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Cardiac glycoside with anti-angiogenesis activity as well as preparation method and application of cardiac glycoside

An anti-angiogenesis and cardiac glycoside technology is applied in medical preparations containing active ingredients, organic active ingredients, cardiovascular system diseases, etc. low cost effect

Inactive Publication Date: 2022-04-08
LANZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although human beings have made great progress in tumors, the treatment of tumors is still a difficult problem to be overcome

Method used

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  • Cardiac glycoside with anti-angiogenesis activity as well as preparation method and application of cardiac glycoside
  • Cardiac glycoside with anti-angiogenesis activity as well as preparation method and application of cardiac glycoside
  • Cardiac glycoside with anti-angiogenesis activity as well as preparation method and application of cardiac glycoside

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] The preparation of embodiment 1 cardiac glycosides

[0043] (1) Soak the dried leaves of Digitalis lanata with methanol for 3 times, each time for 7 days, and concentrate the methanol extract under reduced pressure to obtain the total extract;

[0044] (2) Extract the total extract obtained in step (1) with ethyl acetate, then carry out chromatographic separation with macroporous resin, and use ethanol-water successively during separation from 0:100, 30:70, 50:50, 80: 20. 95:5 v / v gradient elution, the collection gradient is ethanol: water = 80:20 eluted fraction;

[0045] (3) The eluted components obtained in step (3) are separated by MCI column chromatography, and methanol / water is used successively during separation from 50:50, 60:40, 70:30, 80:20, 90:10, 100:0 v / v gradient elution, the fraction of methanol / water=80:20 was collected.

[0046] (4) The components obtained in step (3) are separated by silica gel column chromatography, and the mobile phase is gradient ...

Embodiment 2

[0055] Example 2 Cardiac Glycosides Antitumor Activity

[0056] Human non-small cell lung cancer cells A549, cervical cancer cells Hela, and breast cancer cells MCF-7 in the logarithmic growth phase were respectively digested to make cell suspensions. After cell counting, 4000 cells per well were seeded in 96-well culture plates. Inoculate 100 μL per well, while keeping the blank group, at 37°C, 5% CO 2 Incubate overnight. After the cells adhered to the wall, the experimental group added 100 μL of test samples containing concentrations of 0, 20, 40, 60, 80, 100, 120, 140, 160, 180, 200 nmol / L (cardiac glycosides prepared in Example 1 ) medium, the control group added an equal volume of medium, placed at 37 ° C, 5% CO 2 After 48 hours of incubation, the culture medium in the 96-well culture plate was sucked off and washed once with sterile PBS. Under dark conditions, 20 μL of 5 mg / mL MTT solution and 100 μL of medium were added. For the control group, 20 μL of MTT solution wa...

Embodiment 3

[0059] Example 3 Cardiac Glycosides Angiogenesis Inhibitory Activity

[0060] Commercially available eggs are sterilized with bromogeramine and incubated in an incubator at a temperature of 38±0.5°C and a relative humidity of 65-70%. Days later, disinfect the air chamber end of the eggshell about 2cm×2cm, and open a window, use ophthalmic curved scissors to clip off the eggshell and shell membrane, open the window area about 1.5cm×1.5cm, moisten it with normal saline and tear off the air chamber Membrane, exposed chick embryo chorioallantoic membrane. A 1cm×1cm polyethylene resin ring was placed on the membrane, and 20 μL of the compound to be tested prepared in saline was added to the ring, and a control group was set. Seal the window with parafilm and continue to incubate for 48 hours, cut off the parafilm, observe the neovascularization of chick embryo chorioallantoic membrane in the polyethylene resin ring under a microscope, count the number of blood vessels with image J...

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Abstract

The invention relates to the technical field of biochemical engineering, in particular to cardiac glycoside with anti-angiogenesis activity and a preparation method and application thereof. According to the invention, the cardiac glycoside compound with anti-angiogenesis activity is separated from a medicinal plant digitalis lanata, and the compound has nano-molar concentration level proliferation inhibition activity on non-small cell lung cancer cells, cervical cancer cells and breast cancer cells, and can be used for preparing anti-tumor drugs; moreover, the compound can significantly inhibit new angiogenesis on a chick embryo chorioallantoic membrane model, and can be used for preparing anti-angiogenesis drugs; meanwhile, the compound is directly extracted and separated from medicinal plants which can be planted on a large scale, the raw materials are easy to obtain, large-scale production can be achieved, the social benefit is remarkable, and the cost is low.

Description

technical field [0001] The invention relates to the technical field of biochemical industry, in particular to a cardiac glycoside with anti-angiogenesis activity and its preparation method and application. Background technique [0002] Tumor is a common disease that seriously threatens human health and life. The global incidence and mortality of cancer are rising rapidly. It has become the leading cause of human death and the most important obstacle to prolonging human life in the world in the 21st century. In order to reduce the morbidity and mortality of tumors, researchers from all over the world are making unremitting efforts for it. Although human beings have made great progress in tumors, the treatment of tumors is still a difficult problem to be overcome. [0003] Tumor growth depends on angiogenesis, which plays an extremely important role in the growth, invasion and metastasis of malignant tumors, and is also considered to be one of the main characteristics of canc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J17/00A61K31/7048A61P9/00A61P35/00
Inventor 高坤杨红英陈建军
Owner LANZHOU UNIVERSITY
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