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Usage of eleutheroside with anti-inflammatory action or aglycone thereof

A technology of aglycone and inflammation, which is applied in the field of medical application of arachnid and its aglycone, which can solve the problems of lagging intervention methods and unsatisfactory curative effect of liver failure

Inactive Publication Date: 2010-02-24
CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since TNF-α is an early inflammatory cytokine, the effect of TNF-α reaches the first peak within 1 hour after being stimulated by LPS, etc., and the intervention method often lags behind. Therefore, the clinical application of anti-TNF-α antibody in the treatment of liver failure has not been ideal. Efficacy

Method used

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  • Usage of eleutheroside with anti-inflammatory action or aglycone thereof
  • Usage of eleutheroside with anti-inflammatory action or aglycone thereof
  • Usage of eleutheroside with anti-inflammatory action or aglycone thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1: Cytotoxicity of Target Drugs

[0046] EZ4U Cell Proliferation and Cytotoxicity Analysis Kit found that both formulas I and II have certain toxic effects on cells. Wherein, formula II is highly toxic to cells, and has an influence on the growth of RAW 264.7 cells when it is greater than 30 μM. The results are shown in figure 1 shown.

Embodiment 2

[0047] Example 2: Effects on RAW 264.7 TNF-α, IL-1β secretion

[0048] ELISA detection of RAW 264.7 medium supernatant revealed that both formulas I and II could reduce the secretion of TNF-α and IL-1β, and within a certain range, they were all in a dose-dependent manner. The specific results are shown in Tables 1-2 below.

[0049] Table 1 ELISA detection of TNF-α, IL-1β levels in Acankoreanogenia A intervention group RAW 264.7 medium supernatant (mean±SD)

[0050]

[0051] LPS - Indicates that no LPS was added to the culture medium, LPS + Indicates the addition of LPS with a final concentration of 100ng / ml in the culture medium. * p, ** P+ Group.

[0052] Table 2 ELISA detection of TNF-α and IL-1β levels in Acankoreoside A intervention group RAW 264.7 medium supernatant (mean±SD)

[0053]

[0054] LPS - Indicates that no LPS was added to the culture medium, LPS + Indicates the addition of LPS with a final concentration of 100ng / ml in the culture medium.

[0055...

Embodiment 3

[0056] Example 3: Effects on RAW 264.7HMGB1 secretion

[0057] The results reflect that both formulas I and II can inhibit the secretion of HMGB1 in a dose-dependent manner within a concentration range of less than 30 μM. For specific results, see figure 2 .

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PUM

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Abstract

The invention relates to a medical usage of eleutheroside and the aglycone thereof, in particular to the application of the glycoside with the following formula I or the aglycone with the formula II in the preparation of the drugs for the diseases caused by inflammatory mediators, wherein, the inflammatory mediators are HMGB1, TNF-Alpha or IL-1 particularly. The glycoside of R1 R2 R3 R4 formula Iis: H COOH H-Beta-D-glc6-Beta-D-glc4-Alpha-L-rha, and the aglycone of formula II is: H COOH H H.

Description

technical field [0001] The present invention relates to the medical use of araquinoside and its aglycone, more specifically, the application of the glycoside represented by the following formula I or the aglycone represented by formula II in the preparation of medicines for diseases caused by inflammatory mediators. [0002] [0003] R1 R2 R3 R4 [0004] Glycoside of formula I: HCOOHH-β-D-glc6-β-D-glc4-α-L-rha [0005] Aglycone of formula II: H COOH H H Background technique [0006] High mobility group box chromosomal protein 1 (HMGB1) is one of the members of the high mobility group box superfamily and is an abundant non-histone nuclear protein. It consists of 214 amino acids, has the function of regulating transcriptional activity, and can promote cell proliferation. HMGB1 becomes an inflammatory mediator, can interact with various inflammatory mediators, participates in the pathogenesis of sepsis, and is an important inflammatory mediator in the late sta...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/704A61K31/56A61K38/17A61K38/19A61K38/20A61P1/16A61P17/02A61P29/00A61P31/00A61P31/20
Inventor 范学工刘洪波刘向前
Owner CENT SOUTH UNIV
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