Salidroside derivative and preparation and application methods thereof

A technology of salidroside and compound, applied in the field of medicine, can solve the problems of strong hydrophilicity, reduce the dosage of drugs, and be difficult, and achieve the effects of good apoptosis and low bioavailability.

Active Publication Date: 2019-03-05
FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This shows that the salidroside molecule has strong hydrophilicity but weak lipophilicity. On the one hand, it is not conducive to the passage of drugs through lipid membranes, and is difficult to be absorbed into tissue cells by the gastrointestinal tract, and it is also difficult to pass through the blood-brain barrier; on the other hand, water-soluble Strong drugs are easily metabolized in large quantities after entering the body, reducing the dose, reducing the efficacy, and weakening the pharmacological activity

Method used

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  • Salidroside derivative and preparation and application methods thereof
  • Salidroside derivative and preparation and application methods thereof
  • Salidroside derivative and preparation and application methods thereof

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Embodiment 1

[0033] The preparation of embodiment 1 salidroside derivatives

[0034] Add 3g (0.01mol) salidroside, 1.06g (0.01mol) sodium carbonate, 0.05g tetrabutylammonium bromide, and 10ml water into a 50ml three-necked flask. In an ice bath, stir until the solid is completely dissolved and the temperature of the system drops below 5°C. Dissolve 1.3ml (0.01mol) of benzoyl chloride in 10ml of ethyl acetate and add to the system. TLC (CHCl 3 :CH 3 OH=4:1) monitor the reaction, and stop the reaction when the raw material point disappears. The liquid was separated, and the aqueous phase was extracted three times with ethyl acetate, each time using 10 ml of ethyl acetate. The organic phases were combined, dried with anhydrous sodium sulfate, and the solvent was evaporated under reduced pressure to obtain a white solid. With silica gel as the stationary phase, (CHCl 3 -CH 3 OH) as the eluent, gradient elution was performed using flash preparative chromatography (model: Biotage isolera ...

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Abstract

The invention discloses a salidroside derivative and preparation and application methods thereof and belongs to the technical field of medicines. The prepared salidroside derivative can solve the problem of poor lipid solubility of salidroside. Compared with the salidroside, the prepared salidroside derivative can achieve higher protective effects on oxygen-glucose deprived-hypoglycemia and reoxygenation-injured human vascular endothelial cells and can be applied to preparing drugs for treating cardiovascular and cerebrovascular diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a salidroside derivative and its preparation method and application. Background technique [0002] Salidroside is the extract of Rhodiola rosea, a traditional Chinese medicine in my country, and it is also the main active ingredient and a marker of the substance basis of its efficacy. Many studies have shown that salidroside has anti-inflammatory, anti-oxidation, and anti-apoptotic effects, and has broad application prospects in the treatment of atherosclerosis and cardiovascular and cerebrovascular diseases. In the treatment of ischemic stroke, salidroside has a neuroprotective effect and a treatment time window of up to 48 hours; at the same time, it has a good inhibitory effect on the apoptosis of vascular endothelial cells under oxidative stress. [0003] However, although salidroside has many curative effects, it has many shortcomings in clinical application. S...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/18C07H1/00A61K31/7032A61P9/14A61P9/00
CPCC07H1/00C07H15/18
Inventor 陈立典洪桂祝褚克丹赖文芳张小琴杨泽霖苏燕青
Owner FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE
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