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Pharmaceutical composition of chlorprothixene and protective effect on cerebral ischemia reperfusion injury

A technology of cerebral ischemia-reperfusion and chlorprothixol, which is applied in the field of biomedicine, can solve the problems that have not yet been reported on the correlation of chlorprothixol cerebral ischemia-reperfusion injury, and achieve the reduction of cerebral ischemia-reperfusion injury, Excellent preventive effect

Inactive Publication Date: 2016-11-09
赵吉永
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] So far, there has been no report on the correlation between chlorprothixene and its pharmaceutical composition and cerebral ischemia-reperfusion injury

Method used

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  • Pharmaceutical composition of chlorprothixene and protective effect on cerebral ischemia reperfusion injury
  • Pharmaceutical composition of chlorprothixene and protective effect on cerebral ischemia reperfusion injury
  • Pharmaceutical composition of chlorprothixene and protective effect on cerebral ischemia reperfusion injury

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1: Compound (I) Separation Preparation and Structure Confirmation

[0018] Separation method: (a) Pulverize Nansha ginseng (2kg), extract with 65% ethanol under hot reflux (20L×3 times), combine the extracts, concentrate until there is no alcohol smell (4L), and successively use petroleum ether (4L×3 times) ), ethyl acetate (4L × 3 times) and water-saturated n-butanol (4L × 3 times) extraction, respectively obtain petroleum ether extract, ethyl acetate extract and n-butanol extract; (b) step (a ) in n-butanol extract with AB-8 type macroporous resin for impurity removal, first elute 12 column volumes with 10% ethanol, then elute 15 column volumes with 70% ethanol, collect 70% eluate, decompress Concentrate to get 70% ethanol elution concentrate; (c) in step (b), 70% ethanol elution concentrate is separated with normal phase silica gel, and the volume ratio is 50:1 (8 column volumes), 25:1 ( 8 column volumes), 15:1 (8 column volumes) and 5:1 (10 column volumes) ...

Embodiment 2

[0021] Example 2: Prevention and treatment of rat cerebral ischemia-reperfusion injury model

[0022] 1. Materials and methods

[0023] 1.1 Animals

[0024] Sixty adult healthy male Sprague-Dawley (SD) rats, SPF grade, weighing 280-300 g, were provided by Beijing Weitong Lihua Experimental Animal Technology Co., Ltd. During the experiment, the feeding environment of the rats was stable, with room temperature (25±2)°C, relative humidity (55±5)%, and light control for 12 hours to alternate day and night.

[0025] 1.2 Reagents and samples

[0026] Chlorprothixene was purchased from Shanghai Jiwei Biotechnology Co., Ltd. Compound (I) is self-made, and the preparation method is shown in Example 1. Edaravone injection (Sinopharm Guorui Pharmaceutical Co., Ltd.). Rabbit anti-mouse GFAP antibody, rabbit anti-mouse Iba1 antibody were purchased from Vector Company; rabbit anti-mouse TNF-α antibody, rabbit anti-mouse IL-1β, rabbit anti-mouse VCAM-1 antibody, rabbit anti-mouse ICAM-1...

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Abstract

The invention discloses a pharmaceutical composition of chlorprothixene and a protective effect on cerebral ischemia reperfusion injury. The pharmaceutical composition of chlorprothixene provided by the invention contains chlorprothixene and a novel structure natural product compound (I) separated from Radix Adenophorae. Chlorprothixene and the natural product can reduce cerebral ischemia reperfusion injury when they act individually, and the two can be combined to achieve a better control effect on cerebral ischemia reperfusion injury, thus being able to be developed into drugs for control of cerebral ischemia reperfusion injury. Compared with the prior art, the pharmaceutical composition provided by the invention has outstanding substantial characteristics and remarkable progress.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to a new application of chlorprothixene, in particular to a pharmaceutical composition of chlorprothixene and its protective effect on cerebral ischemia-reperfusion injury. Background technique [0002] Chlorprothixene is trans-2-chloro-9-(3-dimethylaminopropylene) thioxanthene, a thioxanthene antipsychotic with sedative and antiemetic effects. It is mainly used clinically for the treatment of schizophrenia, mania and reactive psychosis, and other mental disorders accompanied by excitement or affective disorders. It is suitable for schizophrenia, neurosis and menopausal depression accompanied by anxiety or anxiety depression. [0003] So far, there has been no report on the correlation between chlorprothixene and its pharmaceutical composition and cerebral ischemia-reperfusion injury. Contents of the invention [0004] The object of the present invention is to provide a pharmaceutical co...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/76A61K31/352A61K31/382A61P9/10
CPCA61K31/352A61K31/382A61K36/342C07D311/76A61K2300/00A61P9/10
Inventor 不公告发明人
Owner 赵吉永
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