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Nardoaristolones B and preparation method and application thereof

A kind of technology of aspect and general formula, applied in the field of plant extract and its preparation

Active Publication Date: 2015-12-16
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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  • Nardoaristolones B and preparation method and application thereof
  • Nardoaristolones B and preparation method and application thereof
  • Nardoaristolones B and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Preparation of active ingredient aristolochone B (extraction and separation process):

[0034] 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, and 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 3 kg of crude extract extract; then use 70% (v / v) ethanol to heat extract the above-mentioned medicinal residues for 3 times, each time for 2 hours, combine the extracts, concentrate under reduced pressure to obtain crude extract Extraction extract 400g; Merge two crude extracts to obtain total extract 3.4kg; Gained crude extract total extract, after water dispersion, extract with equal volume of sherwood oil, ethyl acetate, n-butanol successively, obtain Petroleum ether part 320g, ethyl acetate part 1kg, n-butanol part 600g,...

Embodiment 2

[0038] The influence of aristolochone B of the present invention on 5-hydroxytryptamine transporter (SERT)

[0039] Using stably transfected hSERT-HEK293 cell line, 4-(4-(dimethylamino)phenyl)-1-methylpyridinium (APP + ) is a fluorescent substrate, and the effect of compound aristolochone B on SERT activity was detected on a high-content system.

[0040] 1) Experimental instruments and reagents

[0041] laboratory apparatus:

[0042] 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)

[0043] Reagents and materials:

[0044] Human embryonic kidney cell line HEK293 (Cell Bank of Type Culture Collection Committee, Chinese Academy of Sciences), hSERTpcDNA3 plasmid (Addgene, plasmid15483), MEM medium (Gibco), APP+ (Sigma), Hoechst33342 (CellSignalingTechnology), 96-well plate (Costar3605)

[0045] 2) Experimental operation process

[0046] First establis...

Embodiment 3

[0065]

[0066] Preparation method: uniformly mix aristolochone B, 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 then The mixture is compressed into tablets, each tablet weighs 250 mg, and the active ingredient content is 10 mg.

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PUM

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Abstract

The invention relates to nardoaristolones B and a preparation method and application thereof. The nardoaristolones B are obtained from rhizomes of valerianaceae nardostachys plant nardostachys chinensis in a separated and purified mode, improve activity of serotonin transporters (SERTs), belong to rare SERT active promoters and can be used for preparing medicine for treating neuropsychiatric diseases such as depression, anxiety disorder, schizophrenia, obsession, neurodegeneration and drug addiction. Meanwhile, the nardoaristolones B can be used for preparing medicine for treating digestion system dysfunction such as an irritable bowl syndrome, slow transit constipation and functional bloating and has important medicine development value.

Description

technical field [0001] The invention relates to a plant extract and its preparation method and application, especially aristolochone B and its preparation method and application. 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-HT neurons in the central nervous system, SERT re-uptakes 5-HT from the synaptic gap into the pre-synaptic neuro...

Claims

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Application Information

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IPC IPC(8): C07C49/643C07C45/78C07C45/79C07C45/80A61K31/122A61P25/18A61P25/22A61P25/24A61P25/28A61P25/30A61P1/00
CPCC07C45/78C07C45/79C07C45/80C07C49/643
Inventor 徐砚通吴红华高秀梅应树松陈应鹏刘艳庭董鹏志朱彦
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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