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Isoamylene radical chromocor derivative, preparation method and uses thereof

A technology of prenyl flavonoids and derivatives, which is applied in sugar derivatives, drug combinations, and pharmaceutical formulations, and can solve problems such as visual impairment, headaches, and facial flushing

Inactive Publication Date: 2008-01-30
TOPHARMAN SHANGHAI +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to clinical side effects such as headache, facial flushing, and visual disturbance

Method used

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  • Isoamylene radical chromocor derivative, preparation method and uses thereof
  • Isoamylene radical chromocor derivative, preparation method and uses thereof
  • Isoamylene radical chromocor derivative, preparation method and uses thereof

Examples

Experimental program
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Effect test

preparation example 1

[0053] Preparation Example 1 Preparation of different solvent extracts of Epimedium

[0054] Take 2 kg of dried Epimedium extract, add water and methanol to suspend, extract 3 times with an equal volume of petroleum ether, concentrate the water layer under reduced pressure to remove methanol, add an equal volume of dichloromethane to extract 4 times, and combine the two The methyl chloride layer was concentrated under reduced pressure, and the dichloromethane was recovered to obtain the dichloromethane extract; the aqueous layer extracted with dichloromethane was extracted 4 times with an equal volume of ethyl acetate, and the ethyl acetate layers were combined and dried over anhydrous sodium sulfate After filtering, concentrate under reduced pressure, reclaim ethyl acetate, obtain ethyl acetate extract; The water layer after ethyl acetate extraction is extracted 4 times with n-butanol of equal volume, combine n-butanol layer, concentrate under reduced pressure, reclaim n-butan...

preparation example 2

[0055] The separation of preparation example 2 icariin-I

[0056] Get 4.5 grams of Epimedium ethyl acetate extract prepared by Preparation Example 1 and adsorb on 9 grams of silica gel, dry and go up the prepared silica gel column (4 * 70cm), with chloroform / methanol=9 / 1, 8 / 2 , 3 / 2 in the order of stripping, and collecting the stripping solution containing icariin-I. After concentration under reduced pressure, 71 mg of icariin-I was obtained through HPLC separation and methanol recrystallization.

preparation example 3

[0057] Preparation Example 3 Separation of Icariin

[0058] Get the 50 gram Epimedium n-butanol extract prepared by Preparation Example 1 to absorb on 100 gram silica gel, go up the prepared silica gel post (6 * 80cm) after drying, with chloroform / methanol=8 / 2, 3 / 2 The sequential dissolution, the eluate containing the icariin part was collected, concentrated, recrystallized with methanol and subjected to 1 Confirmed by H-NMR and analyzed by HPLC, 6.025 g of icariin was obtained.

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Abstract

The invention relates to a series of derivatives (I) of isopentenyl flavonoid and preparation methods and uses thereof. The pharmacology experiments show that: the compounds can inhibit cGMP specific phosphodiesterase, in particular to selectively inhibiting phosphodiesterase V (PDE5), and have wide application in the treatment and prevention of sexual function trouble and the improvement of vascoconstriction related diseases.

Description

technical field [0001] The present invention relates to a series of prenylflavone derivatives. Pharmacological experiments show that these compounds can inhibit cGMP-specific phosphodiesterases, especially phosphodiesterase V (PDE5) effectively, and are widely used in the treatment or prevention of sexual dysfunction and diseases related to improving vasoconstriction . At the same time, it provides a theoretical basis for drug research and development, and has great application and development value. Background technique [0002] Erectile dysfunction (ED) is a common and frequently-occurring disease in middle-aged and elderly men. Research in recent years has shown that nitric oxide plays an important role in the process of penile erection. With the elucidation of the physiological role of nitric oxide and the .NO / cGMP pathway, breakthroughs have been made in the research and development of drugs for treating ED. At the same time, the research on the mechanism of action ...

Claims

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Application Information

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IPC IPC(8): C07H17/07A61K31/7048A61P15/10A61P15/00A61P13/08A61P9/00A61P29/00A61P27/00
CPCC07D311/30C07H17/07A61P9/00A61P13/08A61P15/00A61P15/10A61P27/00A61P29/00
Inventor 沈敬山张树军郭洪利陈新建棘玉荣赵树军年亦丰
Owner TOPHARMAN SHANGHAI
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