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Method of extracting paclitaxel and derivatives thereof from taxus plants

A technology of yew and paclitaxel, applied in the direction of organic chemistry and the like, can solve the problems of inability to apply taxane, waste of resources, etc., and achieve the effects of low solvent usage, improved utilization rate, and reduced cost

Active Publication Date: 2013-06-12
沈阳北创医学检验所有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to solubility reasons, this method cannot be applied to the extraction of other taxanes, resulting in a waste of resources

Method used

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  • Method of extracting paclitaxel and derivatives thereof from taxus plants
  • Method of extracting paclitaxel and derivatives thereof from taxus plants
  • Method of extracting paclitaxel and derivatives thereof from taxus plants

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] After collecting samples of branches and leaves of Mandia and European yew, place them in an oven at 50°C and dry them, crush them into 10-mesh dry powders, weigh 20 g of the powders and add them to two round-bottomed flasks, then add 60 mL of 1% N, Aqueous solution of N-dimethylformamide, sonicated for 5h, statically filtered, and the filter residue was sonicated with 60mL extract solution for 5h, repeated 5 times, combined extract solution 5 times, passed through AB-8 macroporous adsorption resin, adsorbed After completion, wash with deionized water until the effluent is colorless, and then elute with 3 times the column volume of absolute ethanol. The eluate is evaporated to dryness under reduced pressure in a rotary evaporator at 40°C and a vacuum of -0.03Mpa to obtain Extract extract. The extract is dissolved in chromatographic grade methanol, and fixed solution is 100mL, and the useful taxane content is detected by HPLC. The content of each component is as follows:...

Embodiment 2

[0022] After the branches and leaves of Taxus chinensis and South China were collected, they were dried in an oven at 50°C and crushed into 80-mesh dry powder. Weighed 20 g of the powder and put them into two round-bottomed flasks, and then added 200 mL of 5% N,N- Aqueous solution of dimethylformamide, sonicate for 0.5h, let stand and filter, then sonicate the filter residue with 200mL extract solution for 0.5h, repeat this twice, combine the extract solution twice, pass through D101 macroporous adsorption resin, , washed with deionized water until the effluent was colorless, and then eluted with 5 times the column volume of 70% ethanol. The eluate was evaporated to dryness under reduced pressure in a rotary evaporator at 40°C and a vacuum of -0.03Mpa. The solid matter was dissolved with chromatographic grade methanol, and fixed solution was 100mL, and the useful taxane content was detected by HPLC. The content of each component is as follows:

[0023]

[0024] .

Embodiment 3

[0026] After collecting samples of roots and hairs of Mandia and European yew, place them in an oven at 50°C and dry them, crush them into 40-mesh dry powders, weigh 20g of the powders and add them to two round-bottomed flasks, then add 100mL of 3% bismuth The aqueous solution of methyl sulfoxide was sonicated for 2 hours, then filtered, and the filter residue was sonicated with 100mL of the extract for 2 hours. This was repeated 3 times. Wash with ionized water until the effluent is colorless, and then elute with 3 times the column volume of 80% ethanol. The eluate is evaporated to dryness under reduced pressure in a rotary evaporator at 40°C and a vacuum of -0.03Mpa. The solid matter was dissolved with chromatographic grade methanol, and fixed solution was 100mL, and the useful taxane content was detected by HPLC. The content of each component is as follows:

[0027]

[0028]

[0029] .

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Abstract

The invention discloses a method of extracting paclitaxel and derivatives thereof from taxus plants. The method comprises the steps of: by taking acqueous solution of N,N-dimethylformamide and / or dimethyl sulfoxide as an extractant, conducting continuous ultrasonic or heating stirring for extraction, adsorbing extracting solution with macroporous adsorption resin, eluting with ethanol, drying the solvent to obtain an extract. With the extracting method, the paclitaxel, 10-deacetyl baccatin III, deacetyltaxol, 7-xylosyl-10-deacetyltaxol, and other useful taxane compounds can be simultaneously extracted, the extracting method has the characteristics of high extracting rate, low cost and the like; the usage amount of organic solvent can be greatly reduced, the environment pollution can be reduced, and large-scale industrial production can be benefited.

Description

technical field [0001] The invention relates to a method for separating and extracting natural organic compounds from plants, in particular to a method for extracting paclitaxel and its derivatives from branches, leaves or roots of yew plants. Background technique [0002] Paclitaxel (abbreviated as T, formula I) is a first-line anticancer drug, and is widely used in the treatment of various solid cancers such as ovarian cancer, breast cancer, and lung cancer. At present, the way of large-scale production of paclitaxel is mainly to directly extract or extract its semi-synthetic precursor - 10-deacetylbaccatin Ⅲ (abbreviated 10-DABⅢ, formula Ⅱ) from Taxus plants, and then synthesize paclitaxel by synthetic means . In addition to the above two compounds, Taxus plants also contain many structurally similar taxane compounds, such as 10-deacetylpaclitaxel (abbreviated 10-DAT), 7-xylose-10-deacetylpaclitaxel (abbreviated 10-DAXT), baccatin, etc., using these compounds, can also ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D305/14
Inventor 栾宏伟张辉
Owner 沈阳北创医学检验所有限公司