Novel application of echinatin

A technology of medicine and compounds, applied in the field of licorice chalcone, can solve the problems of high price, limited use, serious side effects, etc., and achieve the effect of reducing the area of ​​liver necrosis, increasing the level of GSH, and reducing the levels of ALT and AST

Active Publication Date: 2016-01-13
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are various kinds of hepatoprotective drugs clinically, but most of them are expensive or have relatively high toxic and side effects, so that their use is limited

Method used

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  • Novel application of echinatin
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  • Novel application of echinatin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Example 1. The activating effect of licorice chalcone on Nrf2

[0058] In this example, the effects of Glycyrrhizin on HepG2 cell viability and Nrf2 / ARE reporter gene activity were investigated.

[0059] 1. Experimental materials and methods

[0060] (1) Glycyrrhiza chalcone was purchased from Chengdu Mansite Biotechnology Co., Ltd. Its proton nuclear magnetic resonance spectrum and carbon nuclear magnetic resonance spectrum are as follows: figure 1 with figure 2 Shown. The human hepatocellular carcinoma cell line HepG2 was purchased from the American Type Culture Collection (ATCC), and the experiments all used cells in the logarithmic growth phase.

[0061] HepG2 cells were stably transfected with Nrf2 luciferase reporter gene using Lipofectamine2000 (Life Technologies), and the resulting cells were called HepG2C8 cells. After inoculating HepG2C8 cells in a 24-well plate for 12 hours, add the specified concentration of licorice chalcone respectively. After 6 hours, the cells...

Embodiment 2

[0066] Example 2. Application of Glycyrrhiza Chalcone in the preparation of products that activate Nrf2 and / or AMPK signal pathways, antioxidant enzyme inducers and anti-aging products

[0067] 1. Experimental materials and methods

[0068] (1) MEFs cells were taken from C57 mouse embryos (Chen Mingyu, Laboratory Animal Science) at 13.5 days of pregnancy. After inoculating the MEFs cells in the logarithmic growth phase in a 6-well plate for 24 hours, add the specified concentration of licorice chalcone, and continue to culture for 6 hours or for a specified time. The supernatant was discarded, and the cells were lysed with TRIZOL buffer (Beijing Quanshijin Biotechnology Co., Ltd.) to extract total RNA. Then qPCR method was used to detect the mRNA levels of HO-1 and NQO-1.

[0069] (2) After 24 hours of inoculation of MEFs cells in a 60mm dish, add the specified concentration of licorice chalcone, and continue to culture for 6 hours or for a specified time. The supernatant was disc...

Embodiment 3

[0084] Example 3 Application of Glycyrrhiza Chalcone in the preparation of an antioxidant enzyme inducer and an anti-skin cancer cell transformation product

[0085] 1. Experimental materials and methods

[0086] (1) JB6P+ cells (American Culture Collection ATCC) in the logarithmic growth phase were inoculated into a 6-well plate for 24 hours, and licorice chalcone of designated concentration was added respectively, and the culture was continued for 72 hours. The supernatant was discarded, and the cells were lysed with TRIZOL buffer to extract total RNA. Then qPCR method was used to detect the mRNA levels of Nrf2, HO-1, Gclc and NQO-1.

[0087] (2) 24 hours after the JB6P+ cells were seeded in the 6-well plate, the specified concentration of licorice chalcone was added respectively, and the culture was continued for 72 hours. The supernatant was discarded, the cells were lysed with RIPA buffer, and the protein concentration was determined by BCA method. 20μg of protein from each s...

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Abstract

The invention discloses novel application of echinatin. The echinatin and at least one of medically acceptable salt, ester, solvate, stereoisomer, tautomer and prodrug of the echinatin are applied to the product which has at least one of the following functions: (1) activating the signal path of Nrf2 and/or AMPK; (2) strengthening the expression of Nrf2, antioxidase and/or metabolic enzymes; (3) resisting aging; (4) inhibiting cell injury and tissue injury caused by oxidation; (5) protecting liver injury; (6) protecting chemical liver injury or oxidative liver injury; and (7) resisting vicious transformation of skin cells. The echinatin can be separated and purified from licorice root. The novel application of the echinatin provides a novel thought to researches and development of echinatin, and a series of novel products with the application are further provided.

Description

Technical field [0001] The invention relates to a new use of licorice chalcone. Background technique [0002] Nrf2 is the core regulator of phase II detoxification or antioxidant enzymes, which can protect cells from oxidative damage. The activation of Nrf2 can enhance the body's antioxidant capacity and the body's ability to detoxify. The use of Nrf2 agonists has been shown to have varying degrees of protection in many diseases. For example, SFN is a compound extracted from broccoli and cabbage. Many literatures have reported the protective effects of SFN on diabetes, cardiovascular diseases and neurodegenerative diseases. Studies have shown that Nrf2 deletion can aggravate the severity of many diseases. For example, compared to the control group, after knocking out Nrf2 in MIN6β cells of the mouse pancreatic islet β cell line, the damage caused by hydrogen peroxide, including cell viability, cell morphology, and apoptosis, was significantly enhanced. Therefore, the discove...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61P39/06A61P1/16A23L33/10A61K8/35A61Q19/00
Inventor 叶敏余四旺王永瑞季帅乔雪唐叔南李紫薇
Owner PEKING UNIV
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