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Application of senkyunolide J to medicaments for resisting cerebral apoplexy

A technology of lisantrolactone and cerebral apoplexy, which is applied in the field of new medical applications of lisanthemum lactone J, and can solve problems such as reducing aggregation

Inactive Publication Date: 2011-08-10
SHANGHAI ZHANGJIANG ENG RES CENT OF MODERN PREPARATION TECH OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still few reports on its pharmacological effects at present, and it is only found that it can reduce the deformable damage of ConA-induced erythrocytes and reduce its aggregation (Shi Zhen Guoyi Guoyao, 2003, 14 (12): 738-739.); Calcium influx in cardiomyocytes and human neuroblastoma (Clin Exp Pharmacology Physion, 1999, 26: 845-846.)
There are no reports or patents on its activity in anti-cerebral ischemia and protection of traumatic brain tissue

Method used

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  • Application of senkyunolide J to medicaments for resisting cerebral apoplexy
  • Application of senkyunolide J to medicaments for resisting cerebral apoplexy
  • Application of senkyunolide J to medicaments for resisting cerebral apoplexy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1. Alcohol extraction chromatographic preparation of Ligustilide J

[0020] Chuanxiong decoction pieces 1kg, after removing impurities, crushed into powder, 70% ethanol 10L reflux extraction twice, 2 hours each time, combined extracts, recovered solvent to obtain about 100g of extract A. The extract is separated by silica gel column chromatography (silica gel is 100-200 mesh or 200-300 mesh column chromatography silica gel, the weight ratio of extract sample to silica gel is 1:30), and the chloroform-methanol volume ratio is 50:1. Elution, the eluent thin-layer silica gel plate (GF 254 ) observed under the ultraviolet lamp 254nm after spotting, collected the part containing chuanxionglide J, and recovered the solvent under reduced pressure; the obtained extract was used in reverse phase C 18 Silica gel column chromatography (extract sample and C 18 Reversed-phase silica gel weight ratio = 1: 30), and discard the eluent after eluting 5BV with methanol-water ...

Embodiment 2

[0021] Embodiment 2. The preparation of Liguscaractone J tablet

[0022] Ingredients Amount per Tablet

[0023] Ligustilide J 100mg

[0024] Dextrin 37.45mg

[0025] Microcrystalline Cellulose 10.5mg

[0026] Starch 17.5mg

[0027] Lactose 10.5mg

[0028] Magnesium Stearate 1.05mg

[0029] According to the prescription amount, Ligustilide J (prepared according to the method of Example 1) was added to dextrin, microcrystalline cellulose, starch, lactose and mixed to make granules, magnesium stearate was added, mixed evenly, and compressed into tablets, namely (Each tablet contains 0.1g of Liguscaractone J). The recommended oral dosage for adults is 1-4 tablets / time, 2-3 times a day.

Embodiment 3

[0030] Embodiment 3. The preparation of Yangchuanxionglide J capsule

[0031] Ingredients Amount Per Capsule

[0032] Ligustilide J 100mg

[0033] Dextrin 37.45mg

[0034] Microcrystalline Cellulose 10.5mg

[0035] Starch 17.5mg

[0036] Lactose 10.5mg

[0037] According to the prescription quantity, mix chuanxionglide J (prepared according to the method of Example 1) dextrin, microcrystalline cellulose, starch and lactose, make granules, fill them into No. 0 hard capsule shells, and polish them to prepare Obtained (each capsule contains chuanxionglide J 0.1g). The recommended oral dosage for adults is 1-4 capsules / time, 2-3 times a day.

[0038] The present invention will be further illustrated by the test example and the pharmacological activity test and results of Liguscaractone J below.

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Abstract

The invention discloses new medicinal application of senkyunolide J shown in a structural formula (I). In the application, the influence of the senkyunolide J on the cerebral blood flow change of rats in a reperfusion model of local cerebral ischemia caused by middle cerebral artery occlusion (MCAO) of the rats and a kalium chloratum (KCL) induced rat cortical spreading depression model is studied by adopting an animal model, and pharmacological results prove that the senkyunolide J can improve the cerebral blood flow of the rats after MCAO molding obviously and can restore and exceed the original cerebral blood flow formed before modeling quickly after reperfusion so as to play a certain role in cerebral protection. In addition, the senkyunolide J can resist the condition that cerebral blood flow descends due to KCL-induced rat local cerebral vasoconstriction, so the senkyunolide J can be used for preparing medicaments for resisting cerebral apoplexy.

Description

technical field [0001] The invention relates to the technical fields of traditional Chinese medicine chemistry and medicine, in particular to a new medical application of senkyunolide J extracted and prepared from Ligusticumchuanxiong Hort. Background technique [0002] Chuanxiong (Ligusticum chuanxiong Hort.) is a plant of the genus Ligusticum in the family Umbelliferae, and its medicinal part is the rhizome. Chuanxiong is a traditional Chinese medicine in my country. It has the effects of promoting blood circulation and promoting qi, dispelling wind and relieving pain. It was listed as a top grade in the Eastern Han Dynasty "Shen Nong's Materia Medica", and it is a commonly used traditional Chinese medicine for treating depression and migraine. [0003] Phthalides are a class of compounds present in Rhizoma Chuanxiong, which have been shown to be active in cardiovascular, blood and smooth muscle. Among them, butylphthalide, which has been studied more, has many activities...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P9/10
Inventor 冯怡徐德生阮克锋梁爽王硕
Owner SHANGHAI ZHANGJIANG ENG RES CENT OF MODERN PREPARATION TECH OF TRADITIONAL CHINESE MEDICINE
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