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Application of ginkgol C17:1 in treatment of liver cancer

A kind of ginkgo phenol, technology for treating liver cancer, applied in the field of biomedicine

Inactive Publication Date: 2014-04-09
JIANGSU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Ginkgo biloba C17: 1 involved in the present invention and its effect on inhibiting SMMC-7721 cell growth and migration, and the activity of inhibiting the growth of nude mice bearing HepG solid tumors in vivo , so far no relevant reports

Method used

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  • Application of ginkgol C17:1 in treatment of liver cancer
  • Application of ginkgol C17:1 in treatment of liver cancer
  • Application of ginkgol C17:1 in treatment of liver cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1: Preparation and analysis of ginkgolic acid homologues

[0040] Preparation of Ginkgolic Acid Homologs Weigh 100 g of dried Ginkgo biloba testa and crush it, ultrasonically extract 5 times the amount of petroleum ether three times, each time for 2 hours, combine the extracts, filter under reduced pressure, evaporate the solvent to obtain a petroleum ether extract. Dissolve the extract in a small amount of petroleum ether and apply it to a silica gel column (Φ3.2×40cm), elute with petroleum ether: ether: formic acid = 89:11:1 (v / v / v), and perform thin-layer chromatography Fluorescence at 254 nm was detected, and the ginkgolic acid fraction was collected; the column was repeated several times. Finally, the ginkgolic acid components were washed with water until neutral, and the eluent was evaporated to obtain a homologous mixture of ginkgolic acids.

[0041] HPLC Analysis of Ginkgolic Acid HomologsVarian high performance liquid chromatography, SinoC...

Embodiment 2

[0043] Embodiment 2: Preparation and analysis of ginkgo biloba homologues

[0044] Preparation of Ginkgol Homologs by Decarboxylation Mix 1.0 g of ginkgolic acid homologs and 0.02 g of NaOH in a flask, stir at 135-140°C until no bubbles are generated, cool the mixture to room temperature, and extract with petroleum ether. Filtration and concentration gave a dark brown oil.

[0045] After the dark brown oil was dissolved in ethyl acetate, the sample was loaded on a silica gel column (a glass column with a diameter of 3.2×40 cm), and the mixed solution of chloroform and chloroform:methanol (the ratio gradually changed from 9:1 to 5:5, V / V) elution, detected by thin-layer chromatography at 254nm fluorescence, collected ginkgo phenol fractions, concentrated to dryness; repeated column once, to obtain the ginkgo phenol homologous mixture.

[0046] HPLC Analysis of Ginkgo Biloba Homologs The mobile phase was methanol: water = 92:8 (v / v); the flow rate was 1 mL / min; the ult...

Embodiment 3

[0047] Example 3: Preparation and identification of Ginkgo biloba C17:1

[0048] Preparation of Ginkgo biloba C17:1 Ginkgo biloba homologues were dissolved in tetrahydrofuran: methanol = 1:1 to form a solution, and ginkgo biloba monomers were separated on an HPLC semi-preparative column ZORBAX SB-C18 (250 × 9.4 mm, 15 μm), and the mobile phase was methanol: water = 90 :10, flow rate 3.0 mL / min; UV detector detects the absorption peak at 275 nm, collects the fraction of Ginkgool C17:1, and repeats once to obtain Ginkgool C17:1 monomer.

[0049] HPLC Analysis of Ginkgo biloba C17:1 Analyze the separated ginkgool C17:1 (analysis conditions are the same as the analysis of ginkgool homologues), and its HPLC analysis chart is shown in figure 2 , figure 2 The peak of ginkgool C17:1 is mainly seen in the concentration, and the peaks of other ginkgool homologues are very small. The purity of ginkgool C17:1 obtained by using the area normalization method is more than 90%. ...

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Abstract

The invention relates to application of ginkgol C17:1 in treatment of liver cancer, belonging to the field of biological drugs. The ginkgol C17:1 is prepared through a method comprising the following steps: preparing ginkgolic acid from gingko (leaves, fruits and episperm); performing heat treatment to decarboxylate the ginkgolic acid; and separating, and purifying to obtain the ginkgol C17:1, wherein structural identification shows that the ginkgol C17:1 has cis / trans isomeric structures. The prepared ginkgol C17:1 can effectively inhibit proliferation of human liver cancer cells SMMC-7721 and inhibit migration of the SMMC-7721 cells in vitro, and drug resistance can not be easily produced; and the prepared ginkgol C17:1 can inhibit growth of nude mouse loaded HepG solid tumors in vivo. The new application of the ginkgol C17:1 provided by the invention is of great importance in preparation of antitumor drugs and especially in preparation of anti-liver cancer drugs.

Description

technical field [0001] The invention belongs to the field of biomedicine, and relates to the application of Ginkgo biloba C17:1 in the treatment of liver cancer, specifically, Ginkgo biloba C17:1 can inhibit the growth of tumor cells, effectively inhibit the migration of SMMC-7721 cells, and inhibit the solid tumor bearing HepG in nude mice growth and should not develop resistance. Background technique [0002] Hepatocellular carcinoma, referred to as liver cancer, is a malignant tumor originating from intrahepatic liver cells, bile duct epithelial cells, endothelial cells and connective tissue stromal cells. It is one of the most common malignant tumors in the world that seriously threaten human health and life. , the death toll ranks second among malignant tumors. [0003] At present, chemical drug therapy is still one of the main means of liver cancer treatment. Although dozens of anti-tumor drugs have been discovered, this does not mean that the research of anti-tumor ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C39/21C07C37/70A61K31/05A61P35/00A61P35/04
CPCC07C37/004C07C39/21
Inventor 杨小明王云飞李月英
Owner JIANGSU UNIV
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