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Application of cycloicaritin in preparation of anti-tumor composition

A technology of cyclic icariin and composition is applied in the directions of antitumor drugs, drug combinations, medical preparations containing active ingredients, etc., to achieve the effect of inhibiting the migration of human umbilical vein endothelial cells

Inactive Publication Date: 2014-06-18
贾晓斌
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there was no report on the antitumor effect of RICT prior to the present invention

Method used

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  • Application of cycloicaritin in preparation of anti-tumor composition
  • Application of cycloicaritin in preparation of anti-tumor composition
  • Application of cycloicaritin in preparation of anti-tumor composition

Examples

Experimental program
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Effect test

Embodiment 1

[0025] Example 1 Study on anti-tumor mechanism of cyclic icarigenin

[0026] Experimental Cyclic Icariin Inhibits the Growth and Tube Formation of Human Umbilical Vein Endothelial Cells HUVEC and Causes Apoptosis

[0027] Culture of cells (HUVEC) Collect sterile fetal umbilical cords of 20-30 cm, cut off the damaged part, and rinse with PBS until there is no blood in the vein. Clamp one end, inject about 8-10ml of 0.25% trypsin into the vein cavity from the other end, and clamp after filling, digest at 37°C for about 20 minutes. Collect the digestive fluid, rinse the vein cavity with M199 flushing solution containing 20% ​​calf serum, resuspend the cells with 5ml of M199 medium containing 20% ​​calf serum, add to a culture bottle, and place at 37°C, 5% CO 2 Incubator cultivation. The 2nd to 5th passage cells were used for experiments.

[0028] MTT test HUVEC with 10 5 cells / mL were inoculated in a 96-well plate, incubated with icariin (5, 10, 20 μg / mL) at 37°C, 5% CO 2 Co...

Embodiment 2

[0060] Preparation of Example 2 Cyclic Icarigenin Microemulsion

[0061] Preparation method: Weigh 3g of OP emulsifier and 3g of glycerol, add 4g of water and mix evenly as the water phase, disperse excess RICT in ethyl oleate, vortex mix, centrifuge at 4000r / min for 5min, take 2g of the supernatant as For the oil phase, drop the oil phase into the water phase under magnetic stirring to obtain a light yellow, clear and transparent RICT microemulsion.

[0062] Encapsulation Efficiency Determination: ZORBAX SB C 18 Column (416mm×150mm, 5μm); mobile phase acetonitrile-water [0.04%H 3 PO 4 -0.06% (C 2 h 5 ) 3 N] (65:35); detection wavelength 270nm; flow rate 1.0mL / min; column temperature 25°C, injection volume 20μL. RICT has a good linear relationship between 5.12 and 61.44mg / L, the regression equation is A=37.522C-18.778, r=0.9998, the average recovery rate is 98.97%, RSD1.3%, and can be used for the encapsulation efficiency of RICT microemulsion determination.

[0063] T...

Embodiment 3

[0064] The effect of embodiment 3 RICT and RICT microemulsion suppressing tumor cell in vitro

[0065] Cells: Human liver cancer cells (HepG2), human breast cancer cells (MDA-MB-435), human lung cancer cells (A549), human cervical cancer cells (HeLa S3), human colon cancer cells (HCT116), purchased from Nanjing Kaiji Biotechnology Co., Ltd. Provided by Technology Development Co., Ltd.

[0066] Drugs and reagents: RICT is provided by the State Administration of Traditional Chinese Medicine Key Research Laboratory of Traditional Chinese Medicine Drug Release System, with a purity of >95%, yellow powder. 5-Fluorouracil (5-FU) Jiangsu Nantong Jingjing Pharmaceutical Co., Ltd., batch number 100403; RPMI Medium1640 medium Gibco company, batch number 1165062; Trypsin (Trypsin, 1250) Serva company, batch number 27043C; RNase (RNsae) Roche company , batch number 94036528; newborn calf serum (NewbomB0vineSerum.NBS) Sanli Biological Products Factory, batch number 20040101; propidium iod...

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Abstract

The invention discloses an application of cycloicaritin in preparation of an anti-tumor composition. The cycloicaritin disclosed by the invention can effectively inhibit growth and pipe formation of HUVEC (Human Umbilical Vein Endothelial Cells) and cause apoptosis to inhibit migration of the HUVEC, and has a remarkable inhibiting effect on highly activated MAPK (Mitogen-Activated Protein Kinase) pathway and AKT pathway. Through the above mechanism, the composition can effective prevent tumors, and particularly can effectively inhibit growth of liver cancer, breast cancer, lung cancer, cervical cancer and colon cancer.

Description

technical field [0001] The present invention relates to a cycloicarigenin (3,5-dihydroxy-2-(4-methoxy-phenyl)-8,8-dimethyl-9,10-dihydro-8H-pyridine Fum[2,3-f]chromen-4-one, 3,5-Dihydroxy-2-(4-methoxy-phenyl)-8,8-dimethyl-9,10-dihydro-8H-pyrano[2, The application of 3-f]chromen-4-one) in the preparation of anti-tumor composition belongs to the field of new application of compounds. Background technique [0002] Cyclic icariin (hereinafter referred to as RICT in this application) is a flavonoid compound obtained by desugaring and forming a ring after the main component icariin in Epimedium decoction pieces is hydrolyzed by acid, and its structural formula as follows: [0003] [0004] According to literature reports, RICT can enhance intracellular alkaline phosphatase activity, promote osteogenic activity, promote bone formation, and inhibit osteoporosis. However, there were no reports on the antitumor effect of RICT prior to the present invention. Contents of the inve...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P35/00
Inventor 贾晓斌蒋俊张振海宋捷
Owner 贾晓斌
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