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New application of chemical component of eucommia bark used as plant estrogen

A technology of estrogens and uses, applied in the field of new uses of Eucommia ulmoides as phytoestrogens

Active Publication Date: 2010-02-17
JIANGXI POZIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The prior art has not found any information about Eucommia ulmoides especially its extract, more particularly its monomeric chemical constituents have phytoestrogens effect

Method used

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  • New application of chemical component of eucommia bark used as plant estrogen
  • New application of chemical component of eucommia bark used as plant estrogen
  • New application of chemical component of eucommia bark used as plant estrogen

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Embodiment 1, the preparation of active ingredient monomer

[0065] Cut 31.5 kg of eucommia medicinal material (purchased from Henan Xinyang Medicinal Material Company) into small pieces, add 315 liters of 95% ethanol to soak overnight, reflux extraction for 2.5 hours, pour out the extract, pour out the extract, add 315 liters of 60% ethanol to the dregs Ethanol was refluxed for 2 hours, the extracts were combined and filtered, and the ethanol was recovered from the filtrate, followed by extraction with petroleum ether, chloroform, ethyl acetate and n-butanol, and the solids were obtained after recovering the solvents respectively. Results: 153g of petroleum ether partial solids, 384g of chloroform partial solids, 126g of ethyl acetate partial solids, and 520g of n-butanol partial solids.

[0066] After 350 g of Eucommia chloroform part was subjected to silica gel column chromatography, 33-36 fractions were subjected to repeated silica gel column chromatography to obta...

Embodiment 2

[0069] Embodiment 2, the structural confirmation of active ingredient

[0070] 11 compounds obtained in Example 1 (i.e., betulinic acid, genipin, aucubin, pinoresinol diglucoside, syringaresin diglucoside, pinoresinol monoglucoside, syringaresin monoglucoside , wogonin, baicalein A, baicalein, and dihydrochalcone 3-O-β-D-glucoside) for structural confirmation (entrusted Tianjin University Analysis and Testing Center detection, 500MHz NMR). The analysis results showed that the structures of these compounds were consistent with those reported in the literature, as follows.

[0071] Betulinic acid, white needle crystal. 1 H-NMR (C 5 D. 5 N, 500MHz): δ4.90 (1H, s, H-29a), 4.72 (1H, s, H-29b), 3.49 (1H, m, H-3), 1.74 (3H, s, H-30) , 1.18(3H, s, H-26), 1.02(3H, s, H-27), 1.01(3H, s, H-23), 0.96(3H, s, H-25), 0.77(3H, s , H-24).

[0072] Betulin, white powder. 1 H-NMR (CDCl 3 , 500MHz): δ4.68, 4.58 (2H, dd, J=11.5, 4.5Hz, H-29), 3.80, 3.33 (2H, dd, J=11.5, 4.5Hz, H-28), 2.3...

Embodiment 3

[0083] Embodiment 3, the activation effect of the compound of the present invention on estrogen receptor

[0084]Cell transfection method was used to observe betulinic acid, genipin, aucubin, pinoresinol diglucoside, syringaresin diglucoside, pinoresinol monoglucoside, syringaresin monoglucoside, wogonin, Selective activation of estrogen receptors by chilesin A, baicalein, and dihydrochalcone 3-O-β-D-glucoside. In fact, estrogen exhibits its biological activity by regulating the transcription of estrogen-responsive genes.

[0085] ER with reporter gene α or ER β The NA fragments were respectively transfected into Hela cells without ER expression, and after the test substance was added to the cell culture medium, it was observed whether the test substance could pass through the ER by detecting the transcriptional activation of the reporter gene. α or ER β exert estrogen-like effects.

[0086] Betulinic acid, genipin, aucubin, pinoresinol diglucoside, syringaresin digluco...

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PUM

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Abstract

The invention discloses a new application of a chemical component of chemical component used as plant estrogen, in particular relates to an application of an eucommia bark extract in preparing a medicine for treating and / or preventing a disease relevant to the estrogen hyposecretion of a mammal (particularly a human). The invention relates to an application of a composition in preparing a medicine for treating and / or preventing a disease relevant to the estrogen hyposecretion of a mammal (particularly a human), which is selected from one or more of the following components: betulinic acid, genipin, aucubin, pinoresinol diglucoside, syringaresinol diglucoside, abietinol monoglucoside, syringaresinol monoglucoside, wogonin, oroxylin A, baicalein and dihydrochalcone 3-O-beta-D-glucoside and a medicine composition containing the eucommia bark extract or an active component in the eucommia bark extract. The eucommia bark extract and a monomer chemical component in the eucommia bark extracthave the effect of effective plant estrogen.

Description

technical field [0001] The invention relates to the new application of several chemical components in the traditional Chinese medicinal material eucommia ulmoides, especially the new pharmaceutical application of the flavonoids, iridoids and lignin chemical components in the eucommia ulmoides as phytoestrogens. Background technique [0002] After women reach menopause, due to the continuous failure of ovaries and the decrease of estrogen secretion, various physiological processes mediated by estrogen are affected, resulting in palpitations, chest tightness, anxiety, depression, irritability, insomnia, memory loss and other physical and psychological symptoms. These symptoms are collectively referred to as menopausal syndrome; osteoporosis due to the effects of reduced estrogen secretion is referred to as degenerative osteoporosis. For the treatment and / or prevention of the conditions mentioned above, a beneficial approach is estrogen supplementation. However, clinical pract...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/46A61P5/30A61P9/00A61P15/12A61P19/10A61P35/00
Inventor 高秀梅王虹苏艳芳王涛刘二伟樊官伟
Owner JIANGXI POZIN PHARMA
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