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Quinaine-quinoline type dimer indole alkaloid compound and its application

A technology of dipolybenzdole alkaloids and quercetin, applied in the directions of drug combination, organic chemistry, organic chemistry methods, etc.

Active Publication Date: 2021-04-30
云南聚和生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The quinine-quinoline type dimindole alkaloid compound provided by the present invention and its use as an anti-inflammatory drug have not been reported yet

Method used

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  • Quinaine-quinoline type dimer indole alkaloid compound and its application
  • Quinaine-quinoline type dimer indole alkaloid compound and its application
  • Quinaine-quinoline type dimer indole alkaloid compound and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020]Example 1: Extraction Separation of Compound Melokhanine K

[0021]After dry and pulverized, it was dried and pulverized, and the filtration was extracted 3 times with a methanol solution having a volume concentration of 80%, and the filtration was removed and the extract was removed, concentrated under reduced pressure, and the sample containing no organic reagent ( The immersed paste was transferred to a large beaker with an acid water (a volume concentration of 0.5% hydrochloric acid), pH to 2-3, extracted 3 times with ethyl acetate, collecting aqueous layer (alkali moiety) sodium hydroxide The pH is 9-10, then extracted 3 times with ethyl acetate, the ethyl acetate layer was collected, and the ethyl acetate extract was concentrated; the ethyl acetate layer extract was coated with a silica gel column, and the silica gel particle diameter was 100- 200 mesh, gradient with chloroform / acetone solution (volume ratio is 1: 0, 1: 1, 0: 1) elution, the total total of 3 portions were...

Embodiment 2

[0028]Example 2: Compound MLOKHANINE K To stimulate macrophages RAW 264.7 to produce NO inhibition in LPS

[0029](1) Experimental method

[0030]Raw 264.7 cell release (2 × 10 per hole is evaluated by detecting the amount of sodium nitrate in the medium by nitrate reductase method.4Cells) allow RAW 264.7 cells to grow on 96-well cell culture plates and in 5% CO2In the environment at 37 ° C for 24 hours; then different concentrations of test samples were added. The test concentration of the test compound of this test was set to 10 μg / ml, 20 μg / ml, 30 μg / ml, and the use of dexamethasone (10 μg / ml). Positive control, LPS as a negative control; continued culture for 2 h, adding LPS (5 μg / ml), continued culture for 24 h, and the culture supernatant was collected; the kit was measured according to nitric oxide (NO) assay kit (nitrate reductase) The method of the method determines the content of NO in the cell, the specific operation is as follows:

[0031]1 Add samples and R1, R2 mixing...

Embodiment 3

[0039]Example 3: Effect of Compound Melokhanine K on LPS-induced Raw264.7 macrophages induced by LPS

[0040](1) Materials

[0041]DMEM culture solution (US GIBCO company), fetal bovine serum (US GIBCO company), RPMI-1640 culture solution (US GIBCO company), phosphate buffer (Shanghai Beyotime), Double-China Hyclone, DMSO (USA) Sigma, MTT (US SIGMA), the compounds of the invention and dexamethasone were formulated with DMSO.

[0042](2) Preparation of test solution

[0043]It is weighed with 1 mg of compound Melokhanine K, and DMSO is dissolved, and the DMEM is not completely cultured to the desired concentration, and the DMSO final concentration is not more than 0.1%.

[0044](3) method

[0045]Take 200 μl of Raw264.7 cell suspension per well (5 × 104A / mL) was inoculated with a 96-well culture plate. After 24 hours, 10 μl of the test compound dilution was added to the culture solution, and the final concentration of the compound Melokhanine K was 10, 20, 30 μmol / L, each concentration. Three comp...

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PUM

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Abstract

The present invention discloses a quinine-quinoline type dimindole alkaloid compound as shown in formula I: wherein, R 1 selected from hydrogen, hydroxy, methoxy, ethoxy, amino, aliphatic, aliphatic amino, amide, halogen; R 2 selected from hydrogen, hydroxy, methoxy, ethoxy, amino, aliphatic, aliphatic amino, amide, halogen; R 3 Selected from hydrogen, hydroxyl, methoxyl group, ethoxyl group, amino group, aliphatic hydrocarbon group, aliphatic amino group, amide, halogen; the RAW 264.7 cell inflammation model induced by LPS in the present invention is effective on quinine-quinoline type dimindole biological Alkaline compounds were evaluated for their anti-inflammatory activity. The experimental results confirmed that the quinine-quinoline type dimindole alkaloid compound had anti-inflammatory activity, and the plant raw materials of Jingdongshan orange were easy to obtain, the price was low, and the alkaloid extraction process was simple; The quinine-quinoline type dimindole alkaloid compound has good development and application prospects in the preparation of anti-inflammatory drugs.

Description

Technical field[0001]The present invention relates to a white cooker-quinoline type diopolyne biologically alkali compound and its application in preparing anti-inflammatory drugs.Background technique[0002]Inflammation is a common multi-occurred disease that threatens human health, mainly as swelling, red, hot, pain, dysfunction, is a vascular system's living tissue to deal with defense response, physical, chemical or organisms such as damage factor. Or exogenous stimuli can cause inflammation. Many diseases or even cancer may have inflammatory responses, and the regulation of inflammatory responses and the treatment is of great significance to human health. In vivo inflammation involves participation in various cells, macrophages are one of the most important cells that control the most important inflammation of the body. The cytokines such as NO, IL-6, and TNF-α produced during the inflammatory reaction are mainly derived from activated macrophages. When LPS stimulates normal cell...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D519/04A61P29/00
CPCA61P29/00C07B2200/07C07D519/04
Inventor 程桂广崔绮敏李芳茹贺停杨美莲曹建新赵天瑞张宏赵燕
Owner 云南聚和生物科技有限公司
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