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Application of (1,2,3-trimethoxybenzene)-acrylonitrile to preparing medicine for improving senileretinamacular degeneration

A technology for trimethoxybenzene and macular degeneration, applied in the fields of biology and medicine, can solve problems such as difficult to effectively control the disease process and limited effect

Active Publication Date: 2019-04-16
XI AN JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The treatment of wet AMD is aimed at destroying and inhibiting new blood vessels. Although there are many treatment methods, such as laser photocoagulation, transpupillary thermotherapy, photodynamic therapy, surgery and radiation therapy, etc., the effect is limited. For the purpose of delaying the further decline of vision, it is difficult to meet the requirements of effective control of the disease process

Method used

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  • Application of (1,2,3-trimethoxybenzene)-acrylonitrile to preparing medicine for improving senileretinamacular degeneration
  • Application of (1,2,3-trimethoxybenzene)-acrylonitrile to preparing medicine for improving senileretinamacular degeneration
  • Application of (1,2,3-trimethoxybenzene)-acrylonitrile to preparing medicine for improving senileretinamacular degeneration

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] (1,2,3-Trimethoxybenzene)-propenone has no toxic and side effects on human RPE cells

[0052] Human RPE cells were treated with (1,2,3-trimethoxyphenyl)-propenone for 24 hours at concentrations of 0.1, 1, 5, and 10 μM. The crystal violet staining method is used to measure the changes in the number of cells. The fuel can specifically attach to the cell surface, and the relative changes in the number of cells can be analyzed by comparing the absorbance. Such as figure 1 A, Crystal violet staining analysis showed that various concentrations of (1,2,3-trimethoxybenzene)-propenone did not change the number of RPE cells. At the same time, the relative viability of the cells was detected by the MTT method, such as figure 1 B, After the cells were pretreated with (1,2,3-trimethoxybenzene)-propenone, the cell viability did not change significantly. These results show that the compound has no toxic side effects on RPE cells. The results are expressed in the form of Mean ± S.E...

Embodiment 2

[0054] (1,2,3-Trimethoxybenzene)-propenone improves mitochondrial function

[0055] Mitochondrial membrane potential is one of the important indicators of mitochondrial function. The higher the mitochondrial membrane potential, the better the mitochondrial function. However, the mitochondrial membrane potential tends to decrease a lot during cell death. We use the classic JC-1 lipophilic cationic dye to detect mitochondrial membrane potential. JC-1 exists in the mitochondrial membrane in the form of a polymer, which produces red fluorescence. JC-1 cannot be aggregated in the mitochondria and exists as a monomer, producing green fluorescence. The ratio of red light / green light can reflect the strength of mitochondrial membrane potential, the higher the ratio, the stronger the membrane potential. Such as figure 2 A, After treatment of RPE cells with (1,2,3-trimethoxyphenyl)-propenone for 24 hours, the mitochondrial membrane potential was significantly increased at both 5 and ...

Embodiment 3

[0057] (1,2,3-Trimethoxybenzene)-propenone can effectively enhance the antioxidant activity of cells

[0058] Reactive oxygen species (reactive oxygen species, ROS) refers to a group of chemically active compounds with oxygen-containing groups, and free radicals are the most important ROS. ROS exist in many forms, such as superoxide anion (O2 - ), hydroxyl radical (OH), hydrogen peroxide (H2O2), etc.

[0059] ROS can be produced in many parts of the cell, but the vast majority of ROS (about 90%) come from mitochondria. Mitochondrial ROS production is the result of oxidative phosphorylation. Excessive ROS can cause oxidative stress and cause damage to RPE cells, eventually leading to the occurrence of AMD. There is also an antioxidant system in the human body, which will be activated under certain conditions to increase the antioxidant capacity of the body and remove excessive ROS. This system is a two-phase enzyme system. The system is composed of a series of enzymes, such...

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Abstract

The invention discloses application of (1,2,3-trimethoxybenzene)-acrylonitrile to preparing medicine for improving senileretinamacular degeneration. The (1,2,3-trimethoxybenzene)-acrylonitrile servesas an antioxidantcapable of activating two-phase enzyme and enhancing the mitochondrial function, has an inhibiting effect on mitochondrial dysfunction caused by acrolein, has an inhibiting effect oncell activity reduction caused by acrolein, and has an inhibiting effect oncell death caused by acrolein. The effect of the (1,2,3-trimethoxybenzene)-acrylonitrile is completed by activating the two-phase enzyme, and the (1,2,3-trimethoxybenzene)-acrylonitrile has wide pharmacological effects of being anticancer, anti-inflammatory, antibacterial and antiviral, treating diabetes, conducting neuroprotection and the like, and is efficient, safe and tidy medicine.

Description

technical field [0001] The invention belongs to the fields of biology and medicine, and particularly relates to the application of (1,2,3-trimethoxybenzene)-propenone in the preparation of medicines for improving age-related macular degeneration. Background technique [0002] Age-related macular degeneration (AMD) is one of the blinding eye diseases that occurs in middle-aged and elderly people. Its etiology is unknown and may be related to multiple factors such as long-term and chronic photodamage of the macula, heredity, metabolism, race, and diet. The research results show that the pathogenesis of AMD is closely related to the atrophy and degeneration of retinal pigment epithelium (RPE) cells. RPE cells are located between the neural retina and the choroid. Under normal conditions, RPE cells play a key role in many important eye functions, such as phagocytosis of photoreceptor extracellular segments, physiological adsorption of neural retina, blood retinal maintenance an...

Claims

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Application Information

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IPC IPC(8): A61K31/12A61P27/02
CPCA61K31/12A61P27/02
Inventor 刘健康李媛冯智辉曹瑞军黄娜
Owner XI AN JIAOTONG UNIV
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