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Application of curcumin analogue CUR5g as novel autophagy inhibitor

A technology of curcumin analogs and autophagy inhibitors, applied in the application field of curcumin derivatives

Pending Publication Date: 2021-08-03
HENAN UNIVERSITY OF TECHNOLOGY
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  • Claims
  • Application Information

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Problems solved by technology

However, the role of CUR5g in inhibiting autophagy and its related pharmacological studies have not been reported at home and abroad.

Method used

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  • Application of curcumin analogue CUR5g as novel autophagy inhibitor
  • Application of curcumin analogue CUR5g as novel autophagy inhibitor
  • Application of curcumin analogue CUR5g as novel autophagy inhibitor

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Embodiment Construction

[0030] The following demonstrates the role of CUR5g as an autophagy inhibitor in combination with specific pharmacological experiments and results examples of the curcumin analogue CUR5g.

[0031] Preparation of A549 cells: A549 cells were cultured by conventional methods, and A549 cells in good growth state and in logarithmic growth phase were selected for use.

[0032] Combining the methods of cell biology and molecular biology, the following experiments were carried out to observe the effect of CUR5g on autophagy inhibition.

[0033] EXAMPLES Experiment 1. Detecting the effect of CUR5g on autophagy of A549 cells by transmission electron microscopy:

[0034] A549 cells were seeded into 100mm culture dishes. Set up the control group: add dimethyl sulfoxide (DMSO) equal to the volume of the drug for 24 hours; set up the experimental group: add 10 μM CUR5g for 24 hours. Rinse the cells twice with pre-cooled 1×PBS, add 5ml of pre-cooled 2.5% glutaraldehyde to the culture dish,...

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Abstract

The invention discloses an application of a curcumin analogue CUR5g as an autophagy inhibitor. According to the invention, the influence of 5g of CURR on A549 cell autophagy is detected through a transmission electron microscope experiment, the influence of 5g of CURR on A549 cell autophagy marker protein level is detected through a protein immunoblotting method, and the influence of 5g of CURR on H157, HepG-2 and MCF-7 cell autophagy marker protein levels is detected through the protein immunoblotting method. The effects of cur5g on autophagy marker protein level of A549 cells under autophagy inhibition and activation conditions were detected by Western blotting, and the effects of cur5g on autophagy initiation protein level of A549 cells were detected by Western blotting. It was proved that cur5g can effectively inhibit the fusion of autophagosomes and lysosomes in vitro, so as to inhibit the autophagy. 5g of CUR5 has a remarkable effect as an autophagy inhibitor, and an attractive prospect is provided for development and application of the autophagy inhibitor.

Description

[0001] 1. Technical field: [0002] The present invention relates to the application of a curcumin derivative, in particular to the application of a curcumin analog CUR5g as a novel autophagy inhibitor. The chemical formula of CUR5g is (3E,5E)-1-methyl-3-(4-hydroxybenzylidene)-5-(3-indolemethylene)-piperidin-4-one. [0003] 2. Background technology: [0004] Chemical formula (3E,5E)-1-methyl-3-(4-hydroxybenzylidene)-5-(3-indole methylene)-piperidin-4-one is abbreviated as CUR5g, and its structural formula is: [0005] [0006] (3E,5E)-1-Methyl-3-(4-hydroxybenzylidene)-5-(3-indolemethylene)-piperidin-4-one has the formula C 22 h 20 N 2 o 2 , the molecular weight is 344.41, and the properties are orange-yellow crystalline powder. [0007] Turmeric is a traditional Chinese medicinal material, which is a diketone chemical component extracted from the rhizomes of Zingiberaceae and Araceae. Curcumin is a kind of phenolic pigment extracted from turmeric. It is the main compon...

Claims

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Application Information

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IPC IPC(8): A61K31/454A61P35/00A61P43/00
CPCA61K31/454A61P35/00A61P43/00
Inventor 张璐陈靖轩吴博文孙纲春杜梅强鹏飞刘志辉高亚美
Owner HENAN UNIVERSITY OF TECHNOLOGY
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