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The use of the C21 steroid compound in the preparation of IDO inhibitor

The technology of a kind of black bone vine and compound, applied in the field of preparation of IDO inhibitor, black bone vine C21 steroid compound

Active Publication Date: 2021-02-05
NANJING BAOHE BIOTECH
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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 there is no C21 steroid in the prior art for the preparation of IDO inhibitors, thereby providing the use of C21 steroids in the preparation of IDO inhibitors

Method used

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  • The use of the C21 steroid compound in the preparation of IDO inhibitor
  • The use of the C21 steroid compound in the preparation of IDO inhibitor
  • The use of the C21 steroid compound in the preparation of IDO inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 Preparation of C21 steroids from Heliconia chinensis

[0033] Get the root of Teng Teng, pulverize it, add 3 times the weight of ethanol aqueous solution with a volume concentration of 95% to extract twice at room temperature, extract for 7 days each time, combine the extracts, concentrate under reduced pressure until there is no alcohol smell, and obtain Teng Teng extract;

[0034] suspending the extract of Rhizoma chinensis in water of 1 times the weight, then extracting twice with chloroform as the extractant, collecting the organic phase of the extract, and then concentrating under reduced pressure to obtain the extract of the chloroform extraction part of Rhizoma Rhizoma;

[0035] Take the extract from the chloroform extraction part of Rhododendron chinensis and purify it by silica gel column chromatography, using petroleum ether as mobile phase A and acetone as mobile phase B, and carry out gradient elution according to the following procedure: first u...

experiment example 1

[0038] Experimental example 1 Study on the inhibitory activity of the C21 steroid compound of the present invention on IDO

[0039] 1. Purpose of the experiment

[0040] The plasmid pcDNA3.1-IDO was used to transfect HEK293 cells to make it highly express IDO, and then the inhibitory activity of the C21 steroid compound of the present invention on IDO was determined at the cellular level.

[0041] 2. Experimental method

[0042] 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 1-2.

[0043] The positive control group used 1-methyltryptophan (1-MT) as the test substance, and the experimental group ...

experiment example 2

[0053] Experimental example 2 Therapeutic effect of the C21 steroid compound of the present invention on ankylosing spondylitis

[0054] 1. Purpose of the experiment

[0055] The mouse model of ankylosing spondylitis was established by proteoglycan immunization method, and then the C21 steroid compound of the present invention was gavaged, and the inflammatory marker serum TNF-α and NF-кB receptor activator ligand ( RANKL) level, and detect serum IDO activity (Kyn / Trp), verify the curative effect of C21 steroid compound of the present invention for ankylosing spondylitis.

[0056] 2. Experimental method

[0057] 2.1 Experimental animals

[0058] Thirty-two healthy male BALB / c mice, weighing (18±2) g, aged 4-5 weeks, were purchased from Shanghai SLAC.

[0059] 2.2 Drugs to be tested

[0060] The saccharidin L and saccharidin H prepared in Example 1 were used as the test drugs.

[0061] 2.3 Experimental grouping and modeling

[0062] After the mice were adaptively fed f...

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Abstract

The invention belongs to the field of medicines or health products and particularly relates to Periploca forrestii C21 steroides in preparation of IDO (indoleamine-2,3-dioxygenase) inhibitors. Researches herein discover that both periplocoside L and periplocoside H have better intracellular IDO inhibitory activity than a positive control 1-MT (1-methyl-tryptophan), have significant IDO inhibitoryactivity, and are suitable for treating cancers, Alzheimer's disease, autoimmune diseases, ankylosing spondylitis, bacterial infections, cataract, mood disorders, and depression or anxiety.

Description

technical field [0001] The invention belongs to the field of medicines or health care products, and in particular relates to the use of the C21 steroid compound of the genus genus 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 studi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61P35/00A61P25/28A61P37/02A61P29/00A61P31/04A61P25/24A61P27/12A61P25/22
CPCA61K31/7048
Inventor 温尧林
Owner NANJING BAOHE BIOTECH
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