Application of genipin amino acid derivative as NF-kappa B inhibitor

A technology of amino acids and derivatives, applied in the field of application of genipin amino acid derivatives as NF-κB inhibitors, achieving good medicinal prospects, easy promotion, and significant curative effect

Active Publication Date: 2013-07-10
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Genipin amino acid derivatives have not been reported to inhibit NF-κB activity except ...

Method used

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  • Application of genipin amino acid derivative as NF-kappa B inhibitor
  • Application of genipin amino acid derivative as NF-kappa B inhibitor
  • Application of genipin amino acid derivative as NF-kappa B inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0259] Example 1 Preparation of Genipin Amino Acid Derivatives

[0260] Genipin amino acid derivatives were prepared according to the method of Fujikama et al. (Fujikama S, Fukui Y, Koga K, Kumada J. (1987) Brilliant skyblue pigment formation from Gardenia fruits. Journal of Fermentation Technology 65:419-424).

[0261] Add 8.8mmol of genipin and 8.8mmol of amino acid to 400mL of PBS (100mmol, pH7.0) solution successively, stir at 80°C for 4h, then pass the obtained genipin amino acid derivative through HP-20 macroporous resin column , separate, and collect the eluate with an absorbance value of 590nm, and dry the collected eluate with a freeze dryer to obtain the finished product of genipin amino acid derivative. The obtained genipin amino acid derivatives are sealed and kept in cold storage at 2-8°C until use.

[0262] Genipin can react with amino acids containing primary amino groups to generate genipin amino acid derivatives of the present invention, such as alanine, vali...

Embodiment 2

[0263] Example 2 Preparation of Genipin Glycine Derivatives

[0264] Add 8.8mmol of genipin and 8.8mmol of glycine to 400mL of PBS (100mmol, pH7.0) solution successively, stir at 80°C for 4h, then pass the obtained genipin glycine derivative through HP-20 macroporous resin column , using a mixed solution of ethyl acetate, methanol, and water as the eluent for elution and separation, wherein the volume ratio of ethyl acetate-methanol-water in the eluent is: 8:3:1, and the eluate is collected. And carry out freeze dryer drying to obtain the finished product of genipin glycine derivative. The obtained genipin glycine derivatives are stored in a refrigerator and sealed at 2-8°C until use.

Embodiment 3

[0265] Example 3 Preparation of Genipin Tyrosine Derivatives

[0266] Add 8.8mmol of genipin and 8.8mmol of tyrosine to 400mL of PBS (100mmol, pH7.0) solution successively, stir at 80°C for 4h, then pass the obtained genipin tyrosine derivative through HP-20 Macroporous resin column, using a mixed solution of ethyl acetate, methanol, and water as the eluent for elution and separation, wherein the volume ratio of ethyl acetate-methanol-water in the eluent is: 8:3:1, collected The eluate is dried in a freeze dryer to obtain the finished product of genipin tyrosine derivative. The obtained genipin tyrosine derivatives are stored in a refrigerator and sealed at 2-8°C until use.

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Abstract

The invention discloses application of a genipin amino acid derivative as an NF-kappa B (nuclear transcription factor kappa-B) inhibitor. The genipin amino acid derivative as the NF-kappa B inhibitor controls the expression of various inflammatory cytokines, major histocompatibility composite gene and adhesion molecules, which participate in the tumor metastasis, and restrains and treats pathological symptoms caused by NF-kappa B activation by blocking the nuclear factor NF-kappa B activation, wherein the symptoms include cancer, autoimmune diseases (such as rheumatoid arthritis), cardiovascnlar and cerebrovascular diseases, acute and chronic inflammations, nervous system disorders (depression, Alzheimer's disease, etc.). The genipin amino acid derivative can restrain the NF-kappa B activity in a dose and time-dependent manner. The invention provides a novel drug source for NF-kappa B inhibitors and NF-kappa B control related diseases.

Description

technical field [0001] The present invention relates to a drug or health food used as an NF-κB inhibitor for preventing, alleviating and / or treating emotional disorders, nervous system diseases (depression) and chronic and acute inflammation, especially for treating NF-κB Drugs or health foods related to abnormal activation of -κB. Background technique [0002] Nuclear transcription factor-κB (nuclear transcription factor kappa-B, NF-κB) was first discovered in B cell nuclear extracts and can specifically bind to the enhancer κB sequence (GGGACTTTCC) of the immunoglobulin κ light chain gene. Protein factor, thus called NF-κB. Under normal physiological conditions, NF-κB is combined with the inhibitory protein factor IκB (Inhibitor ofκB) in the cytoplasm and is in an inactive state. [0003] When exogenously stimulated, IκB kinases (IKK, including IKKα and IKKβ) are activated and can phosphorylate the inhibitory protein factor IκB at specific sites of amino acid terminal se...

Claims

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Application Information

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IPC IPC(8): A61K31/435A61P35/00A61P37/00A61P9/00A61P29/00A61P25/00A61P25/24A61P25/28A61P19/02A23L1/305
Inventor 崔元璐王强松胡利民高秀梅田俊生王跃飞
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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