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Phenylpropanoid compound and preparation method and application thereof

A kind of technology of phenylpropanoid and compound, applied in phenylpropanoid compound and preparation field thereof

Inactive Publication Date: 2017-02-22
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Acorus tatarinowii is a plant of the genus Calamus in the family Araceae, which has the effects of removing dampness and harmonizing the stomach, resuscitating phlegm, refreshing the mind and improving intelligence. The reported biological activities of Acorus tatarinowii include (1) acting on the nervous system, such as antidepressant, sedative and Convulsions, brain protection and intelligence development, (2) acting on the cardiovascular system, such as lowering fat and slowing down the heart rate, (3) acting on the respiratory system, such as treating chronic bronchitis and bronchial asthma, (4) inhibiting bacteria, (5) ) anti-cancer, etc.; the chemical components of Acorus calamus include volatile oil, lignans, phenolic acids, alkaloids, flavonoids, etc., and in terms of active material basis, there are many reports on volatile components, and few reports on non-volatile components

Method used

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  • Phenylpropanoid compound and preparation method and application thereof
  • Phenylpropanoid compound and preparation method and application thereof
  • Phenylpropanoid compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Preparation of active ingredient phenylpropanoids (extraction and separation process)

[0042] Herbal decoction pieces of Shichangpu were purchased from Anhui Jiren Pharmaceutical Co., Ltd. (batch number: 120519, specification: 1kg / bag, origin: Anhui), about 20kg, decocted 3 times with 8, 6, and 6 times the amount of water, 1.5h each time , combined extracts, recovered under reduced pressure to a small volume (80L), filtered through D101 macroporous resin column chromatography, ethanol-water (v / v) gradient elution, recovered solvent under reduced pressure, obtained 30%, 50%, 70%, 95% 4 ethanol eluates.

[0043] The 30% ethanol eluate was dispersed in water and adjusted to pH=3-4 with formic acid, extracted three times with an equal volume of n-butanol, and the n-butanol extract was recovered under reduced pressure to obtain a dry extract, which was dissolved in water and subjected to ODS column chromatography (methanol-water gradient elution), obtain 6 components, wher...

Embodiment 2

[0056] The influence of phenylpropanoid compound of the present invention on 5-hydroxytryptamine transporter (SERT)

[0057] Using stably transfected hSERT-HEK293 cell line, 4-(4-(dimethylamino)phenyl)-1-methylpyridinium (APP + ) is a fluorescent substrate, and the effect of phenylpropanoids on SERT activity is detected on a high-content system.

[0058] 1) Experimental instruments and reagents

[0059] laboratory apparatus:

[0060] 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)

[0061] Reagents and materials:

[0062] Human embryonic kidney cell line HEK293 (Cell Bank of Type Culture Collection Committee, Chinese Academy of Sciences), hSERTpcDNA3 plasmid (Addgene, plasmid 15483), MEM medium (Gibco), APP+ (Sigma), Hoechst 33342 (Cell Signaling Technology), 96-well plate (Costar 3605)

[0063] 2) Experimental operation process

[0064]First est...

Embodiment 3

[0084]

[0085]

[0086] Preparation method: uniformly mix phenylpropanoid compound, lactose and starch according to the above ratio, pass through a 200-mesh sieve, moisten evenly with water, dry the wetted mixture and sieve, add magnesium stearate, and press the mixture Tablets, each weighing 250mg, with an active ingredient content of 10mg.

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PUM

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Abstract

The invention provides a phenylpropanoid compound in acorus calamus and a preparation method and application thereof. The compound is obtained through separation and purification of (R)-1,2-split-ring ceplignan, (2S,3R)-ceplignan and (2R,3S)-ceplignan from acorus gramineus rhizomes, has 5-hydroxytryptamine transporter (SERT) adjusting activity, can be applied to preparation of drugs for resisting depression, anxiety disorder, schizophrenia, obsessive-compulsive disorder neurodegeneration and other diseases and preparation of drugs for treating drug addiction, digestive system dysfunction and other diseases, and has important drug development value.

Description

technical field [0001] The invention relates to the field of traditional Chinese medicine research, in particular to phenylpropanoid compounds and their preparation methods and applications. 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 af...

Claims

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Application Information

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IPC IPC(8): C07D307/86C07C65/24A61P25/24A61P25/22A61P25/18A61P25/28A61P25/00A61P25/30A61P1/00
CPCC07C51/42C07C65/24C07D307/80C07D307/86
Inventor 吴红华徐砚通董鹏志梁爽应树松刘艳庭高秀梅张鹏
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE