CN102526028A - Application of esculetin - Google Patents
Application of esculetin Download PDFInfo
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- CN102526028A CN102526028A CN2012100453074A CN201210045307A CN102526028A CN 102526028 A CN102526028 A CN 102526028A CN 2012100453074 A CN2012100453074 A CN 2012100453074A CN 201210045307 A CN201210045307 A CN 201210045307A CN 102526028 A CN102526028 A CN 102526028A
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- esculetin
- ischemia
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Abstract
The invention discloses the application of esculetin (Esculetin), the molecular formula of the esculetin is c9h6o4, and chemical structural formula is
; The esculetin is applied to the protection damaged to Cerebral Ischemia-reperfusion in Mice. The esculetin reduces brain infarction area in mouse brain in artery ischemia Reperfusion injury wound model, to experimental mouse injection esculetin is obvious, improves the neuroethology ability of mouse.
Description
Technical field
The present invention relates to a kind of esculetin, specifically, relate to a kind of application of esculetin.
Background technology
Apoplexy is that one group of cerebral tissue is because of acute hemorrhage or ischemia; And produce that paralysis, speech are unfavorable, numb limbs and tense tendons, dizzy, nauseating, vomiting, walking are unstable, stupor even dead ACVD, have sickness rate height, disability rate height, mortality rate is high and relapse rate is high characteristics.In China resident cause of death ordering that Ministry of Public Health was announced in 2008, cerebrovascular has become the primary cause of death.Apoplexy not only causes human health infringement and life to threaten, and returns patient and family thereof and brings heavy medical treatment, economy and burden on society with society.According to statistics, the lethal apoplexy accounts for 27%, and most of apoplexy patient is survived and leave over the deformity that paralysis, aphasia etc. have a strong impact on quality of life.Chinese scholar research shows that the ratio of China's recurrent apoplexy is up to 37%～40%, and 25%～33% apoplexy patient will outbreak once more in 3～5 years.
The target spot of cerebral ischemia nerve injury protection is the emphasis of infrastest and clinical research always.Along with going deep into of research, the pathophysiological process of cerebral ischemia is understood and understanding gradually.Though research worker has been carried out positive intervention to these damage mechanism of cerebrovascular, yet except early stage application organizes type plasminogen activator thromboembolism treatment, does not still have the efficacious therapy means.Therefore the research worker of various countries in the hope of the mortality rate and the disability rate that can reduce stroke patient, and alleviates social burden all actively seeking effective clinical neuroprotective drug.
Esculetin is to have antiinflammatory, antioxidation, improve the extensively Coumarins medicine of pharmacological action such as apoptosis, also can improve the death of the neurocyte that the neurotoxicity of nmda receptor mediation causes.Therefore, esculetin is used for clinical cerebral ischemia treatment and has certain feasibility.
Summary of the invention
To the limitation that is used in human ischemic encephalopathy medicine at present, it is wide in the hope of searching out a kind of treatment time window to the invention discloses the natural low toxicity compounds of a kind of screening, and the medicine esculetin that toxic and side effects is few is to the protection of mouse brain ischemical reperfusion injury.
Esculetin:
[English name] Esculetin
[another name] aesculetin, esculetin, 6,7-dihydroxycoumarin, aesculetin, aesculetin.
[molecular formula] C
9H
6O
4
[structural formula]
[relative molecular weight or atomic weight] 178.15
[fusing point (℃)] 268～270 ℃
[classification] belongs to coumarin kind compound
[character] white or faint yellow acicular crystal, odorless, mildly bitter flavor.
[dissolving situation] is dissolved in diluted alkaline and shows blue-fluorescence, dissolves in hot ethanol and glacial acetic acid, is dissolved in ether and water hardly.
[source] derives from the rutaceae Folium Citri Limoniae, in bark of Oleaceae plant bitter poplar Chinese ash and Semen daturae, Flos Daturae, the Radix Rehmanniae plant etc.
[purposes] itself is a kind of antimicrobial drug, and dysentery bacterium is had inhibitory action, can be used for treating acute bacillary dysentery, and have relieving asthma, phlegm-dispelling functions, also can be used to treat chronic tracheitis, zoopery shows to have significant antiinflammatory action and certain bacteriostatic activity; Also be a kind of anti-asthmatic, the effect of relievining asthma is obvious, and have eliminate the phlegm, the effect of antitussive.
The invention discloses the application of esculetin in the protection of mouse brain ischemical reperfusion injury, it has represented good protective action on mouse brain ischemical reperfusion injury model on the one hand, and this medicine is possessing natural sex and hypotoxic characteristics simultaneously.
Compared with prior art, the present invention has the following advantages:
Said esculetin in mouse brain medium-sized artery ischemical reperfusion injury model, to experimental mouse inject esculetin obvious reduced brain infarction area, improved the neuroethology ability of mice.
Above-mentioned explanation only is the general introduction of technical scheme of the present invention, understands technological means of the present invention in order can more to know, and can implement according to the content of description, below with preferred embodiment of the present invention and conjunction with figs. specify as after.
