Medicinal use of 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

Active Publication Date: 2011-09-28
CHIATAI QINGCHUNBAO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] 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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  • Medicinal use of lithospermi naphthoquinone compounds
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  • Medicinal use of lithospermi naphthoquinone compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] The mixture of compounds with general formula (I) can also be obtained directly from Comfrey by the following method

[0034] Take Xinjiang comfrey (Arnebia euchroma (Royle) Johnst) medicinal herb decoction pieces 100Kg (purchased from Yantai Medicine Mall), leaching 3 times with 1500L petroleum ether at 55°C for 3 hours each time, concentrating the extract and recovering the solvent to obtain About 4.2Kg 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.

[0035] 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

[0036] The content of acetylarkanin in comfrey extract is 25.1%; the content of isovalerylarkanin + α-methylbutyrylarkanin...

Embodiment 2

[0038] Preparation of Shikonadhiquinone Monomer Compound

[0039] 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 respectively, 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 crystal-β,β-Dimethacryloylarkanin. α-Methylbutyryl arcanin and isovaleryl arcanin cannot be separated on silica gel column chromatography, which 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 the use of lithospermi naphthoquinone compounds in the preparation of phosphodiesterase 4 inhibitor. The invention also discloses the use of the lithospermi naphthoquinone compounds in the preparation of medicines for treating asthma and chronic obstructive pulmonary diseases, the use in the preparation of medicines for treating inflammatory bowel diseases, the use in the preparation of medicines for treating rheumatoid arthritis, particularly the use in the preparation of medicines for treating ulcerative colitis and Crohn disease. The invention also discloses the medicinal use of one or several of lithospermi extracts.

Description

technical field [0001] 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 [0002] 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 nucleotides. The large PDE family includes 11 families (PDE1-11) with different cAMP and / or cGMP specificities [FRANCISSH, TURKO IV, CORBIN JD. Cyclic nucleotide phosphod...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P1/04A61P11/00A61P11/06A61P1/00A61K31/122
Inventor 刘军锋刘珂范华英邵萌于翠翠于黎鑫赵海青窦玉梅梁丽娟
Owner CHIATAI QINGCHUNBAO PHARMA
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