Application of 7,8-dihydroxyflavone (DHF) to preparation of drug for treating retinal degenerative diseases

A technology of dihydroxyflavone and retinal degeneration, applied in 7 fields, can solve the problems that have not yet been seen

Inactive Publication Date: 2017-01-04
EYE & ENT HOSPITAL SHANGHAI MEDICAL SCHOOL FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, there is no report on the treatment of retinal degenerative diseases by 7,8-dihydroxyflavone

Method used

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  • Application of 7,8-dihydroxyflavone (DHF) to preparation of drug for treating retinal degenerative diseases
  • Application of 7,8-dihydroxyflavone (DHF) to preparation of drug for treating retinal degenerative diseases
  • Application of 7,8-dihydroxyflavone (DHF) to preparation of drug for treating retinal degenerative diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: DiI reverse labeling cell counting method to detect the protective effect of 7,8-dihydroxyflavone on damaged retinal ganglion cells (RGCs)

[0023] ①Experimental objects and groups

[0024] Experimental object: adult male SD rats (about 200g);

[0025] Randomly divided into experimental group, negative control group, and positive control group (n=5); the experimental group was further divided into 4 subgroups, and 7,8-DHF 4uL of four concentrations of 1uM, 5uM, 10uM and 20uM were injected into the vitreous cavity respectively , the negative control group was injected with 0.1% DMSO solution 4uL into the vitreous, and the positive control group was injected with 0.5ug / uL BDNF 4uL into the vitreous;

[0026] Brain-Derived Neurotrophic Factor (BDNF) has a significant protective effect on retinal neurons. It has been confirmed in various animal models such as optic nerve contusion and transverse injury that BDNF can protect retinal ganglion cells (RGCs) and prom...

Embodiment 2

[0033] Example 2 Apoptosis in situ cell apoptosis detection method (TUNEL detection) to observe the anti-apoptosis test of 7,8-dihydroxyflavone on damaged retinal ganglion cells (RGCs)

[0034] ①Experimental objects and groups

[0035] Experimental object: adult male SD rats (about 200g);

[0036] They were randomly divided into experimental group, negative control group and positive control group (n=3). The experimental group was injected with 5uM concentration of 7,8-DHF 4uL into the vitreous, the negative control group was injected with 0.1% DMSO solution 4uL, and the positive control group was injected with 0.5ug / uL BDNF 4uL;

[0037] ②Establishment and administration of optic nerve contusion animal model: After general anesthesia by intraperitoneal injection of ketamine (80mg / kg) and xylazine (12mg / kg), SD rats were cleaned and disinfected around the left eye, and circularly cut open the bulbar conjunctiva of the outer canthus , Open Tenon's capsule, bluntly dissect the...

Embodiment 3

[0042] Example 3 GFAP immunohistochemical detection to observe the effect of 7,8-dihydroxyflavone on maintaining the microenvironment of damaged retinal ganglion cells (RGCs)

[0043] Glial fibrillary acidic protein (GFAP) is a cytoplasmic filamentous protein that exists in different glial cells of the central nervous system and is an indicator reflecting the extracellular microenvironment. Studies have shown that the expression of GFAP increases High is a non-specific marker of damage to the central nervous system, and the activation of glial cells is one of the important reasons for the loss of RGCs in glaucoma and other optic nerve diseases. Immunohistochemical detection and semi-quantitative analysis were performed on the expression level of GFAP in the retinal sections of each group, and the protective effect of 7,8-DHF on retinal ganglion cells was indirectly reflected by comparing the differences in the expression level of GFAP among the groups;

[0044] ①Experimental o...

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PUM

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Abstract

The invention belongs to the pharmaceutical field and relates to an application of 7,8-dihydroxyflavone (DHF) to preparation of a drug for treating retinal degenerative diseases. Through adult SD rat optic nerve contusion model experiments, the results show that 7,8-DHF can achieve the effects of reducing apoptosis of retinal ganglion cells and increasing the survival rate and has obvious protective effects on injured retinal neurons. 7,8-DHF is used for further treating the retinal degenerative diseases by protecting the injured retinal neurons, wherein the retinal degenerative diseases include glaucoma, macular degeneration, retinitis pigmentosa, ischemic optic neuropathy and traumatic optic nerve contusion. The invention also provides a novel small molecular drug preparation with 7,8-DHF as the main active ingredient. Obvious protective effects can be generated for the injured retinal neurons by locally delivering the drug to the vitreous cavities of eyes.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to the new application of 7,8-dihydroxyflavone in pharmacy, in particular to the application of 7,8-dihydroxyflavone in protective medicine for treating retinal degenerative diseases. Background technique [0002] The prior art discloses that retinal neuron apoptosis and axonal degeneration are the common pathological basis of retinal degenerative diseases such as glaucoma, age-related macular degeneration, and retinitis pigmentosa. As the world's first irreversible blinding eye disease, for example, glaucoma is characterized by progressive retinal ganglion cell loss and axonal degeneration, and the clinical manifestations are typical nerve atrophy and visual field defect. At present, in clinical practice, the treatment of glaucoma is mainly to reduce intraocular pressure by drugs or surgery. However, a considerable number of patients continue to deteriorate their visual function despite satis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P27/02
Inventor 莫晓芬麦尔哈巴·肖开提荣先芳熊佳伟
Owner EYE & ENT HOSPITAL SHANGHAI MEDICAL SCHOOL FUDAN UNIV
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