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Use of sinomenine derivates in treating autoimmune disease through antagonism TNF-alpha signaling pathway

A technology for autoimmune diseases and signaling pathways, applied in allergic diseases, drug combinations, pharmaceutical formulations, etc., can solve the problems of high price, reduced curative effect, and large dosage

Inactive Publication Date: 2009-07-22
SHANGHAI INST OF BIOLOGICAL SCI CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still insurmountable defects in antibody therapy, for example, the dosage is large and the price is expensive; repeated administration is prone to produce neutralizing antibodies, which reduces the curative effect

Method used

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  • Use of sinomenine derivates in treating autoimmune disease through antagonism TNF-alpha signaling pathway
  • Use of sinomenine derivates in treating autoimmune disease through antagonism TNF-alpha signaling pathway
  • Use of sinomenine derivates in treating autoimmune disease through antagonism TNF-alpha signaling pathway

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Preparation of compounds of formula I

[0049] The compound of formula I (code number 1032, which will be used in the following examples) can be obtained by referring to the method of Chinese patent application CN200510024478.9.

Embodiment 2

[0051] Determination of Immunosuppressive Activity of Sinomenine Derivatives

[0052] First, specific mitogens (ConA, LPS) of T cells or B cells were added to the culture system of mouse spleen cells to stimulate the proliferation of T or B cells, and then respectively in different concentration gradients (when measuring the IC50 of the first group of compounds, Select the concentration near the sudden change area of ​​the curve as the gradient, and then when each group of compounds is measured, make corresponding adjustments according to the concentration gradient of the first group) add sinomenine (as shown in formula II, code number 1000, in the following examples) This code will be used) and its derivatives (including 1032 obtained in Example 1), after 48 hours with 3 The H incorporation method was used to measure the proliferation of lymphocytes, and the IC was calculated 50 value to measure its effect on the biological activity of immune cells.

[0053] see results fi...

Embodiment 3

[0056] Determination of Toxicity of Sinomenine Derivatives

[0057] Add sinomenine (as shown in formula II) and its derivatives (including 1032 obtained in Example 1) with different concentration gradients in the culture system of mouse spleen cells, add MTT (thiazolium) in 42 hours, 48 The reaction was terminated after 1 hour, and the OD value was measured with a spectrophotometer, and the CC50 value was calculated by the following formula to characterize the toxicity. Taking sinomenine as a control, the levels of each derivative relative to sinomenine were observed.

[0058]

[0059] see results figure 2 .

[0060] The results showed that the toxicity of several derivatives was significantly lower than that of sinomenine (code 1000), and their safety was better.

[0061] Based on the data in Examples 1 and 2, compound 1032 with high activity and low toxicity was selected from many derivatives for the following curative effect and mechanism research.

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Abstract

The invention discloses application of sinomenine derivatives in the treatment of autoimmune diseases by antagonizing a TNF-alpha signaling pathway, namely application of the sinomenine derivatives shown in a formula I, wherein the sinomenine derivatives can be used for preparing a composition for preventing or treating the autoimmune diseases. The invention also discloses application of a compound shown in the formula I in preparation of a tumor necrosis factor-alpha (TNF-alpha) signaling pathway inhibitor composition.

Description

technical field [0001] The present invention relates to the field of medicine. More specifically it relates to the use of sinomenine derivatives. Background technique [0002] Autoimmune disease has become a serious disease that directly threatens human life and health and affects the quality of life because of its high incidence and no effective treatment. For example: the incidence of rheumatoid arthritis (Rheumatoid Arthritis, RA) in the general population in my country is as high as 0.35-0.4%, and there is an increasing trend year by year. RA is an organ-specific autoimmune disease. The lesions mainly involve the large and small joints of the whole body, eventually leading to joint ankylosis and loss of self-care ability. Similarly, ankylosing spondylitis and systemic lupus erythematosus seriously endanger human health because there is no effective treatment. [0003] Basic research and clinical observations have shown that Th1 cell-mediated cellular immunity and Th2 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4985A61P37/02
Inventor 孙兵姚祝军邹嘉周海滨马钊
Owner SHANGHAI INST OF BIOLOGICAL SCI CHINESE ACAD OF SCI
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