Application of amino acid modified amino tetraphenylporphyrin compound in prevention and treatment of fibrosis

An aminotetraphenylporphyrin, amino acid technology, applied in the field of medicine, can solve the problems of poor prognosis of patients, lack of treatment methods, and high mortality

Pending Publication Date: 2021-11-12
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

With the continuous development of industrialization, the incidence of pulmonary fibrosis is increasing year by year, but due to the lack of effective treatment methods, the prognosis of patients is poor and the mortality rate is high, which seriously affects human health.

Method used

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  • Application of amino acid modified amino tetraphenylporphyrin compound in prevention and treatment of fibrosis
  • Application of amino acid modified amino tetraphenylporphyrin compound in prevention and treatment of fibrosis
  • Application of amino acid modified amino tetraphenylporphyrin compound in prevention and treatment of fibrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Embodiment 1 Amino acid modified amino tetraphenyl porphyrin compound (LD 4 )Synthesis

[0048] Boc-Lys(Boc)-OH (467.67mg, 1.35mmol) was placed in the reaction flask, N 2 Add dry THF 20ml under protection, and stir with a magnet. Cool to -17°C, add triethylamine (197.60 μl, 1.42 mmol) and ethyl chloroformate (131.10 μl, 1.38 mmol) to react for 1 h, a white precipitate is formed, filter and discard the precipitate. Tetraaminoporphyrin (202.40mg, 0.30mmol) was dissolved in 15ml THF, the above filtrate was added, and the reaction was stirred at room temperature for 14h. TLC (dichloromethane:methanol:ammonia=60:1:0.6) monitored the progress of the reaction. After the reaction was complete, the reaction solution was poured into ice water to precipitate a precipitate, which was filtered and washed three times with water to obtain a purple solid. Finally, separation by column chromatography (eluent: dichloromethane: methanol: ammonia water = 30:1:0.4) yielded 596.13 mg of ...

Embodiment 2

[0050] Embodiment 2 Amino acid modified aminotetraphenylporphyrin compound (LD 4 ) to prevent and treat intestinal fibrosis

[0051] Amino acid-modified aminotetraphenylporphyrin compound LD prepared in Example 1 of the present invention 4 The in vivo experimental process of treating dextran sodium sulfate (DSS)-induced intestinal fibrosis in mice comprises the following steps:

[0052] The normal group of C57BL / 6J mice drank purified water, and the rest of the groups drank 1.5% DSS water for one week, purified water for two weeks, followed by 2% DSS water for one week for two weeks, and then circulated 2% DSS water for one week to establish Intestinal fibrosis model. The mice were randomly divided into 6 groups, 10 in each group, and the treatment method was as follows: 1.Control group (normal saline); 2.DSS group (DSS drinking water); 3.LD 4 -PDTL group (DSS drinking water and low-dose LD 4 60μg / kg enema); 4.LD 4 -PDTM group (DSS drinking water and medium dose LD 4 1...

Embodiment 3

[0061] Embodiment 3 Amino acid modified aminotetraphenylporphyrin compound (LD 4 ) to prevent and treat intestinal fibrosis

[0062] Amino acid-modified aminotetraphenylporphyrin compound LD prepared in Example 1 of the present invention 4 The in vivo experimental process of treating trinitrobenzenesulfonic acid (TNBS)-induced intestinal fibrosis in rats comprises the following steps:

[0063] Rats were fasted for 24 h before model induction and anesthetized with 10% chloral hydrate. Intestinal fibrosis model was established by injecting 150 mg / kg TNBS into the colon of rats with a 3 mm diameter polyethylene rubber catheter (inserted 8 cm proximal to the anorectum). The rats were randomly divided into 6 groups, 6 in each group, and the treatment method was as follows: 1.Control group (normal saline); 2.TNBS group (TNBS enema); 3.LD 4 -PDTL group (TNBS and low-dose LD 4 , 60μg / kg, both enema); 4.LD 4 -PDTM group (TNBS and medium dose LD 4 , 120μg / kg, both enema); 5.LD 4 ...

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Abstract

The invention discloses application of an amino acid modified amino tetraphenylporphyrin compound in prevention and treatment of intestinal fibrosis and pulmonary fibrosis. The amino acid modified amino tetraphenylporphyrin compound has the following structure: experiments prove that the amino acid modified amino tetraphenylporphyrin compound can obviously relieve colonic inflammation and fibrosis degree and inhibit secretion and deposition of collagen in colonic tissues in a large and small mouse intestinal fibrosis model constructed by photodynamic therapy of sodium dextran sulfate and trinitrobenzene sulfonic acid, and inhibit epithelial-mesenchymal transition degree by inhibiting expression of AOC1 so as to prevent and treat intestinal fibrosis. The amino acid modified amino tetraphenylporphyrin compound can obviously relieve lung tissue inflammation and fibrosis degree in a small mouse pulmonary fibrosis model constructed by photodynamic therapy of bleomycin so as to prevent and treat pulmonary fibrosis.

Description

technical field [0001] The invention belongs to the field of medicines, in particular to the use of amino acid modified aminotetraphenylporphyrin compounds for preventing and treating intestinal fibrosis and pulmonary fibrosis, in particular to the use of four lysine modified aminotetraphenylporphyrin compounds in the preparation of anti-inflammatory drugs. Intestinal fibrosis and application of anti-pulmonary fibrosis drugs. Background technique [0002] Intestinal fibrosis is an overactive, irreversible injury-healing response to chronic inflammation and injury in the gut. Repeated infiltration of a large number of chronic inflammatory cells will lead to abnormal accumulation of extracellular matrix (ECM) and massive proliferation of interstitial cells, resulting in intestinal fibrosis [1,2] . Intestinal fibrosis is a common complication of inflammatory bowel disease, and its prevalence is significantly higher in Crohn's disease than in ulcerative colitis. Intestinal wa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61P11/00
CPCA61K41/0071A61P11/00A61P1/00
Inventor 刘天军荣玉美朱娜洪阁
Owner 天津海润家和创新医药研究有限责任公司
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