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Application of lanostane-type triterpene

A lanostane-type, neovascularization technology, applied to medical preparations containing active ingredients, organic active ingredients, drug combinations, etc., can solve the problem of angiogenesis that has not been reported yet

Active Publication Date: 2019-04-23
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

One of the other 4 papers is to introduce that King Kong can treat animal virus infection and its use in the preparation of animal antiviral drugs, and the other three are patents on King Kong’s anti-tumor activity, but they are mainly researched on the inhibition of tumor growth , there is no report on angiogenesis

Method used

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  • Application of lanostane-type triterpene
  • Application of lanostane-type triterpene
  • Application of lanostane-type triterpene

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 Compound extraction and separation

[0023] 1. Extraction and separation

[0024] The 2.0kg stems and leaves of Jingangzhuan were dried in the shade and pulverized, and soaked in 95% ethanol for 3 times for 7 days each time. The extracts were combined and concentrated under reduced pressure to obtain an extract (200g), which was extracted with ethyl acetate to obtain an ethyl acetate fraction ( 80g). Use MCI-gel (30%-100%) for separation, wherein the second part is separated with silica gel, the eluent is petroleum ether-acetone (20:1-1:1), select the third part, use reverse phase liquid Chromatography, eluting with acetonitrile / water (64:36, 3 mL / min) and collecting over 27 minutes gave the compound.

[0025] 2. Structure identification of compounds

[0026] white amorphous powder; 1 H NMR (400MHz, CDCl 3 ,δin ppm,J in Hz):δ H 3.29(1H,dd,J=4.6,11.6,H-3),5.59(1H,m,H-28a),5.59(1H,m,H-28b),0.75(3H,s,H-18), 1.08(3H,s,H-19),0.84(3H,d,J=6.5Hz,H-21),1.31(3H,...

Embodiment 2

[0027] Example 2 Inhibition of Endothelial Cell Migration by Compounds

[0028] 1. Experimental materials, instruments and reagents

[0029] 1 Experimental material

[0030] 1.1 Drugs: compounds isolated in this laboratory (kansenonol)

[0031] Avastin

[0032] 1.2 Cell line:

[0033] Human umbilical vein endothelial cells (HUVEC) were preserved by our group.

[0034] 2. Preparation method of main test reagents

[0035] 2.1 DMEM preparation method: take 10.4g DMEM dry powder, 2g NaHCO 3 , 50 mg penicillin, 100 mg streptomycin, dd H 2 O 800mL, fully mixed with a magnetic stirrer, adjusted to pH 7.4 with HCl, sterilized by filtration with a 0.22 μm filter, packaged in aliquots, and stored at 4°C for later use.

[0036]2.2 PBS solution preparation method: NaCl 8.0g, KCl 0.2g, Na 2 HPO 4 1.44g, KH 2 PO 4 0.24g, add water to make up to 1L, sterilize at high temperature and autoclave, and store at 4°C for later use.

[0037] 2.3 Preparation method of trypsin: dissolve ...

Embodiment 3

[0053] Example 3 Inhibitory effect of compound on rat arterial ring formation

[0054] 1. Experimental materials, instruments and reagents

[0055] 1 Experimental material

[0056] 1.1 Drugs: compounds isolated in this laboratory (kansenonol)

[0057] 1.2 Animals:

[0058] SD rat, SPF grade, female, body weight (250) g

[0059] 2. Preparation method of main test reagents

[0060] 2.1 DMEM preparation method: take 10.4g DMEM dry powder, 2g NaHCO 3 , 50 mg penicillin, 100 mg streptomycin, dd H 2 O 800mL, fully mixed with a magnetic stirrer, adjusted to pH 7.4 with HCl, sterilized by filtration with a 0.22 μm filter, packaged in aliquots, and stored at 4°C for later use.

[0061] 2.2 PBS solution preparation method: NaCl 8.0g, KCl 0.2g, Na 2 HPO 4 1.44g, KH 2 PO 4 0.24g, add water to make up to 1L, sterilize at high temperature and autoclave, and store at 4°C for later use.

[0062] 2.3 Matrigel solution: Matrigel is diluted 1:1 with serum-free ECM medium.

[0063] ...

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Abstract

The invention belongs to the field of Chinese medicine and particularly relates to an extraction process of lanostane-type triterpene and application of lanostane-type triterpene in preparation of medicaments for inhibiting angiogenesis. The extraction process has the advantages that the new application of a triterpenoid obtained from hedge euphorbia is provided. It is shown by experiments that the triterpenoid has an obvious inhibition effect on HUVEC migration and arterial rings of rats. It is indicated that the triterpenoid has angiogenesis resistance activity and can serve as an angiogenesis inhibitor applied to treatment of neovascularization dependence and neovascularization-related diseases such as tumors, arthritis, macular disease and atherosclerosis.

Description

[0001] Technical field of triterpenes [0002] The invention belongs to the technical field of medicine, and in particular relates to a compound extracted from diamond, which has the application of a medicine for inhibiting the formation of new blood vessels. Background technique [0003] Angiogenesis refers to the growth of new capillary blood vessels derived from existing capillaries and post-capillary venules. Tumor angiogenesis is an extremely complex process, which generally includes steps including vascular endothelial matrix degradation, endothelial cell migration, endothelial cell proliferation, endothelial cell conduit branching to form vascular rings, and formation of new basement membranes. [0004] Angiogenesis is the most basic and important physiological process in the human body, and it is also an important way to maintain the stability and integrity of the body and the function of tissues and organs. Under normal physiological conditions, angiogenesis only occ...

Claims

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Application Information

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IPC IPC(8): A61K31/575A61P35/00
Inventor 戚微岩刘晨高新梅徐寒梅
Owner CHINA PHARM UNIV
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