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Application of coumarins compounds and method for extracting coumarins compounds from winter daphne

A technology of methoxy coumarin and Daphne, which is applied in the directions of active ingredients of heterocyclic compounds, organic chemistry, antiviral agents, etc., can solve the problems of many side effects and difficult drug synthesis.

Inactive Publication Date: 2013-04-10
GUIYANG COLLEGE OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved by the present invention is to overcome the defects of difficult synthesis and many side effects of existing drugs for the treatment of hepatitis C, and provide three kinds of natural coumarin compounds for the preparation of hepatitis C virus NS3 / 4A protease inhibitors and the treatment of hepatitis C Hepatitis drug application, while providing daphne ( Daphne papyracea Wall. ex Steud. var. crassius cula Rehd.) Method for extracting, isolating and purifying three compounds

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Embodiment 1: Extraction, separation and purification of compound

[0052] The Daphne medicinal material was collected from Guiyang, Guizhou in March 2005, and was identified as Daphne ( Daphne papyracea Wall. ex Steud. var. crassius cula Rehd.), the plant specimens are deposited in the Laboratory of Chinese Medicine Chemistry, Department of Pharmacy, Guiyang College of Traditional Chinese Medicine (specimen number GY200503D).

[0053] Take 5.5kg of Daphne daphne plant, crush it, heat and reflux extraction with 80-95% ethanol (the weight ratio of solid to liquid is 1:6) for 3 times, combine the extracts, and concentrate the extracts under reduced pressure until the relative density is 1.05-1.35 at 30°C. The extract was dispersed in water (the weight ratio of solid to liquid was 1:2), and then extracted three times with an equal volume of ethyl acetate. The extracts were combined, concentrated under reduced pressure and dried to obtain 132 g of ethyl acetate dry extra...

Embodiment 2

[0055] Example 2: It has been verified by experiments that the inhibition rates of the three compounds on hepatitis C virus protease NS3 / 4A at 100 mg / mL are respectively: daphnetin 69.9%, 7-hydroxy-8-methoxycoumarin 72.5% daphnetin and 79.5% daphnetin can be used to prepare medicines for treating hepatitis C.

Embodiment 3

[0056] Embodiment 3: Take daphnetin, daphnetin, and 7-hydroxy-8-methoxycoumarin or more than one or two, dry, pulverize, add appropriate auxiliary materials, and make granules, capsules, Pharmaceutically acceptable dosage forms such as tablets, oral liquids, soft capsules, and drop pills.

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Abstract

The invention discloses application of three coumarins compounds namely daph-neticin, daphnetin and 7-hydroxy-8-methoxycoumarin in preparation of a hepatitis c virus protease NS3 / 4 A inhibitor and hepatitis c treating medicines, and a method for extracting, separating and purifying the coumarins compounds from winter daphne (Daphnepapyracea Wall.ex Steud.var. crassiuscula Rehd.). The three coumarins materials have strong inhibition effect on hepatitis c virus protease NS3 / 4 A, are high in activity and can be used for preparing the medicines for preventing and treating hepatitis c independently; or the coumarins materials can be compounded with other components for preventing and treating hepatitis c; besides, the inventor extracts and separates the three coumarins compounds from the winter daphne plant for the first time by the modern plant chemical separation and purification technology; and the purity of the compounds is 98%; and the compounds can be applied as chemical standard substances for medicine test.

Description

technical field [0001] The present invention relates to the field of pharmaceutical technology, in particular to the pharmaceutical application of coumarin compounds and its Daphne papyracea Wall. ex Steud. var. crassius cula The method extracted from Rehd.). Background technique [0002] Hepatitis C, which is caused by human infection with hepatitis C virus, has become the most difficult health problem in the world. At present, 170 million people in the world have been infected. Without drug treatment, long-term infection with hepatitis C virus will develop into chronic hepatitis, liver necrosis, liver cancer and other diseases. Currently the most effective treatment method is pegylated interferon combined with zimbavir. This method has an effective rate of less than 50% for the treatment of type I hepatitis C that is prevalent in developing countries. Long-term use of interferon has many side effects, such as : Reduction of white blood cells, platelets, neutrophils an...

Claims

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Application Information

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IPC IPC(8): A61K31/37A61P31/14C07D311/18C07D493/04
Inventor 危英马超美服部征雄梁光义汪冶危莉
Owner GUIYANG COLLEGE OF TRADITIONAL CHINESE MEDICINE
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