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Toadpoison ligand extract as well as preparation method and application thereof

A technology of bufagenin and bufagenin, which is applied in the field of bufagenin extract and its preparation and application, and can solve the problems of high incidence, complex components, and failure to control

Inactive Publication Date: 2008-05-14
SHANDONG LUYE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the current toad preparations, such as toad analgesic ointment, toad injection, cinobufacin injection, and compound toad skin capsules, are still used as crude extracts, and the ingredients are extremely complex. , indole alkaloids (such as 5-hydroxytryptamine, bufotryptamine, bufathiophene, etc.), it also contains amino acids, reducing sugars, steroids, peptides and other types of chemical components
Therefore, in clinical use, toad preparations have the following two main disadvantages: ① low rate of killing tumor cells, ② high incidence of allergic reactions, vascular irritation symptoms, gastrointestinal and cardiac toxicity and other adverse reactions, which are all Due to the failure to remove the ineffective and adverse reaction ingredients, and the failure to control the real effective ingredients

Method used

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  • Toadpoison ligand extract as well as preparation method and application thereof
  • Toadpoison ligand extract as well as preparation method and application thereof
  • Toadpoison ligand extract as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Preparation of Bufagenin Extract

[0022] Take 10kg of dry toad skin and extract 4 times with 80% ethanol, the amount of alcohol used is 9 times, and the extraction time is 120 minutes each time, the filtrate is combined, and the filtrate is decompressed to recover the ethanol until it has no alcohol smell, and puts it on AB-8 macroporous resin Column (manufactured by Tianjin Nankai University Chemical Plant), first eluted with water, then eluted with 30% ethanol, and then eluted with 80% ethanol, collected the latter, recovered the solvent under reduced pressure, and extracted the aqueous solution with an equal amount of ethyl acetate Twice, the ethyl acetate layer was decompressed to recover the solvent, and dried to obtain 42 g of toad skin extract, the content of bufagenin was 55.3%, which contained 15.1% cinobufagin and 15.8% cinobufagenin.

Embodiment 2

[0023] Example 2: Preparation of Bufagenin Extract

[0024] Take 1 kg of dried toad venom and extract 4 times with 80% ethanol, the amount of alcohol used is 9 times, and the extraction time is 120 minutes each time, the filtrate is combined, and the filtrate is decompressed to recover ethanol until it has no alcohol smell, and put it on the AB-8 macroporous resin column (produced by the No. 2 chemical factory of Nankai University in Tianjin), elute with water first, then elute with 30% ethanol, then elute with 80% ethanol, collect the latter, recover the solvent under reduced pressure, and dry to obtain 172g of Bufagenin extract , in terms of cinobufagin, the content of bufagenin is 70.3%, which contains 20.1% cinobufagin and 17.8% lipobufagenin.

Embodiment 3

[0025] Example 3: Preparation of Bufagenin Extract

[0026] Take 2 kg of dried toad venom and extract twice with 95% ethanol, the amount of alcohol used is 10 times, and the extraction time is 90 minutes each time, the filtrate is combined, and the filtrate is decompressed to recover ethanol until it has no alcohol smell, and puts it on AB-8 (Tianjin Nankai University Chemical plant production) macroporous resin column, first eluted with water, then eluted with 40% ethanol, then eluted with 95% ethanol, collected the latter, reclaimed the solvent under reduced pressure, dried to obtain 332g of bufagenin extract, Based on cinobufagin, the content of bufogenin is 85.6%, which contains 21.4% cinobufagin and 20.3% lipobufagenin.

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Abstract

The invention provides a bufadienolides extraction extracted from the toad skin or the toad venom; wherein, the weight percentage of the bufadienolides (accounted by the cinobufagin) can reach above 55%. The invention adopts the extraction method that: the toad venom, the toad skin or the bufo siccus is extracted by the ethanol; after the recovery of the ethanol, the macroporous resin column on the concentration liquid is eluted by the water and the low concentration alcohol, and is eluted by the high concentration alcohol, then the final product is gained through collecting the eluent and reducing the pressure of the recovery solvent to pass drying or extraction. The invention has an advantage that: the invention also provides the drug composition using the extraction as the active component, the suppressing the tumour cells active function of the extraction and the application in the preparation of the anti-tumor drug.

Description

technical field [0001] The invention relates to a bufagenin extract extracted from toad skin or toad venom, a preparation method and application thereof. Background technique [0002] There are more than 250 species of toads distributed all over the world. There are nearly 10 species in my country, and the three main species are Bufo bufo andrewsi Schmidt, Bufo bufo gargarizans Cantor and Bufo melanostitus Schneider. The name of toad was first recorded in "Famous Doctors", and as early as "Shen Nong's Materia Medica", it contained the nature, flavor and indications of "shrimp". "Materia Medica Mengguan": "Pungent in taste, cool in air, and slightly poisonous", "Materia Medica Zaixin": enters the four meridians of the heart, liver, spleen, and lung. Ancient and modern prescriptions are widely used to pull out toad to reduce swelling, relieve pain and kill insects, strengthen the heart and diuresis. [0003] Commonly used Chinese medicinal materials based on toads include t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K35/56A61P35/00A61K35/65
Inventor 邱鹰昆姜永涛陈继永何杰张英
Owner SHANDONG LUYE PHARMA CO LTD
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