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Application of icaritin in preparation of Nrf2 agonist

A technology of icariin and agonist, which can be applied to medical preparations containing active ingredients, respiratory diseases, organic active ingredients, etc., and can solve problems such as icariin that has not yet been seen

Inactive Publication Date: 2015-06-10
AFFILIATED HUSN HOSPITAL OF FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Icaritin is a flavonoid compound, which exists in a small amount in Epimedium herba. Some studies have disclosed that it has pharmacological effects such as anti-tumor and anti-osteoporosis. So far, there has been no evidence of icariin as an Nrf2 agonist. to report

Method used

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  • Application of icaritin in preparation of Nrf2 agonist
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  • Application of icaritin in preparation of Nrf2 agonist

Examples

Experimental program
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Effect test

Embodiment 1

[0023] Example 1 The effect of icariin (ICT) on the injury of alveolar type II epithelial cells (A549) mediated by cigarette smoke extract (CSE)

[0024] The cytotoxic effect of CSE on A549 cells was detected by MMT method. The results showed that, compared with the negative control group, different concentrations of CSE (2.5%, 5%, 10%) could reduce the cell viability of A549 cells in a concentration-dependent manner (pfigure 1 shown), the test results showed that icariin (ICT) could attenuate the damage of alveolar type II epithelial cells (A549) mediated by cigarette smoke extract (CSE).

Embodiment 2

[0025] Example 2 Effect of icariin (ICT) on Nrf2 nuclear translocation

[0026] Quantitative analysis of Nrf2 nuclear protein by western blot showed that Nrf2 nuclear translocation increased compensatoryly after 2 hours of CSE stimulation (p figure 2 , image 3 shown), the experimental results show that icariin (ICT) can increase Nrf2 nuclear translocation and can act as an Nrf2 agonist.

Embodiment 3

[0027] Example 3 Effect of icariin (ICT) on the expression of Nrf2 downstream antioxidant gene GCLM

[0028] After 5% CSE intervened in A549 cells for 24 hours, the expression of GCLM mRNA decreased, and at the same time, the level of GSH, a downstream product of GCL, also decreased (p Figure 4 , Figure 5 shown);

[0029] The GCL is the rate-limiting enzyme for GSH synthesis, and consists of a catalytic subunit GCLC and a regulatory subunit GCLM.

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Abstract

The invention belongs to the field of medicine preparation, and relates to an application of icaritin in preparation of an Nrf2 agonist. The icaritin intervention trial is carried out on an in-vitro oxidative stress model which is built by stimulation of a cigarette smoke extract. The result shows that the icaritin is capable of inducing Nrf2 phosphorylation, promoting expression of an anti-oxidative gene GCL, and increasing synthesis of an endogenous antioxidant GSH, so as to resist alveolar epithelial cell injuries induced by the cigarette smoke. Nrf2 gene is silenced by an RNA jamming technology; and the icaritin is capable of promoting the expression capacity of the anti-oxidative gene GCL to be reversed. An experiment result shows that the icaritin provided by the invention can be used for preparing the Nrf2 agonist, and further preparing medicines for resisting smoking-induced lung injuries. Furthermore, the invention provides a pharmaceutical composition for activating Nrf2. The pharmaceutical composition contains the icaritin in the formula (I) and a pharmaceutically acceptable carrier. The formula is as shown in the specification.

Description

technical field [0001] The invention belongs to the field of medicine preparation. It relates to the new medical application of icariin, in particular to the application of icariin in the preparation of Nrf2 pathway agonists. Background technique [0002] Studies have reported that nuclear factor-erythroid-2-related facror-2 (Nrf2) is a transcription factor discovered in recent years that is related to anti-oxidative stress. Under normal physiological conditions, most of Nrf2 is combined with Keap1 in the cytoplasm and is in an inactive state. However, when the redox balance in the internal environment is broken, Nrf2 can be phosphorylated, and the phosphorylated Nrf2 dissociates from Keap1 and enters the nucleus, where it further binds to the antioxidant response element ARE, thereby activating a series of downstream antioxidant genes Transcribed to resist oxidative stress damage, the genes include: GCL, GPx, GST, etc. Some studies have confirmed through animal experimen...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P11/00
Inventor 董竞成吴金峰徐海林徐金华
Owner AFFILIATED HUSN HOSPITAL OF FUDAN UNIV
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