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Method for separating and purifying paclitaxel from taxus chinensis branches and leaves or bark

A technique for separating and purifying branches and leaves of Taxus chinensis, which is applied in the field of natural medicine extraction, can solve the problems of low efficiency, difficulty in large-scale production, complicated operation and the like, and achieves the effects of simple operation, high-efficiency separation and good repeatability.

Inactive Publication Date: 2014-12-24
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because these taxane compounds are very similar to paclitaxel in terms of chemical structure and polarity, the separation of paclitaxel is difficult and the separation and purification process is complicated.
[0003] At present, the separation and purification methods of paclitaxel mainly include: (1) column chromatography, but the operation is relatively complicated, the efficiency is not high, and different fillers are required to be used in combination; (2) preparative high-performance liquid chromatography, which requires high equipment and reagents , the cost is high, and it is difficult to produce on a large scale; (3) high-speed countercurrent chromatography requires a large number of experiments to select a suitable solvent system; (4) supercritical fluid extraction, the equipment cost is high, and the purity of the extracted compound is low

Method used

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  • Method for separating and purifying paclitaxel from taxus chinensis branches and leaves or bark
  • Method for separating and purifying paclitaxel from taxus chinensis branches and leaves or bark
  • Method for separating and purifying paclitaxel from taxus chinensis branches and leaves or bark

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] 1. Treatment of yew branches and leaves

[0064] (1) Crush yew branches and leaves and pass through a 24-mesh sieve. Take 500 g of powder and add methanol at a ratio of 1:10 (g / mL), soak for 5 h, ultrasonically extract for 1 h, and filter to obtain the filtrate. The residue is calculated as 1: Add methanol at a ratio of 10 (g / mL) and repeat the extraction for 1 h, repeat once, and combine the filtrates.

[0065] (2) The filtrate was concentrated under reduced pressure below 60°C to obtain the extract (48.75 g). The obtained extract was ultrasonically dispersed in water, extracted 3 times with petroleum ether (1:1, v / v); the water layer was obtained after standing and separated, and the water layer was extracted 3 times with ethyl acetate (1:1, v / v ), the ethyl acetate layer was concentrated to dryness under reduced pressure to obtain ethyl acetate extract (3.36 g).

[0066] 2. Basic alumina column chromatography

[0067] (1) Take the ethyl acetate extract obtained in...

Embodiment 2

[0084] 1. Treatment of yew bark

[0085] (1) Take yew tree bark and crush it and pass it through a 24-mesh sieve. Take 500 g of the powder and add methanol at a ratio of 1:10 (g / mL), soak for 5 h, reflux for 1 h, and filter to obtain the filtrate. : Add methanol at a ratio of 10 (g / mL) and repeat the extraction for 1 h, repeat once, and combine the filtrates.

[0086] (2) The filtrate was concentrated under reduced pressure below 60°C to obtain the extract (40.62 g). The obtained extract was ultrasonically dispersed in water, extracted 3 times with petroleum ether (1:1, v / v); the water layer was obtained after standing and separated, and the water layer was extracted 3 times with ethyl acetate (1:1, v / v ), the ethyl acetate layer was concentrated to dryness under reduced pressure to obtain ethyl acetate extract (4.26 g).

[0087] 2. Basic alumina column chromatography

[0088] (1) Take the ethyl acetate extract obtained in step 1, add an appropriate amount of dichloromethan...

Embodiment 3

[0105] 1. Treatment of yew branches and leaves

[0106] (1) Take yew branches and leaves and pass through a 24-mesh sieve. Take 500 g of powder and add methanol at a ratio of 1:5 (g / mL), soak for 5 hours, reflux for 1 hour, and filter to obtain the filtrate. The residue is calculated as 1: Add methanol at a ratio of 5 (g / mL) and repeat the extraction for 1 h, repeat twice, and combine the filtrates.

[0107] (2) The filtrate was concentrated under reduced pressure below 60°C to obtain the extract (45.85 g). The obtained extract was ultrasonically dispersed in water, extracted twice with petroleum ether (1:0.5, v / v); the water layer was obtained after standing and separated, and the water layer was extracted twice with ethyl acetate (1:0.5, v / v ), the ethyl acetate layer was concentrated to dryness under reduced pressure to obtain ethyl acetate extract (3.18 g).

[0108] 2. Basic alumina column chromatography

[0109] (1) Take the ethyl acetate extract obtained in step 1, ad...

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Abstract

The invention discloses a method for separating and purifying paclitaxel from taxus chinensis branches and leaves or bark. The method comprises the following steps: firstly, immersing taxus chinensis branches and leaves or bark by methanol, carrying out ultrasonic extraction or reflux extraction, and concentrating at reduced pressure to obtain an extract; secondly, and extracting the extract sequentially by petroleum ether and ethyl acetate to obtain an ethyl acetate extract; thirdly, carrying out chromatography on the ethyl acetate extract through an alkaline aluminum oxide column to obtain a paclitaxel-enriched component, and treating the paclitaxel-enriched component by utilizing a partial precipitation method which uses methanol-water as a system to obtain a crude paclitaxel product; and finally, refining to obtain paclitaxel with purity over 98.5 percent by using flash chromatography as a separation means and methanol-water as an eluting system. The method is simple and convenient to operate, has the advantages of low cost, good repeatability, high efficiency and high product purity, and can be used for large-scale production of paclitaxel.

Description

technical field [0001] The invention belongs to the technical field of natural medicine extraction. More specifically, it relates to a method for separating and purifying paclitaxel from branches, leaves or bark of Taxus chinensis. Background technique [0002] Southern yew ( Taxus chinensis var. Mairei), also known as beautiful yew, is a plant of Gymnospermae, Taxaceae, and Taxus. As one of the most widely distributed yew plants, it is mainly distributed in the Yangtze River Basin, Nanling Mountains and other places. It is the main tree species for the production of anticancer drug Taxol in my country. Paclitaxel is a unique secondary metabolite of Taxus genus. It is one of the most anticancer active natural compounds, and it is also the most popular new anticancer drug in the international market. The mechanism of action of paclitaxel is to promote tubulin polymerization, inhibit depolymerization, maintain tubulin stability, and inhibit cell mitosis. It is mainly used ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D305/14
CPCC07D305/14
Inventor 徐新军梁智坤陶俊妃
Owner SUN YAT SEN UNIV
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