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Glycerinone C and its preparation method and application

A kind of rosin ketone, the technology of aspect, is applied in the field of plant extract and preparation thereof, can solve the problems such as no SERT inhibitory activity report etc.

Active Publication Date: 2018-06-29
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The chemical components of Gansong include sesquiterpenes, triterpenes, iridoids, coumarins, phenolic acids, flavonoids, etc. Sesquiterpenes are the main components, but there are no reports on the SERT inhibitory activity of these compounds

Method used

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  • Glycerinone C and its preparation method and application
  • Glycerinone C and its preparation method and application
  • Glycerinone C and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] The preparation of active ingredient Nicaproterone C compound (extraction and separation process):

[0032] The decoction pieces of Gansong medicinal material were purchased from Anhui Jiren Pharmaceutical Co., Ltd. (batch number: 110709, specification: 1kg / bag, place of origin: Sichuan), about 20kg. 20kg of Nardinus rhizome is extracted 3 times with 70% (v / v) ethanol, each time for 48 hours, the combined extracts are concentrated under reduced pressure to obtain 3kg of crude extract; time, each 2 hours, combined extracts, concentrated under reduced pressure to get 400g of crude extract extract; combined two crude extracts to get total extract 3.4kg; the total extract of gained crude extract, after water dispersion, was sequentially Carry out extraction with petroleum ether, ethyl acetate, n-butanol of equal volume, obtain petroleum ether part 320g, ethyl acetate part 1kg, n-butanol part 600g, water layer 1.2kg; Petroleum ether part 320g is subjected to silica gel colum...

Embodiment 2

[0036] Effects of Compounds of the Invention on Serotonin Transporter (SERT)

[0037] Using stably transfected hSERT-HEK293 cell line, 4-(4-(dimethylamino)phenyl)-1-methylpyridinium (APP + ) is a fluorogenic substrate, and the effect of the compound Ninosinone C on SERT activity was detected on a high-content system.

[0038] 1) Experimental instruments and reagents

[0039] laboratory apparatus:

[0040] High-content Operetta system and Columbus data management and analysis system (PerkinElmer), ultra-clean bench, pipette gun (1000μL, 200μL, 20μL, 10μL, 2.5μL, Eppendorf, USA)

[0041] Reagents and materials:

[0042] Human embryonic kidney cell line HEK293 (Cell Bank of Type Culture Collection Committee, Chinese Academy of Sciences), hSERT pcDNA3 plasmid (Addgene, plasmid 15483), MEM medium (Gibco), APP + (Sigma), Hoechst 33342 (CellSignaling Technology), 96-well plate (Costar 3605)

[0043] 2) Experimental operation process

[0044] First established and identified a c...

Embodiment 3

[0062]

[0063] Preparation method: uniformly mix carbosinone C, lactose and starch according to the above ratio, pass through a 200-mesh sieve, moisten evenly with water, dry the wetted mixture and then sieve, add magnesium stearate, and then press the mixture into tablets , each tablet weighs 250mg, and the active ingredient content is 10mg.

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PUM

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Abstract

The invention relates to kanshone C and a preparation method and application thereof. The kanshone C is obtained from rhizomes of valerianaceae nardostachys plant nardostachys chinensis in a separated and purified mode, inhibits activity of serotonin transporters (SERTs), can be used for preparing medicine for treating neuropsychiatric diseases such as depression, anxiety disorder, schizophrenia, obsession, neurodegeneration and drug addiction and digestion system dysfunction diseases such as slow transit constipation, an irritable bowl syndrome and functional bloating and has important medicine development value.

Description

technical field [0001] The present invention relates to a kind of plant extract and its preparation method and application, especially naminosinone C and its preparation method and application. Background technique [0002] Serotonin transporter (SERT) is a transmembrane transporter with high affinity for 5-HT, containing about 630 amino acid residues, and its coding gene (SLC6A4) is located on chromosome 7 and 11, respectively. It consists of 14 exons of about 35kb. The SERT protein contains 12-13 transmembrane regions, the N-terminal and C-terminal are located in the cytoplasm, there is a cAMP-dependent protein kinase binding site near the N-terminal, and there is an extracellular region between the third and fourth transmembrane regions. The cyclic portion of is the N-linked glycosylation site. [0003] SERT belongs to Na + / Cl - Dependent transporter, mainly located in 5-HTergic neurons. SERT re-uptakes 5-HT from the synaptic cleft into presynaptic neurons, directly...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D303/32C07D301/32A61K31/336A61P25/24A61P25/22A61P25/18A61P25/28A61P25/30A61P1/00A61P1/10A61P1/14
CPCC07D301/32C07D303/32
Inventor 徐砚通吴红华高秀梅刘艳庭陈应鹏应树松董鹏志朱彦
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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