

[0047] Resin: Cl-Resin

[0048] Route: Solid phase Fmoc(9-fluorenylmethoxycarbonyl)

[0049] Condensation: DIC+HOBT

[0050] To protect: Piperidine

[0051] Instrument: Fully automatic synthesizer

[0052] 3. Specific steps:

[0053] a. Connect the -COOH of the first amino acid (V valine) to Cl-Resin with DIEA, and then block the unreacted functional grou...

Embodiment 2

[0071] Add this product (TAT-PBD) and control polypeptide to the medium of mouse hippocampal neurons cultured in vitro for 20 days to a final concentration of 50 micrograms per milliliter, fix the cells with 4% paraformaldehyde solution one hour later, and carry out Immunostaining, as attached figure 1 As shown, it can be observed that the number of dendritic spines of neurons treated with TAT-PBD was significantly increased.

Embodiment 3

[0073] Acute brain slices of wild-type mice were prepared, and whole-cell electrophysiological recordings were performed in the CA3-CA1 loop of the hippocampus, and TAT-PBD polypeptide (50 mg / ml) was added to the intracellular fluid. The results show (as attached figure 2 shown), compared with the control group, PBD could significantly increase the amplitude of LTP.

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Abstract

The invention discloses a neuropeptide and a synthesis method and application thereof, wherein the neuropeptide has an amino acid sequence shown by SEQIDNO:1. According to the amino acid sequence represented by the SEQIDNO:1, valine is used as a first amino acid,-NH2 of the valine is exposed, then the-NH2 of the valine is condensed with-COOH of second amino acid-arginine to form an amide bond, other amino acids are sequentially connected, and finally tyrosine is to obtain the neuropeptide. Compared with the prior art, the neuropeptide has the following advantages: 1. the neuropeptide product can effectively improve defects of experimental animal social memory, and no adverse reaction is observed; 2. functional areas of the neuropeptide is a sequence on an endogenous protein, and cell rejection reaction may not be caused; 3. a signaling pathway activated by the neuropeptide is a known nervous system specific signaling pathway; 4. the product can effectively change the activity and state of neurons; and 5. the essence of the product is an amino acid sequence, is easy to degrade, and may not cause bodily organ loads.

Description

technical field [0001] The invention relates to a neuropeptide and its synthesis method and application, belonging to the technical field of polypeptides and its synthesis. Background technique [0002] Nervous system diseases mainly refer to diseases that occur in the central nervous system, peripheral nervous system, and autonomic nervous system, and are mainly manifested by dysfunction of sensory, motor, consciousness, and autonomic nerves, also known as neuropathy. The clinical manifestations of diseases that occur at the skeletal muscle and neuromuscular junction are often not easily distinguished from those caused by damage to the nervous system itself, so muscle diseases are often discussed together with neuropathy. A disease in which the central nervous system is affected by pathogenic factors (especially when the organic disease of the nervous system cannot be detected) and the main manifestation is mental activity disorder is called psychosis. As the saying goes, ...

Claims

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Application Information

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IPC IPC(8): C07K7/08C07K1/08C07K1/06C07K1/04A61K38/10A61P25/28A61P25/00A61P25/18
CPCA61K38/00C07K7/083Y02P20/55
Inventor 刘安周子凯谢维
Owner SOUTHEAST UNIV
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