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

A technology of use and compound, which is applied in the field of medical application of the total alkaloids and monomeric alkaloids of eucalyptus, and can solve the problems that the inhibitory effect has not been reported.

Active Publication Date: 2011-12-28
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, 1kg of the bitter wood was heated and extracted with 10 liters of 75% ethanol for 2 hours each time. The extracts were combined, and the ethanol was recovered in vacuo at 60°C. The pH was adjusted to 11 with concentrated ammonia water, and extracted 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 steps of pH adjustment with concentrated ammonia water—ethyl acetate extraction were repeated, and finally 17.1 g of total alkaloids were obtained. 600g column chromatography silica gel (200-300 mesh) was packed with chloroform wet method, 10g total alkaloids were dissolved in absolute ethanol, mixed with 15g column chromatography silica gel (100-120 mesh), and the sample was loaded with chloroform Methanol gradient elution (initial solvent is chloroform)...

preparation example 3

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

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

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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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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4375A61P3/10A61K36/185A61P1/00A61P19/02A61P7/00A61P29/00A61P1/02A61P9/04A61P1/18
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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