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Application of compound EPZ031686 in preparing drug for treating vascular aging related diseases

A technology of EPZ031686, 1. EPZ031686, applied in the field of pharmaceuticals, can solve problems such as the vascular aging effect of EPZ031686 that has not yet been reported

Inactive Publication Date: 2018-11-02
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 pharmacological effects of EPZ031686 on delaying vascular aging

Method used

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  • Application of compound EPZ031686 in preparing drug for treating vascular aging related diseases
  • Application of compound EPZ031686 in preparing drug for treating vascular aging related diseases
  • Application of compound EPZ031686 in preparing drug for treating vascular aging related diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1 EPZ031686 prevents aging phenotype of rat aortic endothelial cells in vitro

[0024] Grouping: 1×105 rat aortic endothelial cells were seeded into a 6cm culture dish and cultured for 3 days to reach 85-90%, and the cells were synchronized for 6-12 hours. They were randomly divided into 6 groups, namely: ① normal control group; ② model group; ③ EPZ031686 (5 μM) group; ④ EPZ031686 (10 μM) group; ⑤ EPZ031686 (15 μM) group; administration: ③-⑤ adding EPZ031686 with a final concentration of 5 μM, 10 μM, and 15 μM, and culturing for 4 hours; Aging model of arterial endothelial cells; total cell protein was extracted, and the protein levels of aging-related phenotype molecules were measured by Western Blot, including: smyd3, VCAM-1, p21; the experimental data were analyzed by one-way analysis of variance, p<0.05, and the results showed that EPZ031686 could Inhibit the expression of senescence-related genes smyd3, VCAM-1, and p21; use the cell senescence β-galactosida...

Embodiment 2

[0026] Example 2 Experiment of EPZ031686 preventing vascular aging phenotype in mice

[0027] Grouping: Randomly select male C57BL mice aged 8-12W and weighing 22-26g in good condition, and randomly divide them into 6 groups, namely: ① normal control group; ② model group; ③ EPZ031686 (5mg / kg / day) group; ④ EPZ031686 (15mg / kg / day) group; ⑤EPZ031686 (25mg / kg / day) group, after intraperitoneal injection of chloral hydrate anesthesia, use povidone iodine to disinfect the skin, and embed the Mini Pump containing AngⅡ in the mouse scapular incision, AngⅡ with 1.5mg The rate of / kg / day was continuously perfused for 4 weeks, administration: ③-⑤ intraperitoneal injection of EPZ03168650 mg / kg / day every day; after 4 weeks, the mice were routinely treated, the aorta was isolated, and part of it was fixed in 4% paraformaldehyde fixative Among them, the other part was stored in liquid nitrogen for later WB detection. The experimental data were subjected to one-way analysis of variance, p<0.0...

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Abstract

The invention belongs to the field of pharmacy and relates to application of a compound EPZ031686 in preparing a drug for delaying aging and improving vascular aging related diseases. According to theapplication, the result of an in vitro aging model experiment shows that the EPZ031686 inhibits protein expression of aging-related phenotype molecules, so that the activity of a cell aging marker -SA-beta-gal can be reduced, cell proliferation conditions are restored and a regulation mechanism of inhibiting cell aging by the EPZ031686 is defined; the result of an in vivo related disease model experiment shows that the EPZ031686 can inhibit the protein expression of the aging-related phenotype molecule; the EPZ031686 has an obvious effect of delaying aging on the aging-related diseases; furthermore, the compound EPZ031686 and a related inhibitor thereof can be used for preparing the drug for treating vascular aging related diseases.

Description

technical field [0001] The present invention belongs to the field of pharmacy, and relates to the new application of compound EPZ031686 in pharmacy, in particular to the application of compound EPZ031686 and its related inhibitors in the preparation of medicines for treating diseases related to vascular aging. Elderly health. Background technique [0002] Studies have confirmed that vascular aging is the cause of cardiovascular-related diseases such as. One of the important factors of hypertension, atherosclerosis, diabetes, etc., in which aging vascular cells always play an important role in the process of its development. Those skilled in the art believe that interfering with the continuous accumulation of aging vascular cells will effectively prevent vascular aging and the occurrence of cardiovascular related diseases. [0003] The prior art discloses that EPZ031686 is a sulfonamide drug and a non-competitive inhibitor of SMYD3. It has been reported that in vitro, EPZ0...

Claims

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Application Information

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IPC IPC(8): A61K31/4545A61P9/00
CPCA61K31/4545
Inventor 朱依谆刘新华杨迪倪挺
Owner FUDAN UNIV
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