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Abrotine, its derivative dihydro-abrotine, artemether, arteether and arte sunate in use of pharmacy

A technology of dihydroartemisinin and artesunate, which is applied in the pharmaceutical field to achieve strong pharmacological effects, good medicinal prospects, and the effect of preventing or treating sepsis

Inactive Publication Date: 2006-09-20
ARMY MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, whether artemisinin and its derivatives are effective against bacterial DNA and sepsis caused by bacteria (gram-positive bacteria and gram-negative bacteria) has not been reported.

Method used

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  • Abrotine, its derivative dihydro-abrotine, artemether, arteether and arte sunate in use of pharmacy

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0022] Experimental example 1. The dose-effect relationship of artemisinin, dihydroartemisinin, artemether and artesunate in inhibiting the release of cytokines induced by CpG-ODN.

[0023] Culture mouse macrophage RAW264.7, adjust the concentration of cell suspension to 2×10 6 / ml, added to a 48-well plate, 0.4ml per well. Set at 37°C CO 2 After culturing in the incubator for 4 hours, the cells were allowed to adhere to the wall, and different concentrations of artemisinin (5, 10, 20, 40, 80 μg / ml) or dihydroartemisinin, artemether, and artesunate were added. Add 10 μg / ml stimulatory CpG ODN (5′-TCC ATG ACG TTC CTG ACG TT-3′), culture in 37°C, CO2 incubator for 4 hours, take cell culture supernatant to test cytokine TNF-α, and then After 4 hours, the cell culture supernatant was taken to test the cytokine IL-6. The concentration of TNF-α and IL-6 in the cell culture supernatant was measured by double-antibody sandwich ELISA method, and the effect of artemisinin or its deri...

experiment example 2

[0027] Experimental example 2. The dose-effect relationship of artemisinin, dihydroartemisinin, artemether and artesunate in inhibiting the release of cytokines induced by heat-killed Escherichia coli.

[0028] Culture mouse macrophage RAW264.7, adjust the concentration of cell suspension to 2×10 6 / ml, added to a 48-well plate, 0.4ml per well. Set at 37°C CO 2 After culturing in the incubator for 4 hours, the cells were allowed to adhere to the wall, and different concentrations of artemisinin (5, 10, 20, 40, 80 μg / ml) or 40 μg / ml of dihydroartemisinin, artemether or artesunate were added, After 2 hours add 1 x 10 6 / ml heat-inactivated Escherichia coli, cultured in a 37°C, CO2 incubator for 4 hours, then took the cell culture supernatant to test the cytokine TNF-α, and after another 4 hours, took the cell culture supernatant to test the cytokine IL-6. The concentration of TNF-α and IL-6 in the cell culture supernatant was measured by double-antibody sandwich ELISA method,...

experiment example 3

[0033]Experimental example 3. Time-effect relationship of artemisinin inhibiting cytokine release induced by CpG ODN.

[0034] Culture mouse macrophage RAW264.7, adjust the concentration of cell suspension to 2×10 6 / ml, added to a 48-well plate, 0.4ml per well. Set at 37°C, CO 2 After culturing in the incubator for 4 hours, the cells were allowed to adhere to the wall, and the time of adding CpG ODN was regarded as the 0 time point, and 20 μg / ml artemisinin was added at -4, -2, -1, 0, 1, and 2 hours respectively, and placed at 37°C, After 4 hours of culture in a CO2 incubator, the cell culture supernatant was taken to measure TNF-α, and after another 4 hours, the cell culture supernatant was taken to test the cytokine IL-6. To clarify the ability of artemisinin to inhibit the release of cytokines from RAW264.7 induced by CpG ODN.

[0035] point in time

Cytokines

TNF-α

(pg / ml)

IL-6

(pg / ml)

-4h

-2h

-1h

0h

1h

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Abstract

An application of arteannuin and its derivatives (dihydroarteannuin, artemether, arteether and artesunate) in preparing the medicines for preventing and treating the sepsis caused by CpG-ODN and bacteria is disclosed.

Description

technical field [0001] The present invention relates to the use of artemisinin and its derivatives dihydroartemisinin, artemether, artether and artesunate, in particular to the use in the pharmaceutical field. Background technique [0002] Bacterial infection is the main cause of death of clinical patients. When the body is infected, bacterial components such as genomic DNA and bacterial endotoxin (LPS) induce TNF-α, IL-1, IL- 6. The release of pro-inflammatory cytokines such as NO leads to the damage of tissues and organs and the occurrence of sepsis. [0003] Artemisia annua belongs to the Compositae family. In 1972, Chinese researchers first isolated an effective antimalarial monomer from the traditional Chinese medicine Artemisia annua, and named it artemisinin. The molecular formula of artemisinin is C15H22O5. According to the chemical reaction, spectral data and X-ray single product diffraction method, it is proved that artemisinin is a new type of sesquiterpene lact...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/55A61P31/04
Inventor 周红王俊郑江
Owner ARMY MEDICAL UNIV
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