Quinoline-aspidospermine bi-indole alkaloid compound and application thereof

A technology of bisindole biology and quinine, which is applied in the field of quinoline- quinine type bisindole alkaloids and its application

Active Publication Date: 2019-10-25
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 quinoline-quinaline type bisindole alkaloid compound provided by the present invention and its use as an anti-inflammatory drug have not yet been reported

Method used

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  • Quinoline-aspidospermine bi-indole alkaloid compound and application thereof
  • Quinoline-aspidospermine bi-indole alkaloid compound and application thereof
  • Quinoline-aspidospermine bi-indole alkaloid compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: Extraction and separation of quinoline-basindole alkaloids

[0021] A total of 10 kg of Dongshan orange samples were taken, dried and crushed, and then extracted with a methanol solution with a volume concentration of 80% for three times, each time for 3 h. After filtering off the filter residue, the extract was combined to obtain 900g of extract. The extract was used with a volume concentration of 0.2%. Dissolve dilute hydrochloric acid and adjust the pH to 2~3, extract 3 times with ethyl acetate, adjust the pH of the extracted acid solution to 9~10 with 5% by volume ammonia water, extract 3 times with ethyl acetate, and collect The ethyl acetate layer was concentrated to obtain 95g of total alkali fraction; the total alkali fraction was passed through a normal phase silica gel column and eluted with petroleum ether-acetone (volume ratio 100:1, 10:1, 1:1), and the eluate was collected and concentrated Obtain 3 parts (Fr.A, Fr.B, Fr.C);

[0022] Fr.A (14.4g) was ...

Embodiment 2

[0035] Example 2: Inhibition of compounds 1, 2, and 3 on LPS-induced NO release from RAW 264.7 cells

[0036] (1) Material

[0037] DMEM medium (Gibco, USA), fetal bovine serum (Gibco, USA), RPMI-1640 medium (Gibco, USA), phosphate buffer (Shanghai beyotime), double antibody (HyClone, USA), DMSO (USA) Sigma company), MTT (American Sigma company), the compound of the present invention and dexamethasone are all prepared with DMSO;

[0038] (2) MTT method to determine the toxicity of compounds 1, 2, and 3 on RAW264.7 cells

[0039] Prepare a cell suspension with a culture medium (DMEM or RMPI1640) containing 10% fetal bovine serum, and take 200μL of RAW264.7 cell suspension (5×10 4 Pcs / mL) inoculate in 96-well culture plate, in 5% CO 2 Incubate in a constant temperature incubator at 37°C for 24 hours; aspirate the medium inside and add 200 μL of 30 μM test compound solution, and add 200 μL DMEM complete culture solution to the blank control group, with a final volume of 200 μL per well; ...

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PUM

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Abstract

The invention discloses a quinoline-aspidospermine bi-indole alkaloid compound. The quinoline-aspidospermine bi-indole alkaloid compound has the structural formulas shown in a formula I and a formulaII (please see the specification for the formula I and the formula II), wherein R1-R4 are correspondingly selected from hydrogen, hydroxy, methoxyl, ethyoxyl, acetyl, alkyl hydrocarbon and halogen. The experiment proves that the compound has the anti-inflammatory activity, the compound provides a lead compound for development of an anti-inflammatory preparation, and development and utilization ofplant medicinal resources are facilitated.

Description

Technical field [0001] The present invention relates to a class of quinoline-basatinine type bis-indole alkaloid compounds and their application in preparing anti-inflammatory drugs. Background technique [0002] Inflammation is a common pathological process in the clinic, which can be born in tissues and organs of various parts of the body, mainly manifested as swelling, redness, heat, pain and dysfunction. After the inflammatory factors act on the body, on the one hand, it triggers tissue cells Damage causes degeneration and necrosis of local tissue cells; on the other hand, it induces the body's anti-disease function to increase, which is beneficial to eliminate inflammatory factors and repair damaged tissues, thereby making the body's internal environment, internal environment and external environment To achieve a new balance between the two, the regulation and treatment of inflammatory response is of great significance to human health. The inflammatory response in the body ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D519/00A61P29/00A61K31/475
CPCA61P29/00C07D519/00
Inventor 程桂广何舒悦李芳茹贺停杨美莲曹建新赵天瑞
Owner 云南聚和生物科技有限公司
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