Application of chemical components of Herba Ecliptae to phytoestrogens

A technology of Eclipta chinensis extract and estrogen, which can be applied to medical preparations containing active ingredients, plant raw materials, organic active ingredients, etc., can solve problems such as large side effects, increased incidence of uterine cancer and breast cancer, etc.

Active Publication Date: 2016-12-07
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Traditional therapies such as estrogen replacement therapy were once popular, but their side effects are relatively

Method used

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  • Application of chemical components of Herba Ecliptae to phytoestrogens
  • Application of chemical components of Herba Ecliptae to phytoestrogens
  • Application of chemical components of Herba Ecliptae to phytoestrogens

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] The preparation of active ingredient in embodiment 1 Eclipta

[0034] Take 20kg Eclipta chinensis (purchased from Anguo Shengshan Pharmaceutical Co., Ltd., batch number: mhl0001, place of origin: Hebei), and extract with 100L of 70% ethanol under heat reflux, each extraction time is 2 hours, a total of 3 extractions. Distilled under reduced pressure at 45°C, concentrated to no alcohol, and the estimated extract mass is about 1kg.

[0035] Dissolve the crude extract in 10L of water, and extract 3 times with an equal amount of petroleum ether and ethyl acetate to obtain 255g of petroleum ether extract (named EPA-P), and 150g of ethyl acetate extract (named EPA-P). EPA-E), aqueous extract 600g (designated as EPA-W).

[0036] The water layer part (EPA-W) 600g, is separated by adsorption of macroporous resin D101, adopts pure water, 30% ethanol, 70% ethanol, pure ethanol for elution, and 30% ethanol eluate is EPA-W-D3.

[0037] The EPA-W-D3 components are 25g in total, mi...

Embodiment 2

[0042] Embodiment 2: Determination of the structure of compound 1-17

[0043] pass 1 H. 13 C-NMR determined the structure of compound 1-17; the determined structure of compound 1-17 is shown in Table 1.

[0044] The model of the NMR instrument is: BRUKER AVANCE Ⅲ 500 superconducting nuclear magnetic resonance spectrometer (TMS is the internal standard, Swiss Bruker company);

[0045] specific:

[0046] Compound 1 was characterized as follows:

[0047] 1 H-NMR (500MHz, pyridine-d 5 ) There are 2 hydrogens in the low field region of the spectrum: δ5.65 (1H, br s, H-12) and 5.25 (1H, br s, H-16). It can be observed in the middle and low field areas: δ3.31 (1H, m) is the H-3 hydrogen signal; δ4.92 (1H, d, J = 7.0Hz, H-1') and δ5.37 (1H, d , J=7.5Hz, H-1") suggest that there are two glucose groups. In the high field area, seven characteristic methyl peak signals can also be observed: δ1.85 (3H, s, H-27), 1.28 (3H,s,H-23),1.19(3H,s,H-30),1.10(3H,s,H-24),1.07(3H,s,H-29),1.0...

Embodiment 3

[0084] The mensuration of compound content in the extract of Eclipta chinensis in embodiment 3

[0085] (a) preparation of reference substance and need testing solution

[0086] Weigh an appropriate amount of each reference substance, weigh them accurately, put them in a 10mL volumetric flask, add methanol-water solution with a volume fraction of 50% to the mark, and obtain the reference substance series solution ①, luteolin 7-O-β-D glucoside (abbreviated as A, 18.15mg), luteolin (abbreviated as B, 4.64mg), eclidein IV (referred to as C, 11.85mg), apigenin (abbreviated as D, 1.56mg), ecliptaside A (referred to as E, 21.50 mg), echinocysic acid-28-O-β-D-glucoside (referred to as F, 2.60mg), echinocysic acid (referred to as G, 8.45mg). Take 1mL each of the reference substance series solutions ① and place them in 10mL volumetric flasks, add methanol-water solution with a volume fraction of 50% to the mark to obtain the reference substance series solutions ②. Take each referen...

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Abstract

An embodiment of the invention discloses application of chemical components of Herba Ecliptae to phytoestrogens, in particular to application of Herba Ecliptae extracts to preparation of medicines for treatment and/or prevention of estrogen secretion abnormality related diseases. The invention further relates to a pharmaceutical composition for treatment and/or prevention of estrogen secretion abnormality related diseases. The pharmaceutical composition comprises the Herba Ecliptae extracts and a medically acceptable carrier or excipient. According to researches, compounds obtained from Herba Ecliptae have different degrees of phytoestrogen effects. Expectably, the compounds or the Herba Ecliptae extracts and the pharmaceutical composition containing the compounds can be used for treatment and/or prevention of estrogen secretion abnormality related diseases and can be further applied to preparation of medicines for treatment and/or prevention of estrogen secretion abnormality related diseases.

Description

technical field [0001] The invention relates to the field of new applications of chemical components of Eclipta chinensis, in particular to the use of chemical components of Eclipta chinensis as phytoestrogens. Background technique [0002] After menopause, estrogen production decreases, leading to problems such as memory loss, hot flashes, fatigue, irritability, and loss of bone density. Traditional therapies such as estrogen replacement therapy were once popular, but their side effects are relatively large, and long-term use can increase the incidence of uterine cancer and breast cancer, so their use is restricted. Then scientists discovered that there is a class of active ingredients of heterocyclic polyphenols in plants that are similar in structure to endogenous estrogen. It can combine with mammalian or human estrogen receptor (estrogenreceptor, ER) to produce estrogen-like or anti-estrogen-like active effect, which is called phytoestrogens (phytoestrogen, PE). Phyto...

Claims

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Application Information

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IPC IPC(8): A61K31/704A61K31/352A61K31/381A61K31/7048A61K31/7024A61K31/235A61K31/575A61K31/366A61K31/56A61K36/28A61P5/30A61P15/12A61P19/10A61P9/00A61P35/00A61P15/14
CPCA61P35/00A61P15/12A61P19/10A61P9/00A61P15/14A61K31/381A61P5/30
Inventor 高秀梅王彧韩立峰苗琳王雪妮刘二伟王虹
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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