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Application of evodiamine in preparing medicine for inhibiting aryl hydrocarbon receptor

An aromatic hydrocarbon receptor and evodiamine technology, which can be used in drug combinations, antipyretics, antitumor drugs, etc., and can solve problems such as influence

Inactive Publication Date: 2011-03-30
THE THIRD AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIV OF PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, whether evodiamine will affect the function of AHR has not been reported yet.

Method used

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  • Application of evodiamine in preparing medicine for inhibiting aryl hydrocarbon receptor
  • Application of evodiamine in preparing medicine for inhibiting aryl hydrocarbon receptor
  • Application of evodiamine in preparing medicine for inhibiting aryl hydrocarbon receptor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1, the physicochemical property of evodiamine

[0026] Molecular weight 303.4Da, insoluble in water, soluble in dimethyl sulfoxide, ethanol, ether, chloroform and other organic solvents, melting point is 278-279 ℃.

[0027] Structural formula see figure 1.

Embodiment 2

[0028] Embodiment 2, evodiamine on cytoplasm AhR and [ 3 Effect of H]-TCDD binding

[0029] by[ 3 H]-TCDD was used as the radioligand, and Wistar rat liver cytoplasm was used as the receptor of AHR for competitive ligand binding experiments.

[0030] The results showed that untagged TCDD inhibited [ 3 H]-TCDD binding to AHR, IC 50 The value is 1.71±0.3nM, and evodiamine can also inhibit [ 3 H]-TCDD binding to AHR, IC 50 The value is 44.8±6.5nM, and its K for binding to AHR i The value is 28.4 ± 4.9 nM.

Embodiment 3

[0031] Example 3, Effect of Evodiamine on TCDD-induced AHR Nuclear Translocation in Lovo Cells

[0032] Lovo cells were treated with control solution, TCDD (0.1 μM), TCDD (0.1 μM) + evodiamine (60 μM) for 4 hours in the in vitro cell culture system, and then fixed with 4% paraformaldehyde for 30 minutes, 5% bovine serum white Protein blocking, rabbit polyclonal anti-AHR antibody, FITC-secondary antibody, DAPI staining of nuclei, and observation of the results under a laser confocal microscope.

[0033] The results showed that treatment of Lovo cells with TCDD (0.1μM) for 4 hours could increase the nuclear translocation of AHR. If Lovo cells were treated with 60 μM evodiamine for 4 hours, the nuclear translocation of AHR induced by TCDD could be prevented. See figure 2.

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Abstract

The invention relates to application of evodiamine in preparing a medicine for inhibiting an aryl hydrocarbon receptor. The medicine for inhibiting the aryl hydrocarbon receptor has the anti-tumor and immunoregulation effects by inhibiting the aryl hydrocarbon receptor, wherein the tumors are breast cancer, endometrial cancer, prostate cancer, lung cancer, gastric cancer, liver cancer, colon cancer and the like; and the immunoregulation is performed aiming at various inflammatory related diseases, such as sepsis, sepsis shock, rheumatic arthritis, rheumatoid arthritis, asthma, acute and chronic glomerulonephritis, and systemic lupus erythematosus. In the application, the evodiamine is an alkaloid component in a traditional Chinese medicine, namely medicinal evodia fruit, has the molecular formula of C19H17NO3 and the molecular weight of 303.4Da, is insoluble, can be dissolved in organic solvents such as dimethyl sulfoxide, ethanol, diethyl ether and chloroform, and has the melting point of 278 to 279 DEG C.

Description

technical field [0001] The invention relates to a novel inhibitor capable of inhibiting the nuclei translocation of aromatic hydrocarbon receptors and its subsequent biological effects. The inhibitor is a traditional Chinese medicine monomer-evodiamine. Background technique [0002] Aromatic hydrocarbons are a class of chemical carcinogens containing benzene rings, common polycyclic aromatic hydrocarbons and halogenated aromatic hydrocarbons. Aromatic hydrocarbons bind to their receptors, ie, aryl hydrocarbon receptors (aryl hydrocarbon receptors, AHR), to activate the receptors, thereby causing the expression of a series of downstream genes and the activation of metabolic enzymes. The aryl hydrocarbon receptor (AHR), a ligand-dependently activated transcription factor, consists of 805 amino acids. The molecule has several functional domains: a basic helix-loop-helix (bHLH) structure located at the N-terminus of the AHR molecule, which is necessary for dimerization of prote...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61P35/00A61P37/02A61P29/00A61P19/02A61P19/04A61P11/06A61P13/12
Inventor 梁华平张醇范霞王希杨雪
Owner THE THIRD AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIV OF PLA
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