Antioxidant application of artemisitene

An artemene and antioxidant technology, which can be used in applications, medical preparations containing active ingredients, antidote, etc., and can solve the problems of termination, no pharmacological activity, and insufficient specificity.

Inactive Publication Date: 2015-08-12
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, its molecular formula is C15H20O5, the chemical structural formula 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 artemisitene
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  • Antioxidant application of artemisitene

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Experimental program
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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 di...

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Abstract

The invention discloses an antioxidant application of artemisitene, and identifies artemisitene as the activator of Nrf2 for the first time in the world. In the cell level, artemisitene can activate Nrf2 and downstream antioxidant protective effect of Nrf2. In a mouse model, artemisitene can prominently inhibit the lung injury induced by bleomycin. As the chemical activator of Nrf2, artemisitene and derivatives thereof have a wide application aspect, can be used as food additive, can prevent human tissue or organism from damages caused by harmful substances or carcinogen, and can prevent or inhibit the happening, development and progress of diseases related with oxidative stress such as diabetes, cardiovascular diseases, neurodegenerative diseases, chronic kidney diseases, lung diseases, and the like.

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 The expression of several genes. The expression products of these genes can remove active oxygen species, chemical carcinogens and other toxic substances 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), which will damage biological macromolecules such as nucleic acids, proteins, and lipids, and seriously affect the physiological functions of cells. A large number of studies have shown that cancer, infl...

Claims

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Application Information

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IPC IPC(8): A61K31/366A23L1/30A61P39/06A61P3/10A61P13/12A61P11/00A61P9/00A61P25/28
Inventor 陈为民徐洋刘博
Owner 金沣实业(东莞)有限公司
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