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Compound with inhibiting activity on NO releasing of macrophage, preparation method and applications thereof

A technology of macrophages and compounds, applied in the field of medicine, can solve the problems of relatively few researches on chemical components, and achieve the effect of good anti-inflammatory effect and wide application prospect.

Active Publication Date: 2020-02-11
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In view of the significant physiological activity of Smilax genus plants, domestic and foreign scholars have conducted a lot of research on Smilax, but the research on its chemical constituents is relatively few, and the material basis of medicinal effect is still to be determined. The role of the compound is of great significance

Method used

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  • Compound with inhibiting activity on NO releasing of macrophage, preparation method and applications thereof
  • Compound with inhibiting activity on NO releasing of macrophage, preparation method and applications thereof
  • Compound with inhibiting activity on NO releasing of macrophage, preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1: the preparation of formula I compound:

[0037] a) Dried and pulverized the rhizome of Smilax smilax, a plant of the Liliaceae family, as a raw material, took 3 kg of raw material, added 30 L of 80v% ethanol aqueous solution, refluxed and extracted twice for 3 hours each time, combined the extracts to obtain a crude extract;

[0038] b) Adjust the crude extract to a pH of 5, filter; dry the filter cake as the extraction material, take 500 mg of the extraction material, add 5 L of ethanol to reflux extraction twice, each time for 20 minutes; combine the extracts, and concentrate under reduced pressure Dissolve in water, filter, and concentrate to obtain the crude extract of Smilax smilax;

[0039]c) Separating the crude extract of Smilax smilax with a solid-phase extraction column, respectively eluting with water and methanol in sequence, performing reverse silica gel column chromatography on the obtained methanol elution site, with a volume ratio of 20:80 ...

Embodiment 2

[0049] Example 2: Inhibitory test of the compound of formula I on the NO release activity of RAW 264.7 mouse macrophages

[0050] 2.1. Culture of RAW 264.7 mouse macrophages:

[0051] RAW 264.7 mouse macrophages were purchased from China Cell Line Bank (Beijing, China) at 37°C, 5% CO 2 Cultured in an incubator, the medium was supplemented with 10% heat-inactivated FBS (fetal bovine serum), 2.05 mM L-glutamine, penicillin (100 U / mL) and streptomycin (100 U / mL).

[0052] 2.2. Sample preparation

[0053] Take 1 mg of the compound of formula Ⅰ, add 1 mL of distilled water, heat and stir to make 1 mL of suspension, centrifuge at 1500 r / m to remove the precipitate, then filter and sterilize with 0.22 μm microporous membrane, store at 4 °C for later use, and evaporate the liquid to dryness at 50 °C under reduced pressure , re-dissolved in the cell culture medium, and filtered with a 0.22 μm microporous membrane before adding the cell culture medium.

[0054] 2.3. Determination of ...

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Abstract

The invention discloses a compound with inhibiting activity on NO releasing of macrophage, a preparation method and applications thereof, wherein the compound has a chemical structure represented by aformula I defined in the specification. According to the invention, the research results show that the compound represented by the formula I can obviously inhibit the excessive release of a macrophage RAW264.7 inflammatory medium NO, and has inhibiting activity on NO releasing of macrophage, so that the compound represented by the formula I has good anti-inflammatory effect, is expected to be used for preparing anti-inflammatory drugs, especially drugs for preventing and / or treating hyperostosis, and has wide application prospect.

Description

technical field [0001] The invention relates to a compound capable of inhibiting the release of NO from macrophages, a preparation method and application thereof, and belongs to the field of medicine. Background technique [0002] Inflammation is the body's defense response to stimuli, often manifested as redness, swelling, heat, pain, and other dysfunctions. When the body is stimulated by foreign pathogens, it often causes excessive release of various inflammatory mediators and excessive activation of inflammatory cells. Macrophages are an important part of the body's defense against foreign invasion. When macrophages are activated by external stimuli, they will produce a large amount of NO, which will further induce the production of inflammatory cytokines. Therefore, inhibiting the release of NO from macrophages is beneficial to prevent or to treat inflammation. [0003] Osteoarthritis, also known as proliferative osteoarthritis, osteoarthritis (OA), degenerative joint ...

Claims

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Application Information

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IPC IPC(8): C07D307/33A61P29/00A61P19/08
CPCC07D307/33A61P29/00A61P19/08C07B2200/07
Inventor 洪燕龙林晓张磊郑项炜王健英
Owner SHANGHAI UNIV OF T C M
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