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Acorus amide compound and its preparation method and application
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A calamus amide and compound technology, applied in the field of calamus amide compounds and their preparation, to achieve the effect of promoting activity
Active Publication Date: 2017-05-10
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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[0006] Acorus tatarinowii is a plant of the genusCalamus 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. Studies have shown that both volatile and non-volatile components of Acorus calamus have good antidepressant activity, while in In terms of the basis of active substances, there are many reports on volatile components, but few reports on non-volatile components
Method used
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[0038]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 resincolumn chromatography, ethanol-water (v / v) gradient elution, recovered solvent under reduced pressure, obtained 30%, 50%, 70%, 95% 4 ethanol eluates.
[0039] 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...
Embodiment 2
[0057] The influence of calamus amide compounds of the present invention on 5-hydroxytryptamine transporter (SERT)
[0058] Using stably transfected hSERT-HEK293 cell line, 4-(4-(dimethylamino)phenyl)-1-methylpyridinium (APP + ) is a fluorescent substrate, and the effect of calamus amide compounds on SERT activity is detected on a high-content system.
[0059] 1) Experimental instruments and reagents
[0060] laboratory apparatus:
[0061] 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)
[0062] Reagents and materials:
[0063] Human embryonic kidneycell line HEK293 (CellBank 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)
[0064] 2) Experimental operation process
[0065] Fi...
Embodiment 3
[0084]
[0085] Preparation method: uniformly mix calamus amide compounds ((E)-feruloyl-γ-butyric acid amide), lactose and starch according to the above ratio, pass through a 200-mesh sieve, and evenly moisten the wetted mixture Dry and sieve, add magnesiumstearate, then compress the mixture into tablets, each tablet weighs 250 mg, and the active ingredient content is 10 mg.
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Abstract
The invention provides a calamusamide compound as well as a preparation method and application of the calamusamide compound. The compound is (E)-methyl- 4-[3-(4-hydroxy-3-methoxyphenyl)acrylamido]butanoate or a (Z)-methyl- 4-[3-(4-hydroxy-3-methoxyphenyl)acrylamido]butanoate enol isomer, is separated and purified from roots and stems of acorus tatarinowii serving as an araceaeacorusplant, has the effect of promoting the activity of a 5-serotonintransporter (SERT), can be used as a drug for treating depressive disorder, anxiety disorder, schizophrenia, obsession, neurodegenerative diseases, drugaddiction or digestive system dysfunction and other diseases, and has an important drug development value.
Description
technical field [0001] The invention relates to the field of traditional Chinese medicine research, in particular to calamusamide compounds and their preparation methods and applications. Background technique [0002] Serotonintransporter (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 proteinkinasebinding 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 affe...
Claims
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Application Information
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