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Application of micromolecular polypeptide for inhibiting neuron apoptosis

A technology of small molecule polypeptide and nerve cell apoptosis, which is applied in the field of biomedicine to achieve the effect of reducing the number of nerve cells, increasing the number of surviving nerve cells, and improving motor function and sensory function.

Active Publication Date: 2016-10-12
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although the curative effect is obvious in experimental research, but no drug has been approved in clinical practice.

Method used

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  • Application of micromolecular polypeptide for inhibiting neuron apoptosis
  • Application of micromolecular polypeptide for inhibiting neuron apoptosis
  • Application of micromolecular polypeptide for inhibiting neuron apoptosis

Examples

Experimental program
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Effect test

Embodiment 1

[0019] The preparation of embodiment 1 small molecule polypeptide

[0020] The amino acid sequence of the small molecule polypeptide is shown in SEQ ID NO.1. Small molecule peptide synthesis was performed on an ABI 431A solid-phase peptide synthesizer (PE Company, USA). Methods The standard fluorenylmethoxycarbonyl (Fmoc) protocol was used, and arginine was coupled twice. Initially select 0.125mmol p-hydroxymethylphenoxymethyl polystyrene resin (HMP resin), extend the peptide chain from the carboxyl terminal to the amino terminal one by one according to the polypeptide sequence, the amount of each amino acid is 0.5mmol, and the mole of the resin The ratio is 4:1. The α-amino acids of various amino acids are protected by Fmoc, and the other side chain protection groups are: Ser (tBu), Glu (OtBu), Arg (Pmc). The first amino acid is connected to the resin with 4-lutidine, the amino acid is activated with 1-hydroxybenzotriazole and dicycloethyl carbon, and after coupling, the Fm...

Embodiment 2

[0022] Example 2 Application of Small Molecular Peptides in Treating Cerebral Hemorrhage in Rats

[0023] 1. Animals: Male SD rats, weighing 250-300 grams, were purchased from the Animal Laboratory of Nantong University and kept in a clean animal room.

[0024] 2. Drugs: small molecule polypeptide treatment group: intraperitoneal injection of 20 nmol / kg body weight of small molecule polypeptide shown in SEQ ID NO.1, a total of 6 animals; blank group: intraperitoneal injection of the same volume of PBS as the treatment group, There are 6 in total.

[0025] 3. Experimental method: Injecting autologous blood into the brain is a common animal modeling method for cerebral hemorrhage. This experiment is used to verify the therapeutic effect of small polypeptide molecules on cerebral hemorrhage. Inject the autologous blood method in the brain, be specifically: 1. give rat (240-260g) 10% chloral hydrate and carry out intraperitoneal anesthesia (3ml / Kg); Expose the skull; ③Use a ster...

Embodiment 3

[0040] In order to further utilize in vitro experiments to verify the protection of the present invention to nerve cells and the verification inhibitory effect on macrophages, PC-12 cells (rat adrenal medulla pheochromocytoma cell line) in vitro injury model and LPS-induced macrophage Cellular inflammation model validation.

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Abstract

The invention discloses an application of a micromolecular polypeptide for inhibiting neuron apoptosis. According to the application, the micromolecular polypeptide with an amino acid sequence represented by SEQ ID No. 1 shown in the description is prepared through reforming and synthesizing a Glis2 structure; meanwhile, a rat model with intracerebral hemorrhage is modeled, the synthesized micromolecular polypeptide serves as a therapeutic drug for rat intracerebral hemorrhage, PBS serves as a blank control, the micromolecular polypeptide serves as a treatment group, shown by treatment on intracerebral hemorrhage, after being treated by the micromolecular polypeptide, the kinetism of the rat with intracerebral hemorrhage is recovered, the limb reflecting power is obviously increased, the quantity of macrophage activated and the expression level of inflammatory factors are obviously inhibited, and the quantity of nerve tissue cells subjected to apoptosis is reduced.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a small molecular polypeptide for inhibiting neuron apoptosis and its application. Background technique [0002] Intracerebral hemorrhage (ICH), also known as cerebral hemorrhage, refers to primary non-traumatic intraparenchymal hemorrhage. The incidence rate is 60-80 / 100,000 per year, accounting for about 20%-30% of all strokes in my country. The case fatality rate is 30-40%. About 60% of ICH cases are caused by high blood pressure combined with arteriosclerosis, and about 30% are caused by rupture of aneurysms or arteriovenous malformations. Other etiologies include cerebral atherosclerosis, blood diseases, and cerebral amyloid angiopathy , anticoagulant or thrombolytic therapy. The mortality rate of ICH in our country is about 10.8%, the vegetative state is about 2.6%, the severe disability rate is about 2.2%, and the moderate disability rate is about 7.2%, which seriousl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/17A61P7/04A61P9/10A61P25/00
CPCA61K38/1709
Inventor 沈爱国刘永华谢丽丽柯开富沈加兵
Owner NANTONG UNIVERSITY
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