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Application of kaempferol and its analogs

A technology of kaempferol and medicine, applied in the field of application of kaempferol and its analogues, to achieve the effects of enhancing the formation of venous blood vessels, strong practicability, cell proliferation and cell migration

Active Publication Date: 2021-05-14
HKUST SHENZHEN RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Modern pharmacological studies have shown that kaempferol has a wide range of pharmacological activities, including antioxidant, anti-inflammatory, antibacterial, anti-cancer, heart protection, anti-diabetic, anti-estrogen, anxiolytic and anti-allergic effects, but there is no kaempferol at present. Reports that it can combine with vascular endothelial growth factor (VEGF) to promote neovascularization and be used as an angiogenesis enhancer

Method used

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  • Application of kaempferol and its analogs
  • Application of kaempferol and its analogs
  • Application of kaempferol and its analogs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1: Preparation of Ginkgo biloba total extract and HPLC fingerprint of Ginkgo biloba total extract

[0039] 1. Method

[0040] Crush the Ginkgo biloba medicinal material, weigh 50g, put it in a volumetric flask, soak and extract it with 1000mL, 50% ethanol for three days, concentrate the extract in vacuum at 60°C to 30mL, and then vacuum freeze-dry to obtain the total extract of Ginkgo biloba, freeze-dried powder Store in vacuum.

[0041] Weigh 100 mg of lyophilized powder, put it in a 15 mL centrifuge tube, add 4 mL of 50% methanol, ultrasonicate for 15 minutes, and centrifuge at 1000 x g for 5 minutes to obtain the supernatant. Filter through a microporous membrane, take the filtrate, and inject it for analysis. The analytical instrument used is Agilent liquid phase with autosampler and binary pump, the chromatographic column is Agilent, Grace VisionHT C18 column (4.6x 250mm, 5μm), and the mobile phase is acetonitrile (solvent A) and 0.2% aqueous formic acid ...

Embodiment 2

[0045] Embodiment 2: Kaempferol promotes (HUVEC) proliferation experiment of human umbilical vein endothelial cells

[0046] Using tetrazolium salt (MTT) colorimetry to observe the positive control group Avastin (Avastin) group on the proliferation inhibition of HUVEC and different concentrations of kaempferol on the proliferation of HUVEC, indicating that kaempferol has a good effect on promoting HUVEC proliferation. Proliferation, and there is a concentration-dependent relationship.

[0047] 1. Method

[0048] HUVEC cells at 5.0×10 3 Cells / mL were inoculated in 96-well culture plate for culture, 100 μL per well, after the cell growth reached 80% confluence, 5 ng / mL VEGF or different concentrations of kaempferol were added to the wells, and MTT solution was added to each well after 48 hours of action 10 μL, continue to culture at 37°C for 4 hours, stop the culture, discard the culture supernatant, add 150 μL DMSO to each well, shake for 10 min to fully dissolve, select a wa...

Embodiment 3

[0052] Embodiment 3: Kaempferol promotes scratch migration experiment of human umbilical vein endothelial cells (HUVEC)

[0053] 1. Method

[0054] HUVEC cells in 20×10 4 Inoculate in a 12-well plate at a density of 12 wells, and let the cells adhere to the wall overnight. After the cells reach 80% confluence, use a 200 μL pipette tip to make a horizontal wound in the middle of each well, discard the medium, and wash with PBS. Once, 5 ng / mL human vascular endothelial growth factor (VEGF), 200 μg / mL Aisiting and different concentrations of kaempferol were added separately to the culture medium, and a blank experiment without drug addition was set up. The changes in the coverage of the cell layer in each well were photographed after 0 and 8 hours using a microscope equipped with a video camera at 50X magnification. Then use TSratch software to digitize the recovery growth rate, and calculate the cell recovery growth rate according to the following formula:

[0055] Recovery r...

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Abstract

The application of kaempferol and its analogs is used for promoting angiogenesis by combining with vascular endothelial growth factor. The invention proposes the new application of kaempferol and its analogues, and firstly invents the means of using kaempferol to promote the angiogenesis induced by vascular endothelial growth factor, which can significantly enhance the proliferation and cell migration of human umbilical vein endothelial cells. In animal models, kaempferol can significantly enhance zebrafish inferior intestinal vein angiogenesis, further clarified its role in promoting angiogenesis, and can be used for the prevention and treatment of ischemic heart disease. The application design of the kaempferol and the analog thereof of the present invention is scientific and practical.

Description

technical field [0001] The invention relates to the field of angiogenesis, in particular to the application of kaempferol and its analogues. Background technique [0002] Angiogenesis is a complex process of generating new blood vessels by stimulating the budding of endothelial cells to form small blood vessel growth and collateral circulation in the surrounding tissue on the basis of the original vascular network. This process involves multiple steps such as the degradation of vascular endothelial extracellular matrix, migration of endothelial cells to the degraded matrix, proliferation, stretching, formation of tubular structures, and production of endothelial extracellular matrix membrane. It mainly includes: degradation of vascular basement membrane in the activation phase; Activation, proliferation, migration; reconstruction of new blood vessels and vascular network is a complex process involving a variety of cells and molecules. Angiogenesis is a complex process of co...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61K31/7048A61P9/14A61P9/10A61P17/02A61K8/60A61K8/49A61Q19/00
CPCA61K8/498A61K8/602A61K31/352A61K31/7048A61Q19/00A61P9/10A61P9/14A61P17/02
Inventor 詹华强胡伟慧董婷霞王怀友
Owner HKUST SHENZHEN RES INST
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