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Application of PPARdelta (Peroxisome proliferator-activated receptor delta) selective antagonist in preparation of drugs for treating psoriasis

An antagonist and selective technology, applied in the field of medicine, can solve the problems of ineffective treatment and inability to treat psoriasis

Inactive Publication Date: 2016-10-12
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report about the application of a PPARδ selective antagonist in the treatment of psoriasis.
[0005] IFN-γ is a TH1-type cytokine, which is highly expressed in psoriasis. Early studies have confirmed that it plays an important role in the development of psoriasis, but studies that inhibit IFN-γ have shown that blocking IFN -gamma does not play a role in the treatment of psoriasis
In addition, PPARδ is related to cardiovascular diseases such as atherosclerosis, but the current clinical efficacy of PPARδ antagonists for the treatment of atherosclerosis is not obvious
Finally, there are still many controversies about the role of PPARδ, such as its pro-proliferation and differentiation effects on keratinocytes

Method used

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  • Application of PPARdelta (Peroxisome proliferator-activated receptor delta) selective antagonist in preparation of drugs for treating psoriasis
  • Application of PPARdelta (Peroxisome proliferator-activated receptor delta) selective antagonist in preparation of drugs for treating psoriasis
  • Application of PPARdelta (Peroxisome proliferator-activated receptor delta) selective antagonist in preparation of drugs for treating psoriasis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1: Expression of PPARδ and its ligand-generated lipase alox8 in psoriatic lesions and IMQ mouse skin

[0034] 1. Experimental method

[0035] 1.1 Expression determination of PPARδ in healthy human skin and psoriatic lesions

[0036] The surgically obtained skin was placed in an appropriate amount of 4% formaldehyde, fixed for 24 hours, and then hyped according to the routine steps of paraffin embedding. For IHC staining, paraffin-embedded sections of 5 mm were washed away in xylene, followed by ethanol gradient elution to de-immobilize. Sections were then placed in citrate and microwaved. Serum was then used as a blocking antibody, incubated at room temperature for 30 minutes, and then incubated with PPARδ primary antibody at 4°C for 10 hours.

[0037] 1.2 Determination of the expression of PPARδ in the skin of WT mice and IMQ mice

[0038]The IHC experiment is the same as the above-mentioned 1.1 Determination of the expression of PPARδ in healthy human skin...

Embodiment 2

[0050] Example 2: Analysis of the curative effect of PPARδ antagonists on IMQ-induced skin psoriasis-like inflammation in mice

[0051] 1. Experimental method

[0052] 1.1 Preparation of GSK3787 solution

[0053] GSK3787 (Shanghai Selleck Company) was pre-dissolved in DMSO, vortexed, and then dissolved in acetone at room temperature to make the final concentration 5uM. The solution was stored in the dark at 4°C and prepared every Monday.

[0054] 1.2 IMQ-induced mouse model preparation, grouping and administration

[0055] FVB / N JCL mice were bred for one week to acclimate to the environment. 24 hours before the experiment, the back of the mice were depilated with depilatory cream. In the GSK group, GSK3787 was given to the hair removal site for 2 consecutive days before IMQ, once a day. IMQ was administered continuously for 6 days, 1 time / day, 50 mg each time. Mice were sacrificed after the last administration. The experiment was divided into blank control group (Vasel...

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Abstract

The invention relates to the technical field of medicine, in particular to application of a PPARdelta (Peroxisome proliferator-activated receptor delta) selective antagonist in preparation of drugs for treating psoriasis. According to the invention, the PPARdelta selective antagonist is used for treating mice psoriasis-like inflammation caused by IMQ, and the result shows that the curative effect of GSK3787 is more significant. According to the invention, the application of the PPARdelta selective antagonist in the treatment of skin diseases is developed, meanwhile the mechanical application of the GSK3787 is extended to the skin field, and a new treatment measure is provided for clinical anti-psoriasis treatment.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a new medical application of a PPARδ selective antagonist. Background technique [0002] Psoriasis is a chronic, inflammatory autoimmune disease that affects about 2-3% of the world's population. Many factors can induce the occurrence of psoriasis. Psoriasis has two major characteristics: hard to recover and easy to relapse, which brings great inconvenience to the treatment of psoriasis. At first, it was thought that psoriasis was caused by an overproliferation of the skin. Later, with the understanding of TH1 cells and IFN-γ, researchers believed that psoriasis is mediated by Th1 cells. Afterwards, people gradually focused on TH17 cells, thinking that it also played a very important role in the occurrence and development of psoriasis. Subsequent clinical drug treatment studies targeting TH17 cells and related cytokines also confirmed that TH17 cell position. [0003] Kerati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/44A61P17/06C12Q1/68
CPCA61K31/44C12Q1/6883C12Q2600/106
Inventor 胡晋红王绪国汪小欢杜秀明赵红霞
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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