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Hasubanane alkaloid compounds as well as preparation method and application thereof

A technology of alkaloids and compounds, applied in the field of medicine, can solve the problems of few reports on structure and biological activity

Active Publication Date: 2021-02-02
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In recent years, there are relatively few reports on the structure and biological activity of alkaloids in Stephania vine

Method used

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  • Hasubanane alkaloid compounds as well as preparation method and application thereof
  • Hasubanane alkaloid compounds as well as preparation method and application thereof
  • Hasubanane alkaloid compounds as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] (1) 1 kg of Stephania vine was cold-soaked 3 times with 75% ethanol, each time for 24 hours (each dosage: 12 L), and the extract was recovered under reduced pressure to obtain a crude extract;

[0030] (2) The ethanol extract obtained in step (1) is dissolved in water, sherwood oil, methylene chloride, ethyl acetate and n-butanol extraction, the volume ratio of the extract and the extraction solvent is 1:1, and each solvent is extracted 5 times, get the extract;

[0031] (3) The extract obtained in step (2) was separated by silica gel column chromatography, and eluted with a mixed solvent of petroleum ether and ethyl acetate at 100:3, 100:7, 100:10, 100:15, and 100:20;

[0032] (4) The 100:7~100:15 fraction obtained in the above step (3) is separated by ODS chromatography, using methanol / water 1:9, 3:7, 5:5, 7:3, 9:1 as the mobile phase gradient elution;

[0033] (5) The methanol:water (3:7~9:1) fraction obtained in the above step (4) is separated by HPLC-UV chromatog...

Embodiment 2

[0053] (1) 1 kg of Stephania vine was cold-soaked 4 times with 85% methanol, each time for 24 hours (each dosage: 15 L), and the extract was recovered under reduced pressure to obtain a crude extract;

[0054] (2) The ethanol extract obtained in step (1) is dissolved in water, sherwood oil, methylene chloride, ethyl acetate and n-butanol extraction, the volume ratio of the extract and the extraction solvent is 1:1, and each solvent is extracted 4 times, Get extracts of different polar parts;

[0055] (3) The extract obtained in step (2) was separated by silica gel column chromatography, and eluted with a mixed solvent of petroleum ether and ethyl acetate at 100:3, 100:7, 100:10, 100:15, and 100:20;

[0056] (4) The 100:7~100:15 fraction obtained in the above step (3) is separated by ODS chromatography, using methanol / water 1:9, 3:7, 5:5, 7:3, 9:1 as the mobile phase gradient elution;

[0057] (5) The methanol:water (3:7~9:1) fraction obtained in the above step (4) is separat...

Embodiment 3

[0060] (1) 1 kg of Stephania vine was refluxed 4 times with 100% ethanol, each time for 24 hours (each dosage: 12 L), and the extract was recovered under reduced pressure to obtain a crude extract;

[0061] (2) The ethanol extract obtained in step (1) is dissolved in water, sherwood oil, dichloromethane, ethyl acetate and n-butanol extraction, the volume ratio of the extract and the extraction solvent is 1:1, and each solvent is extracted 5 times, Get extracts of different polar parts;

[0062] (3) The extract obtained in step (2) was separated by silica gel column chromatography, and eluted with a mixed solvent of dichloromethane and methanol at 100:0, 100:1, 100:3, 100:5, 100:7, and 100:10;

[0063] (4) The 100:1-100:7 fraction obtained in the above step (3) was separated by ODS chromatography, and the mobile phase was gradient eluted with acetonitrile / water 1:9, 3:7, 6:4, and 8:2;

[0064] (5) Acetonitrile obtained in the above step (4): water (3:7~8:2) fraction is separat...

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Abstract

The invention belongs to the technical field of medicines, and relates to hasubanane alkaloid compounds as well as a preparation method and application thereof, in particular to five hasubanane alkaloid compounds as well as a preparation method and application thereof. The structure of the compounds is shown in the specification, wherein R1, R2, R3 and R4 are hydrogen, C1-C4 alkyl, cinnamoyl and 3, 4-dimethoxybenzoyl. The compounds can be used for preparing medicines for preventing or treating neurodegenerative diseases and cancers.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to lianhuashi alkaloid compounds and their preparation methods and applications, in particular to five lianhuashi alkaloid compounds and their preparation methods and applications. Background technique [0002] Stephania japonica (Thunb.) Miers is a plant of the genus Stephania of the family Menispermaceae, also known as male mouse vine, no plaster, small green vine, wild peach grass, etc. It is common in Sichuan, Hubei, Hunan, and Jiangsu and Zhejiang areas. Bitter in taste and cold in nature, it has the effects of expelling wind and activating collaterals, diuresis and swelling. [0003] In recent years, there are relatively few reports on the structure and biological activity of alkaloids in Stephania vine. The invention provides the structure, preparation method and application of five new alkaloids isolated and identified from Stephania vine and their application in developing...

Claims

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Application Information

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IPC IPC(8): C07D491/08A61K31/407A61P25/00A61P35/00
CPCA61P25/00A61P35/00C07D491/08
Inventor 李宁陈刚
Owner SHENYANG PHARMA UNIVERSITY
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