Application of atisane type diterpenoid

A technology of attane and diterpenes, applied in the field of traditional Chinese medicine, can solve the problems such as angiogenesis that have not been reported for the time being

Inactive Publication Date: 2019-05-17
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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 oth

Method used

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  • Application of atisane type diterpenoid
  • Application of atisane type diterpenoid
  • Application of atisane type diterpenoid

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0022] Example 1 Compound extraction and separation

[0023] 1. Extraction and separation

[0024] The stems and leaves of Jingangshu 2.0kg were crushed and soaked in 95% ethanol 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 the ethyl acetate fraction ( 80g). Use MCI-gel (30%-100%) for separation. The second part is separated by silica gel. The eluent is petroleum ether-acetone (20:1-1:1). Select the third part and use reverse phase solution. It was separated by phase chromatography, eluted with acetonitrile / water (50:50, 3 mL / min), and collected in 13 minutes to obtain the compound.

[0025] 2. Structural identification of the compound

[0026] The compound is white powder, 1 H NMR(400MHz, CDCl 3 ,δin ppm,J in Hz):δ H 1.07(3H,s,H-18),1.04(3H,s,H-19),1.10(3H,s,H-20),3.56(1H,d,J=8.1Hz,H-17a),3.42 (1H, d, J = 8.1 Hz, H-17b). 13 C NMR(125MHz, CDCl 3 ,δin pp...

Example Embodiment

[0027] Example 2 Inhibition of compound on endothelial cell migration 1. Experimental materials, instruments and reagents

[0028] 1 Experimental materials

[0029] 1.1 Drugs: compounds isolated in our laboratory (atisane-3-oxo-16,17-diol)

[0030] Avastin

[0031] 1.2 Cell line:

[0032] Human umbilical vein endothelial cells (HUVEC) are preserved by our group.

[0033] 2 Preparation methods of main test reagents

[0034] 2.1 DMEM preparation method: take 10.4g DMEM dry powder, 2g NaHCO 3 , 50mg penicillin, 100mg streptomycin, ddH 2 O 800mL, mix thoroughly with a magnetic stirrer, adjust the pH to 7.4 with HCl, filter and sterilize with a 0.22μm filter, subpackage, store at 4°C for later use.

[0035] 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 the volume to 1L, autoclave at high temperature, store at 4℃ for later use.

[0036] 2.3 Trypsin preparation method: dissolve in PBS solution, stir overnight at 4°C, filter and ste...

Example Embodiment

[0052] Example 3 The inhibitory effect of compound on the formation of rat arterial ring 1. Experimental materials, instruments and reagents

[0053] 1 Experimental materials

[0054] 1.1 Drugs: compounds isolated in our laboratory (atisane-3-oxo-16,17-diol)

[0055] 1.2 Animals:

[0056] SD rat, SPF grade, female, body weight (250)g

[0057] 2 Preparation methods of main test reagents

[0058] 2.1 DMEM preparation method: take 10.4g DMEM dry powder, 2g NaHCO 3 , 50mg penicillin, 100mg streptomycin, ddH 2 O 800mL, mix thoroughly with a magnetic stirrer, adjust the pH to 7.4 with HCl, filter and sterilize with a 0.22μm filter, subpackage, store at 4°C for later use.

[0059] 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 the volume to 1L, autoclave at high temperature, store at 4℃ for later use.

[0060] 2.3 Matrigel solution: Matrigel is diluted 1:1 with serum-free ECM medium.

[0061] 2. Experimental method

[0062] The rats ...

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Abstract

The invention belongs to the field of traditional Chinese medicine, and in particular relates to an extraction process of atisane type diterpenoid and application thereof in preparing an anti-angiogenic drug. The application has the advantage that the novel use of a diterpenoid compound obtained from euphorbia antiquorum is provided. An experiment shows that the compound has an obvious inhibitoryeffect on HUVEC migration and rat arterial rings, indicating that the compound has anti-angiogenic activity and can be used as an angiogenesis inhibitor in the treatment of neovascular-dependent and neovascular-related diseases such as tumors, arthritis, maculopathy and atherosclerosis.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicines, and in particular relates to a compound extracted from jingangan, which has the application of drugs for inhibiting the formation of new blood vessels. Background technique [0002] 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. [0003] 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, angiogenesis only occurs ...

Claims

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Application Information

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IPC IPC(8): A61K31/122A61P9/00A61P35/00A61P19/02A61P27/02A61P9/10
Inventor 戚微岩刘晨高新梅徐寒梅
Owner CHINA PHARM UNIV
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