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Use of propargyl cysteine and analogue thereof in preparation of drug for treating immunity-related inflammation diseases

A cysteine, inflammatory disease technology, used in drug combinations, allergic diseases, antipyretics, etc., can solve problems such as related diseases that have not yet been seen

Inactive Publication Date: 2013-09-11
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] But so far, there is no report about activating PPAR-γ to regulate immune inflammatory response and treat related diseases caused by inflammatory response

Method used

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  • Use of propargyl cysteine and analogue thereof in preparation of drug for treating immunity-related inflammation diseases
  • Use of propargyl cysteine and analogue thereof in preparation of drug for treating immunity-related inflammation diseases
  • Use of propargyl cysteine and analogue thereof in preparation of drug for treating immunity-related inflammation diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The effect of SPRC on the release of chemokines from mouse peritoneal macrophages and mouse RAW264.7 macrophages

[0046] ①H 2 Effect of S Donor SPRC on the Release of Inflammatory / Inducible Chemokines from Mouse Macrophages

[0047] Through the study of primary macrophages and mouse RAW264.7 macrophages, different concentrations of SPRC (1μM, 50μM, 100μM, 200μM) were cultured for different times, supernatants were collected at different time points, and MIP was detected by ELISA -1α and MIP-1β levels; With the prolongation of culture time, the levels of MIP-1α and MIP-1β released by resting cells increased continuously, indicating that these chemokines are spontaneously secreted, and SPRC can be dose- and time-dependent. Inhibition of MIP-1α and MIP-1β secretion.

[0048] The results showed that SPRC could significantly inhibit the spontaneous secretion of MIP-1α and MIP-1β from RAW264.7 macrophages;

[0049] ②The effect of SPRC on the release of chemokines from pri...

Embodiment 2

[0053] Effects of SPRC on cytokine release from mouse peritoneal macrophages and mouse RAW264.7 macrophages

[0054] Based on the results of the above-mentioned Example 1, whether SPRC affects the release of pro-inflammatory cytokines and anti-inflammatory cytokines is detected; the results show that different depths of SPRC (1 μM, 50 μM, 100 μM, 200 μM) cultivate RAW264. 18h, 24h), TNF-α, IL-1β, IL-6 and IL-10 levels in the supernatant were measured by ELISA; SPRC (1μM, 50μM, 100μM) can promote the secretion of IL-10 in a time-dependent manner (such as image 3 A, B shown); SPRC (100μM) can significantly promote IL-10 (as shown in image 3 C) and IL-6 (as Figure 4 A) release, while SPRC (1 μM, 50 μM, 100 μM, 200 μM) can significantly reduce the secretion of TNF-α and IL-1β.

Embodiment 3

[0055] Embodiment 3SPRC improves mouse RAW264.7 macrophage STAT-3 transcriptional activity

[0056] By detecting the effects of transcription factors NF-κB, STAT-3 and AP-1 on the release of cytokines and chemokines by SPRC, the results showed that SPRC (1μM, 50μM, 100μM, 200μM) was cultured with RAW264.7 cells for 24h, extracted Nucleoprotein DNA binding experiments showed that SPRC (100 μM) could significantly increase the transcriptional activity of STAT3, but had no effect on the transcriptional activities of NF-κB and AP-1 (such as Figure 6 A, B, C shown).

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Abstract

The invention belongs to the pharmaceutical field and relates to a use of propargyl cysteine and an analogue thereof in preparation of a drug for treating immunity-related inflammation diseases. The propargyl cysteine and the analogue thereof can be used for treating the related diseases caused by inflammation by activating the expression of peroxide roliferator-activated receptor-gamma. According to the in-vitro cell experiment result, the propargyl cysteine can be used for treating the immunity-related inflammation diseases by activating the peroxide roliferator-activated receptor-gamma, relieving the inflammatory response of macrophage and macrophage system RAW 264.7 cell, increasing the expression of cystathionine-gamma-lyase in the cell, promoting the generation of anti-inflammatory factor interleukin-10 and restraining the effects of tumor necrosis factor-alpha, macrophage inflammatory protein-1alhpa and macrophage inflammatory protein-1beta.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to the new application of propargyl cysteine ​​and its analogs in pharmacy, in particular to the application of propargyl cysteine ​​and its analogs in the preparation of medicines for treating immune-related inflammatory diseases. Background technique [0002] At present, studies have found that peroxisome proliferator-activated receptor-γ (PPAR-γ) acts as a ligand to activate nuclear receptors to regulate lipid and glucose metabolism, and PPAR-γ can negatively regulate inflammatory responses; Negative regulation of inflammatory responses antagonizes the effects of transcription factors NF-κB and AP-1 through transcriptional repression. [0003] It has been reported that diallyl disulfide (DADS), a fat-soluble component in garlic, can increase the expression of PPAR-γ in 3T3-L1 preadipocytes; h 2 S has a protective effect on cardiovascular. The propargyl cysteine ​​(SPRC) and its analogs i...

Claims

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Application Information

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IPC IPC(8): A61K31/198A61P37/02A61P29/00
Inventor 朱依谆马达夫·巴提亚
Owner FUDAN UNIV
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