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Application of 3,5,3',4'-trihydroxy-stilbene-3'-b-D-glucoside in preparation of medicines for treating cancers

A technology of trizaperoside and drugs, which is applied in the field of application of trizaperoside in the preparation of drugs for treating cancer, and can solve problems such as cancer recurrence and drug resistance of cancer cells

Active Publication Date: 2015-06-03
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are many types of drugs clinically used for cancer treatment, but most drugs are taken for a long time, and the side effects are unbearable for patients, and long-term use of a drug is likely to make cancer cells develop drug resistance, which can easily lead to cancer recurrence. The development of cancer drugs is of great significance

Method used

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  • Application of 3,5,3',4'-trihydroxy-stilbene-3'-b-D-glucoside in preparation of medicines for treating cancers
  • Application of 3,5,3',4'-trihydroxy-stilbene-3'-b-D-glucoside in preparation of medicines for treating cancers
  • Application of 3,5,3',4'-trihydroxy-stilbene-3'-b-D-glucoside in preparation of medicines for treating cancers

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1MTT method detects the cytotoxic effect of trizapereside on human tumor cells cultured in vitro and human normal cells

[0041] Take A549, HCT116, colo205, HL-60, BGC-823, CCRF-CEM, MDA-MB-231, HepG2, 95-D, ZR-75-30, PANC-1, PC-3 in the logarithmic growth phase and MRC-5 cells, the adherent cells were first digested and then prepared with fresh culture medium to make 4-5×10 4 per mL, add 100 μL to each well of a 96-well plate, and place at 37°C, 5% CO 2 Cultured in an incubator. After 24 hours, the samples were added, and the test sample tristilbene, the positive control doxorubicin (DOX) and the solvent excipient hydroxypropyl-β-cyclodextrin were diluted with PBS(-) to a final concentration of 100, 10, 1, 0.1, 0.01, 0.001, 0.0001 μg / mL, diluted and added to each well (10 μL / well), set 3 replicate wells for the same sample and the same concentration. After continuing to culture for 72 hours, add 20 μL of 5 mg / mL MTT solution to each well, place in the inc...

Embodiment 2

[0049] Example 2 Curative effect of tristilbene on nude mouse xenograft model of human tumor

[0050] The well-grown A549 solid tumor was cut into uniform small pieces about 3 mm in size under aseptic conditions, and a piece was inoculated subcutaneously in the right armpit of each nude mouse with a trocar. Thirteen days after inoculation, the tumors were regrouped according to the size of the tumors, and the nude mice with too large and too small tumors were eliminated. The average tumor volume of each group was basically the same, and the following 5 groups were set up:

[0051] Blank control group: sterile normal saline (0.9% sodium chloride injection); (25mL / kg, iv×14); 12 nude mice;

[0052] Positive control group: CTX (30mg / kg, iv×7); diluted with sterile saline; 8 nude mice;

[0053] Test group 1: Trizastilbene L (25mg / kg, iv×14); diluted with PBS(-); 8 nude mice;

[0054] Test group 2: Tristilbene M (50mg / kg, iv×14); diluted with PBS(-); 8 nude mice;

[0055] Test g...

Embodiment 3

[0080] The preparation of embodiment 3 medicines

[0081] Weigh the following raw materials:

[0082]

[0083]

[0084] The above raw materials are pulverized, mixed uniformly, granulated, dried, and compressed into tablets to obtain trizaperidin tablets.

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Abstract

The invention relates to the technical field of medicine preparation, and in particular relates to application of 3,5,3',4'-trihydroxy-stilbene-3'-b-D-glucoside in preparation of medicines for treating cancers. The cytotoxic effect of the 3,5,3',4'-trihydroxy-stilbene-3'-b-D-glucoside on 12 human tumor cells cultured in vitro and a human normal cell is tested through an MTT method; and the 3,5,3',4'-trihydroxy-stilbene-3'-b-D-glucoside has a relatively good inhibiting effect on proliferation of a human lung cancer cell line, a human colon cancer cell line, a human erythroleukemia cell line, a human gastric cancer cell line and a human breast cancer cell line, and has no inhibiting action on proliferation of human normal cells. The curative effect of the 3,5,3',4'-trihydroxy-stilbene-3'-b-D-glucoside on a nude mouse transplantation tumor of a human lung cancer cell line A549 is also tested. The result shows that the 3,5,3',4'-trihydroxy-stilbene-3'-b-D-glucoside has obvious inhibiting action on proliferation of the nude mouse transplantation tumor of the human lung cancer cell line A549 after continuous intravenous injection for 14 days; and the dose-effect relationship is obvious.

Description

technical field [0001] The invention relates to the technical field of medicine preparation, in particular to the application of tristilbeside in the preparation of medicines for treating cancer. Background technique [0002] Lhasa rhubarb is a plant of the Polygonaceae Rhubarb genus. It is produced in eastern Tibet, Sichuan and other places. It is born in hillside grasslands at an altitude of 4200-4600 meters. Patent CN101244129A researches the chemical composition and biological activity of Lhasa rhubarb, and finds that Lhasa rhubarb has a high content of stilbene compounds, and the extract with stilbene compounds as the main component has the effect of preventing and treating cardiovascular and cerebrovascular diseases . [0003] Tristilbene is a stilbene compound extracted from Lhasa rhubarb with a content of 3%-5%. It can also be extracted or chemically synthesized from taro rhubarb, Hetao rhubarb and North China rhubarb. Chemical name: (E)-1-(3,5-dihydroxyphenyl)-2-(...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7034A61P35/00A61P35/02
Inventor 陈云建杨兆祥张建文王萍
Owner KPC PHARM INC
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