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Application of L-aspartic acid beta-hydroxamate in preparation of drugs for inhibiting choroidal neovascularization, and choroidal neovascularization treatment method

A hydroxamate and aspartic acid technology, applied in drug delivery, pharmaceutical formulation, drug combination, etc., can solve the problems of retinal and choroidal atrophy, side effects, intraocular infection, etc., and achieve the effect of inhibiting choroidal neovascularization

Inactive Publication Date: 2019-05-28
WENZHOU MEDICAL UNIV
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Problems solved by technology

At present, anti-VEGF antibodies are widely used clinically (including bevacizumab, ranibizumab, etc.), but repeated intravitreal injections of anti-VEGF antibodies will produce serious side effects: including retinal and choroidal atrophy caused by long-term use of VEGF antibodies; repeated vitreous cavity Injections induce retinal detachment, intraocular infection, urgent need for better treatment options

Method used

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  • Application of L-aspartic acid beta-hydroxamate in preparation of drugs for inhibiting choroidal neovascularization, and choroidal neovascularization treatment method
  • Application of L-aspartic acid beta-hydroxamate in preparation of drugs for inhibiting choroidal neovascularization, and choroidal neovascularization treatment method
  • Application of L-aspartic acid beta-hydroxamate in preparation of drugs for inhibiting choroidal neovascularization, and choroidal neovascularization treatment method

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Embodiment Construction

[0016] experimental method:

[0017] Using the animal model of exAMD, in C57 / B6 mice, using Krypton red laser (0.05 s interval, 0.07 s duration, and 240 mW power), do fundus irradiation to create CNV mouse model. Serine racemase competitive inhibitor, L-Aspartic acid β-hydroxamate (l-Aspartic acid β-hydroxamate) was injected intravenously at a dose of 6 mg / kg on the day before laser and 3 mg / kg on the third day after laser. -hydroxamate, L-ABH). On day 7 after laser injury, choroid / retinal pigment epithelial cells (RPEs) were spread and stained with Alexa Fluor 594-conjugated isolectin GS-IB4 to analyze CNV volume. And using primary RPEs in vitro, study the inhibitory effect of L-ABH on the production of VEGF and MCP-1 induced by TNFα in RPEs. And use RPEs and macrophage co-culture, research L-ABH pretreatment RPEs, inhibit the migration of macrophages.

[0018] Intravenous injection of L-ABH inhibits laser-induced choroidal neovascularization as a result of figure 1 shown...

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Abstract

The invention discloses application of L-aspartic acid beta-hydroxamate in preparation of drugs for inhibiting choroidal neovascularization, and a choroidal neovascularization treatment method. Through intravenous injection of the L-aspartic acid beta-hydroxamate, secretion of VEGF and MCP-1 by TNF alpha-induced RPE is inhibited, so that the choroidal neovascularization is suppressed, and seriousside effects, such as retinal and choroidal atrophy, retinal detachment and intraocular infection, caused by repeated intravitreal injection of anti-VEGF antibodies are avoided.

Description

technical field [0001] The invention specifically relates to the technical field of choroidal neovascularization, in particular to the application and method of L-aspartic acid β-hydroxamate in the preparation of drugs for inhibiting choroidal neovascularization. Background technique [0002] Choroidal neovascularization (CNV) is an important pathological feature of exudative age-related macular degeneration (exAMD) main cause of loss. At present, anti-VEGF antibodies are widely used clinically (including bevacizumab, ranibizumab, etc.), but repeated intravitreal injections of anti-VEGF antibodies will produce serious side effects: including retinal and choroidal atrophy caused by long-term use of VEGF antibodies; repeated vitreous cavity Injections induce retinal detachment, intraocular infection, and better treatment options are urgently needed. Contents of the invention [0003] In order to avoid the defects of the prior art, the present invention provides an applicat...

Claims

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Application Information

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IPC IPC(8): A61K31/198A61P27/02
CPCA61K31/198A61P27/02A61K9/0019
Inventor 吴圣洲吴梦娟刘依美
Owner WENZHOU MEDICAL UNIV
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