Application of Asteraceae cyclopeptides as cGAS-STING (stimulator of interferon genes) signal channel inhibitor

A signaling pathway and compound technology, which is applied in the application of Compositae type cyclic peptides as cGAS-STING signaling pathway inhibitors, and the application field in the preparation of medicines for treating related diseases, can solve the problems of low extraction efficiency, poor repeatability and controllability, The complex process and other problems have achieved the effect of diversifying dosage forms and medication methods and wide clinical application prospects.

Active Publication Date: 2017-11-10
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these methods generally have disadvantages such as low extraction efficiency, complicated process, large sample loss, poor repeatability and controllability.

Method used

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  • Application of Asteraceae cyclopeptides as cGAS-STING (stimulator of interferon genes) signal channel inhibitor
  • Application of Asteraceae cyclopeptides as cGAS-STING (stimulator of interferon genes) signal channel inhibitor
  • Application of Asteraceae cyclopeptides as cGAS-STING (stimulator of interferon genes) signal channel inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Preparation of Asteraceae type cyclic peptide compounds Astins A-H (1-8) and Astins K-P (9-14): (see the preparation method flow process figure 1 shown)

[0032] Take aster (Aster tataricus L.) dry root and rhizome 10Kg, after drying, pulverizing and soaking in methanol overnight, extract with methanol hot reflux, a total of three extractions, 4 hours for the first time, 4 hours for the second time, 3 hours for the third time hours, the combined extracts were concentrated under reduced pressure to obtain 4.6Kg of methanol extract. The extract was subjected to silica gel column chromatography, eluted with chloroform / methanol (100:0, 9:1, 8:2, 7:3, 1:1, 0:100) gradient elution, and combined with cyclic peptide TLC detection method containing Each fraction of the cyclic peptide was used to obtain the total cyclic peptide part (212.6g); each of the following processes must be combined with the cyclic peptide TLC detection method to guide the separation and purification. T...

Embodiment 2

[0034] The Asteraceae-type cyclic peptide compounds Astins A-H (1-8) and Astins K-P (9-14) prepared in Example 1 were tested in MEF cells for their effects on the expression of genes downstream of the cGAS-STING signaling pathway activated by DNA analogue ISD stimulation. The experimental principles, methods and results are as follows:

[0035] Experimental principle: In the innate immune signal transduction pathway, the cGAS-STING signaling pathway can recognize foreign DNA pathogenic microorganisms that invade the body. Exogenous DNA stimulation can induce the expression of downstream type I interferon genes and interferon-stimulated genes. Therefore, under the stimulation of exogenous DNA (DNA analogue ISD), the activation of the cGAS-STING signaling pathway can be reflected by detecting the expression of the downstream genes IFNβ, IFNα4 and CXCL10, so as to evaluate the effect of the compound on the activation of the cGAS-STING signaling pathway.

[0036] Experimental met...

Embodiment 3

[0040] Example 1 The effect of Astin C (3), a composite cyclic peptide compound prepared in Example 1, on the expression of IFNβ protein in mouse serum induced by HSV-1.

[0041] Experimental principle: The expression of IFNβ protein in the body is a marker event of the innate immune anti-infection response. After the expression of IFNβ, it can activate the interferon receptor (IFNR) signal transduction pathway to induce the expression of cytokines and inflammatory factors such as interferon-stimulated genes, and then By recruiting NK cells or further activating molecular mechanisms such as adaptive immune responses, the invading pathogenic microorganisms are eventually cleared. Therefore, after DNA virus HSV-1 infects mice, the activation of the body's anti-innate anti-infection immune response can be reflected by detecting the expression of IFN-β in the mouse serum, thereby evaluating the effect of the compound on the body's innate anti-infection immune response. influences....

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Abstract

The invention discloses an application of Asteraceae cyclopeptides or pharmacologically admissible salts thereof as a cGAS-STING (stimulator of interferon genes) signal channel inhibitor as well as an application of the Asteraceae cyclopeptides or the pharmacologically admissible salts thereof as the cGAS-STING signal channel inhibitor to preparation of drugs for treating cGAS-STING signal channel abnormally activated diseases. The Asteraceae cyclopeptides are natural compounds, adopt diverse forms and administration ways and have extensive clinical application prospect.

Description

technical field [0001] The invention belongs to the pharmaceutical technology, and in particular relates to the application of a compositae type cyclic peptide as cGAS-STING signaling pathway inhibitor, and its application in the preparation of drugs for treating related diseases. Background technique [0002] Innate immunity is the first line of defense of the host's immune system. In the long process of biological evolution, the pattern recognition receptors in host cells can recognize the conserved components of invading pathogenic microorganisms, such as nucleic acid molecules, LPS, etc., and sense the invasion of pathogenic microorganisms, and the infection signal passes through the downstream linker Proteins, kinases, and transcription factors deliver, induce the expression of type I interferons and pro-inflammatory cytokines, and ultimately clear invading pathogenic microorganisms. Over the past few decades, studies have analyzed in detail the signal transduction mec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/12A61P29/00A61P35/00A61P37/02A61K36/28
CPCA61K36/28A61K38/12
Inventor 谭宁华王琛汪哲李森林徐会敏宋立华
Owner CHINA PHARM UNIV
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