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

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. ...

AI Technical Summary

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, hyperlipidemia, inflammation, bacterial and viral infections and other diseases, but so far no berberine has been reported. Use of its derivatives in the preparation of IDO inhibitors

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