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Novel bufadienolide compound as well as preparation method and uses thereof

A technology of bufadienolactone and total bufadienolactone, which is applied in the field of new bufadienolactone compounds and their preparation and application, and can solve problems such as uncontrollable, high incidence, and allergic reactions

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

[0008] However, the current toad preparations are all used as crude extracts, and the ingredients are extremely complex, except for bufagenin, bufatoxin, and indole alkaloids (such as 5-hydroxytryptamine, bufotryptamine, bufathione, etc.) , also contains various types of chemical components such as amino acids, reducing sugars, steroids, and peptides
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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  • Novel bufadienolide compound as well as preparation method and uses thereof
  • Novel bufadienolide compound as well as preparation method and uses thereof
  • Novel bufadienolide compound as well as preparation method and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1: Preparation of Bufadienolactone Extract

[0046] Get toad skin 10kg and extract 2 times with 95% ethanol, the amount of alcohol used is 8 times, and the time of each extraction is 60 minutes, the combined filtrate, the filtrate decompresses and reclaims ethanol to no alcohol smell, and puts it on a D101 macroporous resin column (Tianjin Nankai University Chemical Plant), first eluted with water, then eluted with 50% ethanol, then eluted with 95% ethanol, collected the latter, reclaimed the solvent under reduced pressure, and dried to obtain 49g of bufadienolactone extract. The content of dienolactone was 32.1%.

Embodiment 2

[0047] Example 2: Preparation of Bufadienolactone Extract

[0048] 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 2 times, the water layer was extracted 3 times with an equal amount of n-butanol, the n-butanol layer was decompressed to recover the solvent, and dried to obtain 26 g of bufadienolactone extract, the content of the total dienolactone was 60.3%.

Embodiment 3

[0049] Example 3: Preparation of Bufadienolactone Extract

[0050] Take 10kg of dry toad skin 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 the ethanol until it has no alcohol smell, and put it on HPD-100 macroporous resin Column (produced by Cangzhou Baoen Chemical Co., Ltd.), first eluted with water, then eluted with 40% ethanol, and then eluted with 95% ethanol, collected the latter, recovered the solvent under reduced pressure, and the crude extract was chromatographed on a silica gel column. Elute with chloroform-methanol gradient, collect and combine the corresponding fractions, recover the solvent, and dry to obtain 15 g of bufadienolactone extract, the content of the total dienolactone is 90.6%.

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PUM

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Abstract

The invention relates to a novel bufadienolides compound and a preparation method and application thereof, and provides a bufadienolides compound having a general formula (I) or pharmaceutical acceptable salts as well as bufadienolides extract or medication composition containing the compound. The compound and the extract have effect for inhibiting tumour cell activity and application to preparation of anti-tumour drugs. The invention also provides the preparation method applicable for industrial production of the compound and the extract.

Description

technical field [0001] The present invention relates to a new compound of bufadienolides or a pharmaceutically acceptable salt thereof, and a bufadienolide extract or a pharmaceutical composition containing the compound. The invention also relates to a preparation method of the compound and its application in inhibiting tumor cells. 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 us...

Claims

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Application Information

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IPC IPC(8): C07J17/00C07J71/00A61K31/585A61P35/00
Inventor 邱鹰昆姜永涛陈继永何杰李振
Owner SHANDONG LUYE PHARMA CO LTD
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