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Sambucus williamsii hance lignan compound and preparation method and application thereof

A technology of compounds and lignans, which is applied in the field of elderberry lignan compounds and their preparation, can solve the problems of insufficient research on lignan components and unexplained mechanism of action

Inactive Publication Date: 2011-08-17
THE HONG KONG POLYTECHNIC UNIV SHENZHEN RES INST +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the research on the above-mentioned lignans is insufficient, and its mechanism of action has not yet been elucidated. Therefore, it is necessary to carry out in-depth research on the lignans in elderberry

Method used

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  • Sambucus williamsii hance lignan compound and preparation method and application thereof
  • Sambucus williamsii hance lignan compound and preparation method and application thereof
  • Sambucus williamsii hance lignan compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: the preparation method of lignans compound in Elderberry

[0026] Take 50 kilograms of dry stems and branches of elderberry, after proper pulverization, heat and reflux extraction with 10 times the amount of 60% ethanol for 3 times, each time for 2 hours. The extracts were combined, and the solvent was evaporated under reduced pressure to obtain 2160 grams of the total extract of Elderberry. Get 1250 grams of elderberry total extract subsequently, dissolve with suitable amount of water, carry out macroporous resin open column chromatography, use the water of 5 times column bed volumes, 30%, 50%, 95% ethanol-water solution gradient elution successively, The eluents of each part were collected, and the solvent was recovered under reduced pressure respectively to obtain 712.5 g of water eluted fraction, 160 g of 30% ethanol eluted fraction, 125 g of 50% ethanol eluted fraction and 111 g of 95% ethanol eluted fraction. Elderberry 50% ethanol eluting part 20.3...

Embodiment 2

[0027]Example 2: Structural analysis of lignans

[0028] 2.1 Structural Analysis of Compound 1

[0029] Yellow oil (methanol), [α] 27 D -1.5° (c=0.67, MeOH). Combining 1H NMR, 13C NMR and DEPT-135, it was determined that the molecular formula of the compound was C20H24O7, and its degree of unsaturation was calculated to be 9.

[0030] On the 1H NMR (400MHz, in CD3OD) spectrum of compound 1, the downfield region gives 8 sets of hydrogen signals, one of which has a single peak integral value of 2. Although there is signal overlap, according to the chemical shift value and coupling constant, it can still be judged that there are 2 ABX coupling systems and 1 trans double bond coupling, and the ABX coupling systems are δ7.01 (1H, d, J=1.8Hz, H -2), δ6.72 (1H, d, J=8.1Hz, H-5) and δ6.83 (1H, dd, J=8.1, 1.8Hz, H-6); δ6.98 (1H, d, J=1.9Hz, H-2'), δ6.86 (1H, H-5') and δ6.86 (1H, H-6'), the trans double bond is δ6.50 (1H, d, J= 16.0 Hz, H-7') and δ6.22 (1H, dt, J=15.8, 5.8 Hz, H-8...

Embodiment 3

[0042] Example 3: Effects of Lignans on Osteoblast-like UMR 106 Cells

[0043] The in vitro anti-osteoporosis activity of the compound prepared in Example 1 was evaluated by the proliferation and ALP activity of rat osteoblast-like UMR 106 cells.

[0044] 3.1 Experimental samples

[0045] The compound obtained in Example 1 refers to the compound guaiacylglycerol-β-coniferyl ether and D-erythro-1-(4-hydroxyl-3-methoxybenzene) obtained in Example 1. base)-2-[-4-(3-hydroxypropyl)-2-methoxyphenoxy]-1,3-propanediol.

[0046] 3.2 Experimental method

[0047] UMR 106 cells were trypsinized and dispersed, seeded in 96-well plates at a density of 4000 cells / well, and cultured in an incubator at 37°C, humidity 95%, and 5% CO2. After cultured in 10% FBS (fetal bovine serum)-DMEM medium for 2 days, cultured again with 1% Charcoal Stripped FBS (fetal bovine serum removed by activated carbon treatment)-Phenol red-free DMEM (DMEM with phenol red removed) sky. The compound described in E...

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Abstract

The invention belongs to the field of Chinese medicinal application, and relates to a sambucus williamsii hance lignan compound and application of the compound in preparation of medicaments and health-care products for relieving and improving menopausal bone related diseases. A levorotatory erythro-guaiacylglycerol-beta-O-4'-conifery ether compound and a dextrorotary erythro-1-(4-hydroxy-3-methoxyphenyl)-2-[-4-(3-hydroxypropanyl)-2-methoxyphenoxy]-1,3-propanediol compound are separated from Chinese medicinal sambucus williamsii hance and have remarkable promotion effect on proliferation and differentiation of osteoblasts by in vitro experiments, the proliferation effect can be blocked by an estrogen receptor blocking agent, and the compounds have no side effect of promoting proliferation of breast cancer cells. The lignan compound serving as an active ingredient has broad application prospect on the aspect of preparing the medicaments and the health-care products for preventing and treating osteoporosis related diseases.

Description

technical field [0001] The present invention relates to an elderberry compound and its preparation method and application, specifically provides a preparation method of a compound isolated from an elderberry extract and a structural analog thereof, and the use of these compounds in Application in the preparation of natural anti-osteoporosis drugs, food or food additives Background technique [0002] Osteoporosis (OP) is a systemic skeletal disease characterized by decreased bone mass and degeneration of bone microstructure, resulting in increased bone fragility and susceptibility to fractures [1]. Bone is an active, constantly remodeling tissue. Bone remodeling is a dynamic equilibrium process consisting of osteoclast-mediated bone resorption and osteoblast-mediated bone formation. After the age of forty, the functions of both osteoblasts and osteoclasts will decline, and the decline rate of osteoblasts is much faster than that of osteoclasts. Bone metabolism is abnormal, ...

Claims

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Application Information

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IPC IPC(8): C07C43/23C07C41/36A61K31/09A61P19/00A61P19/10A23L1/28A23L1/30
Inventor 黄文秀姚新生肖辉辉戴毅
Owner THE HONG KONG POLYTECHNIC UNIV SHENZHEN RES INST
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