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Application of cycloartane type triterpenoids compound of cimicifuga rhizome for anti-osteoporosis and menopausal syndrome

A technology for cyclic jackfruit alkane and jackfruit alkane, applied in the field of triterpenoids, can solve the problems of no indication of active ingredients, no report of cichoside compounds, risk of breast cancer, endometrial cancer, etc., and achieve the effect of less side effects

Inactive Publication Date: 2007-10-24
NANJING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although hormone replacement therapy is the first choice for the prevention and treatment of postmenopausal osteoporosis, long-term use has the potential risk of breast cancer and endometrial cancer
The long-term effects of bisphosphonates have not been fully proven
[0009] The Chinese invention related to the present invention has CN1111427C (application date on February 8, 1999) has introduced the utilization of Radix Cimicifugae and proposed to utilize Radix Cimicifugae extract (60-80% ethanol extraction extract extract with normal hexane after extracting, then use acetic acid Ethyl acetate extraction, the product of ethyl acetate extract purified with activated charcoal) for the use of drugs for promoting bone formation and anti-absorption and traditional organic solvent extraction methods, but no active ingredient is indicated
Another invention (applied date on July 31, 2003, publication number CN1475296A) proposed the extraction and preparation method of Cimicifuga extract (being Cimicifuga saponin), and proposed the content of Cimicifuga saponin and the role of the extract in promoting bone formation and Anti-absorption and the use of drugs and health products in the treatment of diseases caused by female estrogen imbalance, such as menopausal syndrome, but there is no specific report on the saponins of Cimicifuga in Cimicifuga

Method used

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  • Application of cycloartane type triterpenoids compound of cimicifuga rhizome for anti-osteoporosis and menopausal syndrome
  • Application of cycloartane type triterpenoids compound of cimicifuga rhizome for anti-osteoporosis and menopausal syndrome
  • Application of cycloartane type triterpenoids compound of cimicifuga rhizome for anti-osteoporosis and menopausal syndrome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Compound extraction and separation and structural identification

[0035] The extraction method of the extract of Cimicifuga cyclopine-type triterpenoids produced in China: the dried rhizomes and Fibrous roots, crushed, heated to reflux with 50-70% ethanol or propanol, extracted 1-4 times. Combine the extracts and concentrate under reduced pressure to remove the solvent in the extracts to obtain ethanol or propanol extract. Dissolve the extract in distilled water or a small amount of 50% ethanol, suspend it in distilled water, add petroleum ether solvent for 1-4 times of extraction, and similarly distill the suspension of the extract in distilled water extracted by petroleum ether with acetic acid Ethyl esters and other esters are extracted for 1-4 times to obtain ester extracts. Concentrate under reduced pressure to remove the solvent in these extracts to obtain ester extracts. Ester extract is dissolved in 95-100% ethanol, by gac column chromatography, r...

Embodiment 2

[0067] Example 2: Anti-resorptive activity

[0068] The compounds in Figures 1 and 2 were prepared in the three concentrations described in the table below with Ham's F-12 culture medium. Use suckling mice 2 days after birth, and inject subcutaneously 45 CaCl 2 (2 Ci), after 2 days, remove the skull, use Ham's F-12 culture medium, at a temperature of 37 ° C, CO 2After pre-cultivation for 24 hours under the condition of 5%, replace the new culture medium, and add 1,25 dihydroxy active vitamin D3 (1,25-(OH) 2 VD 3 , final concentration 10 -10 M) and each compound (see the table below for the final concentration, 200; 20 and 2 micromolar) continued to culture for 3 days under the same conditions as the pre-cultivation, and measured the amount of 45 Ca (measured value 1). Renew this culture medium, continue to cultivate under the same conditions as pre-cultivation again for 3 days, and measure the amount released into the culture medium in the same way. 45 Ca (measured valu...

Embodiment 3

[0074] Example 3: Anti-resorptive activity

[0075] The compound in Example 2 was formulated into 3 kinds of concentrations described in the table below like Example 2, 200; 20 and 2 micromoles.

[0076] 45 Ca release rate (%)

1,25 dihydroxyactive vitamin

D3

58.15±1.78

Normal group (without 1,25 dihydroxyl activity

vitamin D3 and compounds)

36.15±1.57 **

compound

2 micromoles (g

Compound concentration is 2 / 3

micromole)

20 micromoles (varies

Compound concentration is 20 / 3

micromole)

200 micromoles (each

Compound concentration is 200 / 3

micromole)

3, 5, 8 mixture

39.18±1.04 **

37.61±3.66 **

14.84±0.10 **

13a, 17, 18 mixture

40.22±2.61 *

29.78±2.30 **

14.10±0.10 **

[0077] Data are expressed as Mean ± SE. Compared with the 1,25 dihydroxyactive vitamin D3 group, there was a significant difference, * , p...

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Abstract

The invention discloses the application of cimig-jackfruit triterpane compound in preventing osteoporosis and climacteric metancholia. The method for preparing said triterpenes compound comprises: collecting dry root of C. dahurica, C. heracleifolia and C. foetida, disintegrating, heating with 50-70% ethanol or propanol, refluxing, extracting for 1-4 times; merging extract, compression condensing to remove dissolvent from extract and getting ethanol or propanol concrete; extracting with benzinum purificatum and acetic acid ethyl ester for 1-4 times, getting ester extract; activated char column chromatography, washing with 95-100% ethanol, separating with positive phase and reverse phase silica gel column, purifying and getting following 24 kinds of triterpenes compound, the compound is cycloartanes.

Description

1. Technical field [0001] The invention relates to triterpenoids (including triterpene glycosides) obtained from three commonly used traditional Chinese medicines, Cimicifuga foetida L., Cimicifuga heracleifolia Komarov and Cimicifuga dahurica (Turcz) Maxim The compound is used as an anti-osteoporosis, climacteric syndrome drug and a health care product. 2. Background technology [0002] Osteoporosis is known as a silent epidemic. It is a common and complex disease in middle-aged and elderly people characterized by decreased bone tissue mass and microstructural degeneration, resulting in increased bone fragility and susceptibility to fracture. According to the statistics of the World Health Organization, there are currently more than 200 million people with osteoporosis. There are 10 million patients in the United States with an estimated direct medical cost of $14 billion. It is estimated that Japan has now reached 10 million, and there is a tendenc...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K36/71A61P19/10A61P15/12A61K31/575
Inventor 李建新
Owner NANJING UNIV
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