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Total toadpoison lactones extraction with anti-tumor function, preparation and application thereof

A technology of total bufolide and anti-tumor effect, which is applied in the direction of anti-tumor drugs, medical preparations containing active ingredients, drug combinations, etc., and can solve problems such as low content of active ingredients, unstable clinical curative effect, and serious adverse reactions , to achieve the effects of low toxic and side effects, inducing tumor cell differentiation, and strong pharmacological effects

Active Publication Date: 2012-01-04
吴宗好
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] It can be seen that most of the alkaloids extracted by the above-mentioned patent method are alkaloid components, while the bufaxin lactone components with significant anti-tumor activity such as repobugenin, cinobufagin, and bufalin are completely lost, and these The method and process are too simple, the content of active ingredients is low, there are many impurities, the stability of the preparation is poor, the quality control index is low, the clinical curative effect is unstable, and the adverse reactions are serious and difficult to control

Method used

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  • Total toadpoison lactones extraction with anti-tumor function, preparation and application thereof
  • Total toadpoison lactones extraction with anti-tumor function, preparation and application thereof
  • Total toadpoison lactones extraction with anti-tumor function, preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Cut 500g of dry toad skin into pieces, reflux extraction with 50-95% methanol for 2-5 times, combine the extracts, recover methanol, centrifuge the concentrated solution, take the supernatant, put it on a polyamide column for adsorption, wash with water first, and then use Elute with 10-95% ethanol, combine the eluent mainly containing bufolide, recover the solvent to obtain the crude product of total bufolide, then extract with chloroform (or ethanol-chloroform mixed solvent), recover the organic solvent to obtain Total bufolide extract with anti-tumor effect;

[0040] In the extract prepared in this example, the determination results of the total bufolide content, the content of bufabugenin, the content of cinobufin base and the content of bufafolin are shown in Table 1.

[0041] Table 1

[0042] group

[0043] Add propylene glycol or Tween 80 as a solubilizer to total bufolide, adjust to 1 mg / ml with water for injection, add 2% to 10% xylitol and 0.1% to 0...

Embodiment 2

[0045] Cut 500g of dry toad skin into pieces, reflux extraction with ether for 2 to 5 times, combine the extracts, recover the ether to dryness, add ethanol to dissolve, absorb on a silica gel column, elute with ether, and combine the elutions mainly containing bufolide liquid, reclaim the solvent to obtain the crude product of total bufolide, then extract through chloroform (or ether-chloroform mixed solvent), recycle the organic solvent to obtain the total bufolide extract with antitumor effect;

[0046] In the extract prepared in this example, the determination results of the total bufotoxin content, the content of bufabugenin, the content of cinobufin base and the content of bufafolin are shown in Table 2.

[0047] Table 2

[0048] group

[0049] Add propylene glycol or Tween 80 as a solubilizer to total bufolide, adjust to 1 mg / ml with water for injection, add 2% to 10% lactose and 0.1% to 0.5% activated carbon, boil for 20 minutes, filter, and use as a medicina...

Embodiment 3

[0050] Example 3 Cut 500 g of dried toad skin into pieces, reflux extract with 50-95% ethanol for 2-5 times, combine the extracts, recover the ethanol until there is no alcohol smell, centrifuge the concentrated solution, take the supernatant, and put it on a cation exchange resin column for adsorption , wash with water first, then elute with ammonia water, combine the eluents mainly containing bufolide, and recover the solvent to obtain the crude product of total bufolide, then extract with ethanol (or ethanol-ether mixed solvent), and recover the solvent The total bufolide extract with anti-tumor effect is obtained;

[0051] In the extract prepared in this example, the determination results of the total bufafinolide content, the content of bufabugenin, the content of cinobufin base and the content of bufafolin are shown in Table 3.

[0052] table 3

[0053] group

[0054] Add solubilizer propylene glycol or Tween 80 to total bufolide, adjust to 1 mg / ml with water ...

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Abstract

The invention discloses a total bufogenin extract with antitumor function and also discloses a preparation method of the extract and application thereof in the preparation of antitumor medicines. The total bufogenin extract of the invention is prepared by organic solvent extraction, column chromatography separation and purification of dried toadskin; the content of total bufogenin is over 80 percent, wherein the content of resibufogenin is over 12 percent, the content of cinobufagin is over 4 percent, and the content of bufotalin is over 10 percent. Compared with the prior art, the invention eliminates bufotenine alkaloid which has irritation, is easy to cause hypersensitivity but has no antitumor activity, efficiently collects the effective part of total bufogenin which has significant antitumor activity, therefore pharmacological action is stronger, the clinical curative effect is higher and the toxic and side effect is lower. The total bufogenin extract can be prepared into variouspharmaceutical preparations for clinical application, therefore the invention has the functions of killing tumor cells, inducing differentiation and apoptosis of tumor cells, inhibiting the neovascularization of tumor cells and lowering the neoplasm metastasis rate, etc.

Description

technical field [0001] The present invention relates to an active ingredient extract with anti-tumor effect, in particular to an extract of total bufolides (bufaxins, bufotoxins) with anti-tumor effect from dry toad skin and the extract The preparation method of the compound, the present invention also relates to the application of the total bufolide extract in the preparation of antitumor drugs, which belongs to the field of traditional Chinese medicine. Background technique [0002] Cancer is a major killer that endangers human life. Research and development of effective anticancer drugs is a common task faced by drug researchers in the world. In the field of research and development of new anticancer drugs, it is the research and development of anticancer drugs that can transform tumor cells into normal cells (induce tumor cell differentiation), induce tumor cell apoptosis, inhibit tumor cell angiogenesis, and reduce tumor metastasis. At the same time, it is also the mos...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61P35/00A61K9/48A61K9/10A61K9/19A61K9/16A61K9/08A61K31/58A61K35/56A61K9/20A61K35/65
Inventor 吴宗好
Owner 吴宗好
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