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Composite, preparation thereof and application of composite in preparing antidepressant drug

A composition, 10-technology, applied in the preparation of antidepressant drugs, the field of composition and preparation thereof, can solve problems such as neurotoxicity and cytotoxicity

Active Publication Date: 2014-02-12
SHANXI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, it has been reported that 17 polyacetylenic compounds have been extracted and isolated from plants of the genus Bupleurum, among which Bupleurum toxin and acetylbupleurum toxin have significant neurotoxicity and cytotoxicity, and other compounds have no activity or toxicity. to report

Method used

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  • Composite, preparation thereof and application of composite in preparing antidepressant drug
  • Composite, preparation thereof and application of composite in preparing antidepressant drug
  • Composite, preparation thereof and application of composite in preparing antidepressant drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1: the preparation of composition

[0022] (1) Preparation of Bupleurum Petroleum Ether

[0023] 5 kg of Bupleurum medicinal material was soaked in 95% ethanol for 12 hours, refluxed and extracted three times, and the extract was concentrated to obtain an extract. The extract was extracted with petroleum ether according to the preparation method of the petroleum ether part of Xiaoyao San compound to obtain the petroleum ether part of Bupleurum.

[0024] (2) Coarse separation of Bupleurum petroleum ether

[0025] Weigh 220 g of the above-mentioned Bupleurum petroleum ether part sample, put it into a chromatographic column, and use petroleum ether: ethyl acetate as the elution system. The above-mentioned silica gel column was sequentially eluted with petroleum ether:ethyl acetate at a ratio of 100:0-100. Silicone GF 254 Thin-layer chromatography plate and petroleum ether-ethyl acetate are used to develop the system to detect fractions. When the components mo...

Embodiment 2

[0084] Embodiment 2: Determination of in vitro activity of the composition

[0085]In vitro 5-HT, NA and DA monoamine transmitter reuptake inhibition tests were carried out on the above-mentioned extracted and separated compounds and their Bupleurum petroleum ether fraction and Xiaoyaosan petroleum ether fraction.

[0086] 1. Experimental materials

[0087] ①Animals

[0088] Strain: SD rats, sex: male, weight: 200-220g, source: Shanghai Slack Experimental Animal Co., Ltd., animal certificate number: SCXK (Shanghai) 2007-0005, feeding: routine feeding in SPF animal room.

[0089] ②Preparation of test samples

[0090] I. Preparation of Compositions

[0091] Composition 1 and Composition 2 were respectively dissolved in 10% DMSO (dimethyl sulfoxide, a commonly used solvent in pharmacology) to prepare a 1 mg / ml solution, and then diluted 10 times to make the concentration 100 μg / ml.

[0092] II. Preparation of Bupleurum Petroleum Ether Fraction

[0093] 12 kg of Bupleurum dec...

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Abstract

The invention relates to a composite which is composed of (2Z, 8Z, 10E)-2,8,10-pentadecane triene-4,6-diyne-1-alcohol and (2Z, 8E, 10E)-2,8,10-pentadecane triene-4,6-diyne-1-alcohol according to the proportion of 1:(1-4) or is composed of (2Z, 8Z, 10E)-2,8,10-heptadecane triene-4,6-diyne-1-alcohol and (2Z, 8E, 10E)-2,8,10-heptadecane triene-4,6-diyne-1-alcohol according to the proportion of 1:(1-4). The composite disclosed by the invention is obtained by being extracted and separated from traditional Chinese medicine radix bupleuri. The result of an in-vitro monoamine neurotransmitter reuptake inhibition experiment shows that the composite disclosed by the invention has triple inhibition effects on the reuptake of 5-HT (5-Hydroxytryptamine), NA (noradrenalin) and DA (Dopamine), is higher than the effective part of ease powder petroleum ether and the part of radix bupleuri petroleum ether in inhibition ratio and is higher than positive control drugs, namely fluoxetine, norpramin and 6-hydroxydopamine, in inhibiting effect. According to the invention, two composites can be applied to prepare a drug used for preventing and curing depression.

Description

technical field [0001] The invention relates to a composition of polyacetylene compounds, in particular to a composition, a preparation method thereof, and an application in the preparation of antidepressant drugs. Background technique [0002] Depression is a common mental illness characterized by high morbidity, relapse and disability. According to WHO's prediction, by 2020, single depression will become the second most disabling disease, and its harm has attracted more and more attention from the medical and health circles. [0003] Modern medical research shows that the pathogenesis of depression is complex, with many causes and various clinical symptoms. After nearly half a century of research on the pathogenesis, the most recognized is the monoamine hypothesis of depression, that is, depression is caused by the deficiency of monoamine neurotransmitters in the human brain, 5-HT, NA and / or DA . The main antidepressants currently used clinically increase the concentrat...

Claims

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Application Information

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IPC IPC(8): A61K31/045A61P25/24
Inventor 高晓霞周玉枝秦雪梅刘佳丽李震宇张丽增田俊生
Owner SHANXI UNIV
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