3-carbonyl hyperin, extraction method and application thereof in preparation of antitumor drugs

A carbonyl begonia ketone and anti-tumor drug technology, applied in the application field of preparing drugs, can solve the problems of unreported pharmacological activity, etc., and achieve the effect of inhibiting the ability of clone formation, inhibiting tumor angiogenesis, and inhibiting tumor growth and metastasis

Active Publication Date: 2020-09-25
TIANJIN NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, no specific pharma

Method used

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  • 3-carbonyl hyperin, extraction method and application thereof in preparation of antitumor drugs
  • 3-carbonyl hyperin, extraction method and application thereof in preparation of antitumor drugs
  • 3-carbonyl hyperin, extraction method and application thereof in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Extraction and identification of 3-carbonyl begonia ketone

[0022] Take 10 kg of Kunming mountain crabapple rhizomes, crush them, pass through a 10-mesh sieve, and ultrasonically extract them three times with 500 L of 95% ethanol, with a starting power of 3 kw and a frequency of 40 kHz, filter and collect the extract, and concentrate the extract under reduced pressure until it has no alcohol smell to obtain a concentrate. The concentrated solution was sequentially extracted with petroleum ether and dichloromethane, the dichloromethane extract was collected, washed 3 times with 2 times the amount of saturated sodium bicarbonate aqueous solution, and the dichloromethane extract was concentrated to a small volume to obtain a sample concentrate. Then mix dichloromethane-methanol-water according to 6:4:1, let stand for 24h to separate layers, take the upper phase as the stationary phase and pump it into the high-speed countercurrent chromatograph, and the lower phase as the ...

Embodiment 2

[0030] Detecting the antitumor activity of 3-carbonyl begonia ketone and begonia ketone in vitro by MTT assay

[0031] Experimental principle: MTT, chemical name 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide), is a general cell staining agent. There is a succinate dehydrogenase related to NADP in the mitochondria of living cells, which can reduce exogenous yellow MTT to insoluble blue-purple crystal formazan (Formazane), which is deposited in the cells. In dead cells, this enzyme disappears, and MTT are not restored. After dissolving Formazane with DMSO, use a microplate reader to detect the change in optical density at a wavelength of 550nm, which can display the survival and growth of cells in the detection system. People often use MTT method to measure the growth inhibitory effect of test drugs on cells, and then evaluate cytotoxicity.

[0032] The purpose of the experiment: To detect the inhibitory activity of 3-carbonyl begonia ketone and the existing com...

Embodiment 3

[0040] Effects of 3-carbonyl begonia ketone on the colony formation ability of lung cancer A549 and H1299 cells

[0041] Experimental principle: Plate colony formation assay is one of the effective methods to measure cell proliferation ability, and the cells that form clones are adherent cells with strong proliferative activity. The cell clone formation rate indicates the number of adherent cells that survive and form clones after inoculation of cells, which can reflect two important traits of cell population dependence and proliferation ability. The clonogenic ability of the tumor cells treated with the compound shows the anti-tumor effect of the compound.

[0042] Experimental procedure: Lung cancer A549 and H1299 cells were inoculated in a six-well plate at 500 cells / well, respectively, and blank control, 2.5 μM 3-carbonyl begonia ketone and 5 μM 3-carbonyl begonia ketone were added. Culture each well in 2mL conventional medium, change the medium every 2-4 days, stop the c...

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Abstract

The invention discloses 3-carbonyl hyperin as well as an extraction method and application thereof in the preparation of antitumor drugs. The structure of 3-carbonyl hyperin is shown as (I). The extraction method of 3-carbonyl hyperin comprises the following steps: 1) crushing roots and stems of tripterygium hypoglaucum, extracting with ethanol, and carrying out reduced pressure concentration to obtain a concentrate; 2) extracting the concentrate with petroleum ether and dichloromethane in sequence, collecting the dichloromethane extract, and concentrating the dichloromethane extract to a small volume to obtain a sample concentrate; 3) separating the sample concentrate in a high-speed counter-current chromatograph, collecting a main component, concentrating the main component under reducedpressure to a small volume, and purifying by gel column chromatography Sephadex-LH20. The compound has remarkable inhibition activity on solid tumors such as lung cancer, can promote apoptosis of tumor cells, inhibits angiogenesis, remarkably inhibits growth and metastasis of tumors in lung cancer tumor-bearing mice, and prolongs the lifetime of the mice. The invention also provides an application of 3-carbonyl hyperin in the preparation of antitumor drugs.

Description

technical field [0001] The invention relates to a new compound extracted from natural plants, an extraction method and its application in the preparation of medicine. Background technique [0002] Kunming Mountain Begonia (Tripterygium hypoglaucum (Lévl.) Hutch) is a plant of the Euonymus family Tripterygium genus, and its roots are mostly used as medicine, which has the effects of dispelling rheumatism, dispelling paralysis and dredging collaterals, and rejuvenating tendons and bones. There are a variety of abietane-type diterpenoids in its medicinal parts, and there are certain Chinese literature on its anti-tumor activity in the prior art reports——Studies on the chemical components of the rhizome of Begonia Kunming (Song Qiang, etc., Journal of Chinese Herbal Medicine, November 2019, 5395-5399) disclosed an abietane-type diterpenoid compound - 3β-hydroxy-4-4-hydroxymethyl-astosin-8,11,13-triene-7-one (the Named as Begonia ketone in the literature), its structural formula...

Claims

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Application Information

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IPC IPC(8): C07C49/747C07C45/78C07C45/79C07C45/80A61K31/122A61P35/00
CPCC07C49/747C07C45/78C07C45/79C07C45/80A61P35/00C07B2200/07C07C2603/26Y02A50/30
Inventor 李西川周晓涛山长亮
Owner TIANJIN NORMAL UNIVERSITY
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