Application of total triterpenes in preparing drugs inhibiting angiogenesis

An angiogenesis and compound technology, applied in drug combination, cardiovascular system diseases, antipyretics, etc., can solve the problems that triterpenoids have not been reported.

Inactive Publication Date: 2012-09-12
SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Triterpenoids are isolated from the root of Actinidia sinensis, and there is no report that this compound inhibits neovascularization and is used as an a

Method used

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  • Application of total triterpenes in preparing drugs inhibiting angiogenesis
  • Application of total triterpenes in preparing drugs inhibiting angiogenesis
  • Application of total triterpenes in preparing drugs inhibiting angiogenesis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 Preparation of triterpenoids 1,2,3,4

[0029] 1. triterpenoid 1 of the present invention, 2,3,4 compounds are prepared by the following method:

[0030] (1) Extraction: extract the dry powder of Actinidia sinensis with 95% ethanol percolation at room temperature, then vacuum evaporate the ethanol to obtain the crude extract of Actinidia sinensis;

[0031] (2) Extraction: disperse the above crude extract with water, then extract with chloroform, and evaporate the chloroform to dryness in vacuum to obtain the chloroform extract;

[0032] (3) Column chromatography: take the chloroform extract in (2) for silica gel column chromatography, the silica gel is 200-300 mesh (3kg), chloroform-methanol gradient elution (100:0, 99:1, 49:1, 19:1, 9:1, 4:1, 7:3, 3:2, 1:1), the amount of each gradient eluent is 4 times the column volume, each 500mL aliquot is collected, and the normal phase silica gel It was detected by layer chromatography, and the same components were c...

Embodiment 2

[0049] Example 2 Effects of triterpenoids 1, 2, 3, 4 on the proliferation of human umbilical vein endothelial cells (HUVEC)

[0050] Purpose and principle: CCK-8 method was used to detect the proliferation of HUVEC, which has been widely used in cell proliferation assay research. CCK-8 reagent contains WST–8 (2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfonic acid benzene) -2H-tetrazolium monosodium salt), which is reduced by the dehydrogenase in the mitochondria of the cell under the action of the electron carrier 1-Methoxy PMS (1-methoxy-5-methylphenazine dimethyl sulfate) to have Highly water-soluble yellow formazan product (Formazan). The amount of formazan produced is directly proportional to the number of viable cells. The absorbance was measured at a wavelength of 450 nm with an enzyme-linked immunosorbent detector, which can indirectly reflect the number of living cells.

[0051] Methods: HUVEC cells were seeded in 96-well plates at 5000 cells per wel...

Embodiment 3

[0057] Example 3 Triterpenoids 1, 2, 3, 4 inhibit the formation of HUVEC tubules

[0058] Purpose and principle: In vitro angiogenesis assay kit was used to investigate tubule formation in HUVEC. Matrigel is a soluble basement membrane matrix extracted from mouse EHS sarcoma. The main components include: laminin, collagen IV, etc., and also contain TGF-β fibroblast growth factor, tissue plasminogen activator and other growth factors naturally expressed in EHS tumors. At room temperature, Matrigel self-aggregates to produce a bioactive matrix material similar to the basement membrane of mammalian cells. HUVEC can adhere to form tubes on Matrigel, which can be used to study the effect of drugs on the formation of tubules by endothelial cells.

[0059] Methods: All operations involving Matrigel were carried out on ice, and the orifice plates and pipette tips used had to be pre-cooled. Add 50 μl of Matrigel solution into a pre-cooled 96-well plate, and place it in a 37°C incu...

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Abstract

The invention relates to application of total triterpenes in preparing drugs inhibiting angiogenesis. The application has the advantages that novel application of the total triterpenes in extractive of Actinidia chinensis roots is provided. An experiment proves that the total triterpenes 1,2,3,4 have remarkable inhibiting effect on multiplication of human umbilical vein endothelial cells (HUVEC) and canaliculization of HUVEC, have anti-angiogenic activity, and can serve as angiogenesis inhibitors. By means of the application of the total triterpenes in preparing the drugs inhibiting the angiogenesis, the anti-angiogenesis effect of the total triterpenes in the extractive of Actinidia chinensis roots is firstly found out, and the total triterpenes can serve as the angiogenesis inhibitors to be applied to treat new blood vessel dependence and new vessel related diseases including tumors, arthritis, skin and eye diseases, atherosclerosis and the like.

Description

technical field [0001] The invention relates to the application of a Chinese herbal medicine monomer, in particular to the application of an angiogenesis-inhibiting triterpenoid isolated from the root of Actinidia sinica actinidia in the preparation of angiogenesis-inhibiting drugs. Background technique [0002] Angiogenesis is the process of sprouting new capillary-based vasculature on existing microvascular beds. At the beginning of angiogenesis, vascular endothelial cells dedifferentiate first. Under various conditions, the vascular basement membrane becomes thinner or disappears, endothelial cells activate, proliferate, migrate, and a new basement membrane forms to cover endothelial cells and vascular smooth muscle cells, and eventually form new blood vessels. [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 ...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61P35/00A61P17/06A61P19/02A61P29/00A61P19/08A61P27/02A61P9/10
Inventor 方超杨国红陈红专朱文君於得红林梦感赵梅杨义芳陆琴王奇巍
Owner SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE
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