Application of orientin in the preparation of drugs for inhibiting angiogenesis

An angiogenesis and orientin technology, applied in the field of biomedicine, can solve the problems of undiscovered orientin patents and literature, and achieve the effect of convenient extraction and purification, low cytotoxicity, and inhibition of angiogenesis

Active Publication Date: 2017-09-26
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Patents and literature on the inhibition of angiogenesis by orientin have not been found

Method used

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  • Application of orientin in the preparation of drugs for inhibiting angiogenesis
  • Application of orientin in the preparation of drugs for inhibiting angiogenesis
  • Application of orientin in the preparation of drugs for inhibiting angiogenesis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Preparation of orientin

[0022] 1. Dry 3.0 kg of Euphorbia euphorbia whole herb, pulverize it, extract it by cold soaking with 95% ethanol for 3 times (7 days each time), recover the solvent to obtain 600 g of ethanol extract, add deionized water to dissolve, and then use petroleum ether , ethyl acetate, and n-butanol extraction to obtain 70 g of petroleum ether extract, 50 g of ethyl acetate extract, and 62 g of n-butanol extract.

[0023] 2. Add an equal amount of silica gel to 50 g of ethyl acetate extract and mix the sample, then carry out silica gel column chromatography, and use petroleum ether: ethyl acetate gradient elution (50:1~0:100); thin layer chromatography (TLC) tracking, combined The ratio of petroleum ether: ethyl acetate is 10:1~5:1 fraction, the pigment is removed by MCI, and then separated by silica gel column chromatography to obtain 20 mg of yellow powder.

[0024] Spectral detection data of the yellow powder: ESI-MS (m / z) 447 [M-H] - . 1 H-NMR...

Embodiment 2

[0027] The inhibitory effect of orientin on angiogenesis was confirmed by the experiment of the inhibitory effect of orientin on human umbilical vein endothelial cells (human vascular endothelial cells, HUVEC).

[0028] Tetrazolium salt (MTT) colorimetric method was used to observe the inhibitory effect of orientin on the proliferation of HUVEC in the positive control group arbutin (UA) group and low, medium and high dose groups, indicating that orientin had a good effect on inhibiting the proliferation of HUVEC. And there is a concentration-dependent relationship.

[0029] (1) HUVEC preparation, grouping and processing

[0030] Digest monolayer cultured cells with 0.25% trypsin, prepare single cell suspension with DMEM medium containing 10% newborn bovine serum, and cells in 5.0×10 4 Cells / mL were inoculated in a 96-well culture plate, 200 μL per well; about 90% of the cultured cells were confluent and replaced with serum-free DMEM culture medium for 24 hours; ), positive c...

Embodiment 3

[0040] Effect of orientin on the migratory ability of HUVEC.

[0041] The cell scratch healing method is one of the methods for measuring the cell movement characteristics; the experimental results show that the positive control group is different from the low, middle and high dose groups. Experiments have confirmed that orientin has the effect of inhibiting the proliferation of HUVEC. In the high-dose group of orientin, there are almost no HUVECs in the scratches, and the inhibitory effect is very obvious.

[0042] In this embodiment, the blank group (DMEM culture fluid), the negative control group (0.1% DMSO), the positive control group (UA50 μ g / mL) and the low, middle and high dose groups of orientin are set with the same embodiment 2, but The orientin medicament used is the orientin 50wt% medicament prepared from the orientin prepared in Example 1.

[0043] (1) HUVEC preparation

[0044] Digest monolayer cultured cells with 0.25% trypsin, prepare single cell suspension ...

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Abstract

The invention discloses the application of a compound orientin in the preparation of an angiogenesis-inhibiting drug. The angiogenesis-inhibiting drug comprises orientin and a pharmaceutically acceptable carrier. The orientin provided by the invention has a strong inhibitory effect on angiogenesis when applied to an angiogenesis inhibitor, is a novel and effective method for treating malignant tumors, and has low cytotoxicity, and is an efficient and low-toxicity inhibiting angiogenesis and then treating The drug resource of cancer is a monomer compound with natural origin, which exists in a variety of Chinese herbal medicines. It is very convenient to extract and purify, and it can also be synthesized.

Description

technical field [0001] The invention relates to the application of orientin in the preparation of drugs for inhibiting angiogenesis, and belongs to the field of biomedicine. Background technique [0002] Angiogenesis is a physiological phenomenon in the human body, which plays an important role in embryonic development and tissue damage repair. Under normal physiological conditions, angiogenesis is strictly regulated, most of which are completely inhibited, and only occur under special conditions such as embryonic development and tissue repair. However, in solid tumors, angiogenesis can get out of control, resulting in malignant results: on the one hand, new blood vessels can bring abundant oxygen and nutrients to tumor cells, and take away metabolites; on the other hand, tumor cells can pass through new blood vessels Move to the distance. If there is no angiogenesis in the tumor, the growth of the tumor will be stagnant or even regressed; if there is angiogenesis in the t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P35/00
Inventor 廖志新胥廉谦施天一叶润贾海洋
Owner SOUTHEAST UNIV
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