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Uses of saponin huane-type sesquiterpene compounds

A technology of sesquiterpene and compound, applied in the field of Gansongpinhulan-type sesquiterpene compound

Active Publication Date: 2020-05-05
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 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

Method used

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  • Uses of saponin huane-type sesquiterpene compounds
  • Uses of saponin huane-type sesquiterpene compounds
  • Uses of saponin huane-type sesquiterpene compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The preparation of the active ingredient isocarpine and carborone E compound (extraction and separation process):

[0037] 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 Gansong rhizome is extracted 3 times with 70% ethanol for 48 hours each time, the combined extracts are concentrated under reduced pressure to obtain 3Kg of crude extract extract; hours, combine the extracts, concentrate under reduced pressure to obtain 400g of crude extract extract; combine two crude extracts to obtain 3.4Kg total extract; Ether, ethyl acetate, n-butanol extract, obtain sherwood oil part 320g, ethyl acetate part 1Kg, n-butanol part 600g, water layer 1.2Kg; Petroleum ether part 320g through silica gel column chromatography (sample silica gel 100- 200 mesh 400g, column silica gel 200-300 mesh 3.3Kg, petroleum ether: ethyl acetate = 10...

Embodiment 2

[0046] Effects of Compounds of the Invention on Serotonin Transporter (SERT)

[0047] 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 system Impact.

[0048] 1) Experimental instruments and reagents

[0049] laboratory apparatus:

[0050] 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)

[0051] Reagents and materials:

[0052] 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)

[0053] 2) Experimental operation process

[0054] First established and identified a ...

Embodiment 3

[0074]

[0075] The preparation method: according to the above ratio, uniformly mix isocarpinene / nearabetinone E, lactose and starch, pass through a 200-mesh sieve, moisten evenly with water, dry the wetted mixture and then sieve, add magnesium stearate, and then The mixture is compressed into tablets, each tablet weighs 250 mg, and the active ingredient content is 10 mg.

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Abstract

The invention provides a novel application of a Pinghuwanxing sesquiterpene compound, namely Isonardosinone or kanshone E, of nardostachys chinensis batal.; the Pinghuwanxing sesquiterpene compound of the nardostachys chinensis batal. is obtained from rhizome of the nardostachys chinensis batal., which belongs to valerianaceae nardostachys plants, by separating and purifying; the sesquiterpene compound has a 5-serotonin transporter (SERT) enhanced activity; the sesquiterpene compound, as a rare SERT activity promoter, is applicable to preparing medicines for treating such neuropsychiatric diseases as depression, anxiety disorder, schizophrenia, obsessive-compulsive disorder, neurodegenerative disease, drug addiction and the like as well as medicines for treating such digestive system dysfunction diseases as slow transit constipation, irritable bowel syndrome, functional abdominal distention and the like; and the sesquiterpene compound has an important medicine development value.

Description

technical field [0001] The present invention relates to the new application of the compound, especially the new application of the saponifolane-type sesquiterpene compound. 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 to 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-HT neurons in the central nervous system, SERT re-uptakes 5-HT from the synaptic gap into the pre-synaptic neuron, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/336A61P25/24A61P25/22A61P25/18A61P25/28A61P25/30A61P1/10A61P1/00
Inventor 徐砚通吴红华应树松陈应鹏刘艳庭朱彦张鹏董鹏志
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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