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Application of natural maca amide compound to preparation of bone mineral density improving products

A technology for increasing bone density and macamide, applied in the field of natural medicinal chemistry, can solve the problems of complex and unclear etiology and pathological mechanisms of osteoporosis, and increased risk of breast cancer and endometrial cancer.

Active Publication Date: 2015-03-25
国珍健康科技(北京)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the mechanism and material basis of Maca's anti-osteoporosis have not been reported, and it is still unclear.
[0004] The etiology and pathological mechanism of osteoporosis are relatively complex, currently believed to be related to hormonal factors, nutritional factors, exercise factors and immune factors, but its pathogenesis is mainly due to changes in the cytokine network system of osteoclastogenesis induced by sex hormone deficiency, which stimulates the osteoclastogenesis. The activity of bone cells is inhibited, and the rate of bone resorption exceeds the rate of bone formation, resulting in a proportional decrease in bone organic matter and inorganic matter.
Estrogen deficiency is the most important pathogenesis of osteoporosis. Estrogen replacement therapy is a traditional method for the prevention and treatment of osteoporosis. However, it will increase the risk of breast cancer and endometrial cancer. Therefore, there are similar choices Plant-selective modulators of action to prevent and treat osteoporosis are the focus of current research

Method used

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  • Application of natural maca amide compound to preparation of bone mineral density improving products
  • Application of natural maca amide compound to preparation of bone mineral density improving products
  • Application of natural maca amide compound to preparation of bone mineral density improving products

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Screening of anti-osteoporosis active substances in Maca in embodiment 1

[0020] Using molecular docking software (iGEMDOCK2.1), using the compounds contained in maca as ligands (Table 1) and estrogen receptors as targets, the Standard Docking method was used to predict the binding of compounds in maca to estrogen receptors Ability, the results are shown in Table 2, macamides have good binding ability, which may have anti-osteoporosis activity. In the binding conformation of macamides and estrogen receptors, the benzylamine structure is the main action structure, so compounds with similar macamide structures ( Wherein R3 is H or hydroxyl or C1-4 alkoxyl group, R4 is C7-C26 saturated or unsaturated aliphatic hydrocarbon group), should also have similar activity.

[0021] Table 1 Compound library in Maca

[0022]

[0023] Table 2 Compounds in maca that bind to estrogen receptors higher than estradiol

[0024]

Embodiment 2

[0025] The preparation of embodiment 2 macamide compound

[0026] Take 1kg of maca root powder, add 10L of 95wt% ethanol and extract under reflux at 50°C for 2 hours, filter, combine the filtrate, concentrate the filtrate under reduced pressure and evaporate the solvent to obtain 234g of crude extract. Get 100g crude extract and carry out silica gel column chromatography to remove impurities, successively elute with dichloromethane containing 10wt%, 20wt%, 30wt%, 40wt%, 50wt%, 60wt%, 70wt% ethyl acetate, collect 40wt% acetic acid The eluate from ethyl ester to 70wt% ethyl acetate was concentrated under reduced pressure and evaporated to dryness to obtain 26 g of fine extract. Take 100g of the refined extract and separate it by preparing a liquid phase, and use dichloromethane containing 10wt% methanol as the mobile phase to obtain 1.23g of compound 1, 1.11g of compound 2, 0.45g of compound 3, 0.78g of compound 4, and 0.97g of compound 5 , 1.02 g of compound 6.

[0027] The o...

Embodiment 3

[0040] Example 3 The effect of macamide compound on the proliferation and differentiation of MC3T3-E1 osteoblasts

[0041]1) Osteoblast culture

[0042] Mouse embryonic osteoblasts MC3T3-E1 were cultured with MEM (10% FBS, 80U / ml penicillin, 80U / ml streptomycin) medium in 5% CO 2 Cultivate in an incubator at 37°C, and change the medium every 3 days.

[0043] 2) MTT experiment

[0044] Digest the adherent cells with 0.25% trypsin, prepare a single cell suspension with MEM (10% FBS) culture medium, and make 1×10 per well 4 The cells were seeded in a 96-well plate with a seeding volume of 100 μl per well. After 24 hours the cells were completely adhered to the wall, they were divided into control groups (without adding drugs, adding the same amount of culture medium), and the concentration was 10 -4 mol / L of diethylstilbestrol, the concentration is 10 -6 mol / L, 10 -5 mol / L and 10 -4 mol / L compound 1 group, the concentration is 10 -4 mol / L compound 2 groups, the concentrat...

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Abstract

The invention discloses application of a maca amide compound and pharmaceutically acceptable salt thereof to preparation of bone mineral density improving products. A maca amide compound monomer is obtained by extracting and separating from Lepidiummeyenii Walp., and is found through in-vitro cell experiments and animal experiments to have an excellent ossification promoting effect and a bone mineral density improving effect; the natural maca amide compound is safe without toxic or side effects.

Description

technical field [0001] The invention relates to the application of natural macamide compounds in preparing products for increasing bone density, and belongs to the field of natural medicinal chemistry. Background technique [0002] Osteoporosis is a disease of bone metabolism. When the bone loss is too fast or the synthesis is abnormal, the bone will become loose and fractures will occur easily. Osteoporosis is a serious disease that endangers public health. It is especially prone to occur in the elderly. It is characterized by severe bone fragility and sensitivity, which can lead to fractures due to internal trauma, which has brought great harm to the lives of the elderly. inconvenient. Osteoporosis is also a complication of multiple systemic diseases clinically, because an important factor in causing death is fractures, especially in postmenopausal women. The degree of aging in today's society is getting worse, and the quality of life of the elderly has become a hot spot...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61P19/10A23L1/30A61K31/165A23L33/105
Inventor 余龙江刘浩金文闻余金龙余洪艳
Owner 国珍健康科技(北京)有限公司
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