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Quassia wood total alkaloid and the medical function of the monocase alkaloid

A technology of application and compound of general formula, applied in the field of medical use of total alkaloids and monomer alkaloids of Momordica fragrans, and can solve problems such as no report on inhibition effect.

Active Publication Date: 2007-09-19
SUZHOU LEINA PHARMA RES DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report on the inhibitory effect of alkaloids contained in bitter wood on the release of TNF-α, IL-1β and other pro-inflammatory cytokines

Method used

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  • Quassia wood total alkaloid and the medical function of the monocase alkaloid
  • Quassia wood total alkaloid and the medical function of the monocase alkaloid
  • Quassia wood total alkaloid and the medical function of the monocase alkaloid

Examples

Experimental program
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Effect test

preparation example 1

[0037] Preparation Example 1: Preparation of Total Alkaloids

[0038] After crushing 1 kg of bitter wood medicinal material, heat and extract with 10 liters of 75% ethanol twice, each time for 2 hours, combine the extracts, recover the ethanol under vacuum at 60°C, adjust the pH value to 11 with concentrated ammonia water, and extract with an equal volume of ethyl acetate 2 times, the extracts were combined, ethyl acetate was recovered, the residue was dissolved with 0.5% hydrochloric acid, and the above step of adjusting the pH with concentrated ammonia water—ethyl acetate extraction was repeated to finally obtain 17.1 g of total alkaloids. High performance liquid phase (HPLC) method is measured, and 4,5-dimethoxy ferric ketone, 4-methoxyl-5-hydroxyl ferric ketone both total content is 52% by weight / weight (w / w).

preparation example 2

[0039] Preparation example 2: the preparation of the total alkaloids of bitter wood

[0040]After crushing 1 kg of bitter wood medicinal material, heat and extract with 10 liters of 75% ethanol twice, each time for 2 hours, combine the extracts, recover the ethanol under vacuum at 60°C, adjust the pH value to 11 with concentrated ammonia water, and extract with an equal volume of ethyl acetate 2 times, the extracts were combined, ethyl acetate was recovered, the residue was dissolved with 0.5% hydrochloric acid, and the above step of adjusting the pH with concentrated ammonia water—ethyl acetate extraction was repeated to finally obtain 17.1 g of total alkaloids. 600g of column chromatography silica gel (200-300 mesh) is wet-packed with chloroform, 10g of total alkaloids are dissolved in absolute ethanol, mixed with 15g of column chromatography silica gel (100-120 mesh), and then mixed with chloroform after loading Gradient elution with methanol (the initial solvent is chlorof...

preparation example 3

[0041] Preparation Example 3: Preparation of 4,5-dimethoxyfermidone and 4-methoxy-5-hydroxyferricone

[0042] 600g of column chromatography silica gel (200-300 mesh) is wet-packed with chloroform, 10g of total alkaloids are dissolved in absolute ethanol, mixed with 15g of column chromatography silica gel (100-120 mesh), and then mixed with chloroform after loading Gradient elution with methanol (the initial solvent is chloroform), 250ml was collected once, checked by TLC, the same items were combined, and silica gel column chromatography was repeated to obtain 2.1g of 4,5-dimethoxyferricone, which was normalized by HPLC Check the purity of 98.7%; 1.7 g of 4-methoxy-5-hydroxyferricone can be obtained, and the purity of HPLC normalized check is 98.2%. , the physical and chemical properties are as follows: yellow needle crystal (acetone), mp 145 ~ 146 ° C, bismuth potassium iodide reaction was positive. IR v max KBr cm -1 : 1670, 1635, 1270, 1110, 1090. 1 H-NMR (400MHz, DMSO...

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Abstract

The invention relates to use of total alkaloid of picrasma quassioides (APO) and two monomer alkaloids 4, 5-dimethoxycantin-6-one) and 4-methoxy-5hydroxycanthin-6-one for preparing pre-inflammatory cytokine inhibitor, wherein the pre-inflammatory cytokine includes TNF-alpha, IL-1beta and the like.

Description

technical field [0001] The present invention relates to total alkaloids of bitter wood and two monomer alkaloids 4,5-dimethoxycantin-6-one (4,5-dimethoxycantin-6-one) and 4-methoxy-5-hydroxy iron Application of 4-methoxy-5-hydroxycanthin-6-one in the preparation of pro-inflammatory cytokine inhibitors. Background technique [0002] Inflammation is the body's defense-based response to the damage caused by various inflammatory factors. The local manifestations of acute body surface inflammation are redness, swelling, pain and dysfunction, while visceral inflammation and chronic inflammation are mostly not obvious. , Inflammation often causes systemic reactions, common ones are fever, increased number of white blood cells in the blood, and varying degrees of degeneration and necrosis in the heart, liver, kidneys and other organs. [0003] Proinflammatory cytokines are mainly secreted by macrophages, including TNF-α, IL-1α, IL-1β, IL-2, IL-6, IL-8, IFN-γ, etc., the most importa...

Claims

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Application Information

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IPC IPC(8): A61K31/4375A61K36/185A61P29/00A61P19/02A61P1/00A61P1/02A61P1/18A61P3/10A61P7/00A61P9/04A61P11/00A61P11/06A61P17/00A61P17/06A61P25/00A61P25/16A61P25/24A61P25/28A61P31/12A61P35/00
Inventor 邵萌刘军锋吴巍韩飞翟大伟滕厚雷
Owner SUZHOU LEINA PHARMA RES DEV
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