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Hexamethoxyflavanone-rhamnosyl-rhamnoside and application thereof

A technology of hexamethoxyflavanone and rhamnosyl, applied in the field of hexamethoxyflavanone-rhamnosyl-rhamnoside and its application, can solve the problem that chemotherapy drugs cannot prevent tumor metastasis and reduce cancer death rate, attack the patient's immune system and other problems, and achieve obvious anti-tumor cell migration and invasion ability, and promote the effect of tumor cell apoptosis

Active Publication Date: 2015-11-18
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, once tumor metastasis occurs, there is no way to remove the metastatic tumors in the whole body by surgery. At this time, the use of "anticancer drugs" is also ineffective; chemotherapy drugs cannot prevent tumor metastasis
Although "anticancer drugs" have shown some effects, there is still no significant reduction in cancer mortality, because the number of circulating tumor cells in patients after surgery is drastically reduced and most of them are in a quiescent state, while chemotherapy drugs only Rapidly growing and dividing tumor cells work, but the use of chemotherapy drugs severely hits the patient's own immune system, tilting the patient's own balance along the unfavorable side

Method used

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  • Hexamethoxyflavanone-rhamnosyl-rhamnoside and application thereof
  • Hexamethoxyflavanone-rhamnosyl-rhamnoside and application thereof
  • Hexamethoxyflavanone-rhamnosyl-rhamnoside and application thereof

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preparation example Construction

[0037] The preparation liquid phase separation conditions in the step (4) are: chromatographic column: AgelaVenusilXBPC18; flow rate: 1-4ml / min; column temperature: 35°C; detection fluorescence excitation wavelength 352nm, emission wavelength 458nm, isocratic elution, The mobile phase is a mixture of methanol and pure water, and the volume ratio of methanol and pure water is 9:11. The injection volume is 200μL, and the 20mg / mL sample is prepared with methanol solvent.

[0038] The operating conditions of the mass spectrometer in the step (4) are: ion source: atmospheric pressure electrospray ion source (ESI); scan mode: full scan in positive ion mode; scan range: 150-800 m / z ; spray voltage (spray voltage): 4.0kV; sheath gas flow rate (sheath gas flow rate): 35 Arb; auxiliary gas flow rate (aux gas flow rate): 5 Arb; ion transfer tube temperature (capillary temperature): 350 ° C; tube diameter voltage (tubelens): 60.00V.

Embodiment 1 9

[0039] The extraction method of the active ingredient of embodiment 1 Murata japonica

[0040] Take 4.2Kg of dried Jiulixiang medicinal materials (twigs) and crush them, and reflux extract them in 5L of 75% ethanol. Each batch of medicinal materials is extracted 3 times for 3 hours each time. Combine and reflux the extracts, concentrate the ethanol under reduced pressure to obtain a syrupy total extract. The total extract was ultrasonically suspended in water, the suspension was extracted with dichloromethane, the extraction ratio was 1:1 (v:v), extracted 4 times, combined and concentrated under reduced pressure, the obtained crude extract was placed on a silica gel column, distilled with ethyl acetate -Petroleum ether was separated by gradient chromatography, the fraction eluted with ethyl acetate was collected, and the solvent was removed by rotary evaporation to obtain the target component with a yield of about 0.09%. The extract was dissolved in an equivalent amount of me...

Embodiment 2

[0041] Embodiment 2 semi-preparative chromatography

[0042] Conditions are, instrument: Waters2695; detector: Waters2475FLR; chromatographic column: AgelaVenusilXBPC18 (10mm×250mm, 5μm); flow rate: 3mL / min; column temperature: 35°C; detection wavelength: λex=352nm, λem=458nm; isocratic Elution and methanol and pure water according to the ratio of 9:11. Inject 200μl of 20mg / mL sample, collect the components of 23-27min, such as image 3 .

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Abstract

The invention belongs to the technical field of medicine, and relates to a hexamethoxyflavanone-rhamnosyl-rhamnoside and application thereof. The hexamethoxyflavanone-rhamnosyl-rhamnoside is prepared by the following steps: carrying out solvent extraction and extraction separation on murraya jasminorage, carrying out silica gel column separation, carrying out further separation by semipreparative chromatography, concentrating, and carrying out freeze-drying to obtain the finished hexamethoxyflavanone-rhamnosyl-rhamnoside product. The antitumor activity evaluation detects that the hexamethoxyflavanone-rhamnosyl-rhamnoside has low cytotoxicity; the hexamethoxyflavanone-rhamnosyl-rhamnoside has obvious inhibiting effects on the adhesion of colon cancer cells HT-29 and Fn (fibronectin) and the adhesion of HUVECs (human umbilical vein endothelial cells); the hexamethoxyflavanone-rhamnosyl-rhamnoside has obvious inhibiting effects on migration capacity (scratch heating experiment) and invasion capacity of HT-29; and the hexamethoxyflavanone-rhamnosyl-rhamnoside has obvious inhibiting effects on mouse in-vivo B16-F10 lung transfer. Therefore, the hexamethoxyflavanone-rhamnosyl-rhamnoside has tumor transfer inhibition activity, can be used for preparing anticancer drugs, and has favorable development and application prospects.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a hexamethoxydihydroflavone-rhamnosyl-rhamnoside and an application thereof. Background technique [0002] Tumor metastasis is a particularly complex process involving multiple steps and factors. This whole process is affected by many factors, such as the tumor itself and the host environment. The scariest aspect of cancer is metastasis, the spread of cells from a primary tumor to distant organs, where they continue to grow without interruption. Currently, despite significant improvements in diagnosis, surgical techniques, patient care, and local and systemic adjuvant therapy, patients often die from cancer metastasis. Circulating tumor cells (CTCs) remaining in "sub-healthy people" after primary tumor surgery are the fatal source of future tumor metastasis. [0003] Primary tumors are mostly organ-localized diseases, but in many patients after surgery, CTCs in the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/07C07H1/08A61P35/04
Inventor 江舟庞雅琼周素霞王建贾力
Owner FUZHOU UNIV
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