Application of

The technology of ester compound and toad is applied in the application field of bufa lactone compound in the research and development of new anti-tumor drugs, and can solve the problems of complex composition, allergic reaction, no Hellebogen and its derivatives, etc.

Inactive Publication Date: 2010-09-15
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the current toad preparations are all crude extracts used as medicine, and the ingredients are extremely complex. In addition to bufoligand, bufotoxin, and indole alkaloids, it also contains amino acids, reducing sugars, steroids, peptides, etc. Various types of chemi...

Method used

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Embodiment 1

[0020] Example 1: Preparation of Bufadienolactone Extract

[0021] Get 10Kg of toad skin and extract 3 times with 95% (v / v) ethanol, the amount of alcohol used for each extraction is 10 times the weight of the sample toad skin, and the extraction time is 120 minutes each time, the filtrate is combined, and the filtrate is concentrated under reduced pressure to 10L , on XAD-4 macroporous resin (Rohm and Haas), first eluted with 3 times column volume of water, then eluted with 3 times column volume of 30% ethanol (v / v), and then eluted with 3 times column volume 95% ethanol (v / v) was eluted, the latter was collected, the solvent was recovered under reduced pressure, and dried to obtain 125 g of bufadienolactone extract.

Embodiment 2

[0022] Example 2: Preparation of helleboregenin

[0023] 75 g of the bufadienolactone extract obtained in Example 1 was separated by preparative HPLC (Waters Xterra C18, A: 0.1% (v / v) formic acid water; B: 0.1% (v / v) formic acid acetonitrile, Gradient conditions: 5% B ~ 25% B, 30min; 25% B ~ 50% B, 22min; 50% B ~ 95% B, 18min; 95% B, 5min, 300nm), from the fifth minute to the 65th minute , the effluent per minute is taken as a component, and a total of 60 components (Fr.1~Fr.60) are collected.

[0024] Fr.13 recovered solvent, separated by HPLC (the chromatographic column is based on silica gel, and the functional ligand is β-cyclodextrin), A: 0.1% formic acid water; B: 0.1% formic acid acetonitrile, gradient conditions: 95% B to 60% B, 40min, 300nm), monitor with ultraviolet, collect chromatographic peak, reclaim solvent, obtain compound I 11mg, HPLC detection content is 99%, its NMR, mass spectrometry, ultraviolet data see Table 1, Table 2, figure 1 , figure 2 , acco...

Embodiment 3

[0029] The cytotoxicity of embodiment three helleboregenins to SMMC-7721 and A549

[0030] Materials SMMC-7721 and A549 cell lines were purchased from the Second Military Medical University in China

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Abstract

The invention relates to antitumor drugs, in particular to application of hellebores aglucon and derivatives thereof, and one or more of pharmaceutically acceptable salts. Experiments of in vitro cell biology show that the compounds can induce cycle arrest of various tumor cells of liver cancer, lung cancer, prostate glands cancer, leucocythemia and the like, remarkably inhibit the cell proliferation, and can be used for preparing drugs for inhibiting the growth of various tumor cells including the liver cancer.

Description

technical field [0001] The present invention relates to antitumor drugs, in particular to the application of a bufolide compound in the research and development of new antitumor drugs; said bufalide compound refers to helleboregenin and its derivatives, including its pharmaceutical acceptable salt; [0002] Background technique [0003] 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 Sinensis, Bufo Sinina and Black-orbited Toad. Ancient prescriptions are widely used in toad detoxification and swelling, ketone killing insects, strengthening the heart and diuresis. At present, there are Chansu Analgesic Ointment, Chansu Injection, Cinobufacin Injection and Compound Chanpi Capsules and other preparations on the market, which are used in clinical anti-tumor, analgesic, diuresis and swelling, and enhance the body's immunity. The clinical use of toad preparations in the a...

Claims

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Application Information

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IPC IPC(8): A61K31/585A61P35/00
Inventor 刘艳芳丁劲张秀莉宁北芳梁鑫淼王红阳
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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