Aristolochane-type sesquiterpenoids and their preparation method and application

A technology of aristolochane and sesquiterpenoids, which is applied to the effective components of hydroxyl compounds, the separation/purification of hydroxyl compounds, the separation/purification of carbonyl compounds, etc.

Active Publication Date: 2017-04-05
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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  • Aristolochane-type sesquiterpenoids and their preparation method and application
  • Aristolochane-type sesquiterpenoids and their preparation method and application
  • Aristolochane-type sesquiterpenoids and their preparation method and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Preparation of the active ingredient aristolochane-type sesquiterpene and its derivatives (extraction and separation process):

[0050]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 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 3.4 kg of total extract; the total extract of the obtained crude extract, after being dispersed in water, is sequentially extracted with an equal volume of petroleum ether, ethyl acetate, and n-butanol to obta...

Embodiment 2

[0066] Effects of Compounds of the Invention on Serotonin Transporter (SERT)

[0067] Using stably transfected hSERT-HEK293 cell line, 4-(4-(dimethylamino)phenyl)-1-methylpyridinium (APP + ) is a fluorescent substrate, and the effect of the aristolochane-type sesquiterpene and its derivatives on SERT activity was detected on a high-content system.

[0068] 1) Experimental instruments and reagents

[0069] laboratory apparatus:

[0070] 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)

[0071] Reagents and materials:

[0072] 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)

[0073] 2) Experimental operation process

[0074] First...

Embodiment 3

[0097]

[0098] Preparation method: uniformly mix aristolochne-9β-alcohol / nabisone / nabisone H / 3-hydroxynabisone H / 3-oxonabisone H, lactose and starch according to the above ratio, and pass 200 Mesh sieve, wet evenly with water, dry the wetted mixture and then sieve, add magnesium stearate, then compress the mixture into tablets, each tablet weighs 250mg, and the active ingredient content is 10mg.

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Abstract

The invention provides a rhizoma nardostachyos birthwort alkane sesquiterpene compound and a preparation method and application thereof. The rhizoma nardostachyos birthwort alkane sesquiterpene compound is obtained through separation and purification from rhizomes of a nardostachys chinensis batal plant of rhizoma nardostachyos, and the compound has 5-serotonin transporter (S-ERT) to enhance activity, belongs to rare SERT activity promoters, can be used for preparing drugs for treating depression, anxiety disorder, schizophrenia, obsessive-compulsive disorder, the neurodegenerative disease, drug addiction and other neuropsychological diseases, and drugs for treating slow transit constipation, irritable bowel syndromes, functional bloating and other dysfunction diseases of the digestive system, and has important medicine development value.

Description

technical field [0001] The invention relates to the field of research and development of traditional Chinese medicines, in particular to aristolochane-type sesquiterpenoids, preparation methods and applications. 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 syna...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C49/643C07C45/78C07C45/79C07C49/737C07C35/37C07C29/74C07C29/76A61K31/122A61K31/045A61P25/24A61P25/22A61P25/18A61P25/28A61P25/30A61P1/00
CPCC07C29/74C07C29/76C07C35/37C07C45/78C07C45/79C07C49/643C07C49/737
Inventor 吴红华徐砚通高秀梅陈应鹏应树松刘艳庭董鹏志朱彦
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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