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Beta-kabarin alkaloids in quassia wood, preparation method and application thereof

A technology of carbaline and alkaloid, applied in the field of traditional Chinese medicine, can solve the problem that the anti-inflammatory effect has not been reported yet, and achieve the effect of good research and development prospect and novel structure.

Active Publication Date: 2009-02-18
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the anti-inflammatory effect of the new compound disclosed in this patent to inhibit the release of inflammatory mediators such as NO, TNF-α and IL-6 has not been reported yet.

Method used

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  • Beta-kabarin alkaloids in quassia wood, preparation method and application thereof
  • Beta-kabarin alkaloids in quassia wood, preparation method and application thereof
  • Beta-kabarin alkaloids in quassia wood, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1: Extraction and separation of alkaloids in bitter wood

[0038] Take 10kg of dried root of Picrasma quassioides, extract under reflux with 60% ethanol, concentrate the extract to dryness, obtain 100g of dry extract, extract 3 times with equal volume of chloroform, and extract with chloroform part, concentrated to dryness under reduced pressure, and weighed 64g, the chloroform extraction part was eluted with cyclohexane-ethyl acetate (50:50-0:100) gradient to obtain 10 fractions PQC1 to PQC10, PQC7 (cyclo Hexane-ethyl acetate 30:70, 18.1g) was subjected to ODS medium and low pressure column chromatography to obtain 9 subfractions PQC7-1 to PQC7-9. Using preparative liquid phase, alkaloids 1-6 were isolated from sub-fraction PQC7-6 (methanol-water 50:50, 650 mg), and alkaloids 1-6 were isolated from sub-fraction PQC7-8 (methanol-water 60:40, 845 mg). Bases 7 and 8, alkaloids 9, 10 and 11 were isolated from subfraction PQC7-9 (methanol-water 70:30, 920 mg). ...

Embodiment 2

[0067] Example 2: Inhibitory activity experiment of bitterwood alkaloids 1-11 on release of nitric oxide (NO) from mouse mononuclear macrophage RAW 264.7 induced by lipopolysaccharide

[0068] Mouse mononuclear macrophage RAW 264.7 (ATCC TIB-71) was cultured in 10% heat-inactivated (56°C, 30min) fetal bovine serum (FBS), 100 U / mL penicillin sodium (Gibco), 100 μg / mL streptavidin in RPMI 1640 (Gibco) medium, 37°C, 5% CO 2 grown in a constant temperature incubator.

[0069] Because NO is extremely unstable, it is quickly metabolized into nitrous acid (NO) in the cell culture supernatant. 2 - ), so the Griess method was used to measure NO in the sample 2 - concentration as an indicator of NO levels. Griess reagent A: 0.1% N-naphthalene diamine dihydrochloride dissolved in water; Griess reagent B: 1% p-sulfanilamide dissolved in 5% H 3 PO 4 middle. Mix reagents A and B in equal volumes before use.

[0070] Dilute RAW 264.7 cells to 5×10 with RPMI 1640 medium 5 cells / mL c...

Embodiment 3

[0073] Example 3: Inhibitory activity experiment of bitterwood alkaloids 1-11 on lipopolysaccharide-induced release of tumor necrosis factor-α (TNF-α) from mouse mononuclear macrophage RAW264.7

[0074] Cell culture is the same as NO release inhibitory activity test.

[0075] The inhibitory activity of TNF-α was tested using the mouse TNF-α ELISA kit (R&D).

[0076] Dilute RAW 264.7 cells to 5×10 with RPMI 1640 medium 5cells / mL concentration, seeded in a 96-well cell culture plate, and added 200 μL of cell suspension to each well. CO 2 After culturing in the incubator for 1 h, add lipopolysaccharide (lipopolysaccharide, LPS) (Sigma) (final concentration 1 μg / mL) and 0.4 μL of different concentrations of test samples dissolved in DMSO to each well, and set up the LPS group at the same time (add LPS, but do not add Test sample, the inhibition rate to TNF-α release is 0%) and blank control group (do not add LPS and test sample, only add 0.4 μ L DMSO, the inhibition rate to TNF...

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Abstract

The present invention provides beta-kabarin alkaloid in India quassiawood, a preparation method thereof and an application thereof. The alkaloid has a structure as shown in Formula (I). In the preparation method, the plant India quassiawood is used as a raw material, an organic solvent and / or water are / is used for extraction, the chromatographic method and / or extraction method are adopted for separation, and the beta-kabarin alkaloid can be produced. The beta-kabarin alkaloid can be used as anti-inflammation medicine for preventing or treating inflammation caused by the releasing of nitrogen monoxide, tumor necrosis factor-alpha and interleukin-6 inflammation medium.

Description

technical field [0001] The invention relates to β-carbalin alkaloids in bitter wood, a preparation method and application thereof, and belongs to the field of traditional Chinese medicines. Background technique [0002] Inflammation is the body's defense-based response to the damage caused by various inflammatory factors, and often causes systemic reactions, such as fever, increase in the number of white blood cells in the blood, and varying degrees of degeneration of the heart, liver, kidney and other organs. Characterized by necrosis. Acute inflammation manifests itself as redness, swelling, heat, pain, and dysfunction as part of the body's defense response. However, chronic inflammation may lead to cancer, diabetes, lung disease, cardiovascular system and nervous system diseases, causing very serious harm to the body and even threatening the life safety of patients. [0003] The persistent existence of inflammatory factors and continuous tissue damage are the root cause...

Claims

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Application Information

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IPC IPC(8): C07D471/04C07D471/14C07D519/00A61K31/437A61P29/00
Inventor 姚新生高昊赵峰焦伟华李晨阳贺飞戴毅周光雄叶文才
Owner JINAN UNIVERSITY
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