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Bilobalide with aquaporin regulating effect and new use of derivative thereof in treating encephaledema

A technology of aquaporin and bilobalide, which is applied in the directions of medical preparations containing active ingredients, drug combinations, organic active ingredients, etc.

Inactive Publication Date: 2015-03-11
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current clinical treatment still lacks the treatment for the formation mechanism of cerebral edema

Method used

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  • Bilobalide with aquaporin regulating effect and new use of derivative thereof in treating encephaledema
  • Bilobalide with aquaporin regulating effect and new use of derivative thereof in treating encephaledema
  • Bilobalide with aquaporin regulating effect and new use of derivative thereof in treating encephaledema

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Preparation of experimental animals and bilobalide and its derivatives

[0062] Experimental animals:

[0063] Female Wister rats (250-300 g) were all raised under standard conditions, ie, a temperature of 22° C. and a humidity of 70%, and the rats had free access to food and water.

[0064] Preparation and identification of bilobalide

[0065] 10kg of green dried ginkgo leaf coarse powder was extracted by reflux with 50% ethanol for 2 hours to obtain an extract. Concentrate or recover the solvent and filter, pass through macroporous resin column chromatography, elute with water and alcohol, concentrate and filter to obtain the filtrate. The filtrate was extracted with an organic solvent, and the organic layer was concentrated and crystallized on standing to obtain 80 g of total lactones. The total lactones were separated by silica gel column chromatography to obtain 20 g of bilobalide.

[0066] The purity of bilobalide is greater than 98% (HPLC, chromatographic col...

Embodiment 2

[0072] Establishment of ischemic injury model in rats with permanent middle artery occlusion (pMCAO)

[0073] Female Wister rats (250-300 g) were anesthetized with chloral hydrate at a concentration of 350 mg / kg. During the experiment, a heating lamp was used to maintain the body temperature of the rats at 37±0.5°C. Through an incision in the middle of the neck, the left common carotid artery (CCA), internal carotid artery (ICA), and external carotid artery (ECA) were isolated. The CCA and ECA were ligated with No. 4 surgical silk suture, the ICA was clamped with microvascular clips, and an incision was made at the distal end. Dip a section of 0.22mm nylon thread coated with polylysine into paraffin, and insert it into the ICA along the incision of the CCA. After removing the microvascular clips, the silk thread was inserted forward quickly to a position 20 mm away from the bifurcation of the ECA and ICA to block the middle artery. The experimental animals were required to ...

Embodiment 3

[0075] Changes of Water Content in Brain Tissue After Embolization

[0076] Determine the water content of the brain tissue 8h, 16h or 24h after measuring pMCAO based on weight, for this purpose, dry the surface of both hemispheres of the brain, transfer to aluminum foil, weigh (this is the wet weight), and then dry overnight in an oven at 105°C . The dried tissue is weighed again (this is the dry weight), and the water content of the brain tissue can be determined by the formula: [(wet weight-dry weight) / wet weight]×100.

[0077] The experimental results are attached figure 2 .

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PUM

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Abstract

The invention belongs to the technical field of medicament, and discloses a bilobalide and a use of derivative thereof in treating encephaledema, especially encephaledema caused by cerebral ischemia. Research results show that the bilobalide can reduce the brain tissue water content and the cerebral infarction area of a permanent medium-sized arterial occlusion model animal. The mechanism of the bilobalide for weakening the formation of encephaledema is to lower the mRNA transcription level of aquaporin 1, 4 and 9 and the expression level of protein in different stages. The bilobalide can be combined with a pharmaceutically acceptable carrier to be prepared into a clinically acceptable injection, a transdermal preparation or an oral administration preparation for treating the encephaledema.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to the application of bilobalide and its derivatives in the treatment of cerebral edema, especially cerebral edema caused by cerebral ischemia. Background technique [0002] Bilobalide is an active ingredient of terpene lactones extracted from Ginkgo biloba. It is an important active ingredient in traditional Ginkgo biloba extract and has strong pharmacological activity. Bilobalide has played a neuroprotective role in hypoxic and ischemic damage to the animal brain (Chandrasekaran, K.; Mehrabian, Z.; Spinnewyn, B.; Drieu, K.; Fiskum, G. Brain research 2001, 922, 282-292.). Can make mitochondria maintain their respiration under ischemic conditions, thereby preventing ischemia-induced reduction in respiration in the liver and brain (Janssens, D.; Delaive, E.; Remade, J.; Michiels, C. Fundamental & Clinical Pharmacology 2000, 14, 193-201.); protective against NO-induced neurotoxicity ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/365A61P9/10A61P7/10
Inventor 游松秦斌秦海明贾娴陈奕南翟兴雯徐慰倬
Owner SHENYANG PHARMA UNIVERSITY
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