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Application of tetracyclic triterpenoids compound in preparing anti-angiogenic drugs

An angiogenesis and drug technology, applied in the field of application of cucurbitacin E in the preparation of anti-angiogenesis drugs, can solve the problems of lack of cucurbitacin E, etc.

Inactive Publication Date: 2010-02-17
EAST CHINA NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have shown that cucurbitacin E has anti-tumor effects, can inhibit diabetic syndrome, inhibit antibody-related glomerulitis, and can also treat acute myeloid leukemia, but there is no cucurbitacin E as an angiogenesis-inhibiting drug. to report

Method used

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  • Application of tetracyclic triterpenoids compound in preparing anti-angiogenic drugs
  • Application of tetracyclic triterpenoids compound in preparing anti-angiogenic drugs
  • Application of tetracyclic triterpenoids compound in preparing anti-angiogenic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1: Cucurbitacin E inhibits proliferation of endothelial cells

[0034] Purpose and principle: Cell proliferation experiment adopts MTS method. The MTS method is an assay that uses a colorimetric method to determine the number of cell proliferations in living cells. NADPH dehydrogenase converts MTS tetrazolium salt compound into a colored substance soluble in tissue culture fluid, and its color depth is highly correlated with the number of living cells of the cell line within a certain range. This model can be used to evaluate the effect of drugs on cell proliferation.

[0035] Method: inoculate a certain amount of endothelial cell suspension in a 96-well plate, add culture medium containing different concentrations of cucurbitacin E for 48-72 hours, then add 20 microliters of chromogen to each well, and incubate for 1-4 hours , Read the light absorbance value in each well at 490 nm on a microplate reader.

[0036] Results and evaluation: Compared with the con...

Embodiment 2

[0037] Example 2: Cucurbitacin E inhibits scratch migration of vascular endothelial cells in vitro

[0038] Purpose and principle: Cell migration test is also called in vitro scratch test. In this experiment, scratches were made on a single layer of endothelial cells at a certain density in the culture plate, observed under a microscope, and the migration of cells at the edge of the scratch to the scratch site was recorded to evaluate the effect of drugs on the migration ability of endothelial cells .

[0039] Method: Inoculate a certain number of cells in a 6-well plate, and when the cells grow to about 80%, draw a line in each well with a 1ml tip of a micropipette. Wash the dead cells with PBS, then add medium containing VEGF and different drug concentrations, and incubate in an incubator at 37°C for about 24 hours until the scratched area of ​​the VEGF165 group is covered with cells.

[0040] Result and evaluation: observe and take pictures under the microscope, see the r...

Embodiment 3

[0041] Example 3: Cucurbitacin E inhibits the migration of vascular endothelial cells in a modified Boyden chamber

[0042]Purpose and principle: The chamber migration experiment of endothelial cells adopts Boyden chamber. The modified Boyden chamber is a kind of petri dish that can be inserted into the cell culture plate. The bottom layer has a polycarbonate filter membrane with a pore size of 8 μm. Under the induction of growth factors, the cells can permeate the side of the membrane and adhere to the medium containing high concentration of The other side of growth factors. This experiment can detect the effect of drugs on the ability of endothelial cells to resist migration.

[0043] Method: Add 0.1% gelatin to the 24-well plate and incubate at 37°C for 30 minutes, discard the gelatin, and wash three times with PBS. Add the endothelial cell medium containing 10% serum and VEGF165 to the 24-well plate in the lower part of the small chamber. Insert the cells into the small...

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Abstract

The invention provides the application of tetracyclic triterpenoids compound cucurbitacins E in preparing anti-angiogenic drugs. The cucurbitacins E can inhibit tumor angiogenesis, arthritis pathological tissue vessel angiogenesis, neovascular eye disease, hemangioma pathological tissue angiogenesis, psoriasis pathological tissue vessel angiogenesis, solid tumor pathological tissue angiogenesis, hemangioma, Kaposi' s sarcoma pathological tissue angiogenesis, leukocythemia, lymphadenoma, myeloma blood cancer and Paget' s disease angiogenesis. The invention also provides the application of a compound containing effective dose of cucurbitacins E and pharmacy acceptable ingredients in preparing the anti-angiogenic drugs.

Description

technical field [0001] The invention relates to a new application of a tetracyclic triterpenoid compound cucurbitacin E (Cucurbitacin E), in particular to the application of the cucurbitacin E in the preparation of drugs for inhibiting angiogenesis. Background technique [0002] Angiogenesis is the process of generating new blood vessels on the basis of existing blood vessels. Angiogenesis has multiple steps: proliferation, migration, invasion and microtubule formation of vascular endothelial cells, recruitment of perivascular cells and acquisition of new matrix membrane. [0003] Angiogenesis usually occurs only in the embryo and later in embryonic development, the reproductive cycle and wound healing. In pathological conditions (solid tumor invasion, migration, diabetic retinopathy, hemangioma, arthritis, psoriasis and atherosclerosis, etc.), the disease is associated with persistent angiogenesis. [0004] Malignant tumors pose a great threat to human health for a long t...

Claims

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Application Information

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IPC IPC(8): A61K31/575A61P35/00A61P35/02A61P19/02A61P29/00A61P27/02A61P17/06
Inventor 易正芳董艳敏张晓丽贺利军张京易庭芳刘明耀宋雅娟
Owner EAST CHINA NORMAL UNIVERSITY
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