Application of artemisinin in preparing medicament for preventing and treating neurological diseases

A kind of artemisinin derivatives, neurological technology, applied in the direction of nervous system diseases, sensory diseases, drug combination, etc., can solve the problems of unclear protective effect of artemisinin and little understanding

Active Publication Date: 2014-07-30
ZHONGSHAN OPHTHALMIC CENT SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, little is known about the effects of artemisinin-like drugs on nerve cells, and at the same tim

Method used

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  • Application of artemisinin in preparing medicament for preventing and treating neurological diseases
  • Application of artemisinin in preparing medicament for preventing and treating neurological diseases
  • Application of artemisinin in preparing medicament for preventing and treating neurological diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 Protective effect of artemisinin on SNP-damaged PC12 nerve cells

[0033] 1. Materials and methods

[0034] (1) Materials and main reagents

[0035] Artemisinin was purchased from Dalian Meilun Biotechnology Co., Ltd.; sodium nitroprusside (SNP) was purchased from Beyontian Institute of Biotechnology; DMEM medium, fetal bovine serum and horse serum were purchased from Gibco, USA; thiazolyl blue (MTT), Dimethyl sulfoxide (DMSO) was purchased from Sigma Corporation of the United States; LY294002 and PD98059 were purchased from Sigma-Aldrich Corporation of the United States; Western blot related reagents were purchased from Guangzhou Biyuntian Biotechnology Research Institute; the antibody Anti-phospho-Akt (Ser473) used in Western Antibody and Anti-phospho-p44 / 42 MAPK (Erk1 / 2) (Thr202 / Tyr204) antibody were purchased from Cell Signaling Technology (Woburn, USA); horseradish peroxidase (HRP)-labeled secondary antibody (IgG) was purchased from The Santa Cruz C...

Embodiment 2

[0078] Example 2 Protective effect of artemisinin on retinal nerve cell RGC-5 damaged by SNP

[0079] 1. Materials and methods

[0080] With embodiment 1.

[0081] 2. Results

[0082] (1) SNP can induce RGC-5 cell damage

[0083] After the RGC-5 cells were deprived of serum, the RGC-5 cells were treated with different concentrations of SNP (62.5-1000 μM) and the RGC-5 cells were cultured in DMEM medium as a control (CTL). After 24 hours of culture, the changes in cell viability were detected by the MTT method. Test results such as Figure 7 As shown, it can be seen that low concentration of SNP promotes cell proliferation (1-250 μM), when it reaches 500 μM, SNP becomes toxic, and at 750 μM, the cell survival rate drops to about 59%. This concentration is used as a model of SNP cytotoxicity.

[0084] (2) Protective effect of artemisinin on SNP-damaged RGC-5 cell viability

[0085] On the basis of the established SNP-induced cell injury model, RGC-5 cells were treated...

Embodiment 3

[0091] Example 3 The protective effect of artemisinin on SNP-injured cortical neurons

[0092] 1. Materials and methods

[0093] With embodiment 1.

[0094] 2. Results

[0095] (1) SNP can induce cortical neuron cell damage

[0096] After cortical neuron cells were deprived of serum, cortical neuron cells were treated with different concentrations of SNP (12.5-1000 μM) and cortical neuron cells were cultured in DMEM medium as a control (CTL). After 24 hours of culture, the changes in cell viability were detected by MTT method. Test results such as Figure 10 As shown, it can be seen that the SNP between 12.5 μmol / L and 100 μmol / L can significantly reduce the survival rate of neurons, and the value of MTT shows a dose-dependent decrease, and the SNP of 50 μmol / L can significantly inhibit neuronal survival. The dose of the SNP for the survival of the neurons following neuronal injury was chosen to be 50 μmol / L.

[0097] (2) Protective effect of artemisinin on SNP-inju...

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Abstract

The invention discloses application of artemisinin and derivatives thereof in preparing medicaments for preventing and treating neurological diseases. In the application, the nerve cell line of rat adrenal pheochromocytoma PC12, retinal nerve cell line RGC-5 and primary cortical neuron are on behalf of experiment objects, sodium nitroprusside and hydrogen peroxide are used to simulate and induce oxidative stress, cell apoptosis and other cell injuries of nerve cells. Researches discover that the artemisinin has a protective effect on sodium nitroprusside and hydrogen peroxide induced cell injury, the protective effect mechanism of the artemisinin and derivatives thereof is primarily discussed, and results indicate that the artemisinin and derivatives thereof can be used as nerve protection medicaments for preventing and treating various neurological diseases, such as various neurodegenerative diseases, acute and chronic neurodegenerative diseases, neurological eye disease and the those neurological diseases mainly related to oxidative stress injuries and cell apoptosis. The application brings a new direction to treatment and prevention of neurological diseases.

Description

technical field [0001] The invention relates to the application of artemisinin in the preparation of medicines for preventing and treating neurological diseases. Background technique [0002] Artemisinin (artemisinin) is a compound extracted from the Asteraceae plant Artemisia annua, which has been widely used in the treatment of various types of malaria. The killing effect of artemisinin on Plasmodium mainly acts on the inner stage of red blood cells. It is less effective for extraerythrocytic and preerythrocytic phases. In addition to its outstanding antimalarial effect, artemisinin also has significant antibacterial and antiviral effects. , Shigella, Mycobacterium tuberculosis, etc. also have a certain inhibitory effect. Sitosterol and stigmasterol extracted from Artemisia annua also have antiviral effects. In addition, artemisinin also has immunomodulatory effects, which can significantly inhibit humoral immunity and promote cellular immunity to a certain extent. In ...

Claims

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Application Information

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IPC IPC(8): A61K31/366A61P25/00A61P27/02
Inventor 郑文华周旋和孟茜王曰康汪海涛张浪闫凤侠赖永长
Owner ZHONGSHAN OPHTHALMIC CENT SUN YAT SEN UNIV
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