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Antioxidant Application of Artemisinin

A technology of artemisinin and antioxidant, applied in the new application field of artemisinin, which can solve the problems of termination, no pharmacological activity, and insufficient specificity

Active Publication Date: 2017-10-24
金沣实业(东莞)有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Unfortunately, due to the discovery that it interacts with many proteins, the specificity is not enough, and the clinical trial was terminated
Some Nrf2 chemical inducers have been found, such as Sulforaphane, BHA, etc., but their mechanism of action is not yet fully understood
[0009] Artemisitene is derived from the plant Artemisia annua, and its molecular formula is C 15 h 20 o 5 , the chemical structure is , in the prior art, there is no experimental data to prove that it has specific pharmacological activity

Method used

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  • Antioxidant Application of Artemisinin
  • Antioxidant Application of Artemisinin
  • Antioxidant Application of Artemisinin

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Embodiment Construction

[0055] The technical scheme of the present invention will be further described below in combination with experiments and experimental data.

[0056] Discovery and characterization of artemisinene as a novel Nrf2 activator

[0057] Using MDA-MB-231 cells stably integrating ARE-luciferase, through high-throughput screening, the inventors identified a new activator of Nrf2, artemisinin, from a chemical molecule library.

[0058] figure 1 In, (A) the chemical structure of artemisinene (B) high-throughput screening of the new Nrf2 chemical inducer artemisinene. MDA-MB231 cells stably integrated with ARE-Firefly luciferase were seeded in 96-well plates. When the cell density reached 80%, they were treated with 1uM artemisinin for 24 hours, and then the luciferase activity was analyzed. 50uM tBHQ treatment was used as a positive control. (C) MDA-MB231 cells were co-transfected with NQO1-ARE-Firefly luciferase and TK-Rellina luciferase. The transfected cells were treated with diff...

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Abstract

The invention discloses the anti-oxidation application of artemisinin, and the inventor identified artemisinin as an activator of Nrf2 for the first time in the world. At the cellular level, artemisinene activates Nrf2 and its downstream antioxidant protective effects. In a mouse model, artemisinin significantly inhibited bleomycin-induced lung injury. As a chemical activator of Nrf2, artemisene and its functional derivatives have broad application prospects. As a food supplement, it can prevent damage to human tissues and organs caused by environmental toxic substances or carcinogens, and can prevent or inhibit oxidative stress. The occurrence, development and progress of hormone-related diseases such as diabetes, cardiovascular disease, neurodegenerative disease, chronic kidney disease and lung disease.

Description

technical field [0001] The present invention relates to a new application of a compound, in particular to a new application of artemisinin. Background technique [0002] The Keap1-Nrf2 signaling pathway is the most important antioxidant defense response (anti-oxidant defense response) system in higher organisms. The activation of the Keap1-Nrf2 signaling pathway can lead to hundreds of Gene expression. The expression products of these genes can remove toxic substances such as reactive oxygen species and chemical carcinogens in the organism, and maintain the redox balance in the organism [1] . Dysregulation of the Keap1-Nrf2 signaling pathway will lead to the accumulation of reactive oxygen species (ROS) in the body, that is, oxidative stress (Oxidative stress), damage nucleic acid, protein, lipid and other biomacromolecules, seriously affecting the physiological function of cells. A large number of studies have shown that cancer, inflammation, neurodegenerative diseases, c...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/366A23L33/105A61P39/06A61P3/10A61P13/12A61P11/00A61P9/00A61P25/28
Inventor 陈为民徐洋刘博
Owner 金沣实业(东莞)有限公司
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