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Novel 19-demethyl resibufogenin compound and application thereof to preparation of antitumor pharmaceutical preparation

A technology for demethylation toad and anti-tumor drugs, applied in the field of natural medicine and chemical medicine, can solve the problems of complex chemical composition of toad skin, and achieve the effect of low toxicity

Active Publication Date: 2015-09-09
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the chemical composition of toad skin is complex, and only about 40 kinds of bufolides have been reported so far (Chemistry&biodiversity,2011:559-567), and its anti-tumor active ingredients need to be further explored

Method used

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  • Novel 19-demethyl resibufogenin compound and application thereof to preparation of antitumor pharmaceutical preparation
  • Novel 19-demethyl resibufogenin compound and application thereof to preparation of antitumor pharmaceutical preparation
  • Novel 19-demethyl resibufogenin compound and application thereof to preparation of antitumor pharmaceutical preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Extraction, separation and structural identification of the compound of Example 1

[0025] (1) Take 11 kg of dried toad skin, grind it into 10-50 mesh toad skin coarse powder with a pulverizer, heat and reflux extraction with 3 times the mass of distilled water at 100°C for 4 times, 1 hour each time; combine the extracts and decompress Concentrate to a density of 1.15, add ethanol and mix evenly to make the alcohol content 80% (v / v), let it stand for 24 hours, absorb the supernatant, concentrate under reduced pressure to obtain the water extract; then extract the toad skin powder after water extraction The residue was heated and refluxed with 3 times the mass of 95% (v / v) ethanol at 80°C to extract 4 times, 1 hour each time; the extracts were combined and concentrated under reduced pressure to obtain the ethanol extract; the total water extract and the total ethanol extract The mixtures were combined, suspended with 6L of water, extracted with 6L of chloroform, and repe...

Embodiment 2

[0036] Example 2 Inhibitory Effect of Bufogargarin A on Tumor Cell Proliferation

[0037] Cells in logarithmic growth phase (human liver cancer cell HepG2, human non-small cell lung cancer cell A549, human cervical cancer cell Hela, human colon cancer cell Lovo, human breast cancer cell MCF-7, human esophageal cancer cell Eca-109) (All cell lines were purchased from American Type Culture Collection, ATCC) Digested with trypsin, centrifuged, resuspended, and counted cells at 1×10 6 / mL inoculated in a 96-well culture plate, 100 μL per well, after the cells adhered to the wall, dilute the drug to be tested into a certain concentration gradient, set 4 parallel replicate wells for each concentration, and set a blank control group and a positive control group at the same time (Doxorubicin), placed in a constant temperature incubator (37 ° C, 5% CO 2Cultured in medium for 72h. Aspirate off the medium, add 30 μL of MTT solution (5 mg / mL) to each well, continue to incubate for 4 h, ...

Embodiment 3

[0041] Example 3 Anti-tumor effect of Bufogargarin A in vivo

[0042] Test method: Kunming mice weighing 18-22 g (purchased from Guangdong Provincial Animal Center) were randomly divided into groups of 10 mice. Tumor cells (S180 ascites tumor cells) were inoculated in the armpits of their right forelimbs with 2×10 7 After 24 hours, intraperitoneal injection was administered once a day, and the animals were sacrificed after 10 days of continuous administration, and the tumors were taken and weighed.

[0043] The tumor inhibition rate was calculated according to the following formula:

[0044] Tumor inhibition rate (%)=[1-(average tumor weight of administration group) / average tumor weight of control group]×100%

[0045] Statistical analysis was processed by t test, and P<0.05 was considered to have significant difference. The results are shown in Table 3.

[0046] Table 3. The inhibitory effect of Bufogargarin A on the growth of mouse S180 solid tumor (n=10)

[0047]

[...

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Abstract

The invention relates to the field of natural drugs and chemical drugs and particularly relates to application of a novel 19-demethyl resibufogenin compound to preparation of an antitumor pharmaceutical preparation. The novel 19-demethyl resibufogenin compound has a structure as shown in the formula I, is named as Bufogargarin A and is extracted and separated from toad skin. The Bufogargarin A disclosed by the invention has remarkable antitumor activity in vitro and vivo and is not observed to have remarkable toxic or side effects under a therapeutic dose so as to have a favorable pharmaceutical prospect and be applied to preparation of the antitumor pharmaceutical preparation. The antitumor pharmaceutical preparation contains Bufogargarin A and the balance of pharmaceutical auxiliary materials or other compatible drugs; the pharmaceutical auxiliary materials can be various pharmaceutical solvents, disintegrating agents, flavoring agents, preservatives, colorants and binding agents; and the antitumor pharmaceutical preparation includes various clinical dosage forms.

Description

technical field [0001] The invention relates to the fields of natural medicine and chemical medicine, in particular to a new 19-demethylbufolide compound and its application in drug preparations for treating tumors. Background technique [0002] Cancer is the number one killer that endangers human life, and the research and development of anticancer drugs has always been a hot topic in the world's medical circles. [0003] Toad skin is the dry skin of Bufo bufo gargarizans Cantor or Bufo melanostictus Schneider, an animal of the Bufo family. It is mainly produced in Zhejiang, Jiangsu, Shandong, Hebei and other places in my country. It is cool in nature, bitter in taste, has the effects of clearing away heat and detoxification, diuresis and reducing swelling. It is mainly used to treat carbuncle, swollen toxin, scrofula, etc. It is often used clinically to treat malignant tumors and chronic bronchitis (Dictionary of Chinese Medicine, 1977: 2713-2714) . Research results in r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00A61K31/585A61P35/00
CPCC07J71/0021
Inventor 叶文才王磊张冬梅李宝晶
Owner JINAN UNIVERSITY
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