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Indole N-glycoside compound, extraction method, and application in preparing drugs for preventing and treating nervous system diseases

A technology of indole azosides and compounds, which is applied in the field of indole azasides, which can solve the problems of no indole azapines and no PC12 cell damage protection, and achieve the effect of protecting cells from damage

Active Publication Date: 2020-03-27
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In a large number of researches on the chemical constituents of Sala chinensis, no indole nitrogen glycoside compounds involved in the present invention
At the same time, there is no relevant report on the protective effect of the indole azoside compounds involved in the present invention on the damage of PC12 cells caused by CoCl2

Method used

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  • Indole N-glycoside compound, extraction method, and application in preparing drugs for preventing and treating nervous system diseases
  • Indole N-glycoside compound, extraction method, and application in preparing drugs for preventing and treating nervous system diseases
  • Indole N-glycoside compound, extraction method, and application in preparing drugs for preventing and treating nervous system diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] The extraction method of indole nitrogen glycoside compound comprises the following steps:

[0068] (1) Take 8.8 kg of dried and mature seeds of Sala chinensis, after coarse crushing, heat and reflux extraction with 10 mass times of 70% ethanol aqueous solution with a volume concentration of 3 times, each time for 3 hours, combine the extracts, and concentrate under reduced pressure to 65°C , to obtain 2.1kg of extract whose relative density is 1.20;

[0069] (2) Disperse the extract obtained in step (1) into distilled water of 5 times by mass, centrifuge to get the supernatant, carry out D101 type macroporous resin open column chromatographic separation (20 × 90cm), and use 4 times of column bed volume successively Water, 20%, 60%, and 95% ethanol aqueous solution were used for gradient elution, and the fractions eluted with 20% ethanol aqueous solution were collected, concentrated under reduced pressure to 65 ° C, and obtained 225 g of extract with a relative density ...

Embodiment 2

[0111] The extraction method of indole nitrogen glycoside compound comprises the following steps:

[0112] (1) Take 8.8 kg of dried and mature seeds of Sala chinensis, after coarse crushing, heat and reflux extraction with 8 mass times of 60% ethanol aqueous solution with a volume concentration of 4 times, each time for 3 hours, combine the extracts, and concentrate under reduced pressure to 65°C , to obtain an extract whose relative density is 1.15;

[0113] (2) the medicinal extract that step (1) is obtained is dispersed into the distilled water of 7 mass times, through HP 20 type macroporous adsorption resin column chromatography (20 * 90cm), with the water of 4 times column bed volume successively, volume concentration is Gradient elution with 20%, 60% and 95% ethanol aqueous solution, collect the fractions eluted with 20% ethanol aqueous solution, concentrate under reduced pressure to 65°C, and extract with a relative density of 1.25;

[0114] (3) Disperse the medicinal ...

Embodiment 3

[0117] The extraction method of indole nitrogen glycoside compound comprises the following steps:

[0118] (1) Take 8.8 kg of dried and mature seeds of Sala chinensis, after coarse crushing, heat and reflux extraction with 9 mass times of ethanol aqueous solution with a volume concentration of 65% for 2 times, each time for 3 hours, combine the extracts, and concentrate under reduced pressure to 65°C , to obtain an extract whose relative density is 1.25;

[0119] (2) Disperse the extract obtained in step (1) into distilled water of 10 mass times, through AB-8 type macroporous adsorption resin column chromatography (20 × 90cm), use 4 times of column bed volume water, volume concentration successively For gradient elution with 20%, 60% and 95% ethanol aqueous solution, collect the fractions eluted with 20% ethanol aqueous solution, concentrate under reduced pressure to 65°C, and extract with a relative density of 1.20;

[0120] (3) Disperse the extract obtained in step (2) into...

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Abstract

The invention discloses an indole N-glycoside compound, an extraction method, and an application in preparing drugs for preventing and treating nervous system diseases. The indole N-glycoside compoundhas a structure represented by a formula (I) in the specification. The indole N-glycoside compound of the invention can effectively protect PC12 cell damages caused by CoCl2, and the result suggeststhat the compound of the invention can be used as a neuroprotective drug.

Description

technical field [0001] The invention relates to the field of traditional Chinese medicine extraction, and relates to an indole nitrogen glycoside compound, an extraction method and an application. Background technique [0002] The indole structure is the most widely existing hybrid structure in nature, and the indole alkaloids are also the most discovered class of alkaloids so far. Many compounds containing indole structures have been confirmed to have significant biological activities, such as anticancer, anti-inflammatory, antibacterial, antiviral, antioxidative and cholinesterase inhibitory, etc. [1-5]. And the indole ring structure also exists widely in many drugs, representative drugs are: anti-inflammatory drug indomethacin [6], small molecule tyrosine kinase inhibitor SU5614 [7], a kind of drug developed by Boehringer Ingelheim Small molecule angiokinase inhibitor Nintedanib[8] for pancreatic cancer chemotherapy, Vinblastine for solid tumors, Vinorel bine for non-sma...

Claims

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Application Information

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IPC IPC(8): C07H19/044C07H1/08A61K31/7056A61P25/00
CPCC07H19/044C07H1/08A61P25/00
Inventor 邱峰张楠康宁丁丽琴曹世杰
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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