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Application of ellagitannins flavone in preparation of antitumor drugs

A technology of ellagitannin flavonoids and anti-tumor drugs, which is applied in the field of application of ellagitannin flavonoids in the preparation of anti-tumor drugs, can solve the problems of high dosage, drug resistance, lack of selectivity, etc. To achieve the effect of simple drug route, inhibition of proliferation and good solubility

Inactive Publication Date: 2015-04-29
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is to overcome the high dosage of clinical antineoplastic drugs in the prior art, the unsatisfactory drug effect, the lack of selectivity, the generation of drug resistance and the inhibition of the toxicity of the hematopoietic system, digestive system, immune system, nervous system and endocrine system. Shortcomings and deficiencies such as side effects provide an application of ellagitannin flavonoids in the preparation of antitumor drugs

Method used

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  • Application of ellagitannins flavone in preparation of antitumor drugs
  • Application of ellagitannins flavone in preparation of antitumor drugs
  • Application of ellagitannins flavone in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1 Thonningianins A inhibits the proliferation of tumor cells of different histological types

[0034] Take vigorously growing human liver cancer HepG-2 cells, human liver cancer Bel-7402 cells, human lung cancer A549 cells and human breast cancer MCF-7 cells, centrifuge at 1000 rpm for 5 minutes, discard the supernatant, and use a mass fraction of 10% fetus Adjust the number of cells in DMEM medium with bovine serum to 3×10 4 / mL, 100μL inoculated in 96-well culture plate, placed in 5% CO 2 After incubating at 37°C for 24 hours in the incubator, the supernatant was discarded, and DMEM medium containing Thonningianins A was added to each group (final concentrations of 20μg / mL, 40μg / mL, 60μg / mL, 80μg / mL and 100μg / mL ). At 37℃, 5% CO 2 Culture in an incubator for 24 hours, discard the supernatant, wash twice with PBS, add 200 μL of serum-free DMEM medium and 20 μL of thiazole blue (MTT) to each well, incubate in the incubator for 4 hours, discard the supernatant, Add...

Embodiment 2

[0036] Example 2 Thonningianins A inhibits the proliferation of liver tumor cells

[0037] Take vigorously growing human liver cancer HepG-2 cells and human normal liver cells LO2, centrifuge at 1000 rpm for 5 minutes, discard the supernatant, and adjust the cell number to 3×10 with DMEM medium containing 10% fetal bovine serum 4 / mL, 100μL inoculated in 96-well culture plate, placed in 5% CO 2 After incubating at 37°C for 24 hours in the incubator, the supernatant was discarded, and DMEM medium containing Thonningianins A was added to each group (final concentrations of 20μg / mL, 40μg / mL, 60μg / mL, 80μg / mL and 100μg / mL ). At 37℃, 5% CO 2 Culture in an incubator for 24 hours, discard the supernatant, wash twice with PBS, add 200 μL of serum-free DMEM medium and 20 μL of thiazole blue (MTT) to each well, incubate in the incubator for 4 hours, discard the supernatant, Add 150 μL of dimethyl sulfoxide (DMSO) to each well, place it in a micro oscillator in the dark for 10 minutes, and ...

Embodiment 3

[0039] Example 3 Real-time quantitative detection of the effect of Thonningianins A on the growth of HepG-2 tumor cells

[0040] Take the vigorously growing HepG-2 tumor cells, centrifuge at 1000 rpm for 5 min, discard the supernatant, and adjust the cell number to 3×10 with DMEM medium containing 10% fetal calf serum 4 / mL, 100μL inoculated in 96-well culture plate with microelectronic sensor, placed in 5% CO 2 , 37 ℃ incubator, using real-time cell electronic sensor system to monitor the culture for 24 hours, discard the supernatant, each group was added DMEM medium containing Thonningianins A (final concentration of 25μg / mL, 35μg / mL and 45μg / mL), the control group was added DMEM medium without Thonningianins A. At 37℃, 5% CO 2 Real-time monitoring and cultivation in the incubator for 24 hours.

[0041] Real-time quantitative monitoring analysis chart shows that Thonningianins A can significantly inhibit the growth of tumor cells HepG-2, and it is concentration-dependent. The c...

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Abstract

The invention belongs to the field of biological medicine and particularly relates to an application of ellagitannins flavone in preparation of antitumor drugs. The structural formula of the ellagitannins flavone Thonningianins A is shown by formula I; the Thonningianins A can effectively inhibit the proliferation of tumor cells and significantly promote cell apoptosis so as to result in death of the tumor cell, moreover, the dosage of the Thonningianins A is low, the toxic or side effect is lower than that of common chemotherapeutics on clinic, the route of administration is simple and the operation is easy.

Description

Technical field [0001] The invention belongs to the field of biomedicine, and specifically relates to an application of ellagitannin flavonoids in the preparation of antitumor drugs. Background technique [0002] Tumor mortality ranks first or second in the world, which greatly threatens human survival and health. Tumor treatment has always been a difficult problem faced by the medical community. Surgery, chemotherapy and radiotherapy are the usual treatment methods. Most of the existing treatment methods have serious side effects, such as bleeding, cognitive impairment, and multiple occurrences, which are mainly related to their non-selective cytotoxicity. For chemotherapy, the resistance of emerging drugs is another serious problem. Finding new anti-cancer drugs with small side effects and selective killing has always been one of the main research goals of scientists around the world. Natural products, including plants, marine life and microorganisms, have always attracted t...

Claims

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Application Information

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IPC IPC(8): A61K31/7024A61P35/00A61P1/16A61P11/00A61P15/14
Inventor 姜建国张恬恬许喜林
Owner SOUTH CHINA UNIV OF TECH
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