Oleanol type benzofuran and its glucoside applied in preparation of anti female hormone deficiency medicine

A technology of estrogen deficiency and oleanol, which is applied in the field of compounds to achieve remarkable curative effect, promote the synthesis of estrogen, and be convenient to use

Active Publication Date: 2010-05-12
CHENGDU DIAO PHARMA GROUP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have reported that oleanol-type benzofurans have antibacterial and antitumor activities (Pauletti PM, Araujo AR et al. Phytochemistry 2000; 597-601; Tsai IL, Hsieh CF, Duh CY. Phytochemistry 1998; 48: 1371-1375; Tsai IL, Hsieh CF, Duh CY, ChenIS.Phytochemistry 1996; 43:1261-1263; Cui B, Chai H et al.Tetrahedron 1997; 53:17625-17632); Literature records or research reports that alcohol benzofuran and its glycosides have the activity of promoting estrogen synthesis

Method used

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  • Oleanol type benzofuran and its glucoside applied in preparation of anti female hormone deficiency medicine
  • Oleanol type benzofuran and its glucoside applied in preparation of anti female hormone deficiency medicine
  • Oleanol type benzofuran and its glucoside applied in preparation of anti female hormone deficiency medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1: Extraction, separation and structure confirmation of oleanol-type benzofuran and its glycosides A, B, C, D, E, F, G, H, I

[0031] Extraction and separation: The seeds of Wasan benzoin were collected from Yongde, Yunnan, and were identified as Styrax perkinsiae. Get 2.2kg (dry weight) of the seeds of Washan Benzoin, pulverize and extract 3 times at room temperature with 80-90% technical alcohol 25L, each for 7 days. The extract was concentrated in vacuo to obtain 550g of the total extract, which was suspended in 5L of hot water, extracted 5 times with petroleum ether, chloroform and n-butanol in sequence, each time with 5L of solvent, and the extract was concentrated respectively to obtain the extract: Petroleum The ether fraction was 16 g, the chloroform fraction was 200 g, and the n-butanol fraction was 120 g. Samples were taken for in vitro activity screening, and both the chloroform and n-butanol fractions showed estrogen-promoting activity. The chlorof...

Embodiment 2

[0053] Example 2: Oleanol-type benzofuran and its glycoside A-I promote the synthesis of estrogen in mouse ovarian granulosa cells:

[0054] Collect mouse ovarian granulosa cells, culture them in a 96-well culture plate, add testosterone or androstenedione (0.5 mM), the raw material required for estrogen synthesis, and add the drug to be tested at a concentration of 100 μg / ml at the same time, at 37 ° C, 5 %CO 2 Cultivate under conditions for 48 hours, collect the supernatant, centrifuge at 1000 rpm for 3min, remove residual cells, and use an enzyme immunoassay kit to detect estradiol (E 2 ) or estrone content, (converted to E with 0.5mM testosterone 2 The maximum value of is taken as 100% formation rate, and the E of the compound is calculated 2 Synthesis rate), the results are shown in the following table 2:

[0055] Table 2. Oleanol-type benzofuran and its glycosides A-I promote the synthesis of E in mouse ovarian granulosa cells 2

[0056]

Embodiment 3

[0057] Example 3: Oleanol-type benzofuran and its glycoside A-I promote the synthesis of estrogen in mouse adipocytes:

[0058] The 3T3-L1 adipocytes of insulin-resistant mice were divided into 2.4×10 5 / well, 1mL / well was inoculated into 24-well culture medium, and E was added after the cells grew into a monolayer 2 Synthesize the desired substrate testosterone (0.5mM), and add the drug to be tested at a concentration of 100 μg / ml at the same time, continue at 37 ° C, 5% CO 2 Conditions were cultivated, and no drug (only testosterone) was used as a control. After 72 hours, the supernatant was drawn, centrifuged at 1000 rpm for 3 min, and residual cells were removed, and the content of estrogen in the supernatant was detected by an enzyme immunoassay kit (converted to E with 0.5mM testosterone). 2 The maximum value of is taken as 100% formation rate, and the E of the compound is calculated 2 Synthetic rate), the results are shown in the following table 3:

[0059] Table 3....

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Abstract

An application of oleanolic benzifuran and its heteroside in preparing the medicine for treating estrin deficiency, ovarian function sanilism, polycystic ovarian syndrome, climacteric syndrome, osteoporosis, ovarian hypofunction, etc, and the medicine in the form of tablet, capsule, etc are disclosed.

Description

technical field [0001] The present invention relates to a new application of a compound, specifically, the present invention relates to the use of oleanol-type benzofuran and its glycoside in the preparation of prevention or treatment of premature ovarian failure, menopausal syndrome, osteoporosis and pubertal hypofunction of the ovary, Use in medicine for polycystic ovary syndrome, infertility, and diseases caused by estrogen deficiency or relative insufficiency. Background technique [0002] Estrogen (especially estrogen) is one of the most important hormones in humans and other higher animals, and has a wide range of physiological functions. 90% of premenopausal women have E 2 , 50%E 1 They come from the ovaries and adrenal glands respectively. In postmenopausal women, due to ovarian atrophy, the ovarian function is significantly reduced, so the secretion of estrogen is greatly reduced. At this time, the estrogen produced by fat cells becomes E in the body. 2 main sour...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/36A61K31/343A61K31/7048A61K9/00A61P19/10A61P15/12A61P15/08A61P15/00
Inventor 李麒麟高小平张国林苏芝李伯刚刘忠荣
Owner CHENGDU DIAO PHARMA GROUP
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