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Use of phenylpropanoid glycosides in the preparation of ido inhibitors

A technology of phenylpropanoid glycosides and inhibitors, applied to medical preparations containing active ingredients, pharmaceutical formulas, allergic diseases, etc., to achieve a significant inhibitory effect on activity

Active Publication Date: 2021-04-30
江苏凯吉生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] For this reason, the technical problem to be solved in the present invention is the problem that no phenylpropanoid glycosides are used for the preparation of IDO inhibitors in the prior art, thereby providing the purposes of phenylpropanoid glycosides in the preparation of IDO inhibitors

Method used

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  • Use of phenylpropanoid glycosides in the preparation of ido inhibitors
  • Use of phenylpropanoid glycosides in the preparation of ido inhibitors
  • Use of phenylpropanoid glycosides in the preparation of ido inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 Preparation of echinacoside

[0035] Get the dry fleshy stem of Cistanche deserticola (Cistanche deserticola Ma), add 10 times the volume concentration of the weight and be 75% ethanol aqueous solution and heat and reflux to extract twice, extract for the first time for 2 hours, extract for the second time for 1 hour, combine the extracts, reduce Concentrate under pressure until there is no alcohol smell, to obtain Cistanche deserticola extract;

[0036]Suspend the extract of Cistanche deserticola in 1 times the weight of water, then use n-butanol as the extractant to extract twice, collect the organic phase of the extract, and then concentrate under reduced pressure to obtain the extract of Cistanche deserticola n-butanol extraction part ;

[0037] Purify the extract from the n-butanol extraction part of Cistanche deserticola through AB-8 macroporous resin column chromatography (the diameter of the macroporous resin column is 8cm, and the column volume is 3...

Embodiment 2

[0040] Example 2 Preparation of equine artemisinin A and equine artemisinin H

[0041] Take Artemisia spicata (Pedicularis spicata), add 9 times the weight of ethanol aqueous solution with a volume concentration of 95%, heat and reflux for extraction twice, the first extraction is 2 hours, the second extraction is 1 hour, the combined extracts are concentrated under reduced pressure to nothing. Alcoholic taste, obtained Artemisia fragrans extract;

[0042] Suspend the extract of Artemisia fringa in 1 times the weight of water, then use n-butanol as the extractant to extract twice, collect the organic phase of the extract, and then concentrate it under reduced pressure to obtain the extract of Artemisia fringae n-butanol extraction part ;

[0043] Purify the extract from the n-butanol extraction part of Artemisia fringae by AB-8 macroporous resin column chromatography (the diameter of the macroporous resin column is 8cm, and the column volume is 3.5L), using water as mobile ...

experiment example 1

[0046] Experimental example 1 Study on the inhibitory activity of echinacoside, equine artemisinin A and equine artemisinin H on IDO

[0047] 1. Purpose of the experiment

[0048] HEK293 cells were transfected with the plasmid pcDNA3.1-IDO to highly express IDO, and then the inhibitory activities of echinacoside, equine artemisinin A and equine artemisinin H on IDO at the cellular level were determined respectively.

[0049] 2. Experimental method

[0050] HEK 293 cells were seeded in a 96-well plate at a density of 2.5X104 cells / well, cultured in DMEM medium (containing 10% fetal bovine serum, 50 U / mL penicillin and 50 mg / mL streptomycin), placed at 37 ° C, humidity 95%, 5% CO 2 cultured in an incubator. After culturing for 24 hours, use liposome Lipofectamin 2000 to mediate pcDNA3.1-hIDO plasmid transfection, and divide them into positive control group and experimental group 1-3. The positive control group uses 1-methyltryptophan (1-MT) as the test product, and the exp...

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Abstract

The invention belongs to the field of medicines or health products, and specifically relates to the use of phenylpropanoid glycosides and pharmaceutically acceptable derivatives thereof in preparing IDO inhibitors. The present invention finds through research that the inhibitory activity of echinacoside, equine artemisinin A and equine artemisinin H on intracellular IDO is better than that of the positive control drug 1-methyltryptophan (1-MT) on intracellular IDO. Inhibitory activity, with significant IDO inhibitory activity, can be used to treat cancer, Alzheimer's disease, ankylosing spondylitis, autoimmune disease, bacterial infection, cataract, mood disorder, depression or anxiety.

Description

technical field [0001] The invention belongs to the field of medicines or health products, and in particular relates to the use of phenylpropanoid glycosides in the preparation of IDO inhibitors. Background technique [0002] IDO (indoleamine-2, 3-dioxygenase) is the only rate-limiting enzyme that catalyzes the metabolism of tryptophan along the kynurenine pathway (KP) outside the liver. , can decompose tryptophan into various metabolites such as L-kynurenine, picolinic acid and quinolinic acid. L-Tryptophan is an amino acid necessary to maintain cell activation and proliferation in the human body, and is also an indispensable component of protein. Its deficiency will lead to abnormal function of some important cells. Since it was discovered in 1967, the mechanism of IDO inhibiting the proliferation of pathogenic microorganisms by degrading tryptophan, and the relationship between IDO and nervous system diseases have been gradually clarified; and studies have confirmed that...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7032A61P35/00A61P37/02A61P25/28
CPCA61K31/7032
Inventor 温尧林
Owner 江苏凯吉生物科技有限公司
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