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Application of pinocembrin raceme in preparation of medicals for cerebral apoplexy

A technology of raceme and pinogenin, which is applied in the field of preparation of the prevention and treatment of stroke drugs by the raceme of pinogenin, can solve the problems of lack of effective treatment of stroke and application restrictions, and achieve the protection of nerve cell damage , improve behavioral changes, and improve the effect of cerebral edema

Active Publication Date: 2010-06-23
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0029] From the above analysis, it can be known that there is still no effective drug for the treatment of stroke except tPA in clinical practice, and even tPA is greatly limited in its application because the treatment time window is only 3 hours

Method used

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  • Application of pinocembrin raceme in preparation of medicals for cerebral apoplexy
  • Application of pinocembrin raceme in preparation of medicals for cerebral apoplexy
  • Application of pinocembrin raceme in preparation of medicals for cerebral apoplexy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Example 1. Preventive and therapeutic effects on apoplexy in stroke-prone spontaneously hypertensive rats (SHRSP)

[0061] 1. Experimental drugs: pinocin racemate for injection, (R)-pinocin for injection and (S)-pinocin for injection, provided by the New Drug Development Office of the Institute of Materia Medica, Chinese Academy of Medical Sciences, (batch number 20050601, Content 2.36%), adopt the method disclosed in 200810084682.3 that is cyclodextrin or cyclodextrin derivatives inclusion racemization and isomer pinazin to prepare, and dissolve in normal saline when used; positive drug nimodipine injection is purchased from Bayer company (Germany).

[0062] 2. Experimental animals and groups:

[0063] Test animals: 110 6-week-old SHRSP rats and 10 normal Wistar rats.

[0064] Test grouping: be divided into normal group namely Wistar rat group, SHRSP rat is divided into model group, nimodipine group, pinocin racemate low, middle and high dose groups at random (dose i...

Embodiment 2

[0123] Example 2. Effect on acute ischemic stroke caused by middle cerebral artery embolism

[0124] Test substance: pinoquinone for injection, provided by the New Drug Development Office of the Institute of Materia Medica, Chinese Academy of Medical Sciences,

[0125] (batch number 20050601, content 2.36%), it is prepared by adopting the method disclosed in 200810084682.3 that cyclodextrin or cyclodextrin derivatives include pinocin racemate, and is dissolved in normal saline when used; the positive drug nimodipine injection is purchased at Bayer AG (Germany).

[0126] Experimental animals: 100 male SD rats, weighing 250-280 grams, were purchased from the Institute of Experimental Animals, Chinese Academy of Medical Sciences. The rats were randomly divided into: sham operation group, model group, pinecone administration group, and nimodipine administration group (3mg / kg).

[0127] Experimental model: using middle cerebral artery occlusion (MCAO) to prepare acute ischemic st...

Embodiment 3

[0198] Embodiment three, acute toxicity study result and evaluation

[0199] The test results show that the LD50 value of SD rats' single intravenous injection of pinecine racemate toxic reaction is 490.9 (367.6-746.7) mg / kg, and the LD50 value of (S)-pinecin toxic reaction is 375.3 (271.2 -538.5) mg / kg, the LD50 value of (R)-pinine toxicity is 347.8 (257.4-466.3) mg / kg. It can be seen from the above that the racemic form of pinocin has a relatively large range of safe drug use. All the drugs had no obvious effect on the body weight of the animals, and the main toxic manifestations were quadriplegia, mild congestion of the liver and lungs.

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Abstract

The invention relates to the medical field, discloses applications of racemes of pinocembrin, racemes of pinocembrin salt, racemes of pinocembrin precursors or racemes of pinocembrin hydrate in preparation of medicals for preventing and treating cerebral apoplexy, and further discloses the application of racemes of pinocembrin in prevention and treatment of acute ischemic stroke.

Description

technical field [0001] The present invention relates to the use of pinocin racemate in the preparation of medicines for preventing and treating cerebral apoplexy. Background technique [0002] (S)-pinenine, chemical name (S)-2,3-dihydro-5,7-dihydroxy-2-phenyl-4H-1-benzopyran-4-one (English chemical name is : (S)2,3-dihydro-5,7-dihydroxy-2-benyl-4H-1-benzopyran-4-one), is a water-insoluble dihydroflavonoid compound, see formula II, is from A natural compound extracted from propolis. The compound is also found in extracts of many plants, including Swiss five-needle pine, eucalyptus leaves, and gum arabic. [0003] Since the 1980s, studies at home and abroad have discovered a variety of pharmacological activities of (S)-pinone, including antibacterial, antiviral, antioxidative, and anti-inflammatory effects. The Chinese Academy of Medical Sciences first discovered that (S)-pinoquinone has the effect of inhibiting vasoconstriction caused by various factors, and also has a pro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P9/10
Inventor 杜冠华王金戌吴松史颖高梅李银贵戚燕申东民光红梅刘海丽刘睿冯小龙
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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