Clear the rattan in c 21 Steroid compounds and their preparation methods and applications

A technology of compounds and steroids, applied to the preparation of steroids and steroids, chemical instruments and methods, etc.

Inactive Publication Date: 2017-08-25
中国人民解放军第二一〇医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But at present domestic and foreign also do not see about customs clearance rattan C 21 Literature reports and patent disclosures of steroidal compounds having the effect of preventing and treating osteoporosis

Method used

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  • Clear the rattan in c <sub>21</sub> Steroid compounds and their preparation methods and applications
  • Clear the rattan in c <sub>21</sub> Steroid compounds and their preparation methods and applications
  • Clear the rattan in c <sub>21</sub> Steroid compounds and their preparation methods and applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] The preparation of embodiment 1 Caulis officinalis active extract

[0052] Take 15 kg of dried Tengguan vine, extract it 3 times with 75% ethanol under reflux, the ratio of solid to liquid is 1:8, each time for 2 hours, recover the solvent under reduced pressure, and concentrate to 10L. Extracted three times with equal volumes of ethyl acetate and n-butanol respectively to obtain 115 g of ethyl acetate extract and 173 g of n-butanol extract.

[0053] Among them, the n-butanol layer is rich in C 21 Steroidal compounds, after content determination, its C 21 Steroid content reaches 82%.

Embodiment 2

[0054] Embodiment 2 separates C from the vine of customs clearance 21 Steroids.

[0055] Get the ethyl acetate layer extract 110g of gained in embodiment 1, adopt silica gel open column chromatography to separate, and mobile phase selects sherwood oil: ethyl acetate (100:1-2:1) and dichloromethane: methanol (100: 5-2:1) gradient elution, the obtained fractions were analyzed by silica gel thin-layer chromatography, and 10 eluates were obtained after combining the same fractions.

[0056] Petroleum ether: ethyl acetate = 100:30 fraction 11.0g was separated, using silica gel column chromatography, petroleum ether: ethyl acetate gradient elution, at 100:40, the yellow solid was separated by Sephadex LH-20, Then HPLC was used to separate and recrystallize to obtain compounds 1-3 and 5.

[0057] Petroleum ether: ethyl acetate = 100:40 fraction 8.9g was separated, using silica gel column chromatography, dichloromethane: methanol gradient elution, at 100:10, the solid part was separ...

Embodiment 3

[0061] Example 3 Determination of the proliferative activity of 11 compounds on MC3T3-E1 osteoblast cell line by MTT detection.

[0062] Experimental operation

[0063] (1) Cell culture

[0064] MC3T3-E1 cell line was cultured in 10% fetal bovine serum, 100 μg·mL -1 Penicillin, 100 μg·mL -1 In the DMEM medium of streptomycin, the cell culture environment was 37°C, 5% CO 2 The constant temperature incubator was used to incubate and grow, digested with 0.25% trypsin, and passaged every other day.

[0065] (2) Sample preparation

[0066] Take the ethyl acetate extract of the ethanol extract of Tengguan vine and the isolated monomer compound, respectively weigh an appropriate amount of sample and dissolve it in DMSO solution to prepare a concentration of 100 μmol L -1 The solution was stored in a refrigerator at 4°C for later use.

[0067] (3) Experimental process and grouping

[0068] Take the MC3T3-El cells in good growth state, after digestion, dilute with DMEM medium co...

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Abstract

The invention belongs to the technical field of medicines, and relates to the preparation of C21 steroid compounds in Tengguanteng and its application in the field of preventing and treating osteoporosis. The present invention discloses a C21 steroid compound of formulas (I) and (II) and salts thereof, R1-R5 as described in the description and claims. The compound of the present invention has good effect of preventing and treating osteoporosis, and can be combined with a pharmaceutically acceptable carrier to prepare clinically acceptable medicine for treating osteoporosis.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to C 21 Preparation of steroidal compounds and their application in the prevention and treatment of osteoporosis. Background technique [0002] In recent years, the incidence of osteoporosis in the elderly population has shown an obvious upward trend, seriously affecting the quality of life of the elderly. In osteoporosis, the number of osteoblasts is relatively insufficient or the function is decreased. If the proliferation ability of osteoblasts can be promoted and the overall function of cells can be improved, the osteogenic ability can be enhanced and the balance of bone metabolism can be improved, which is important for the prevention of osteoporosis. effect. Through a large number of research reports, we know that traditional Chinese medicine has a comprehensive and overall regulation effect on bone metabolism, has the effect of preventing and treating osteoporosis, and has fe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J71/00C07J75/00A61K31/58A61P19/10
Inventor 袭荣刚王晓波白爽高慧媛王达
Owner 中国人民解放军第二一〇医院
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