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

A kind of vascular abnormality, the technology of ursanthin, which is applied in the application field of ursanthin in the preparation of a drug for inhibiting abnormal angiogenesis

Inactive Publication Date: 2013-08-14
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 ursophyllin (the ursophyllin used in the following examples is prepared by the following method)

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

Embodiment 2

[0023] Example 2: Effect of Arbutin on the Proliferation of Human Umbilical Vein Endothelial Cells (HUVEC) (MTT)

[0024] Human umbilical vein endothelial cells (HUVEC) were incubated at 37°C in 5% CO 2 After culturing under the above conditions for 24 hours, it was seeded into a 96-well plate at a density of 3000 cells per well, and after culturing for another 24 hours under the above conditions, the argophyllin was prepared into 0.1, 0.5, 1.0, 2.5, 5.0, 10.0 mg / L of different concentrations of liquid, and added to 96-well plate, at 37 ° C, 5% CO 2 The culture was continued for 72 hours under the condition of 2, 20 μL of MTT (3-(4,5-dimethylthiazole-2)-2,5-diphenyltetrazolium bromide) was added to each well and the incubation was continued for 4 h, and the upper For the supernatant, 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] Experimental results such as image 3 As shown, ...

Embodiment 3

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

[0027] Take fresh eggs at a temperature of 37.8°C, CO 2The concentration was 5%, and the humidity was suitable for incubation for 7 days. 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 delivery carrier, which was placed on the allantoic membrane. Administration groups with different concentrations of 5.0, 10.0, and 15.0 mg / L were administered, and a blank group (normal saline group) and a positive control drug group (dexamethasone group) were set up, and the window was sealed with sterile transparent tape, and continued under the above conditions. After incubation for 48 h, fixative solution (methanol: acetone = 1:1) was added dropwise to the administration site to fix the blood vessels for 15 min. The area of ​​blood vessels in the picture was calculated with Image P...

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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 herbal medicinal ingredients and compounds for inhibiting angiogenesis, and in particular relates to the application of arbutin in the preparation of drugs for inhibiting abnormal angiogenesis. 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 balance, and it only occurs in several processes such as embryogenesis, wound healing and women's menstrual cycle. However, once this balance is broken, it will be accompanied by the emergence of many diseases and disorders of the immune system. 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 serious diseases such as cancer, rheumatoid arthritis, diabetic blindness, and systemic lupus eryt...

Claims

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Application Information

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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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