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Application of cerebroside compound

A technology for cerebrosides and compounds is applied in the application field of preparing medicines for treating post-ischemic brain injury, which can solve the problems of difficulty in separation and purification, and achieve the effects of significant therapeutic effect, reduction of cerebral infarction area and high yield.

Inactive Publication Date: 2010-05-12
NANJING MEDICAL UNIV +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Coupled with its similar structure, it brings great difficulties to the separation and purification

Method used

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  • Application of cerebroside compound
  • Application of cerebroside compound
  • Application of cerebroside compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] The method for preparing cerebroside A and cerebroside B from Gallus pilosulae, the concrete steps are:

[0033] (1) Pulverization: the dried Gallinarum gallinarum sample (1.5kg) (Yanyuan County, Sichuan Province) is pulverized to 100~10 orders;

[0034] (2) Solvent extraction: the pulverized gallinaceous fungus is packed into a 15-liter container, and methanol (7.5 liters) is shaken and extracted in a shaker for 3 days to obtain the gallinaceous fungus extract (151.3g); Subsequently, the extract was distributed with 90% aq.MeOH and n-hexane, and the resulting 90% aq.MeOH solution was concentrated and then distributed with water and n-butanol, and the n-butanol solution was concentrated under reduced pressure to obtain n-butanol layer sample (16.0 g);

[0035] (3) separation and purification: n-butanol layer sample with ODS open column (solvent system is MeOH: H 2 (0=90:10, 95:5, 100:0) separation; then, the sample containing the target compound (95% aq.MeOH fraction,...

Embodiment 2

[0037] The physicochemical characteristics and the qualitative identification of chemical structure of cerebroside A and cerebroside B that embodiment 1 obtains:

[0038] Physicochemical properties of cerebroside A: [α] 25 D+4.5 (c 0.46, MeOH); Infrared spectrum (KBr) values: 3371, 2921, 2853, 1643, 1536, 1468, and 1081cm-1; m / z 728 (M+H)+;, chemical shift value: C (150MHz, DMSO+2%D2O): 173.91, 135.08, 131.26, 131.05, 123.61, 103.56, 77.00, 76.63(76.62, CH-OD), 73.49(73.46), 71.20(71.17), 70.81(70.71), 70.25( 70.20), 68.86, 61.33 (61.21), 53.04 (53.00, CH-ND-), 39.90, 34.53, 32.23, 31.36, 29.10, 28.98, 28.74, 27.49, 27.38, 24.61, 22.14, 15.83, and 13.95.

[0039] Cerebroside B: The chemical structure of cerebroside B was determined using the same method as that of cerebroside A, and it was found that the difference between cerebroside B and A in structure (including three-dimensional structure) is that B is in the fatty chain There are two more methylene groups than A. Phy...

Embodiment 3

[0041] The animal pharmacology experiments of cerebroside A (JNGZ-A) and cerebroside B (JNGZ-B) described in the present invention are carried out to prove their application in the preparation of medicines for treating brain injury after ischemia.

[0042] The degree of neurological damage due to different forms of cerebral ischemia varies. The main pathological manifestations of middle cerebral artery occlusion are infarction and cerebral edema in the striatum, cerebral cortex, and hippocampus, which have a very high mortality and disability rate. Global cerebral ischemia selectively damages central nervous cells sensitive to hypoxia (such as nerve cells in the CA1 area of ​​the hippocampus), resulting in memory loss. Therefore, the present invention will use the classic middle cerebral artery occlusion (middle cerebral artery occlusion, MCAO) operation to simulate cerebral apoplexy, establish an animal model of global cerebral ischemia with vertebral artery and common caroti...

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Abstract

The invention provides application of a cerebroside compound (cerebroside A and cerebroside B) extracted and prepared from termitomyces in the preparation of medicaments for treating brain injury after cerebral ischemia. Through pharmacological experiments, the invention confirms that the cerebroside compound has significant therapeutic effect on ischemic brain injury, can permeate blood-brain barriers, reduces the area of cerebral infarction caused by cerebral ischemia, alleviates cerebral edema, reduces neuronal cell death, simultaneously promotes the recovery of motor and cognitive function after stroke, and reduces stroke mortality. The invention develops novel medicament use of the cerebroside compound, and provides a novel therapeutic medicament for treating stroke diseases.

Description

technical field [0001] The invention belongs to the field of natural medicinal chemistry. The invention mainly relates to the application of cerebroside compound extracted from Gallus pilosulae in the preparation of medicine for treating post-ischemic brain injury. Background technique [0002] Cerebral ischemic disease is one of the most common clinical diseases, with the characteristics of high morbidity, disability and mortality, which seriously threatens human health. With the gradual aging of the world's population, the incidence of ischemic brain injury is increasing year by year, but so far there is still a lack of effective prevention and treatment measures at home and abroad. The high sensitivity of central nervous cells to hypoxic injury and the lack of regenerative ability are considered to be the main reasons for the sequelae of stroke. Ischemic brain injury mainly includes (1) partial cerebrovascular occlusion (cerebral infarction) and (2) reduction or interru...

Claims

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Application Information

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IPC IPC(8): A61K31/7032A61P9/10C07H15/10C07H1/08
Inventor 陈玲戚建华戚智白银阳孙恺悦张卓高丽娟
Owner NANJING MEDICAL UNIV
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