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Use of pogostemonis alkane type sesquiterpene compound as vegetative female sex normone

A patchoulane and sesquiterpene technology, which is applied in the direction of diseases, drug combinations, ketone active ingredients, etc., can solve the problems of weakening the protective effect of progesterone, achieve good development and medicinal prospects, easy to use, Source Rich Effects

Active Publication Date: 2009-04-15
SHANGHAI JAHWA UNITED
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the protective effect of progestins appears to diminish with long-term use, and hormone replacement therapy (HRT) is thought to be associated with a 35-40% increased risk of breast cancer

Method used

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  • Use of pogostemonis alkane type sesquiterpene compound as vegetative female sex normone
  • Use of pogostemonis alkane type sesquiterpene compound as vegetative female sex normone
  • Use of pogostemonis alkane type sesquiterpene compound as vegetative female sex normone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Isolation and Purification of Compound Cyperene-6,9-diacetoxy-3-ol

[0022] The dried and crushed rhizome (1 kg) of Cyperus rotundus was soaked in methanol at room temperature and extracted completely (3 days / time, 8 L / time×3). Concentrate the extract under reduced pressure to obtain methanol extract (132 g), distribute the extract with water-ethyl acetate, concentrate the ethyl acetate layer to obtain 65 g of extract, and the ethyl acetate extract contains various sesquiterpene components. The ethyl acetate extract was applied to a silica gel column, and after gradient elution with petroleum ether-ethyl acetate (100:1~0:100), the fraction eluted with petroleum ether-ethyl acetate (8:2) was washed with Sephadex LH- 20 to remove impurities, and then through silica gel column chromatography, separate a colorless oil, C 19 h 28 o 5 , Soluble in chloroform.

[0023] 1 H NMR (CDCl 3 , 300MHz) δ0.73(3H, s), 0.94(3H, d, J=7Hz), 1.04(3H, s), 1.73(3H, s), 1.95(3H, s), 2.21...

Embodiment 2

[0026] The estrogenic activity of the compound was determined by using the estrogen-sensitive cell line—human breast cancer cell MCF-7. MCF-7 cells cultured in phenol red-free DMEM (containing 10% CDT-FBS) for 4 days were seeded in 96-well culture plates (4×10 3 each / well) for 24 hours, discard the old culture medium after the cells adhered to the wall, add different concentrations of samples (total volume 200 μl / well), each dose group was incubated at 37 ° C, 5% CO 2 , after incubation for 5 days at relative saturated humidity, the absorbance (A) of each well was measured at a wavelength of 570 nm by MTT colorimetry, and the average value and proliferation rate were calculated.

[0027] result:

[0028]

[0029] ** : p<0.01.

[0030] It can be seen from the results in the table that the compound cyperene-6,9-diacetoxy-3-ol significantly stimulates the proliferation of MCF-7 cells and has estrogen activity.

Embodiment 3

[0031] Embodiment 3 mouse toxicity test

[0032]According to the conventional method, the mice were randomly divided into two groups, and each group was fed with a certain concentration of cyperene-6,9-diacetoxy-3-ol, observed for 7 days, and the cyperene-6,9 -LD of diacetoxy-3-ol 50 4.9 and 3.6 g / kg, respectively.

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Abstract

The present invention relates to a patchoulic alkyl-type sesquiterpene compound and its application. Said invention also provides its chemical structure formula, said compound can be made into medicine and cosmetic for preventing and curing the diseases due to deficiency of estrogen and estrogenic metabolic regulation disturbance.

Description

technical field [0001] The present invention relates to the new application of patchoulane-type sesquiterpenoids, in particular to the preparation of such compounds for the prevention and treatment of diseases caused by estrogen deficiency or sex hormone metabolism, especially disorders of estrogen metabolism regulation and uses in cosmetics. Background technique [0002] Women experience irregular menstrual cycles around age 40, which marks the onset of menopause. This period of endocrine system changes is called menopause, and it can last a decade or more. It is the result of failure of follicular growth and decreased response to gonadotropins. The result of the lack of follicles is that the production of estrogen decreases and eventually stops completely. Various symptoms may accompany it, such as hot flashes, depression, anxiety, confusion, insomnia, etc. In addition to this, decreased estrogen production may cause serious health problems such as osteoporosis, cardia...

Claims

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Application Information

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IPC IPC(8): A61K31/12A61P9/00A61P13/08A61P15/12A61P19/10A61P25/28A61P35/00
Inventor 赵亚魏少敏胡昌奇
Owner SHANGHAI JAHWA UNITED