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

A cyclic jackfruit and osteoporosis technology, applied in the field of triterpenoids, can solve problems such as no active ingredient, no report of cichoside compound, breast cancer, endometrial cancer risk, etc., and achieve less side effects. Effect

Inactive Publication Date: 2010-05-12
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

[0033] Example 1: Compound extraction and separation and structural identification

[0034] 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

[0066] Example 2: Anti-resorptive activity

[0067] with Ham's F-12 medium figure 1 and 2 The compounds in were made into 3 kinds of concentrations described in the table below. Use suckling mice 2 days after birth, and inject subcutaneously 45 CaCl 2 (2Ci), after 2 days, remove the skull, use Ham's F-12 culture medium, at a temperature of 37 ° C, CO 2 After 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 -10M) 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 value 2). Ta...

Embodiment 3

[0074] Example 3: Anti-resorptive activity

[0075] The compound in embodiment 2 is dubbed into 3 kinds of concentrations described in the following table equally with embodiment 2, 200; 20 and 2 micromole.

[0076] Its anti-bone resorption activity was detected in the same manner as in Example 2, and the following results were obtained.

[0077]

[0078] Data are expressed as Mean ± SE. Compared with the 1,25 dihydroxyactive vitamin D3 group, there was a significant difference, * , p** , p<0.01.

[0079] The results clearly show figure 1 and 2 The mixture of compounds 3, 5, 8, 13a, 17, 19 has a strong inhibitory effect on the bone resorption induced by 1, 25 dihydroxyactive vitamin D3. The activity of the mixture was much stronger than that of the individual compounds alone, suggesting a synergy of activity between the compounds. Therefore, a mixture of triterpene saponins is better than using a single triterpene saponin from Cimicifuga.

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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 condensingto 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 columnchromatography, 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, known as a silent epidemic, is a common, middle-aged and elderly population characterized by decreased bone tissue volume and microstructural degeneration, resulting in increased bone fragility and a more complex disease prone to fractures. 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 tendency to continue to increase. W...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61K36/71A61P19/10A61P15/12A61K31/575
Inventor 李建新
Owner NANJING UNIV
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