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Preparation and application of neolignan compounds in angelica sinensis

A technology of compound and composition, applied in the field of 2,7'-epoxy-8,9'-new lignan enantiomers

Pending Publication Date: 2022-04-22
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are few studies on "guitou" in the literature, and the research on the chemical components is mainly concentrated on ethanol or methanol extracts, which is inconsistent with the way traditional Chinese medicine is decocted in water [6-13]

Method used

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  • Preparation and application of neolignan compounds in angelica sinensis
  • Preparation and application of neolignan compounds in angelica sinensis
  • Preparation and application of neolignan compounds in angelica sinensis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Embodiment 1, compound 1, (+)-1 and (-)-1 are new lignan compounds extracted, separated and purified from Angelica sinensis, and the separation and purification process is as follows:

[0058] After 97kg of dried angelica heads are pulverized, extract with distilled water, 300L of water each time, continue to heat for 30min after boiling, extract three times, combine the filtrate, recover the solvent under reduced pressure to obtain the extract, separate with HP20 macroporous resin column chromatography, and then use water (650L), 50% ethanol (500L) and 95% ethanol (250L) were eluted, and the solvent was recovered under reduced pressure to obtain the corresponding eluted fractions (A-C). Among them, component B (1.6kg) was suspended in water, treated with CHP 20 MCI resin, and eluted with water, 30% ethanol, 50% ethanol, and 95% ethanol in sequence to obtain subcomponents B1-B4. B4 (10g) and C (135g) were combined, and then subjected to normal phase silica gel column ch...

experiment example 1

[0062] Experimental Example 1, sedative-hypnotic effect, compound (+)-1 and (-)-1 on synergistic effect of pentobarbital sodium inducing sleep in mice

[0063] Experimental animals: ICR mice, male, weighing 18-22 g, were purchased from the Experimental Animal Center of the Chinese Academy of Medical Sciences. Before the experiment, the animals were acclimatized to the environment for at least 3 days, the room temperature was kept at 25±1°C, and they had free access to food and water. All handling of animals followed the requirements of the Ethics Committee of the International Association for the Study of Pain.

[0064] Test compounds: the test substances are compounds (+)-1 and (-)-1, and the positive drug is YZG-331.

[0065] Method: Give the mice a gastric or intraperitoneal injection of the test substance or solvent control, and 15 minutes later intraperitoneal injection of pentobarbital sodium (32 mg / kg) and start timing, observe and record the disappearance time of the ...

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Abstract

The invention belongs to the technical field of medicines, discloses preparation and application of neolignan in angelica sinensis, and particularly relates to remarkable sedative and hypnotic effects of novel neolignan compounds. Animal experiment results prove that the compounds (+)-1 and (-)-1 have obvious sedative and hypnotic effects and are expected to become drugs for treating mental diseases related to insomnia, convulsion, epilepsy / anxiety and depression.

Description

technical field [0001] The invention relates to new 2,7'-epoxy-8,9'-new lignan enantiomer obtained by extraction, separation and purification from Chinese medicine Angelica sinensis, and its derivatives and medicinal salts for the preparation, prevention and treatment of insomnia, Convulsions, epilepsy and other diseases. It belongs to the field of medical technology. Background technique [0002] Currently, clinically used sedative-hypnotic drugs mainly include diazepam, oxazepam, zolpidem, eszopiclone, zopiclone, etc. GABAa receptor agonists, melatonin receptor agonists represented by ramelteon (ramelteon) and tasimelteon (tasimelteon), etc., were developed by Merck and launched in the United States in 2014. Orexin receptor antagonists represented by suvorexant and antidepressants with sedative and hypnotic effects. However, most clinically used drugs have certain side effects, such as benzodiazepines. Drugs are prone to tolerance, dependence and withdrawal symptoms, ...

Claims

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Application Information

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IPC IPC(8): C07C62/34C07C51/47A61K31/192A61P25/20
CPCC07C62/34C07C51/47A61P25/20C07C2602/12C07B2200/07
Inventor 石建功张建军陈有哲郭庆兰徐成博姜剑伟朱承根王贵彬唐波
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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