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Application of propargyl cysteine and analogues thereof in preparation of medicaments for preventing and treating diseases related to cardiovascular system inflammation

A technology for cysteine ​​and inflammatory diseases, applied in cardiovascular system diseases, drug combinations, pharmaceutical formulations, etc., can solve the problems of uncontrollable dosage and volatility

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

It has been reported that sodium hydrosulfide inhibits cardiovascular inflammatory response, but sodium hydrosulfide t 1 / 2 Too short, volatile, unable to control the dosage; and propargyl cysteine ​​and its analogs can exert a protective effect on cardiovascular by releasing hydrogen sulfide
[0004] However, so far, there have been no reports on the effects of propargyl cysteine ​​and its analogues on cardiovascular system inflammatory diseases, including coronary heart disease, atherosclerosis, etc.

Method used

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  • Application of propargyl cysteine and analogues thereof in preparation of medicaments for preventing and treating diseases related to cardiovascular system inflammation
  • Application of propargyl cysteine and analogues thereof in preparation of medicaments for preventing and treating diseases related to cardiovascular system inflammation
  • Application of propargyl cysteine and analogues thereof in preparation of medicaments for preventing and treating diseases related to cardiovascular system inflammation

Examples

Experimental program
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Effect test

Embodiment 1

[0029] Example 1 The protective effect of propargyl cysteine ​​on the inflammatory response of rat H9c2 cardiomyocytes in vitro

[0030] Grouping: Divide 1×10 5 Cardiomyocytes 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 low dose of propargyl cysteine ④ medium-dose propargyl cysteine ​​group; ⑤ high-dose propargyl cysteine ​​group; ⑥ instrumental medicine group (PAG or LY). Administration: ③-⑤ Add propargyl cysteine ​​with a final concentration of 0.01 μM, 0.10 μM, 1 μM, ⑥ PAG or LY was administered for 30 minutes in advance, and SPRC was incubated for 30 minutes. LPS (10 μg / ml) was added to culture to induce the inflammatory response of H9c2 cardiomyocytes; mRNA was extracted, and the transcription levels of inflammation-related genes were determined by RT-PCR; the determined inflammation-related genes: tum...

Embodiment 2

[0031] Example 2 Effect of propargyl cysteine ​​on the regulation mechanism of inflammatory response in rat H9c2 cardiomyocytes in vitro

[0032] Grouping: Divide 1×10 5 A H9c2 cardiomyocyte was planted 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 low propargyl cysteine dosage group; ④ medium-dose propargyl cysteine ​​group; ⑤ high-dose propargyl cysteine ​​group; ⑥ instrumental medicine group. Administration: ③-⑤ Propylcysteine ​​was added at a final concentration of 0.01 μM, 0.10 μM, and 1 μM, ⑥ PAG or LY was administered for 30 minutes in advance, and SPRC was incubated for 30 minutes. After adding LPS body (10μg / ml) for 15min, the cell protein was collected, and Western blotting was used to measure the activation of ERK1 / 2Akt, MAPK and NF-κB p65. The results showed that propargyl cysteine ​​inhibited the effect of LPS...

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Abstract

The invention belongs to the field of pharmacy, and relates to the application of propargyl cysteine and analogues thereof in preparation of medicaments for preventing and treating diseases related to cardiovascular system inflammation. Through in-vitro cell experiments, the results show that the propargyl cysteine and the analogues thereof can inhibit the expression of the mRNA and the protein of tumor necrosis factor alpha, interleukin-1beta and monocyte chemoattractant protein-1, increase the content of hydrogen sulfide in myocardial inflammation tissues, inhibit the expression of the mRNA of inducible nitric oxide synthase, cyclooxygenase-2 and intercellular adhesion molecule-1 related to the myocardial cells expressed inflammation, inhibit the activation of pathways ERK1 / 2 and NF-kB related to the inflammation in the myocardial cells, activate protein kinase B (Akt), and inhibit the production of oxygen free radicals in the myocardial cells, and can be prepared into the treatment medicaments for treating the diseases, such as ischemic heart disease, atherosis or myocardial infarction, related to the cardiovascular system inflammation.

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 preparation of propargyl cysteine ​​and its analogs in the preparation of drugs for preventing and treating inflammation-related diseases of the cardiovascular system purposes; the cardiovascular system inflammation-related diseases, including atherosclerosis and inflammation-related diseases. Background technique [0002] Cardiovascular disease is one of the leading causes of death in developed and developing countries in recent years; such diseases include atherosclerosis, coronary heart disease, etc. At present, studies have confirmed that inflammation is one of the primary pathogenic factors of cardiovascular diseases, and inflammatory responses always play an important role in the development and prognosis of cardiovascular diseases; therefore, interfering with immune-related inflammatory resp...

Claims

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Application Information

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IPC IPC(8): A61K31/198A61P9/10
Inventor 朱依谆潘礼龙刘新华龚其海
Owner FUDAN UNIV
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