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

A technology for isopentenyl stilbene and inflammatory diseases, which is applied in the application field of isopentenyl stilbene in the preparation of medicines for the treatment of inflammatory diseases, and can solve the problems of limited effect of PMNs respiratory burst inhibition and the like

Active Publication Date: 2019-10-25
煌途医药(无锡)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, wortmannin, some macrolide antibiotics and non-steroidal anti-inflammatory drugs have been clinically used in the treatment of inflammatory diseases, but the inhibitory effect on PMNs respiratory burst is limited

Method used

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

[0020] Example 1 Preparation of isopentenyl stilbene (±)-dichrome pirochol D in dichroma jackfruit

[0021] 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 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. Frac...

Embodiment 2

[0022] Example 2 Structural identification of isopentenyl stilbene (±)-dichrome pirolenol D in dichroma jackfruit

[0023] (±)-Dichroic pirophenol D, a yellow amorphous powder (methanol). HR-ESI-MS gives quasi-molecular ion peaks m / z 447.2526 ([M-H] - , Calculated value: 447.2541), determine its molecular formula as C 29 h 36 o 4 . (±)-Dichroic pirochol D 1 H NMR spectrum (600 MHz, methanol- d 4 ) is very similar to the known bis-prenyl substituted stilbene hypargystilbene D. Compared with hypargystilbene D, (±)-dichromophorol D has an additional set of proton signals of 3-methyl-2-butenyl isopentenyl. This suggests that (±)-dichromobolol D is a triisopentenyl substituted stilbene derivative. In the HMBC spectrum of (±)-dichromol D, we observed H 2 -25 ( δ H 2.33) and C-5 ( δ C 43.0), C-6 ( δ C 33.2), C-16 ( δ C 141.6), and H-26 ( δ H 5.32) Correlation with C-5 ( Figure 7 ). This indicates that a 3-methyl-2-butenyl type isopentenyl substitut...

Embodiment 3

[0026] Example 3 (±)-Cytotoxicity evaluation experiment of dichromol D to rat PMNs

[0027] 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 the su...

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Abstract

The invention relates to isopentenyl stilbene and application thereof to preparation of drugs for treating inflammatory diseases. The isopentenyl stilbene is a new compound separated from artocarpus styracifolius Pierre which is a moraceae artocarpus plant, is named (+ / -)-artocarpus styracifolius phenol D, 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 1.5+ / -0.22 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 prenyl stilbene in two-color jackfruit in the preparation of medicines for treating inflammatory diseases. Background technique [0002] Neutrophils (PMNs) are a direct effector cell of nonspecific immunity and an important hallmark of inflammatory responses. When the body suffers from trauma or infection, it proliferates, differentiates, matures, and enters the tissue through the blood stream, playing a key role in the occurrence, development and outcome of inflammation. Under normal circumstances, PMNs are relatively rare in tissues, and PMNs in the circulation are also in an inactive state. When pathogenic bacteria invade the body, PMNs are activated, and the activated PMNs produce a large number of inflammatory mediators such as oxygen free radicals, protein granzymes, and cytokines through "respiratory burst" and degranulation. While these mediators...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D311/78A61K31/352A61P29/00
CPCA61P29/00C07D311/78
Inventor 任刚李文艳袁金斌易文芳林沁华邓文赞
Owner 煌途医药(无锡)有限公司
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