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Digmarone a compound and its preparation method and application
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A kind of technology of glycansenone and compound, which is applied in the field of glycansenone A compound and its preparation, and achieves the effect of promoting activity
Active Publication Date: 2018-05-01
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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The chemical constituents of Gansong include sesquiterpenes, triterpenes, iridoids, coumarins, phenolic acids, flavonoids, etc. Sesquiterpenes are its main components, and among them, there are many research reports on Gansinone and Aristolochne. Other active ingredients, especially small or trace ingredients, are rarely reported, and the biological activity and related mechanisms need to be further discovered
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[0042] The decoction pieces of Gansong medicinal materials were purchased from Anhui Jiren Pharmaceutical Co., Ltd. (batch number: 110709, specification: 1Kg / bag, place of origin: Sichuan), about 20Kg, 20Kg of Gansong rhizome was extracted with 70% ethanol for 3 times, each time for 48 hours, Combine the extracts, concentrate under reduced pressure to obtain 3Kg of crude extract extract; then heat extract the above-mentioned medicinal residues with 70% ethanol for 3 times, each time for 2 hours, combine the extracts, concentrate under reduced pressure, and obtain 400 g of crude extract extract; Combine the two crude extracts to obtain a total extract of 3.4Kg; the total extract of the obtained crude extract, after being dispersed in water, is sequentially extracted with an equal volume of petroleumether, ethyl acetate, and n-butanol to obtain 320 g of petroleumether fractions, Ethyl...
Embodiment 2
[0056] Effect of the compound Dinarkanshone A (Dinarkanshone A, DNK-A) of the present invention on 5-hydroxytryptamine transporter (SERT)
[0057] Using the stably transfected hSERT-HEK293 cell line, using 4-(4-(dimethylamino)phenyl)-1-methylpyridinium (APP+) as the fluorescent substrate, the SERT activity of the compound digicrone A was detected on a high-content systemImpact.
[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 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)
[0063] 2) Experimental op...
Embodiment 3
[0082]
[0083] Preparation method: uniformly mix digicone A, 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 magnesiumstearate, and then mix the mixture Compressed tablets, each tablet weighs 250mg, and the active ingredient content is 10mg.
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Abstract
The present invention provides Dinarkanshone A (Dinarkanshone A, DNK‑A) compound and its preparation method and application, the compound is (2'R, 4aR, 4'aR, 5S, 8'S, 8'aS)‑1 ‑Hydroxy‑4a,4',5,8'a‑Tetramethyl‑8'‑(propane‑1‑en‑2‑yl)‑1',2',4a,4'a,5,5', 6,6',7,7',8',8'a-dodecahydro-[2,2'-binaphthalene]-3(4H)-one, is a plant of the genus Nardinus ( Nardostachys chinensis Batal.) isolated and purified from the rhizome, has strong activity of serotonintransporter, and can be used in the preparation of drugs for antidepressant, anxiety, schizophrenia, obsessive-compulsive disorder, neurodegenerative diseases and other diseases. application.
Description
technical field [0001] The invention relates to the field of research on traditional Chinese medicines, in particular to a digicone A compound and a preparation method and application thereof. 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 to 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, direct...
Claims
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Application Information
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