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Pharmaceutical application of 12-dehydroxy-21-hydroxy protopanoxadiol

A technology of ginsengdiol and dehydroxylation, which is applied in the chemical industry, can solve the problems of less reports on ginsengdiol, and achieve obvious effects of inhibiting proliferation and tumor inhibition

Inactive Publication Date: 2012-03-07
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But, about 12-dehydroxyl-21-hydroxyl protopanaxadiol report of the present invention is less

Method used

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  • Pharmaceutical application of 12-dehydroxy-21-hydroxy protopanoxadiol

Examples

Experimental program
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Effect test

Embodiment 1

[0035] Example 1 MTS method to measure the growth inhibitory effect of 12-dehydroxyl-21-hydroxyl protopanaxadiol on liver cancer cells

[0036] 3000 QGY cells (purchased from the Cell Bank of the Chinese Academy of Sciences) were inoculated into 96-well plates, cultured for 24 hours to make them adhere to the wall, and then 12-dehydroxy-21-hydroxyprotopanaxadiol (purchased from the Shanghai Institute of Materia Medica, Chinese Academy of Sciences) was added. ), 6 concentration gradients were set, and 3 replicate wells were set for each concentration. Cells at 37°C, 5% CO 2 After culturing for 72 hours under the same conditions, the culture medium was discarded, and the cell viability was measured with an MTS kit (Promega).

[0037] The test method is: wash the cells once with serum-free medium, and add the pre-prepared MTS chromogenic solution according to the amount of 100 μl / well (add 2ml of solution 1 and 100μl of solution 2 to 10ml of serum-free medium, and mix well). A ...

Embodiment 212

[0040] Example 21 2-Dehydroxyl-21-hydroxyprotopanaxadiol's growth inhibitory effect on human leukemia cells

[0041] Using cck-8 kit (Japan Dojin Chemical Research Institute) detection.

[0042] step:

[0043] 1) K562 cells (purchased from ATCC) were evenly seeded in a 96-well plate, with 10,000 cells per well.

[0044] 2) Waiting to adhere to the wall, add medicine after overnight, add medicine (12-dehydroxy-21-hydroxyprotopanaxadiol concentrations are 50, 16.67, 5.56, 1.85, 0.62 μM, each concentration has 3 replicate wells.

[0045] 3) After culturing for 48 hours, replace the complete medium with a mixture of serum-free medium and CCK8 (10:1), and incubate in a 37°C incubator for 2 hours.

[0046] 4) Take 450nm as the measurement wavelength and 650nm as the reference wavelength, and measure the reading on a microplate reader.

[0047] Results: The IC50 value of 12-dehydroxy-21-hydroxyprotopanaxadiol on k562 cells was 5.22 μM.

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Abstract

The invention belongs to the fields of chemical engineering and medicaments and relates to application of 12-dehydroxy-21-hydroxy protopanoxadiol in preparation of antitumor medicaments. The invention provides the application of the 12-dehydroxy-21-hydroxy protopanoxadiol in preparation of the antitumor medicaments. Tumor cells comprise liver cancer, leukaemia, adenocarcinorma of lung or pancreatic cancer. The 12-dehydroxy-21-hydroxy protopanoxadiol belongs to natural products and has a certain clinical utilization value. A micromolecular compound provided by the invention as a new antitumor medicament or an assistant component of the medicament is developed; the antitumor effect is obvious; the micromolecular compound is environmental friendly; and the invention provides a new way and means for treating and curing tumors.

Description

technical field [0001] The invention belongs to the fields of chemical industry and medicine, and relates to the application of 12-dehydroxyl-21-hydroxyprotopanaxadiol in the preparation of antitumor drugs. Background technique [0002] 12-dehydroxy-21-hydroxy protopanaxadiol, the structural formula is as follows. [0003] [0004] In 1967, Chen et al. analyzed its structure (Dryobalanone, a 21-hydroxydammarane triterpene. Cheung, Hee-Tai. Et al. Tetrahedron. Letters (1967), (29), 2807-9.). [0005] The following year, another report introduced the method of extracting the compound from the dipterocarp tree. Take the dipterobalsam extract, go through alumina (light petroleum solvent, benzene and chloroform) chromatography to obtain dipterocaractone, and then react with methanol containing sodium borohydride to obtain 12-dehydroxyl-21-hydroxyl protopanaxadiol Alcohol (Compound III, R=OH. Constituents of Dipterocarpaceae resins. II. Structure of dryobalanone from Dryobala...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61P35/00A61P35/02
Inventor 余龙唐丽莎刘祖龙胡立宏王正
Owner FUDAN UNIV
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