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Application of jzy-13 and compound in preparation of medicament for treating psoriasis

A compound and technology for psoriasis, which is applied in the field of pharmaceuticals for the treatment of psoriasis, can solve the problems of insufficient and insufficient keratinocytes, and achieve good market prospects

Active Publication Date: 2021-07-09
山东君瑞医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, there are not many studies on keratinocytes at present, and the methods for treating psoriasis are not enough, and there is room for continuous improvement and research

Method used

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  • Application of jzy-13 and compound in preparation of medicament for treating psoriasis
  • Application of jzy-13 and compound in preparation of medicament for treating psoriasis
  • Application of jzy-13 and compound in preparation of medicament for treating psoriasis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1 Isolation and culture of keratin forming cells

[0022] Take the leather tissue after menopausculectomy, immediately put it in PBS with gentamicin, amphotericin, and then remove blood after surgery. In advance, the horny formation of HKGS, chimmycin / amphotericin (500x) is added, and the tissue is placed in the culture medium, remove skin tissue, cutting the skin tissue into small pieces, about 5mm x5mm, plus DISPASE II Enzyme (1.2U / mL) is 4 ° C to prevent light overnight; the epidermis and leather were separated, and the epidermal was digested with 0.5% pancreatic enzyme at 37 ° C, and the time was about 5-lomin, and the DMEM medium containing 10% serum was digested. The 200 mesh is ground, filtered, centrifuged, and PBS washed twice, using antibiotic epidermal cell culture medium retransmitted, paving; 3-4 days of cells can be attached, fibroblasts are not growing in epidermal medium, The epithelial cells are gadily in the formation, and the cell fusion reach...

Embodiment 2

[0023] Example 2 Preparation of keratin forming cell inhibitor compounds

[0024] Usopine (48.1 g, 0.211 mol), dimethyl-N, N-diethyl amino phosphate (34.82 g, 0.211 mol), a mixture of dried tetrahydrofuran (1250 mL) was heated to 35 ° C to prepare a transparent solution, and 1H-tetrazole (44.25 g, 0.632 mol) was added at a time at 27 ° C, and then stirred at room temperature (22 ° C) for 1 hour. After the addition of phosphite dimethyl esters were confirmed by TLC, a acetone-dry ice was cooled with acetone-dry ice, and an aqueous solution (84 ml, 0.607 mol) of 70% tert-butyl hydroperoxide was added dropwise therein. The ice bath was removed, gradually warmed to room temperature, and TLC was subjected to TLC to confirm the disappearance of the phosphite and the production of phosphoric acid dimethyl, and then the reaction was terminated with aqueous solution of 10% sodium sulfite at 0 ° C. Ethyl acetate (1250 mL) was added to the reaction solution and the organic layer was separate...

Embodiment 3

[0025] Example 3 Oral forming cell inhibitor polypeptide screening

[0026]Phage random 12 peptide kit kit (Ph.D.TM-12PHAGE DISPLAY PEPTIDE LIBRARY KIT) was purchased from NEW ENGLAND BIOLABS, and the host bacteria were E.COLI ER2738.

[0027] Random doubral peptide phage display library biometric screening: Pretreatment of microplate using 0.1 mol / L Multi-lysine, 1) Package: Oral forming cells prepared by Example 1 1 × 10 6 The / ml package was overnight by a microplate, a wet cartridge in a 4 ° C, and then added to the fixed liquid (glutaraldehyde), then washed 3 times; 2) binding: blocking buffer [0.1 mo l / lnahco 3 (pH8.6), 5mg / ml BSA, 0.02% NaN 3 [Closed, TBST washing board 6 times, 10 μL of the original library was diluted with 90 μl of TBST, and the microporous was added, and the temperature was mild and shaken for 60 min. 3) Elution: Turn off the liquid, wash the plate 10 times, add 0.2 mol / l glycine-hydrochloric acid buffer (pH2.2) 100 μl / hole, and shake the room...

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Abstract

The present invention relates to the use of JZY-13 and compounds in the preparation of medicaments for treating psoriasis. The combination of JZY-13 and compounds can synergistically inhibit the proliferation of keratinocytes, which has a good effect. Through the mouse model It has also been proved that the combination of drugs has the effect of treating psoriasis, and has a good market prospect.

Description

Technical field [0001] The present invention relates to the use of the pharmaceutical field, and specific applications involving JZY-13 and the compounds in the preparation of a medicament for the treatment of psoriasis. Background technique [0002] Psoriasis, commonly known as psoriasis, histopathological manifestation is mainly expressing cytoplasses underwent hypercapsulation, dermal layer capillary hyperplasia, expansion, inflammatory cell infiltration, the most common clinical manifestation is red or pink Plaque, scales, etc. Psoriasis is about 3% of the world's population. The disease is higher in European chhassiasis, 0.75% ~ 2.9%, with an average of 2%, more than 2% in the United States, most countries in Asia <1%, China in 1984 national survey results of 0.123%, Zhang Jianzhong equals ( In 2007 ~ 2008, the disease rate of psoriasis of six urban residents in mainland China was investigated, and the result was 0.47%. The prevalence of mainland China and Taiwan has incr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/661A61K38/10A61P17/06
CPCA61K31/661A61K38/10A61P17/06A61K2300/00
Inventor 张海涛王青
Owner 山东君瑞医药科技有限公司
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