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Application of pentapeptide KLPGF in inhibiting AChE activity

A technology for inhibiting activity and active peptides, which is applied in the application field of pentapeptide KLPGF inhibiting AChE activity, and can solve the problems of complex pathogenesis and adverse reactions.

Inactive Publication Date: 2018-05-18
BOHAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These chemically synthesized inhibitors slow disease progression but cause some adverse effects
At the same time, in view of the complexity of the pathogenesis of senile dementia, the etiological mechanism has not been fully elucidated, therefore, it is one of the main trends of current research to find multi-target molecules with high efficiency, low toxicity and no side effects

Method used

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  • Application of pentapeptide KLPGF in inhibiting AChE activity
  • Application of pentapeptide KLPGF in inhibiting AChE activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] The measurement of AChE, BChE inhibitory activity of egg white active peptide in vitro of embodiment 1

[0018] 140 μL of sodium phosphate buffer (pH 8.0), 20 μL of test sample solution (50 μg / mL) and 20 μL of ChE / BChE solution were mixed and incubated at room temperature for 15 minutes. Then 10 μL DTNB and 10 μL Ch / BCh were added to the mixture. The absorbance value of each group was detected (20min) by a microplate reader at 412nm.

[0019] Inhibition rate%=(Abs control-Abs sample) / Abs control×100%

[0020] where Abs represents the absorption value.

[0021] The results showed that the peptide KLPGF has good anti-senile dementia activity. When its concentration is 50 μg / mL, the inhibition rate to AChE is 61.23%, and the inhibition rate to BChE is 3.29%.

Embodiment 2

[0022] Example 2 Molecular docking

[0023] The crystal structure (1EVE) of AChE was obtained from the PDB database, and it was set as a receptor protein by means of DS, and the active center position was (2.855796, 64.576950, 67.98141). The peptide sequence with the highest activity in step 1 was docked with AChE by CDOCKER, and the parameters were set as follows: Top Hit 10, Pose Cluster Radius 0.1.

[0024] The results showed that the peptide KLPGF could tightly bind to AChE, and the interaction between KLPGF and AChE involved Tyr70-Trp84-Gly118-Gly119-Trp279-Asp285-Ser286-Ile287-Phe330-Phe331-Tyr334-His440-Gly441 amino acid residues. It has strong interaction with the catalytic site of AChE (Tyr70, Trp84, Gly118, Gly119, Trp279, Tyr334, His440). The results of the interaction between peptide KLPGF and AChE are as follows figure 1 shown.

Embodiment 3

[0025] Example 3 Toxicity Prediction

[0026] The potential toxicity of the peptide was predicted by ToxinPred, and SVM score <0 indicated no toxicity. The measurement results are shown in Table 1, and the results showed that the SVM score of the peptide KLPGF was <0, indicating no toxicity.

[0027] Table 1 Toxicity prediction results of egg white peptides

[0028]

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Abstract

The invention discloses an application of pentapeptide KLPGF in inhibiting AChE activity. The amino acid sequence of AChE inhibiting peptide is Lys-Leu-Ro-Gly-Phe (KLPGF). The KLPGF activity peptide can effectively inhibit the AChE activity, improve the level of brain neurotransmitter acetyl choline and play the effect of preventing senile dementia. The AChE inhibiting peptide is simple in structure, safe and free from toxicity; the AChE inhibiting property is strong and can be used for developing healthcare food or drug for assisting to release or treat the senile dementia.

Description

technical field [0001] The invention belongs to the technical field of food processing, and in particular relates to the application of a pentapeptide KLPGF to inhibit the activity of AChE. Background technique [0002] Alzheimer's disease (AD), also known as senile dementia, is a common neurodegenerative disease among the elderly. According to the World Health Organization, approximately 9.9 million new cases of dementia are diagnosed each year. It is estimated that the total number of dementia patients will be close to 75 million in 2030, and even double to 132 million by 2050. As a result, dementia has become a major health problem affecting the elderly population worldwide. [0003] The pathogenesis of senile dementia is very complex and is the result of the interaction of multiple factors. Data have shown that the formation of Alzheimer's disease is related to inflammation, oxidation, loss of cholinergic transmission and the presence of neurofibrillary tangles. Rega...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/08A61P25/28A23L33/10
CPCA23V2002/00A61K38/08A23L33/10A23V2200/30
Inventor 于志鹏武思佳赵文竹
Owner BOHAI UNIV
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