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Biflavone compound and application thereof to preparation of medicine for treating cancer

A compound and cancer technology, applied in the field of cancer treatment and drug preparation, can solve the problems of unclear material basis, lack of preparation of high-content total flavonoid active compounds, uncontrollable quality, etc.

Active Publication Date: 2016-05-11
FUJIAN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, in the prior art, there is no report on the specific active compounds in the anti-tumor components of cypress cypress, so there are disadvantages such as unclear material basis and uncontrollable quality, and there is a lack of reports on the preparation of high-content total flavonoid active compounds

Method used

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  • Biflavone compound and application thereof to preparation of medicine for treating cancer
  • Biflavone compound and application thereof to preparation of medicine for treating cancer
  • Biflavone compound and application thereof to preparation of medicine for treating cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Example 1 Preparation of Compound 1

[0063] 1. Sample processing of Shishangbai

[0064] After cutting the dry whole plant of Shishangbai into small segments less than 5mm, it is extracted with 70% ethanol by condensing and refluxing, and concentrated by rotary evaporation at low temperature (40-50°C) to obtain ethanol extract extract. Add 10 times the volume (m / v) of double-distilled water to suspend the extract, and extract it with equal volumes of petroleum ether, dichloromethane and ethyl acetate in sequence. paste. Take the ethyl acetate extract and perform the following steps to prepare the compound of the present invention.

[0065] 2. HPLC preparation and separation

[0066] The preparative column is an Agilent SB-C18 column (250mm×21.2mm, 7μm), mobile phase acetonitrile-water (44:56, v / v), flow rate 7ml / min, detection wavelength 280nm, room temperature, sample volume is 100μL. Separated by high performance preparative liquid chromatography, such as figure 1 ( fig...

Embodiment 2

[0082] Example 2 Evaluation of in vitro anticancer activity of compound 5

[0083] The compound 5 prepared above was used to evaluate the anticancer activity in the following human tumor cell lines in vitro.

[0084] 1. Compound solution preparation: accurately weigh a certain amount of compound 5, dissolve it with dimethyl sulfoxide (DMSO), and dilute to the concentration of 500, 250, 125, 62.5, 31.25 μg / mL with the growth medium of each cell. 5 concentrations of the test solution, the positive control drug doxorubicin preparation solution was sequentially diluted with the growth medium of each cell into 3 concentration test solutions of 5, 2.5, 1.25μM.

[0085] 2. Cell lines and cell culture

[0086] Seven human tumor cell lines, including 5 adherent tumor cell lines: human gastric cancer cell line (MKN-45), non-small cell lung cancer (A549), nasopharyngeal carcinoma (CNE1, CNE2), large cell lung cancer (PC -9); 2 kinds of tumor cells are suspension type: human acute promyelocytic ...

Embodiment 3

[0096] Example 3 Evaluation of anti-cancer activity of compound 5 in animal model

[0097] The compound 5 prepared above was used to evaluate the anticancer activity in the following human tumor cell lines in vitro.

[0098] 1. Cell lines and laboratory animals

[0099] Human non-small cell lung cancer cell line A549 cells were purchased from the cell bank of the Shanghai Chinese Academy of Sciences and cryopreserved by the School of Pharmacy, Fujian Medical University.

[0100] BALB / c nude mice aged 3-4 weeks, weighing 18±2g (male), purchased from Shanghai Slack Laboratory Animal Co., Ltd., laboratory animal license number: SCXK (Shanghai) 2012-0002, animal certificate number: 2007000537438 .

[0101] Nude mice are housed in a SPF-level laminar flow system every 6 cages. Nude mice are given standard food and drinking water every day, keep light and dark cycle experiment (12 / 12h), room temperature 25±2℃, humidity 50±10 %, change the drinking water and litter after autoclaving every da...

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Abstract

The invention provides a compound with formula I or medicinal salt of the compound. The invention further provides a pharmaceutical composition containing the compound and application of the compound to cancer treatment.

Description

Technical field [0001] The present invention relates to a biflavonoid compound, its pharmaceutical composition and its use in the treatment of cancer. Specifically, the present invention provides diflavonoid compounds extracted and prepared from Cypress cypress, and used in cancer treatment and medicine preparation. Background technique [0002] Stone cypress is the dry whole plant of Selaginella (Selaginella) plant dark green Selaginella (Selaginella doederleinii Hieron). Modern pharmacological studies have found that Shishangbai or its combination can enhance the metabolism of cancer patients and the function of the reticuloendothelial system, and its active ingredients have been studied. Reported studies have found that Cypress contains alkaloids, plant sterols, saponins, etc., such as hordenine-O-α-L-rhamnopyranoside, N-methyl Tyramine-O-α-L-rhamnopyranoside (N-methyltyramine-O-α-L-rhamnopyranoside) and so on. In addition, it was also found that Cypress cypress contains tw...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/30C07D311/40A61K31/352A61P35/00A61P35/02
CPCC07D311/30C07D311/40A61K9/0019A61K31/352A61P35/00A61P35/02
Inventor 林新华姚宏李少光吴尤佳眭玉霞
Owner FUJIAN MEDICAL UNIV
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