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A stilbene derivative in two-color jackfruit and its use in the preparation of medicines for treating inflammatory diseases

An inflammatory disease, stilbene technology, applied in the field of medicine, can solve problems such as excessive activation of PMNs

Active Publication Date: 2019-10-29
JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, under some pathological conditions, PMNs are overactivated and generate a large amount of ROS, leading to severe inflammatory diseases

Method used

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  • A stilbene derivative in two-color jackfruit and its use in the preparation of medicines for treating inflammatory diseases
  • A stilbene derivative in two-color jackfruit and its use in the preparation of medicines for treating inflammatory diseases
  • A stilbene derivative in two-color jackfruit and its use in the preparation of medicines for treating inflammatory diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1 Preparation of stilbene derivative (±)-dichrome pirolenol C in dichroma jackfruit

[0022] Take 13.9 Kg of jackfruit root, extract by leakage with 95% ethanol, and concentrate the extract under reduced pressure to obtain 1.3 Kg of extract. The extract was suspended in 1 L of water, extracted successively with petroleum ether, chloroform, ethyl acetate and n-butanol (volume ratio 2:1), and concentrated to dryness respectively. Take 118.9 g of the extract from the chloroform extraction part, mix the sample with HP-20 macroporous adsorption resin (weight ratio 1:1), put it on the HP-20 type macroporous adsorption resin column (column specification: 10*45 cm), and mix with ethanol-water (0~95%) gradient elution to obtain 6 fractions Frs. H1-H6. 50% ethanol eluted fraction Fr. H4 (44.8 g) was subjected to ODS column chromatography (column size: 4*22 cm), MeOH -H 2 O (volume ratio 6:4, 7:3, 8:2, 9:1, 10:0) gradient elution to obtain 15 fractions Frs. H4O1-H4O15. ...

Embodiment 2

[0023] Example 2 Structural identification of stilbene derivative (±)-dichrome pirolenol C in dichroma jackfruit

[0024] (±)-Dichroic pirochol C, a yellow amorphous powder (methanol). HR-ESI-MS gives quasi-molecular ion peaks m / z 379.1907 ([M-H] - , Calculated value: 379.1915), determine its molecular formula as C 24 h 28 o 4 . (±)-Dichroic pirochol C 1 H NMR spectrum (600 MHz, methanol- d 4 ) shows the following proton signals: a set of aromatic ABX spin-coupled system protons δ H 7.16 (1 H, d, J = 8.5 Hz, H-7), 6.31 (1 H, dd, J = 8.5, 2.5 Hz, H-8) and 6.16 (1 H, d, J= 2.5 Hz, H-10); a pair of meta-coupled aromatic protons δ H 6.24 (1 H, d, J =2.3 Hz, H-4) and 6.19 (1 H, d, J = 2.3 Hz, H-2); a set of 1,1-dimethylallyl isoprene substituent protons δ H 5.84 (1 H, dd, J = 17.9, 10.4 Hz, H-23), 4.95 (1 H, dd, J = 17.9,1.3 Hz, H α -24), 4.94 (1 H, dd, J = 10.4, 1.3 Hz, H β -24), 1.14 (3H, s, H 3 -21) and 0.99 (3H, s, H 3 -twenty two). In ad...

Embodiment 3

[0027] Example 3 (±)-Cytotoxicity evaluation experiment of dichromophorol C on rat PMNs

[0028] Rat PMNs were isolated and purified using the following experimental procedures. Take clean SD rats (Jiangxi University of Traditional Chinese Medicine Experimental Animal Center, animal qualification certificate number: JZDW2011304), take 9 mL of blood from the orbit, and drop it vertically into a glass centrifuge tube that has been anticoagulated with 1 mL of 1% heparin sodium. Add 4.5% dextran T-500 saline solution at a ratio of 5:1, mix well, and let stand at 4°C for about 1 hour. Take the supernatant, add it to the centrifuge tube pre-filled with lymphocyte separation medium at a ratio of 3:1, 800 rpm (275 g ) Centrifuge for 15 minutes, take out the centrifuge tube, the tube is divided into three layers, the upper layer is light yellow serum, the middle white misty area is monocytes and lymphocytes, and the lower layer is PMNs that settle to the bottom of the tube. Discard t...

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PUM

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Abstract

The invention relates to a stilbene derivative and application thereof to preparation of drugs for treating inflammatory diseases. The stilbene derivative is a new compound separated from artocarpus styracifolius Pierre which is a moraceae artocarpus plant, is named (+ / -)-artocarpus styracifolius phenol C, and has a structure as shown in the following description. The compound has strong inhibitory activity on rat polymorphonuclear neutrophils (PMNs) respiratory burst, the IC50 is 4.24+ / -0.58 muM, and the compound can be further used for preparing the drugs for treating the inflammatory diseases, and is used in clinical treatment of various oxidative damage, such as rheumatoid arthritis, compensatory anti-inflammatory response syndrome (CARS) and systemic inflammatory response syndrome (SIRS), caused by the excessive activation of PMNs.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of a stilbene derivative in jackfruit dicolor in the preparation of medicines for treating inflammatory diseases. Background technique [0002] Neutrophils (PMNs) are hematopoietic stem cells derived from the bone marrow. After differentiation and development in the bone marrow, they enter the blood or tissues and act as direct effector cells of the body's nonspecific immunity. When foreign pathogens invade, PMNs are activated, consume a large amount of oxygen, and produce highly reactive superoxide anions, hydroxyl radicals, hydrogen peroxide and hypochlorous acid and other reactive oxygen species (ROS). This phenomenon is called "neutrophils" Explosive breathing." The ROS produced by neutrophil respiratory burst has two physiological functions: on the one hand, it can efficiently eliminate invading pathogenic microorganisms and maintain the health of the bod...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D311/78A61K31/352A61P29/00A61P19/02
CPCA61K31/352A61P19/02A61P29/00C07D311/78
Inventor 任刚李文艳袁金斌易文芳林沁华陈优婷
Owner JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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