CN1323583A - Medicinal use of beta-ecdysterone - Google Patents
Medicinal use of beta-ecdysterone Download PDFInfo
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- CN1323583A CN1323583A CN 01113995 CN01113995A CN1323583A CN 1323583 A CN1323583 A CN 1323583A CN 01113995 CN01113995 CN 01113995 CN 01113995 A CN01113995 A CN 01113995A CN 1323583 A CN1323583 A CN 1323583A
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- ecdysterone
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Abstract
The invention relates to a medical usage of a B-ecdysis sterone. It is expected to be as a new medicine to prevent and cure senile dementia, improve brain functions, and treat brain disease and anti-senescence. B-ecdysis sterone can be used to prepare the medicine to improve symptom of brain's ischemia and blood vessel spasm, to treat brain disease caused by ischemia. The medicine used to treat brain's ischemia diseases included such medicines that provides effects of improving brain functions, curing senile dementia and balancing normal physiological functions. This invention provides a new way to develop and utilize natural medical resources.
Description
The present invention relates to medical technical field, exactly is a kind of medical usage of β-ecdysterone.
" β-ecdysterone " is the effective ingredient monomer of separation and Extraction from Chinese medicine (Radix Rhapontici, Radix Achyranthis Bidentatae, Radix Cyanotis vagae etc.).Report is arranged during both at home and abroad to the pharmacological action of β-ecdysterone, no matter β-ecdysterone still is that all the stimulation in rats liver is proteic synthetic rapidly in vitro tests in vivo, the aggregate velocity of regulating mRNA, promote nucleic acid and proteinic synthetic, promote lipid metabolism, improve atherosclerosis, hyperglycemia influences the metabolism of cholinergic nerve of centrum mediator and improves immunoregulation effect.
The objective of the invention is to clearly propose the new medical usage of β-ecdysterone, β-ecdysterone can significantly improve symptoms of cerebral ischemia, improves cerebral vasospasm, improves brain function, strengthen ability of learning and memory, free radical resisting damage, the defying age of body, the learning memory injury and the early stage senile dementia disease people that improve due to the disordered brain function are improved effects such as learning and memory.The present invention makes β-ecdysterone can expect to become new control senile dementia, improves brain function, treats cerebral ischemia diseases and antidotal newtype drug, and provides new approach for developing natural pharmaceutical resources.
The present invention finds that through a large amount of screening active ingredients on the basis of ancient medical book record and modern study report, we study with the pharmacological action that improves effects such as disordered brain function centaurea monanthos Georgi treatment cerebrovascular.Simultaneously systematic study has been carried out in the pharmacological action of its chemical constituent and main active (β-ecdysterone).Result of study show β-ecdysterone to the control senile dementia, improve brain function, treatment cerebral ischemia diseases and antidotal effect is very remarkable.Concrete result of study is as follows:
1, the pharmacological effect effect of centaurea monanthos Georgi extract
At dosage is that the ethanol extraction of 1.56-6.25g/kg (amounting to the crude drug amount) has remarkable anti-cerebral anoxia and cerebral ischemia effect, reduce the content of brain lipid peroxide and lipofuscin, obstacle, spatial discrimination sexual disorders are consolidated in the memory that memory acquisition disturbance that antagonism scopolamine, the eleventh of the twelve Earthly Branches barbital sodium cause and cyclohexane imines, sodium nitrite are caused, and improve the initiatively formation rate of avoidance conditioned reflex of rat.Antiplatelet aggregative activity.
2, the pharmacological effect effect of β-ecdysterone
1) evidence, β-ecdysterone can significantly improve scopolamine in inverted U amount effect curve mode in the 1.8-14.4mg/kg dosage range, the mouse memory acquired disturbance that diazepam causes, the mouse memory that the ring acetimide causes are consolidated mouse memory bad and that ethanol causes and are reproduced disappearance.And this amnemonic improvement of proof can be the blocking-up of noncompetitive glutamate receptor antagonists ketamine.
