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Novel application of Pinghuwanxing sesquiterpene compound of nardostachys chinensis batal.

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

Active Publication Date: 2016-08-24
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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  • Novel application of Pinghuwanxing sesquiterpene compound of nardostachys chinensis batal.
  • Novel application of Pinghuwanxing sesquiterpene compound of nardostachys chinensis batal.
  • Novel application of Pinghuwanxing sesquiterpene compound of nardostachys chinensis batal.

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Preparation of the active ingredients isosinone and rosinone E compound (extraction and separation process):

[0037] Decoction pieces of Gansong medicinal materials were purchased from Anhui Jiren Pharmaceutical Co., Ltd. (batch number: 110709, specification: 1Kg / bag, place of production: Sichuan), about 20Kg. Extraction of 20Kg of pine rhizome with 70% ethanol 3 times for 48 hours each time. Combine the extracts and concentrate under reduced pressure to obtain 3Kg of crude extract; then use 70% ethanol to heat extract the above medicine residue 3 times, 2 times each After hours, the extracts were combined and concentrated under reduced pressure to obtain 400g of crude extract extract; the two crude extracts were combined to obtain the total extract 3.4Kg; the total crude extract obtained was dispersed in water, and then an equal volume of petroleum Ether, ethyl acetate, and n-butanol were extracted to obtain 320g of petroleum ether, 1Kg of ethyl acetate, 600g of n-butano...

Embodiment 2

[0046] Effect of the compound of the present invention on serotonin transporter (SERT)

[0047] Using the stably transfected hSERT-HEK293 cell line, 4-(4-(dimethylamino)phenyl)-1-methylpyridinium (APP+) was used as the fluorescent substrate to detect the SERT activity of the compound diglycolinone A on a high-content system Impact.

[0048] 1) Experimental equipment and reagents

[0049] laboratory apparatus:

[0050] High-content Operetta system and Columbus data management and analysis system (PerkinElmer), clean bench, pipette (1000μL, 200μL, 20μL, 10μL, 2.5μL, Eppendorf, USA)

[0051] Reagents and materials:

[0052] Human embryonic kidney cell line HEK293 (Cell Bank of the Type Culture Collection Committee of the Chinese Academy of Sciences), hSERT pcDNA3 plasmid (Addgene, plasmid 15483), MEM medium (Gibco), APP+ (Sigma), Hoechst 33342 (Cell Signaling Technology), 96 wells Plate (Costar 3605)

[0053] 2) Experimental operation process

[0054] First, established and identified a cel...

Embodiment 3

[0074]

[0075] Preparation method: according to the above ratio, evenly mix isoglycosinone / glycosinone E, lactose and starch, pass a 200-mesh sieve, and evenly moisten with water, dry the moistened mixture and sieve again, add magnesium stearate, and then The mixture was compressed into tablets, each weighing 250 mg, and the active ingredient content was 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 a new use of the compound, especially the new use of a saccharine sesquiterpene compound. Background technique [0002] Serotonin transporter (SERT) is a transmembrane transporter with high affinity for 5-HT, containing about 630 amino acid residues. Its coding genes (SLC6A4) are located on chromosomes 7 and 11, respectively. It is composed of 14 exons about 35kb. The SERT protein contains 12 to 13 transmembrane regions. The N-terminus and C-terminus are located in the cytoplasm. There are cAMP-dependent protein kinase binding sites near the N-terminus. Between the third and fourth transmembrane regions, one is located outside the cell. The cyclic part of is an N-linked glycosylation site. [0003] SERT belongs to Na + / Cl - Dependent transporters are mainly located in 5-HTergic neurons in the central nervous system. SERT re-uptakes 5-HT from the synaptic cleft into the presynaptic neurons, which directly affects the 5-HT co...

Claims

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Application Information

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Patent Type & Authority Applications(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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