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Green separating and structuring method of anit-cancer components in taxus chinensis

A structural method and technology of yew, applied in chemical instruments and methods, preparation of sugar derivatives, sugar derivatives, etc., can solve problems such as imperfect theory, small production scale, weak process level, etc., and achieve the goal of increasing process added value Effect

Inactive Publication Date: 2014-11-05
徐燕锋
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  • Application Information

AI Technical Summary

Problems solved by technology

Although my country is rich in yew resources, the scaled extraction of paclitaxel was developed relatively late, and it did not begin until the 1990s.
Moreover, it mainly provides raw materials for paclitaxel for clinical use in developed countries, the technology level is weak, and the theory is not yet perfect.
In practical applications, the production scale is small and the market penetration rate is low
It causes a serious waste of resource utilization and it is difficult to realize the maximum added value

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0014] First, four taxane compounds were extracted from the branches and leaves of Taxus chinensis by ultrasonic extraction. The main indicators were: the extraction solvent was 80% ethanol solution; the extraction solid-liquid ratio was 1:30; for 3 times.

[0015] 10-deacetylbaccatin III, 7-xylosyl-10-deacetyl paclitaxel, tricuspid The contents of mannine and paclitaxel are 5.12%, 6.23%, 15.97% and 3.85%, respectively, which are 13.54 times, 12.19 times, 10.41 times and 20.48 times of the content of each substance obtained by the traditional resin separation method. The recoveries of the four compounds were 94.96%, 77.32%, 88.09% and 95.25%, respectively.

[0016] The method for purifying 10-deacetylbaccatin III and 7-xylosyl-10-deacetyl paclitaxel by normal phase silica gel column chromatography for the four compounds after separation; After purification by reverse phase silica gel column chromatography for paclitaxel and cephalomannine, 10-deacetylbaccatin III, 7-xylosyl-...

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Abstract

A green separating and structuring method of anit-cancer components in taxus chinensis. Branches and leaves of the taxus chinensis are employed as raw materials. Research of extraction, separation and structure modification of taxol and other three taxanes is carried out. A high-efficiency rapid separation operation is carried out to the four substances through a resin chromatography method. In addition, the other three taxanes are converted to form the taxol or docetaxel which is anti-cancer drug. A conclusion is described as follows: conditions of detection, extraction, resin chromatography and purification of the four substances are determined and the structure modification of the other three taxanes, after being purified, is carried out so that the other three taxanes are converted to form the taxol or the docetaxel.

Description

technical field [0001] The present invention uses yew branches and leaves as raw materials to study the extraction, separation and structural modification of paclitaxel and other three taxanes. Background technique [0002] At present, in the research on the extraction, separation and semi-synthesis of paclitaxel and other taxane compounds, the most studied is the extraction and separation of paclitaxel from yew plants. However, other taxane compounds have only been identified in their structures and have not been studied in depth. Among them, the extraction method is the most reported, and almost all extraction methods are used in the extraction research of taxanes, including traditional methods such as solvent cold soaking method, heat reflux method, Soxhlet extraction method, and the super superiority that appeared later, However, it is limited to laboratory research and is difficult to realize industrial production. [0003] In addition, the separation methods for taxa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D305/14C07H17/04C07H1/08
CPCC07D305/14C07H1/08C07H17/04
Inventor 徐燕锋
Owner 徐燕锋