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2,4'-biphenol compound with angiogenesis inhibiting effect and pharmaceutica use thereof

A technology of biphenol and compounds, which is applied in the preparation of organic compounds, organic chemistry, organic active ingredients, etc.

Inactive Publication Date: 2013-10-30
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

We isolated a new 2,4′-biphenol compound from Magnolia officinalis, which has good angiogenesis-inhibiting effect, and there are no reports about its compound structure and angiogenesis-inhibiting effect

Method used

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  • 2,4'-biphenol compound with angiogenesis inhibiting effect and pharmaceutica use thereof
  • 2,4'-biphenol compound with angiogenesis inhibiting effect and pharmaceutica use thereof
  • 2,4'-biphenol compound with angiogenesis inhibiting effect and pharmaceutica use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1: the preparation of formula I compound

[0032] 1. Take 100 kg of Magnolia officinalis medicinal material, crush it into a coarse powder, add 70% ethanol to extract, the amount of ethanol is 8 times of the weight of the medicinal material respectively, the extraction time is 2 hours each time, and the extraction times are 3 times.

[0033] 2. Filtrate the extract, combine the filtrates, and concentrate under reduced pressure at 60°C to form an extract.

[0034] 3. Add 10 times the amount of 5% sodium hydroxide solution to the extract, stir to dissolve, let it stand until the solution is clear, filter, then add hydrochloric acid to adjust the pH value to 2-3, stand overnight, filter, and get acid precipitate .

[0035] 3. The acid precipitate was washed with deionized water until neutral, dried and pulverized to obtain the precipitate.

[0036] 4. Take the precipitate, add dichloromethane to reflux and extract, the amount of solvent used is 5 times of the ...

Embodiment 2

[0043] Example 2: Inhibitory effect of the compound of formula I on the proliferation of human vascular endothelial cells.

[0044] Human umbilical cord vascular endothelial cells (HUVEC, provided by the Third School of Clinical Medicine, Peking University). Cultured in 1640 medium (Gibco company) containing 10% fetal bovine serum (FBS, Gibco company) (37 ° C, 5% CO 2 , 95% humidity), the fourth-generation cells were inoculated in a 96-well culture plate at a density of 4000 / 50 μl, and a control group, a drug group with various concentration gradients and a blank control were set, and 3 replicate holes were made in each group. When the cell growth density reached 70%, 5 μl of the compound solutions of formula I (dissolved in DMSO) with various concentration gradients were added to make the final concentrations respectively 1000 μM, 100 μM, 10 μM and 1 μM. The control group was added with 5 μl DMSO, and the culture was continued (1640 medium, 10% FBS) after 48 hours, add 20 μl...

Embodiment 3

[0045] Example 3: Inhibitory effect of the compound of formula I on the tube-forming ability of human vascular endothelial cells.

[0046] Add 200 μl of BD Matrigel to each well of a 24-well culture plate to make it polymerized into a gel, and take the fourth-generation human umbilical vein endothelial cell (HUVEC, provided by the Third Clinical Medical College of Peking University) suspension and press 3.0×10 -4 Cells / 500 μl were inoculated into a 24-well plate coated with Matrigel, and a control group and drug groups with various concentration gradients were set, and 10 μl of the compound of formula I with concentration gradients (1 μM, 5 μM, 10 μM, 50 μM, 100 μM, dissolved in DMSO), the control group was added with 10 μl of sterile DMSO, and three replicate wells were made for each group. 37°C, 5% CO 2 , and cultured at 95% humidity for 24 hours, observed the formation of vascular endothelial cell tubes under an optical microscope, and counted 4 low-magnification fields pe...

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Abstract

The invention discloses 5- allyl-3'-(2,3-diallyl)-2,4'-biphenol novel compound (formula I) which is obtained by separating dry tree bark, root bark and wig bark from magnolia biloba (Magnolia officinalis Rehd. et Wils.var.biloba Rehd.et Wils ) of traditional Chinese medicine schisandra sphenanthera mangnolia officinalis (Magnolia officinalis Rehd. et Wils). According to the angiogenesis inhibiting activity research, the compound of the formula I has a good angiogenesis inhibiting effect. The 2,4'-biphenol compound can be used for preventing and treating the diseases including tumors, diabetic retinopathy, rheumatism, psoriasis, hemangioma and the like.

Description

technical field [0001] The invention relates to a natural 2,4'-biphenol compound with angiogenesis-inhibiting activity and its application in preparation of related diseases technical background [0002] In order to meet its own metabolism and a large demand for nutrients, tumors need abundant blood vessels in and around them to maintain energy and nutrients for tumor growth. If there is no angiogenesis, the growth of the primary tumor will not exceed 1~ 2mm, there will be no infiltration and metastasis. Tumor cells or tissues have the ability to initiate and promote angiogenesis. Studies have shown that not only the growth, invasion and metastasis of solid tumors depend on angiogenesis, but also the growth and metastasis of hematological malignancies (such as malignant lymphoma, lymphocytic leukemia, etc.) are closely related to angiogenesis. Therefore, inhibiting tumor angiogenesis is closely related to blocking the occurrence, development, invasion and metastasis of tum...

Claims

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Application Information

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IPC IPC(8): C07C39/21C07C37/70A61K31/065A61P35/00A61P3/10A61P9/10A61P29/00A61P17/06
Inventor 陈世忠王弘张宝宝
Owner PEKING UNIV
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