Method for extracting taxane active ingredients from Chinese yew efficiently

A technology for taxanes and active ingredients, applied in chemical instruments and methods, organic chemistry, preparation of sugar derivatives, etc., can solve the problems of consumption of organic solvents, high safety, hidden dangers of environmental protection, low extraction yield, etc. The amount of organic solvent used, the effect of reducing the cost of separation and purification, and reducing the difficulty of separation and purification

Active Publication Date: 2013-11-27
浙江大德龙生物技术有限公司
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  • Abstract
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Problems solved by technology

The biggest problem that these methods exist is that extraction yield is low (generally about 70%), causes huge waste of re

Method used

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  • Method for extracting taxane active ingredients from Chinese yew efficiently

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Case 1: ① Set up the experimental device according to the accompanying drawings in the instruction manual, add 500 g of fresh branches and leaves of Taxus chinensis (three-year-old) into the extraction container (10-DABIII content 0.01%, paclitaxel content 0.004%, 7-xylosyl paclitaxel content 0, tricuspid mannine content 0.001%), add 200g of macroporous resin in the resin column, add 5 liters of 0.2% formic acid aqueous solution in the extraction solvent turnover heating tank, the extraction solvent temperature is controlled at 30~60 ℃, circulation extracts 24 hours, washes with methanol 1000ml Removing the resin column, extracting and concentrating the eluate after concentrating and recovering methanol to obtain extractum 0.96g, HPLC assay extractum (10-DABIII content 5.21%, paclitaxel content 0, 7-xylosyl paclitaxel content 0, cephalomannine content 0%) 10-DABIII extraction yield 99.8%.

[0021] ② Replace the extraction solvent with (50%) methanol aqueous solution to ...

Embodiment 2

[0023] ① Build the experimental device according to the accompanying drawings in the instruction manual, add 500 g of dried branches and leaves of Taxus chinensis (three-year-old) (10-DABIII content 0.025%, paclitaxel content 0.008%, 7-xylosyl paclitaxel content 0, cephalomannine) into the extraction container Content 0.002%), add macroporous resin 200g in the resin column, add 5 liters of 0.5% acetic acid aqueous solution in the extraction solvent turnover, add 0.5% acetic acid aqueous solution in the tank, control the temperature of the extraction solvent at 30~60 ℃, circulate and extract for 24 hours, use methanol 1000ml to elute the resin column After the eluate was concentrated and recovered methanol, it was extracted and concentrated to obtain 2.5g of extractum, which was determined by HPLC (10-DABIII content 5%, paclitaxel content 0, 7-xylosyl paclitaxel content 0, cephalomannine content 0%) The extraction yield of 10-DABIII was 100%.

[0024] ② Replace the extraction s...

Embodiment 3

[0026] ① Build the experimental device according to the accompanying drawings in the instruction manual, add 500 g of southern yew bark (ten years old) (0.01% of 10-DABIII content, 0.02% of paclitaxel content, 0.05% of 7-xylosyl paclitaxel content, Alkali content 0.002%), add 200g of macroporous resin in the resin column, add 5 liters of 0.5% formic acid aqueous solution in the extraction solvent turnover adding tank, the extraction solvent temperature is controlled at 30~60 ℃, circulation extracts 16 hours, elutes resin with 1000ml of methanol column, the eluate is concentrated and recovered after methanol is extracted and concentrated to obtain 0.98g of extract, which is determined by HPLC (10-DABIII content 5.1%, paclitaxel content 0, 7-xylosyl paclitaxel content 25.5%, cephalomannine content 0 %) 10-DABIII extraction yield 100%, 7-xylosyl paclitaxel extraction yield 100%.

[0027]② Replace the extraction solvent with (60%) ethanol aqueous solution to extract the slag after...

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Abstract

The invention discloses a method for extracting taxane type active ingredients from Chinese yew efficiently. The method comprises the following steps of: firstly extracting with water, further extracting with alcohol, and further purifying by a traditional purification method to get paclitaxel, 10-deacetyl baccatin III, taxol-7-xyloside, cephalomanine and other non-water-soluble taxane type substance monomers. According to the method disclosed by the invention, macroporous resin is applied to the extraction process, the extraction yield of the active ingredients is far higher than that of a traditional extraction method, the using quantity of an organic solvent is further significantly reduced, and the method is suitable for large-scale production of the paclitaxel and comprehensive extraction of other taxane active ingredient substances.

Description

technical field [0001] The invention relates to a method for efficiently extracting effective components of taxanes such as paclitaxel, 10-deacetylbaccatin III, 7-xylosyl paclitaxel, and cephalomannine from Taxus chinensis, especially the macroporous resin The method applied in the extraction process greatly improves the extraction efficiency and reduces the production cost. Background technique [0002] 10 Deacetylbaccatin III (10-DABIII), 7-xylosyl paclitaxel, cephalomannine and other taxanes are medicines for the synthesis of anticancer drugs paclitaxel (taxol) and docetaxel (docetaxel) intermediate. Paclitaxel is a medicinal ingredient extracted or semi-synthesized from the bark, roots and branches of Taxus chinensis, and docetaxel is a new semi-synthesized compound. Paclitaxel and docetaxel have a broad anticancer spectrum, and are effective against drug-resistant tumor cells such as cisplatin and doxorubicin. Paclitaxel and docetaxel can combine with tumor cell tubu...

Claims

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Application Information

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IPC IPC(8): C07D305/14C07H17/04C07H1/08
Inventor 李兰星李宁宇
Owner 浙江大德龙生物技术有限公司
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