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Application of a combination of small molecular compounds in the preparation of drugs for preventing and treating retinal damage diseases

A small molecule compound, retinal damage technology, used in drug combinations, sensory diseases, cardiovascular system diseases, etc., can solve problems such as poor efficacy, achieve the effect of protecting structural integrity and normal function, and preventing retinal damage

Active Publication Date: 2022-07-05
ZHONGSHAN OPHTHALMIC CENT SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For dry AMD, there are currently no effective drugs, or existing treatments are not effective

Method used

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  • Application of a combination of small molecular compounds in the preparation of drugs for preventing and treating retinal damage diseases
  • Application of a combination of small molecular compounds in the preparation of drugs for preventing and treating retinal damage diseases
  • Application of a combination of small molecular compounds in the preparation of drugs for preventing and treating retinal damage diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1. Crystal violet staining and bright field photography

[0029] 1. Experimental materials and procedures

[0030] 1.1 Preparation of cell culture medium: DMEM / F12+10% fetal bovine serum+1% P / S double antibody (penicillin+streptomycin).

[0031] 1.2 Combination preparation of small molecule compounds:

[0032] NU7441: Dilute NU7441 powder with ultrapure water, and the final concentration of the stock solution is 3mM.

[0033] Ergothioneine: The ergothioneine powder was diluted with ultrapure water, and the final concentration of the stock solution was 30 mM.

[0034] RepSox: The NU7441 powder was diluted with ultrapure water, and the final concentration of the stock solution was 3mM.

[0035] Mixing the three small-molecule compound mother liquors in equal volumes becomes the small-molecule compound combination.

[0036] 1.3 Sodium iodate preparation: Sodium iodate (SI) was directly diluted with culture medium, and the final concentration was 10 μM.

[0037...

Embodiment 2

[0050] Example 2. Cell viability experiment (CCK8 staining)

[0051] (1) Method

[0052] 1. Experimental materials and procedures

[0053] 1.1 Preparation of cell culture medium: DMEM / F12+10% fetal bovine serum+1% P / S double antibody.

[0054] 1.2 Combination preparation of small molecule compounds:

[0055] NU7441: Dilute NU7441 powder with ultrapure water, and the final concentration of the stock solution is 3mM.

[0056] Ergothioneine: The ergothioneine powder was diluted with ultrapure water, and the final concentration of the stock solution was 30 mM.

[0057] RepSox: The NU7441 powder was diluted with ultrapure water, and the final concentration of the stock solution was 3mM.

[0058] Mixing the three small-molecule compound mother liquors in equal volumes becomes the small-molecule compound combination.

[0059] 1.3 Sodium iodate preparation: Weigh sodium iodate powder, dissolve it in an appropriate amount of medium, and dilute it directly. The final concentration ...

Embodiment 3

[0068] Example 3. Animal experiment-RPE cell layer spreading

[0069] (1) Method

[0070] 1. Animal Injection

[0071] 1.1 The injected animals were male C57 / BL6 mice for 4 to 6 weeks. The experiment was divided into: negative control group CTR (PBS), model control group (sodium iodate), and experimental group was sodium iodate + small molecule compound combination co-treatment group (NU7441 at 8 mg / kg; ergothioneine at 80 mg / kg; RepSox at 8 mg / kg).

[0072] 1.2 Sodium iodate injection The intraperitoneal injection was used: sodium iodate was dissolved in PBS, and the injection dose of each animal was 25 mg / kg, calculated according to the body weight of the animal.

[0073] 1.3 Intraperitoneal injection of small molecule compound combination: dissolve the small molecule in PBS to prepare a mother solution and dilute it in equal volume. Calculated by animal body weight, the final injection dose of each animal is NU74418mg / kg; Ergothioneine 80mg / kg; RepSox 8mg / kg.

[0074] ...

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Abstract

The invention relates to the field of biotechnology, and specifically discloses the application of a combination of small molecular compounds in the preparation of a medicament for preventing and treating retinal damage diseases. The combination of small molecule compounds can effectively antagonize cell death and dysfunction caused by oxidative stress on retinal pigment epithelial cells. It can effectively protect retinal pigment epithelial cells and thus protect the structural integrity and normal function of the entire retinal layer cells. It can be used for prevention and potential Treating retinal damage caused by oxidative stress is particularly beneficial for preventing and / or treating retinal damaging diseases such as age-related macular degeneration. In addition, the present invention verifies through experiments that the combination of small molecule compounds has no obvious pharmacological toxicity, and can effectively control the occurrence and development of retinal damage diseases, providing new opportunities for the development of the unknown biological activity of the combination of small molecule compounds and future clinical therapeutic effects. theoretical support.

Description

technical field [0001] The invention relates to the field of biotechnology, in particular to the application of a combination of small molecular compounds in the preparation of a medicament for preventing and treating retinal damage diseases. Background technique [0002] Age-related macular degeneration (AMD) is a disease that causes central visual field loss, abnormal color and dark vision, and visual degeneration, and is the leading cause of blindness in the elderly population. The macula is a special structure with a diameter of about 1.5 mm in the center of the posterior pole of the retina. It is mainly responsible for fine vision, color vision, etc. As the most sensitive part of vision, once the macula is damaged, it will seriously affect the central vision, and the loss of central vision may Barriers to daily activities such as face recognition, driving, and reading. AMD is divided into wet AMD and dry AMD. Wet AMD is manifested by choroidal neovascularization, retin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/5377A61K45/06A61P9/10A61P27/02A61P39/06A61K31/4172A61K31/444
CPCA61K31/4172A61K31/5377A61K31/444A61K45/06A61P27/02A61P9/10A61P39/06A61K2300/00
Inventor 欧阳宏王力
Owner ZHONGSHAN OPHTHALMIC CENT SUN YAT SEN UNIV
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