Anti-osteoporosis acacetin derivative and preparation method thereof

An anti-osteoporosis and acacetin technology, which is applied in bone diseases, drug combinations, organic chemistry, etc., can solve the problems of decreased oral bioavailability, poor solubility of acacetin, and inability to fully dissolve, so as to be beneficial to osteoporosis. The deposition, post-processing is simple, the effect of environmental pollution is small
CN112876446AInactive Publication Date: 2021-06-01张洪胜
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
张洪胜
Publication Date
2021-06-01
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses an anti-osteoporosis acacetin derivative and a preparation method thereof, and belongs to the technical field of pharmaceutical chemistry synthesis. The method comprises the following steps: under the protection of nitrogen, adding acacetin and 2,4-dimethoxy benzyl chloride into an organic solvent, reacting for 6-8 hours under the action of alkali, and carrying out silica gel column chromatography separation and recrystallization to finally obtain the acacetin derivative. According to the invention, pathological experiments find that the acacetin derivative can inhibit bone resorption increase and bone tissue destruction caused by lack of female hormone, can also improve the blood calcium concentration and is beneficial to bone deposition, which indicates that the new compound has a certain prevention and treatment effect on osteoporosis caused by lack of female hormone.
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Description

technical field

[0001] The invention belongs to the technical field of chemical drug synthesis, and relates to an anti-osteoporosis acacetin derivative and a preparation method thereof. Background technique

[0002] Acacetin is a natural flavonoid compound widely found in acacia, chrysanthemum, acacia and so on. In addition to the traditional effects of relieving stagnation and calming the nerves, regulating qi and dredging collaterals, acacetin also has the effect of anti-osteoporosis. However, the solubility of acacetin in water is very poor, so that it cannot be fully dissolved in the aqueous solution of the gastrointestinal tract, and the dissolution rate is reduced, which eventually leads to a decrease in its oral bioavailability. Drugs with poor water solubility usually require high doses to be released after oral administration. Reach therapeutic plasma concentrations, but high doses of drugs may have certain side effects on the human body. Therefore, it is necessar...

Claims

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