2) the chmice acute anoxia that β-ecdysterone can resist significantly that normal pressure is airtight, several different methods such as broken end, sodium nitrite, potassium cyanide and bilateral ligation cause, ischemia and because the generation of the cerebral tissue lipid peroxide that cerebral anoxia causes;
3) β-ecdysterone can obviously suppress cerebral edema and brain that the mouse brain ischemia causes and knits calcium content;
4) β-ecdysterone has significant antiplatelet aggregation;
5) β-ecdysterone has remarkable increase dog cerebral blood flow, promotes effects such as cerebrovascular regeneration, is expected to develop to become to have the newtype drug for the treatment of the cerebral vasospasm disease.
6) experiment in vivo and vitro shows: β-ecdysterone has the effect of remarkable removing free radical, as effects such as lipofuscin generations in the inhibition body, points out it to have anti-aging effects;
7) β-ecdysterone can significantly improve the ability of learning and memory of normal mouse.
Advantage of the present invention is: the present invention finds that β-ecdysterone has remarkable increase dog cerebral blood flow, promote cerebrovascular regeneration, effects such as significant antiplatelet aggregation make it be expected to develop and become the newtype drug with treatment cerebral vasospasm disease, and this is one of characteristic of the present invention.Recent research proves that also β-ecdysterone has the effect of remarkable removing free radical, and this is two of a characteristic of the present invention.Research proves that also β-ecdysterone also has very strong nootropic effect, antioxidation, obviously suppresses cerebral edema and brain that the mouse brain ischemia causes and knit effects such as calcium content; help protecting body; defying age is is especially prevented and treated the effect of alzheimer disease disease, and this is three of a characteristic of the present invention.In addition, this product toxicity is lower, in the drug efficacy study process, does not see the toxic reaction that produces animal, is suitable for medical usage, and this is four of a characteristic of the present invention.
Feature of the present invention is: the β-ecdysterone of structure shown in formula I improves symptoms of cerebral ischemia, improves cerebral vasospasm as preparation, the application in the medicine of treatment cerebral ischemia diseases.
Formula I
The medicine of described cerebral ischemia diseases comprises the medicine that improves brain function and treatment senile dementia disease and the effect of centre of equilibrium nervous system normal physiological function.The medicine of described cerebral ischemia diseases also comprises the medicine of anticoagulant effect.
The present invention is described in further detail below in conjunction with embodiment.Following examples are represented practicality of the present invention, and the present invention is not limited.
Embodiment 1:
β-ecdysterone (ECR) is to the influence of normal learning ability of mice
???Drug(mg/Kg) | Errors number | The number of animals of makeing mistakes (%) |
????Control ????ECR(1.8) ????ECR(3.6) ????ECR(7.2) ????ECR(14.4) | ?????1.2±0.8 ?????2.1±1.0 ?????1.3±0.7 ?????0.3±0.5 **?????0.5±0.5 * | ???????80 ???????100 ???????90 ???????30 ???????50 |
n=10;
*p<0.05,
**p<0.01
Embodiment 2: β-ecdysterone (ECR) is to the influence of scopolamine (SCO) induced mice learning disorder
?????Drug(mg/Kg) | Errors number | The number of animals of makeing mistakes (%) |
