A kind of application of lanostane type

A lanostane-type, angiogenesis technology, which is applied to medical preparations containing active ingredients, pharmaceutical formulations, antitumor drugs, etc., can solve the problem of angiogenesis that has not been reported yet.

Active Publication Date: 2019-10-15
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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  • A kind of application of lanostane type
  • A kind of application of lanostane type
  • A kind of application of lanostane type

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1 compound extraction, separation

[0024] 1. Extraction and separation

[0025] Dry and pulverize 2.0kg stems and leaves of King Kong, and soak 3 times with 95% ethanol, each time for 7 days, the extracts are combined, concentrated under reduced pressure to obtain extract (200g), and extracted with ethyl acetate to obtain the ethyl acetate part ( 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, and use reverse phase liquid Separated by phase chromatography, eluted with acetonitrile / water (64:36, 3mL / min), and collected in 27 minutes to obtain the compound.

[0026] 2. Identification of the structure of the compound

[0027] 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,s,H-26),1.31(3H,...

Embodiment 2

[0028] Inhibition of Example 2 Compounds on Migration of Endothelial Cells

[0029] 1. Experimental materials, instruments and reagents

[0030] 1 Experimental materials

[0031] 1.1 Drugs: Compounds (kansenonol) isolated in our laboratory

[0032] Avastin

[0033] 1.2 Cell lines:

[0034] Human umbilical vein endothelial cells (HUVEC) were preserved by our research group.

[0035] 2 Preparation methods of main test reagents

[0036] 2.1 DMEM preparation method: take 10.4g DMEM dry powder, 2g NaHCO 3 , 50mg penicillin, 100mg streptomycin, ddH 2 O 800mL, fully mixed with a magnetic stirrer, adjusted to pH 7.4 with HCl, sterilized by filtration with a 0.22μm filter, aliquoted, and stored at 4°C for later use.

[0037] 2.2 PBS liquid preparation method: NaCl 8.0g, KCl 0.2g, NaCl 2 HPO4 1.44g, KH 2 PO 4 0.24g, add water to make up to 1L, sterilize under high temperature and high pressure, and store at 4°C for later use.

[0038] 2.3 Preparation method of trypsin: diss...

Embodiment 3

[0054] Inhibitory effect of embodiment 3 compound on rat arterial ring formation

[0055] 1. Experimental materials, instruments and reagents

[0056] 1 Experimental materials

[0057] 1.1 Drugs: Compounds (kansenonol) isolated in our laboratory

[0058] 1.2 Animals:

[0059] SD rats, SPF grade, female, body weight (250) g

[0060] 2 Preparation methods of main test reagents

[0061] 2.1 DMEM preparation method: take 10.4g DMEM dry powder, 2g NaHCO 3 , 50mg penicillin, 100mg streptomycin, ddH 2 O 800mL, fully mixed with a magnetic stirrer, adjusted to pH 7.4 with HCl, sterilized by filtration with a 0.22μm filter, aliquoted, and stored at 4°C for later use.

[0062] 2.2 PBS liquid preparation method: NaCl 8.0g, KCl 0.2g, NaCl 2 HPO 4 1.44g, KH 2 PO 4 0.24g, add water to make up to 1L, sterilize under high temperature and high pressure, and store at 4°C for later use.

[0063] 2.3 Matrigel solution: Dilute Matrigel 1:1 with serum-free ECM medium.

[0064] 2. Exper...

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PUM

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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] Triterpene technical field [0002] The invention belongs to the technical field of medicines, and in particular relates to a compound extracted from Japonica japonica, which has the application of drugs for inhibiting the formation of new blood vessels. Background technique [0003] Angiogenesis refers to the growth of new capillary blood vessels from pre-existing capillaries and postcapillary venules. Tumor angiogenesis is an extremely complex process, which generally includes steps such as degradation of vascular endothelial matrix, migration of endothelial cells, proliferation of endothelial cells, formation of vascular rings by branching of endothelial cells, 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 functions of tissues and organs. Under normal physiological conditions, angiogene...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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