Application of berberine and derivatives thereof in preparation of indole amine 2, 3-dioxygenase inhibitor

A technology of dioxygenase and derivatives, applied in the field of medicine, can solve the problems such as the use of berberine and its derivatives that are not seen, and achieve the effect of broad application prospects

Inactive Publication Date: 2010-09-29
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In the past ten years, several documents have reported that berberine and its derivatives are clinically used to treat tumors, diabetes, cardiovascular diseases, hyperlipide

Method used

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  • Application of berberine and derivatives thereof in preparation of indole amine 2, 3-dioxygenase inhibitor
  • Application of berberine and derivatives thereof in preparation of indole amine 2, 3-dioxygenase inhibitor
  • Application of berberine and derivatives thereof in preparation of indole amine 2, 3-dioxygenase inhibitor

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Experimental program
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Embodiment 1

[0039] 1) Detection of IDO inhibitory activity:

[0040] Reaction conditions: 50mM potassium phosphate buffer (pH 6.5), 40mM vitamin C, 400ug / ml catalase, 20uM methylene blue, substrate L-tryptophan and the sample to be tested were mixed, and the mixture was incubated at 37°C for 5 minutes. Then add IDO enzyme to the above mixture, react at 37°C for 30 minutes, add 200ul of 30% (w / v) trichloroacetic acid to terminate the reaction, and heat the reaction system at 65°C for 15 minutes to complete the reaction from formyl The conversion of kynurenine to kynurenine, and then 12000rpm rotation for 10 minutes, the supernatant was mixed with an equal volume of 2% (w / v) p-dimethylaminobenzaldehyde in acetic acid solution, and kynurenine reacted with it The resulting yellow color can be observed at 490nm using a microplate reader.

[0041] The test results show that the inhibitory effect of berberine, jatrorrhizine hydrochloride and palmatine hydrochloride on IDO is better than that of...

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Abstract

The invention relates to novel application of berberine and derivatives thereof in preparation of medicines, in particular to application of berberine and derivatives thereof in preparation of indole amine 2, 3-dioxygenase IDO inhibitor, belonging to the medicine field. According to IDO inhibition activity detection, reversible inhibition judgment, inhibitor type judgment, Ki value determination and median effective inhibition concentration IC50 determination, the results show that berberine is reversible inhibitor and inhibition constant Ki is 8muM; and jatrorrhizine hydrochloride and palmatine hydrochloride are irreversible inhibitors, and the median effective inhibition concentrations IC50 thereof are respectively 123muM and 126muM. When the berberine and the derivatives thereof disclosed in the invention are used as IDO inhibitors, the application prospect is wide and the IDO inhibitors can be used for treating serious diseases such as cancers, AIDS, Alzheimer diseases, tristimania, cataract and the like with pathological feature of IDO-mediated tryptophan metabolism.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to the new application of berberine and its derivatives in pharmacy, in particular to the use of berberine and its derivatives in the preparation of indoleamine 2,3-dioxygenase (IDO) inhibitors use. Background technique [0002] The prior art discloses that indoleamine 2, 3-dioxygenase (Indoleamine 2, 3-dioxygenase, IDO) is an enzyme containing heme in a cell, and is the only enzyme outside the liver that can catalyze the metabolism of tryptophan. It is the rate-limiting enzyme that breaks down along the kynurenine pathway to produce a series of metabolites including quinolinic acid [1] . [0003] IDO is related to many physiological and pathological processes. Studies on pregnant mouse models have found that syncytiotrophoblast cells and antigen-presenting cells at the maternal-fetal interface can synthesize IDO, and the dynamic changes in IDO expression are consistent with embryogenesis. ...

Claims

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Application Information

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IPC IPC(8): A61K31/4745A61P35/00A61P37/00A61P25/28A61P25/22A61P25/24A61P27/12A61P25/18
Inventor 杨青于存静匡春香郑茂发
Owner FUDAN UNIV
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