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Medical application of radix arnebiae seu lithospermi naphthoquinone compounds

A compound, the technology of comfrey extract, applied in the field of medicine, can solve the problems such as no report on the therapeutic effect

Inactive Publication Date: 2014-04-23
SUZHOU LEINA PHARMA RES DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] However, the inhibitory effect of shikonaquinones on PDE4, as well as the therapeutic effect on asthma and chronic obstructive pulmonary disease, have not been reported on the therapeutic effect on inflammatory bowel disease, especially ulcerative colitis and Crohn's disease.

Method used

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  • Medical application of radix arnebiae seu lithospermi naphthoquinone compounds
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  • Medical application of radix arnebiae seu lithospermi naphthoquinone compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Mixtures of compounds of general formula (I) can also be obtained directly from Comfrey by the following method

[0035] Take 100Kg of decoction pieces of Xinjiang comfrey (Arnebiaeuchroma (Royle) Johnst) medicinal material (purchased from Yantai Medicine Mall), extract 3 times with 1500L petroleum ether at 55°C, each time for 3 hours, concentrate the extract to recover the solvent, and obtain about 4.2Kg of the extract was chromatographed on a 70kg silica gel column, eluted with petroleum ether-ethyl acetate system, and 2.1kg of Comfrey extract was obtained by TLC.

[0036] After HPLC analysis, the high performance liquid chromatography conditions are mobile phase: acetonitrile-water-formic acid (700:300:0.5), flow rate: 1ml / min, detection wavelength: 518nm, column temperature: 30°C. Calculate the content according to the peak area normalization method

[0037] The content of acetylarkanin in comfrey extract is 25.1%; the content of isovalerylarkanin + α-methylbutyryl...

Embodiment 2

[0039] Preparation of Shikonadhiquinone Monomer Compound

[0040] The comfrey extract obtained in Example 1 was subjected to silica gel column chromatography and eluted with the ratio of petroleum ether:ethyl acetate=100:1; 100:1; 100:2; 100:4, and the obtained eluate was evaporated to dryness After the solvent, use petroleum ether or petroleum ether-ethyl acetate and methanol to recrystallize at a certain ratio to obtain reddish-brown granular crystals-acetylarkanin, bright red scaly crystals-deoxyarkanin, reddish-brown Flaky crystals - β, β - dimethylacryl arcanin. α-Methylbutyryl arcanin and isovaleryl arcanin cannot be separated on silica gel column chromatography, it is a spot (color band), which can be separated by preparing liquid phase. The separation conditions are: mobile phase: THF: H2O=45:55; flow rate: 1ml / min; detection wavelength: 515nm. The red viscous α-methylbutyryl akanin and the red viscous isovaleryl akanin can be separated.

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Abstract

The invention discloses application of radix arnebiae seu lithospermi naphthoquinone compounds to preparation of medicaments for treating Crohn's disease. The invention further discloses medical application of one or more radix arnebiae seu lithospermi extracts with a formula shown in the specification.

Description

[0001] This application is a divisional application with the application number "201010132461.6" and the application name "Medical Use of Shikonadhiquinone Compounds". technical field [0002] The invention belongs to the technical field of medicine, and specifically refers to the use of shikonaquinone compounds in the preparation of a specific medicine. Background technique [0003] Cyclic nucleotides (cAMP and cGMP) are important second messengers in cells, regulating many biological activities in various cells, including cell growth, differentiation and migration, gene expression, mediator secretion, smooth muscle contraction, neurotransmitter-induced Various biological reactions, synaptic functions, lipid and glucose metabolism, etc. Cyclic nucleotide phosphodiesterases (phosphodiesterases, PDE) are the only intracellular decomposition pathway of cyclic nucleotides, so PDE inhibitors can regulate a series of biological functions by hindering the decomposition of cyclic n...

Claims

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Application Information

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IPC IPC(8): A61K31/122A61K31/222A61P1/00A61P29/00
Inventor 刘珂范华英
Owner SUZHOU LEINA PHARMA RES DEV
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