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Application of kumata kenin in preparation of abnormal vascular proliferation inhibition medicines

A kind of vascular abnormality and technology of ursophyllin, which is applied in the field of application of ursophyllin in the preparation of drugs for inhibiting vascular abnormality

Inactive Publication Date: 2014-08-06
KUNMING UNIV OF SCI & TECH TECH IND SALES MANAGEMENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the present invention, ursophyllin is a flavonoid compound isolated from Sage ganxie, which has anti-oxidant, antibacterial and anti-inflammatory pharmacological activities. It has not been reported that this compound can be used as an angiogenesis inhibitor to inhibit angiogenesis. Activity

Method used

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  • Application of kumata kenin in preparation of abnormal vascular proliferation inhibition medicines
  • Application of kumata kenin in preparation of abnormal vascular proliferation inhibition medicines
  • Application of kumata kenin in preparation of abnormal vascular proliferation inhibition medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1: the preparation of ursanthin (the ursanthin used in the following examples is prepared by the following method)

[0020] In the experiment, 7.3 kg of dry sage (whole plant) was used, crushed through a 60-mesh sieve, and ultrasonically extracted 5 times with 100% acetone (20 L each) at room temperature, and the extract was concentrated under reduced pressure to obtain 300 g of crude extract; The obtained crude extract was placed on a normal phase silica gel column (80-100 mesh, Qingdao Ocean Chemical Industry) (dry method for sample loading), followed by pure petroleum ether, petroleum ether-ethyl acetate mixed solution (petroleum ether: ethyl acetate) 9:1, 3:1, 1:1, 3:7) elution, collect each part of the eluent, concentrate under reduced pressure, detect with TLC, and combine the fractions with roughly the same composition; for petroleum ether:acetic acid Ethyl ester = 1:1 eluate fraction (52 g) was separated, the separation method was normal phase silica ...

Embodiment 2

[0023] Example 2: The effect of ursin on the proliferation of human umbilical vein endothelial cells (HUVEC) (MTT)

[0024] Human umbilical vein endothelial cells (HUVEC) were incubated at 37°C, 5% CO. 2 After culturing under the above conditions for 24 hours, it was inoculated into a 96-well plate at a density of 3000 cells per well, and after culturing for another 24 hours under the above conditions, ursin was prepared into 0.1, 0.5, 1.0, 2.5, 5.0, 10.0 mg / L of different concentrations of drug solutions, and added to 96-well plates at 37°C, 5% CO 2 Continue to incubate for 72 hours under the same conditions, add MTT (3-(4,5-dimethylthiazole-2)-2,5-diphenyltetrazolium bromide) 20 μL per well and continue to incubate for 4 hours, discard the Add 150 μL DMSO to each well, shake for 1 h, and measure the absorbance OD value at 490 nm on a microplate reader (see figure 2 ).

[0025] The experimental results are as image 3 As shown, when the concentration of ursanthin was 2...

Embodiment 3

[0026] Example 3: Experiment on the inhibitory effect of ursanthin on chicken embryo allantoic membrane angiogenesis

[0027] Take freshly bred eggs at a temperature of 37.8 °C, CO 2The concentration was 5%, incubated for 7 days under suitable humidity conditions, a window (1 × 1 cm) was opened at the end of the air chamber, and a sterile filter paper sheet with a diameter of 6 mm was used as the drug carrier, which was placed on the allantoic membrane. 5.0, 10.0, 15.0 mg / L administration groups with different concentrations were administered, and a blank group (normal saline group) and a positive control group (dexamethasone group) were set, and the window was sealed with sterile transparent tape, and continued under the above conditions After 48 hours of incubation, a fixative solution (methanol:acetone=1:1) was added dropwise to the administration site to fix the blood vessels for 15 minutes. The blood vessel area in the picture was calculated with Image Pro Plus (IPP, ver...

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Abstract

The invention discloses an application of kumata kenin in preparing abnormal vascular proliferation inhibition medicines. According to the application, kumata kenin serves as an abnormal vascular proliferation inhibitor, and can be used for treating diseases such as cancers, rheumatic arthritis, diabetic blindness and systemic lupus erythematosus which are caused by internal abnormal vascular proliferation. Experiments prove that the kumata kenin has an obvious inhibition function on the abnormal vascular proliferation. Consequently, the kumata kenin can be used for preparing the abnormal vascular proliferation inhibition medicines.

Description

technical field [0001] The invention belongs to the field of botanical medicinal components and angiogenesis-inhibiting compounds, in particular to the application of ursin in the preparation of angiogenesis-inhibiting drugs. Background technique [0002] Angiogenesis is an important physiological and pathological process in the body. Under normal circumstances, its promotion and inhibition are in a state of dynamic equilibrium, which only occurs in several processes such as embryo formation, wound healing and women's physiological cycle. However, once this balance is broken, many diseases and immune system disturbances will follow. Especially when the angiogenesis-promoting factors in the body exceed the angiogenesis-inhibiting factors, the balance will be biased towards the formation of new blood vessels, which may lead to the occurrence of serious diseases such as cancer, rheumatoid arthritis, diabetic blindness, and systemic lupus erythematosus. . [0003] The angiogen...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P35/00
Inventor 李宝才朱路平庄文婷李鹏向诚何静秦谊张敉戴伟锋
Owner KUNMING UNIV OF SCI & TECH TECH IND SALES MANAGEMENT
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