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Cardiac glycoside compound and preparation method as well as application thereof
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A compound, cardiac glycoside technology, applied in the field of medicine, can solve the problem that the cost performance cannot meet the needs of clinical treatment and so on
Inactive Publication Date: 2015-04-22
THE KEY LAB OF CHEM FOR NATURAL PROD OF GUIZHOU PROVINCE & CHINESE ACADEMY OF SCI
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Problems solved by technology
Although a variety of biological technologies and drugs have shown beneficial effects on tumor treatment, their cost performance still cannot meet the needs of clinical treatment.
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Embodiment 1
[0024] Example 1: Preparation of compound bufalin-3b-acrylate:
[0025] Take the toad venom medicinal material, cut it into pieces, add 10-30 times the amount of 30-95% methanol or ethanol and reflux 2-8 times, each time for 3-5 hours, until the extract is colorless, combine all the extracts, and recover the solvent under reduced pressure. Dry to obtain the total extract; the total extract is dissolved in methanol, the sample is mixed with silica gel for column chromatography, and the normal phase silica gel column chromatography (300 ~ 400 mesh) is separated, and the volume ratio is 100: 0 ~ 0: 100 chloroform / Gradient elution with methanol mixed solvent, followed by prefabricated silica gel plate for detection, silica gel thin layer chromatography TLC development system is a mixed solvent with a volume ratio of chloroform / methanol of 100:10, and the collection containing compound C 27 h 36 o 5 Fractions, recovered solvent concentrated to dryness; ODS reverse-phase column, ...
Embodiment 2
[0026] Example 2: Identification of the structure of the compound bufalin-3b-acrylate:
[0027] Using spectroscopic techniques, including ultraviolet, infrared, nuclear magnetic resonance, and high-resolution mass spectrometry, the compound in Example 1 is identified; its spectral data are as follows: colorless crystals, mp: 204-205 °C; EI-MS m / z : 440[M] + , 368, 350, 325, 214. HR-EI-MS: 440.2565 [ M ] + , (calculated value: 440.2563, error: 0.2 milli-mass units); [α] = -5°( c 0.023, CHCl 3 ); UV ( CHCl 3 ) lambda max : 300 nm ( 0.563 ); IR( KBr ) ν max : 3507, 1718, 1540, 1630, 1540, 1451, 1406, 1296, 1201, 1048, 835 cm -1 , 1 H-NMR and 13 See Table 1 for C-NMR data.
Embodiment 3
[0028] Example 3: Anti-A549 human lung cancer cell line activity test of compound bufalin-3b-acrylate in vitro:
[0029] The tumor cell line used in the experiment was A549 (human lung cancer cell line) provided by Wuhan China Center for Type Culture Collection. The sulforhodamine B protein staining method (SRB) was used, and the test included a blank control group, a standard control group, a positive control group (doxorubicin) and three different concentrations (1.00×10 -3 mol / L, 1.00×10 -4 mol / L, 1.00×10 -5 mol / L) samples to be tested, and three parallels were set for each concentration. The operation steps are as follows: the human tumor cell A549 leukemia cell line was incubated at 37 °C, 5% CO 2 After culturing under the same conditions for 72 h, the culture medium was discarded, the cells were fixed with 10% cold TCA, and placed at 4 °C for 1 h. After 1 h, wash 5 times with distilled water, dry naturally in air, add 100 μL of 4 mg / mL SRB solution (dissolved in ...
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Abstract
The invention provides a cardiac glycoside compound and a preparation method as well as an application thereof, and relates to the technical field of medicines. The cardiac glycoside compound is called as bufalin-3b-acrylic ester, has the molecular formula of C27H36O5 and the following structural formula and is prepared from toad venom as a traditional Chinese medicine in a separating manner. According to an antitumor test in vitro, the cardiac glycoside compound can be used for obviously inhibiting A549 human lung cancer cell strains and K562 human leukemia cell strains, wherein IC50 (half maximal inhibitory concentration) values are respectively 7.16*10<-3>mu mol / L and 6.83*10<-3>mu mol / L. Therefore, a novel chemical entity or a leading compound for developing an anti-tumor medicine is provided, i.e., the approach with an important value for developing and utilizing the traditional Chinese medicine is realized. The invention further discloses the method for preparing the cardiac glycoside compound bufalin-3b-acrylic ester from the traditional Chinese medicine toad venom in the separating manner.
Description
technical field [0001] The invention relates to the technical field of medicine, in particular to a cardiac glycoside compound and its preparation method and application. Background technique [0002] In recent years, with the increasingly serious environmental pollution and the aging population, tumors have become the number one cause of human death. According to the survey, in my country, 1.4-1.5 million cancer deaths and 1.8-2 million cancer cases occur each year. Among urban residents, the cause of death from cancer is 24.4%, among rural residents it is 18.3%, and it is expected that the morbidity and mortality of some common tumors such as lung cancer will increase significantly. The major topic of disease prevention and control research in the world is one of the core issues to be solved urgently by the whole society, especially in the medical field. Drug therapy is one of the main means of tumor prevention and treatment, and the only means of systemic treatment and ...
Claims
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Patent Type & Authority Patents(China)
IPC IPC(8): C07J19/00A61K31/585A61P35/00A61P35/02
Inventor 张援虎徐冉徐梅郝小江
Owner THE KEY LAB OF CHEM FOR NATURAL PROD OF GUIZHOU PROVINCE & CHINESE ACADEMY OF SCI
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