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Novel application of glycosyl modified polyphenol compounds

A polyphenolic compound and glycosyl modification technology, which is applied in the direction of effective components of hydroxyl compounds, drug combinations, anti-toxins, etc., can solve the problem that the pathogenesis of pulmonary fibrosis is not completely clear, the disease cannot be fundamentally treated, and the treatment effect is not good, etc. problems, achieve good lung protective function, good anti-oxidation effect, reduce oxidative stress and inflammatory response

Active Publication Date: 2018-04-24
天津海润家和创新医药研究有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the pathogenesis of idiopathic pulmonary fibrosis is not completely clear, and there is a lack of effective treatment methods in clinical practice. Only glucocorticoids are used for symptomatic treatment, but the therapeutic effect is not good, and long-term use has serious side effects [8]
In 2014, the US FDA approved pirfenidone and nintedanib for the treatment of idiopathic pulmonary fibrosis, but these two drugs can only delay the development of the disease, and cannot fundamentally treat the disease [9]

Method used

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  • Novel application of glycosyl modified polyphenol compounds
  • Novel application of glycosyl modified polyphenol compounds
  • Novel application of glycosyl modified polyphenol compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1 Preparation of glycosyl-modified polyphenolic compounds (R=H)

[0049] Take 1.8D-xylose, 9.4g pyrogallic acid, heat to 130°C to melt, stir and react for 24h, purify and separate to obtain 4.0g of glycosyl-modified polyphenol compound (R=H), the yield is 87.0%.

Embodiment 2

[0050] Example 2 Preparation of glycosyl-modified polyphenolic compounds (R=CH 3 )

[0051] Take 3.8g of the glycosyl-modified polyphenol compound (R=H) prepared in Example 1, add 20ml of ethanol, then add 1.4g of anhydrous potassium carbonate and 8.6g of methyl iodide, stir and react at 60°C for 5h, purify and separate to obtain glycosyl-modified 4.0g of polyphenolic compounds (R=CH 3 ), yield 86.4%.

Embodiment 3

[0053] The in vivo experimental process of the glycosyl-modified polyphenol compound obtained in Example 1 of the present invention for treating lung injury in mice caused by acute paraquat poisoning includes the following steps:

[0054] 42 Kunming mice were randomly divided into blank control group, model group (paraquat 300mg / kg), positive control group (paraquat 300mg / kg+vitamin C100mg / kg), low-dose treatment group (paraquat group 300mg / kg+sugar Glycosyl-modified polyphenol compound 200mg / kg), medium-dose treatment group (paraquat group 300mg / kg+glycosyl-modified polyphenol compound 400mg / kg), high-dose treatment group (paraquat group 300mg / kg+glycosyl-modified polyphenol compound 800mg / kg). The paraquat stock solution was diluted with distilled water, administered orally, and the positive control group was intraperitoneally injected with vitamin C injection 24 hours after exposure. Saline solution, the blank control group and the model group were orally gavaged with the...

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Abstract

The invention discloses an application of glycosyl modified polyphenol compounds as drugs for relieving paraquat poisoning and treating pulmonary fibrosis. The glycosyl modified polyphenol compounds have the structure shown in the description. The glycosyl modified polyphenol compounds have a good oxidation resistance function and a lung protection function and have a notable protection function on lung injury caused by paraquat, and a mechanism is related with reduction of formation of oxygen radicals, relieving of oxidative stress and inflammatory reaction, increase of content of GSH in blood serum and SOD in lung tissue and reduction of content of MDA and HYP in lung tissue. The glycosyl modified polyphenol compounds can effectively inhibit bleomycin-induced pulmonary fibrosis of mice,and the mechanism is related with reduction of expression of TGF-beta 1, IL-6, alpha-SMA, P-smad2, type I collagen and type III collagen in lung tissue, increase of content of GSH and SOD in blood serum and reduction of the content of HYP in lung tissue.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to the use of sugar-modified polyphenol compounds for treating paraquat poisoning and pulmonary fibrosis, in particular to the use of xylose-modified pyrogallic acid in preparing medicines for rescuing paraquat poisoning and treating pulmonary fibrosis application. Background technique [0002] Paraquat, whose main component is 1,1'-dimethyl-4,4'-dichlorodipyridine, is a fast-killing herbicide with strong toxicity to humans and animals[1]. According to literature reports [2], oral administration of 7-8ml of paraquat stock solution at a concentration of 20% can cause death, and the mortality rate is as high as 60%-88%, and most of the survivors have acute lung injury and pulmonary interstitial fibrosis , the prognosis is poor. In addition, paraquat poisoning can also damage organs such as the heart, liver, kidney, adrenal gland, central nervous system, skeletal muscle, and sple...

Claims

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Application Information

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IPC IPC(8): A61K31/05A61K31/09A61P11/00A61P39/02
CPCA61K31/05A61K31/09
Inventor 刘天军曹波洪阁
Owner 天津海润家和创新医药研究有限责任公司
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