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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

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 compound extraction, separation

[0023] 1. Extraction and separation

[0024] 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 (50:50, 3mL / min), and collected for 13 minutes to obtain the compound.

[0025] 2. Identification of the structure of the compound

[0026] The compound is a 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 ...

Embodiment 2

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

[0028] 1 Experimental materials

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

[0030] Avastin

[0031] 1.2 Cell lines:

[0032] Human umbilical vein endothelial cells (HUVEC) were preserved by our research 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, 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.

[0035] 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.

[0036] 2.3 Preparation method of trypsi...

Embodiment 3

[0052] Inhibition of Embodiment 3 Compounds Forming Rat Arterial Rings 1. Experimental Materials, Instruments and Reagents

[0053] 1 Experimental materials

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

[0055] 1.2 Animals:

[0056] SD rats, 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, 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.

[0059] 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.

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

[0061] 2. Experimenta...

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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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