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An octapeptide and its application in the preparation of medicines for improving memory

A technology for improving memory and medicines, applied in applications, medical preparations containing active ingredients, peptides, etc., can solve the problems of being easily degraded by proteases or polypeptide enzymes in the body, low bioavailability, poor stability, etc., and achieve no toxic side effects , Improve memory impairment, prolong the effect of shelf life

Active Publication Date: 2022-05-10
RONGCHENG TAIXIANG FOOD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, peptide drugs also have disadvantages such as poor stability, short half-life, low bioavailability, and easy degradation by proteases or peptide enzymes in vivo, which greatly limits their application.

Method used

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  • An octapeptide and its application in the preparation of medicines for improving memory
  • An octapeptide and its application in the preparation of medicines for improving memory
  • An octapeptide and its application in the preparation of medicines for improving memory

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] The synthesis of polypeptide WCPFSRSF by solid-phase synthesis includes the following steps: swelling and washing the dichloro resin, removing the Fmoc protecting group, adding the constituent amino acids of the polypeptide for condensation reaction, and repeating the process of removal-protection-condensation until all amino acids are connected . Purified by reverse-phase high-performance liquid chromatography to obtain pure polypeptide (>95%).

Embodiment 2

[0044] Effect of octapeptide on glutamate-induced neuronal cell survival. like figure 1 As shown, the cell survival rates of 50 μM and 100 μM WCPFSRSF treatment were 69.03±1.21% and 87.00±3.21%, respectively. The drug of positive control: the survival rate of cells treated with cerebrolysin (0.5 mg / mL) was 67.58±1.79%.

[0045] The test results show that the octapeptide WCPFSRSF has a better neuroprotective effect.

Embodiment 3

[0047] Determination of lactate dehydrogenase (lactate dehydrogenase, LDH)

[0048] SH-SY5Y cells were divided into 2×10 5Cells / mL were inoculated in a transparent 96-well plate, and culture medium was added. Six wells were set up for each experimental group, and blank wells and control wells were set up at the same time. After 24 hours, the medium was discarded, the model group was replaced with a medium containing 37.5mM glutamic acid, and the sample group was replaced with a medium containing both glutamic acid and samples, while cerebrolysin (0.5mg / mL) was used as a positive control , the blank group and the control group were replaced with fresh medium, and cultured for 24 hours. The culture was terminated before the detection, the supernatant was taken, and the lactate dehydrogenase kit was used for detection according to the instructions.

[0049] like figure 2 As shown, the test results showed that the LDH release rate of the glutamic acid treatment group was 136....

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Abstract

The invention discloses an octapeptide and its application in preparing medicines for improving memory. The amino acid sequence of the polypeptide is: Trp-Cys-Pro-Phe-Ser-Arg-Ser-Phe (WCPFSRSF). The octapeptide of the invention can improve the memory impairment of mice induced by sleep deprivation, and can significantly inhibit the excitotoxicity and oxidative stress of nerve cells. The polypeptide of the present invention can be used alone as a drug for improving memory, or can be used in combination with other active ingredients that can improve memory, and can also be prepared into microcapsules to improve the digestive stability and bioavailability of the polypeptide in the gastrointestinal tract. And shelf life, so as to be better applied to the field of medicine.

Description

technical field [0001] The invention relates to an octapeptide and its application in preparing medicines for improving memory. Background technique [0002] Glutamate is the major amino acid excitatory neurotransmitter in the brain. When glutamate accumulates too much in the synaptic cleft, the high extracellular concentration of glutamate leads to overstimulation of glutamate receptors, which in turn leads to calcium overload and leads to oxidative stress and apoptosis, which ultimately leads to cell damage and neuron loss, and even trigger neurodegenerative diseases. Conversely, elevated calcium ion flux further exacerbates oxidative stress and accelerates neuronal death, a phenomenon known as excitotoxicity. The excitotoxicity of glutamate is the main cause of neuronal death, which is closely related to a variety of neurological diseases such as Alzheimer's disease and ischemic stroke. Therefore, the neuronal cell model of glutamate damage is often used in the study o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/06A61K38/08A61K45/06A61P25/28A23L33/18A23P10/30
CPCC07K7/06A61K45/06A61P25/28A23L33/18A23P10/30A61K38/00A23V2002/00A23V2200/322A23V2250/55A23V2250/1868A23V2250/1846A23V2250/18A23V2250/214A23V2250/1842A23V2250/712A23V2250/71A23V2250/54252A23V2200/224A23V2250/5114A23V2250/5432A23V2300/10A23V2300/48A23V2250/5026A23V2250/5118A23V2250/511
Inventor 赵谋明张琪杨青王金梅位正鹏苏国万曾海英沈源庆沈萍萍
Owner RONGCHENG TAIXIANG FOOD
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