Description of drawings
Accompanying drawing described herein is used to provide further understanding of the present invention, constitutes the application's a part, and illustrative examples of the present invention and explanation thereof are used to explain the present invention, do not constitute improper qualification of the present invention.In the accompanying drawings:
Fig. 1 is the esculetin molecular structural formula.
Fig. 2 is the esculetin of mouse peritoneal injection 100mg/kg, after ischemia pours into 24 hours after 75 minutes again, carries out the rectangular histogram of neuroethology assessment.
Fig. 3 is the esculetin of mouse peritoneal injection 100mg/kg, after ischemia pours into 24 hours after 75 minutes again, and the rectangular histogram of TTC dyeing back statistical brain infarct size.
Fig. 4 is the esculetin for mouse peritoneal injection different proportion, after ischemia pours into 24 hours after 75 minutes again, and the rectangular histogram of TTC dyeing back statistical brain infarct size.
The specific embodiment
Below with reference to accompanying drawing and combine embodiment, specify the present invention.
One. mouse brain medium-sized artery ischemia model:
1. mice
ICR is male, 23-25g
2. line bolt
6-0 nylon wire, end encapsulate silica gel makes it become the line bolt that diameter is about 0.22mm
3. operating process
Lumbar injection 350mg/kg chloral hydrate is anaesthetized, and external carotid artery is inserted into the middle cerebral artery initial part to internal carotid artery from the mice right side with the line bolt, blocks its blood flow and pulls out Outlet bolt realization perfusion again after 75 minutes.
Two. the neuroethology scoring
Mice after 24 hours, carries out the neuroethology scoring at ischemia-reperfusion:
0 minute: impassivity afunction symptom;
1 minute: receive in the offside forelimb when carrying tail, can not stretch fully;
2 minutes: during walking to sideway swivel;
3 minutes: topple over to offside;
4 minutes: can not walk or go into a coma.
Double-blind method is adopted in scoring, by having neither part nor lot in personnel's completion that experiment is divided into groups.
Three. operating process
To test mouse and be divided into Sham (sham operated rats) at random; Esc (esculetin group); I/R (ischemia/reperfusion group), I/R+Esc group (esculetin+ischemia/reperfusion group) (n=5), at ischemia preceding two hours; Give the Esc of mouse lumbar injection 100mg/kg, through pouring into again behind 75 minutes the ischemia 24 hours.Earlier the mice for survival carries out the neurobehavioral functional assessment, and the anesthesia back is put to death and got brain then, and 37 ℃ of TTC dyeing 30 minutes is taken pictures and calculated the area of cerebral infarction.
Further explain the neuroprotective effect of this medicine in conjunction with figure:
Referring to shown in Figure 1, be esculetin molecular structural formula of the present invention.
Referring to shown in Figure 2, preceding 1 hour Esc of ischemia to mouse peritoneal injection 100mg/kg, ischemia poured into after 75 minutes 24 hours again.Carry out the neuroethology assessment, the neurobehavioral function of I/R+Esc group has had tangible improvement with respect to the I/R group.This improvement has statistical significance.
Referring to shown in Figure 3, preceding 1 hour Esc of ischemia to mouse peritoneal injection 100mg/kg, ischemia poured into after 75 minutes 24 hours again.TTC dyeing back statistical brain infarct size.The brain infarction area of I/R+Esc group obviously reduces with respect to the I/R group.This change has statistical significance.
Referring to shown in Figure 4, preceding 1 hour of ischemia injects the Esc of 100mg/kg, 50mg/kg, 10mg/kg respectively to mouse peritoneal, and ischemia poured into after 75 minutes 24 hours again.TTC dyeing back statistical brain infarct size.The brain infarction area of I/R+Esc (100mg/kg) group and I/R+Esc (50mg/kg) group is all organized less than I/R.The area of the infarct size of I/R+Esc (10mg/kg) group and I/R group is suitable.The neuroprotective that this medicine is described has dose dependent.
The above is merely the preferred embodiments of the present invention, is not limited to the present invention, and for a person skilled in the art, the present invention can have various changes and variation.All within spirit of the present invention and principle, any modification of being done, be equal to replacement, improvement etc., all should be included within protection scope of the present invention.
Claims (1)
1. the application of esculetin, the molecular formula of said esculetin are C
9H
6O
4, its chemical structural formula does
It is characterized in that: said esculetin is applied to the protection to the mouse brain ischemical reperfusion injury.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012100453074A CN102526028A (en) | 2012-02-27 | 2012-02-27 | Application of esculetin |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012100453074A CN102526028A (en) | 2012-02-27 | 2012-02-27 | Application of esculetin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102526028A true CN102526028A (en) | 2012-07-04 |
Family
ID=46334858
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2012100453074A Pending CN102526028A (en) | 2012-02-27 | 2012-02-27 | Application of esculetin |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102526028A (en) |
-
2012
- 2012-02-27 CN CN2012100453074A patent/CN102526028A/en active Pending
Non-Patent Citations (1)
| Title |
|---|
| YEON HEE KONG ET AL: "Neuroprotective and Anti-inflammatory Effects of Phenolic Compounds in Panax ginseng C.A. Meyer", 《JOURNAL OF GINSENG RESEARCH 》 * |
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| PB01 | Publication | ||
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Application publication date: 20120704 |