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Molecular engram polymer of vinblastine, and preparation method

A technology of molecular imprinting and vinblastine, applied in the field of organic polymer compounds, can solve the problems of high purification loss, irreversible adsorption, and unsatisfactory product purity, and achieve the effect of strong selectivity and high affinity

Inactive Publication Date: 2007-05-09
SOUTHERN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The one-time column uses basic alumina as the column packing, and isocratic or gradient washing is generally used in different proportions such as benzene-petroleum ether, benzene-chloroform, benzene-dichloromethane, dichloromethane-chloroform, ethyl acetate-petroleum ether, etc. Take off, this method is the method for large-scale production at present, and shortcoming is that the purity of product is unsatisfactory [Gedeon R, Vegyeszeti GRT.Isolation of vinblastine and leurosine[P].Hung: 153200, 1966-10-22.(CA 1967 , 66:118854)]
The second column passing method is to treat the crude extract with a dextran gel column and a silica gel column successively, and the product has better purity [Gunasekera SP.Method of isolating vinblastine[P]. WO: 8803135, 1988-05-05.( CA 1988,109:134967)], but the dextran gel used in this method is more expensive, and repeated use will cause irreversible adsorption and poor separation effect
However, due to the extremely low content of vinblastine in plants and the presence of a large number of compounds with similar chemical structures and properties, it is not only difficult to separate by conventional column chromatography, but also has a lot of losses during the purification process, and it is difficult to obtain high purity and high concentration simultaneously. Yield products, so it is extremely necessary to find more effective separation materials
So far, there are no reports about vinblastine molecularly imprinted polymers

Method used

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  • Molecular engram polymer of vinblastine, and preparation method
  • Molecular engram polymer of vinblastine, and preparation method
  • Molecular engram polymer of vinblastine, and preparation method

Examples

Experimental program
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Effect test

preparation example 1

[0025] First add 0.1 mmol of vinblastine to the ampoule, add 0.5 mmol of methacrylic acid and 1.5 ml of toluene, and shake repeatedly on the oscillator for 60 minutes. Then add 4.5 mmol of ethylene glycol dimethacrylate and 15 mg of azobisisobutyronitrile, mix well by ultrasonication for 10 minutes, then blow with nitrogen for 5 minutes, vacuumize and seal the tube with an alcohol torch. The polymerization was initiated thermally and allowed to polymerize in a 60°C water bath for 18 hours. After the polymerization reaction is complete, the monolith is obtained in the polymerization tube, the tube is broken and the monolith is broken into smaller particles, and the resulting irregular shaped particles are sieved to 25-75 microns. To remove fine particles (<25 microns) in the 25-75 micron fraction, the material was repeatedly settled with acetone until the supernatant became clear. Then the obtained particles were transferred to a paper casing and placed in a Soxhlet extractor ...

preparation example 2

[0027]First add 0.1 mmol of vinblastine to the ampoule, add 0.5 mmol of methacrylic acid and 1.5 ml of toluene, and shake repeatedly on the oscillator for 60 minutes. Then add 4.5 mmol of ethylene glycol dimethacrylate and 15 mg of azobisisobutyronitrile, mix well by ultrasonication for 10 minutes, then blow with nitrogen for 5 minutes, vacuumize and seal the tube with an alcohol torch. The polymerization was initiated thermally and allowed to polymerize in a 40°C water bath for 24 hours. After the polymerization reaction is complete, the monolith is obtained in the polymerization tube, the tube is broken and the monolith is broken into smaller particles, and the resulting irregular shaped particles are sieved to 25-75 microns. To remove fine particles (<25 microns) in the 25-75 micron fraction, the material was repeatedly settled with acetone until the supernatant became clear. Then the obtained particles were transferred to a paper casing and placed in a Soxhlet extractor d...

preparation example 3

[0029] First add 0.1 mmol of vinblastine to the ampoule, add 0.5 mmol of methacrylic acid and 1.5 ml of toluene, and shake repeatedly on the oscillator for 60 minutes. Then add 4.5 mmol of ethylene glycol dimethacrylate and 15 mg of azobisisobutyronitrile, mix well by ultrasonication for 10 minutes, then blow with nitrogen for 5 minutes, vacuumize and seal the tube with an alcohol torch. The polymerization was initiated thermally and allowed to polymerize in a water bath at 80°C for 10 hours. After the polymerization reaction is complete, the monolith is obtained in the polymerization tube, the tube is broken and the monolith is broken into smaller particles, and the resulting irregular shaped particles are sieved to 25-75 microns. To remove fine particles (<25 microns) in the 25-75 micron fraction, the material was repeatedly settled with acetone until the supernatant became clear. Then the obtained particles were transferred to a paper casing and placed in a Soxhlet extract...

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PUM

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Abstract

This invention discloses a vinblastine molecular imprinted polymer, which has the imprinting sites of the template molecule vinblastine. The vinblastine molecular imprinted polymer is prepared by heat-initiated polymerization of vinblastine 1 part, functional monomer 3-10 parts, crosslinker 10-50 parts and appropriate pore-forming agent at 40-80 deg.C. The obtained vinblastine molecular imprinted polymer has unique affinity, high selectivity and excellent molecular reorganization to vinblastine, and can be used as separation filler for extracting, separating and enriching vinblastine from natural plants and biological samples.

Description

technical field [0001] The invention relates to an organic polymer compound, in particular to an alkaloid molecularly imprinted polymer, and also relates to a preparation method of the polymer. Background technique [0002] Vinblastine is a dimeric indole alkaloid with obvious anti-tumor activity isolated from Vinca rosea L. (Catharanthus roseus G.Don) which can inhibit tubulin assembly and prevent Spindle filaments form, thereby arresting mitosis in metaphase. It is mainly used clinically to treat Hodgkin's disease and chorioepithelial carcinoma, and also has certain curative effects on lymphosarcoma, melanoma, ovarian cancer, leukemia, etc. It is one of the most widely used anticancer drugs at present. The source of vinblastine is mainly natural plants, but the content in natural plants is extremely low, only a few parts per million to a few parts per hundred thousand. Although it can be obtained by chemical synthesis and semi-synthesis, the cost is relatively high; Tiss...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08J9/26C08F2/44C08F20/18C08K5/09
Inventor 朱全红冯建涌杨卫东
Owner SOUTHERN MEDICAL UNIVERSITY
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