Alkyl resorcinol compound and uses thereof

A technology of alkyl resorcinol and compounds, which is applied in the field of alkyl resorcinol compounds, and can solve problems such as structural and functional abnormalities and lack of compounds

Active Publication Date: 2019-04-02
BEIJING TECHNOLOGY AND BUSINESS UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Retinal pigment epithelial cells are one of the central links of the disease. The abnormal structure and function of RPE cells caused by long-term oxidative stress is considered to be an important cause of the above-mentioned eye diseases. Compounds that inhibit oxidative damage to macromolecules

Method used

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  • Alkyl resorcinol compound and uses thereof
  • Alkyl resorcinol compound and uses thereof
  • Alkyl resorcinol compound and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0089] ARPE-19 (human retinal pigment epithelial cells) at 1×10 per well 4 The number of cells was inoculated and cultured, and 100 μL of DME / F12 medium (10% FBS) was added to each well of a 96-well plate. After culturing for 24 hours, add the alkylresorcinol compound ARs medium containing 0.2 μg / mL, 1 μg / mL, and 5 μg / mL, wherein the alkylresorcinol ARs is heptadecylresorcinol , the blank group and the hydrogen peroxide control group were replaced with fresh medium. After drug intervention for 24 hours, each well was replaced with 100 μL of DME / F12 (5% BSA) serum-free medium for starvation treatment for 30 minutes. After the starvation treatment, each group was replaced with 100 μL DME / F12 (5% BSA) serum-free medium containing 300 μM H 2 o 2 Oxidation induction treatment for 24h. After the oxidative induction, each group was replaced with DME / F12 (5% BSA) serum-free medium containing 0.5 mg / mL MTT, and continued to culture for 4 h. After the culture, centrifuge at 1800rpm...

Embodiment 2

[0092] ARPE-19 with 1×10 per well 4 The number of cells was inoculated and cultured, and 100 μL of DME / F12 medium (10% FBS) was added to each well of a 96-well plate. After culturing for 24 hours, add the alkylresorcinol compound ARs medium containing 0.2 μg / mL, 1 μg / mL, and 5 μg / mL, wherein the alkylresorcinol ARs is heptadecylresorcinol , the blank group and the hydrogen peroxide control group were replaced with fresh medium. After 24 hours of drug intervention, wash each well with 200 μL HBSS, add 100 μL HBSS containing 50 μmol / mL DCFDA without CO 2 Incubate for 60min. Finally, after washing with 200 μL HBSS, add 100 μL DME / F12 (5% BSA) serum-free medium containing 300 μmol / L H 2 o 2 Oxidation induction 24h. And the fluorescence intensity was detected under the conditions of excitation wavelength 488nm and emission wavelength 530nm.

[0093] Such as figure 2 As shown, compared with the control group, 300 μmol H 2 o 2 The resulting intracellular ROS production rate...

Embodiment 3

[0095] ARPE-19 with 1×10 per well 5 The number of cells was inoculated and cultured, and 2000 μL DME / F12 medium (10% FBS) was added to each well of a 6-well plate. After culturing for 24 hours, add the alkylresorcinol compound ARs medium containing 0.2 μg / mL, 1 μg / mL, and 5 μg / mL, wherein the alkylresorcinol ARs is heptadecylresorcinol , the blank group and the hydrogen peroxide control group were replaced with fresh medium. After drug intervention for 24 hours, add 2000 μL DME / F12 (0.5% BSA) serum-free medium containing 300 μM H 2 o 2 Oxidation induction 0.5h. extract nuclear protein

[0096] Such as image 3 As indicated, 300 μM H 2 o 2 The effect increases the expression of Nrf2 protein in the nucleus of ARPE-19 cells by 33%. Under the intervention of ARs, the expression of Nrf2 protein in the nucleus increased significantly, and under the intervention of 5 μg / mL ARs, the expression of Nrf2 protein in the nucleus increased significantly by 80%. ARs significantly in...

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Abstract

The present invention relates to an alkyl resorcinol compound and uses thereof, and specifically provides uses of an alkyl resorcinol compound represented by the following general formula (I), a pharmaceutically acceptable salt, a solvate, a stereoisomer and a tautomer thereof in preparation of pharmaceutical compositions or preparations for prevention and / or treatment of eye diseases. According to the present invention, the alkyl resorcinol compound has excellent treatment effects on eye diseases such as age-related macular degeneration, diabetic retinopathy, xerophthalmia and the like. The formula (I) is defined in the specification.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to the use of alkyl resorcinol compounds (ARs). Background technique [0002] Oxidative stress is one of the culprits in the pathogenesis of a series of eye diseases such as AMD, diabetic retinopathy (DR), dry eye, conjunctivitis, keratitis, uveitis and glaucoma. Relevant antioxidant treatments, such as vitamins A, C, E and zinc oxide, can reduce fundus lipid deposition, geographic atrophy and choroidal neovascularization and other lesions. Oxidative stress usually refers to the imbalance of oxidation and antioxidant system in the body, the increase of reactive oxygen species (ROS) and nitrogen free radicals, which in turn leads to tissue cell damage. [0003] With the growth of age, oxidative damage also gradually increases, and the retina due to its own strong metabolism, high oxygen consumption, long-term photodamage, and its own phagocytic function produces more oxygen free radicals,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C39/08A61P3/10A61P27/02A61P27/06
CPCA61K31/05A61P3/10A61P27/02A61P27/06C07C39/08
Inventor 王静刘洁郝一铭
Owner BEIJING TECHNOLOGY AND BUSINESS UNIVERSITY
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