???????Control ???????SCO(3.0) ???ECR(1.8)+SCO(3.0) ???ECR(3.6)+SCO(3.0) ???ECR(7.2)+SCO(3.0) ???ECR(14.4)+SCO(3.0) | ??????0.1±0.3 ??????1.5±0.9 ΔΔ???????????1.4±1.2 ???????0.3±0.5 **??????1.3±0.8 ??????0.8±0.6 | ???????10 ???????90 ΔΔ?????????????70 ???????30 *???????90 ???????70 |
n=10;
ΔΔp<0.01?compared?with?control?group;
*p<0.05,
**p<0.01?compared?with?SCO?group
Embodiment 3: β-ecdysterone (ECR) is to the anoxybiotic influence of chmice acute
1) the airtight anoxia in mice that causes of normal pressure
???Drug(mg/Kg) | Number of animals | Time-to-live (min) |
Control ECR (3.6) ECR (7.2) ECR (14.4) nimodipine (250) | ?????11 ?????10 ?????10 ?????10 ?????10 | ??????13.6±1.6 ??????14.8±2.2 ??????14.6±1.6 ?????15.8±0.9 **?????23.3±2.5 ** |
**p<0.01?compared?with?Control?group
2) sodium nitrite causes anoxia in mice
???????Drug(mg/Kg) | Number of animals | Time-to-live (min) |
???????NaN0 2(800) ???ECR(7.2)+NaNO 2(800) ???ECR(14.4)+NaNO 2(800) nimodipine (250)+NaNO 2(800) | ???11 ???10 ???10 ???10 | ??????8.2±0.9 ??????9.4±1.6 ?????9.8±1.2 **?????9.6±1.2 ** |
**P<0.01?compared?with?NaNO
2(800)group
Embodiment 4: β-ecdysterone (ECR) is to the influence of chmice acute ischemia
??Drug(mg/Kg) | Number of animals | Time-to-live (min) | Survival rate (%) |
Control ECR (7.2) ECR (14.4) nimodipine (250) | ???10 ???10 ???10 ???10 | ?????298.9±186.3 ?????295.6±152.1 ?????489.3±156.8 *?????519.1±161.2 * | ?????10 ?????10 ?????60 *?????60 * |
*p<0.05?compared?with?NaNO
2(800)group
β-ecdysterone can obviously prolong the time-to-live that the bilateral carotid arteries ligation causes the cerebral ischemia mice, improves survival rate.Further studies show that, can suppress the variation of body temperature decline, cerebral edema and brain calcium content that cerebral ischemia causes.
Embodiment 5: β-ecdysterone (ECR) is organized the influence of lipid peroxide content to the cerebral anoxia mouse brain.
??????Drug(mg/Kg) | Number of animals | Lipid peroxide content (nmol/g wt.) |
???????Control ???????KCN(4.5) ???ECR(7.2)+KCN(4.5) ???ECR(14.4)+KCN(4.5) | ?????10 ?????10 ??????9 ??????9 | ??????140.74±14.16 ??????256.36±45.39 ΔΔΔ???????????205.83±46.13 *?????163.80±55.72 *** |
ΔΔΔP<0.001?compared?with?control?group;
*p<0.01,
***p<0.001?compared?with?KCN?group
Embodiment 6: β-ecdysterone (ECR) is to the effect of platelet aggregation
???Drug | Dosage (μ g/ μ l) | Sample number (propping up) | Platelet aggregation rate (%) | Platelet aggregation inhibition rate (%) |
Normal saline piracetam ECR ECR ECR | ????????-- ???????160 ????????32 ????????16 ?????????8 | ?????10 ?????10 ?????10 ?????10 ?????10 | ???????43.6±4.9 ??????30.7±2.3 ***??????26.1±6.7 ***??????29.6±8.4 ***??????37.0±4.6 ** | ????????29.59 ????????40.14 ????????31.19 ????????15.14 |
**p<0.01,
***p<0.001?compared?with?control?group
Embodiment 7: β-ecdysterone (ECR) is to the effect of dog cerebral blood flow
Group | Drug dose (mg/Kg) | Before the administration (ml/min) | After the administration (ml/min) | |||
??????40min | ???????70min | ???????100min | ?????160min | |||
Normal saline nimodipine ECR ECR | ???-- ???100 ???5.0 ???10.0 | ??38.3±4.4 ??39.3±10.8 ??44.3±10.6 ??38.5±10.7 | ????39.0±4.7 ????54.5±8.8 ????63.8±18.2 *???64.3±12.4 ** | ?????43.3±3.4 ????59.8±6.7 ***????67.0±14.8 *????79.8±21.3 * | ??????40.5±6.1 ??????45.3±6.9 ???54.8±5.65 *???92.8±11.6 ** | ????41.3±3.2 ????50.3±12.1 ????57.0±19.6 ????82.5±31.8 * |
*p<0.05,
**p<0.01,
***p<0.001?compared?with?H
2O?group
Claims (3)
2, the medical usage of a kind of β-ecdysterone according to claim 1 is characterized in that: the medicine of cerebral ischemia diseases comprises the medicine that improves brain function and treatment senile dementia disease and the effect of centre of equilibrium nervous system normal physiological function.
3, the medical usage of a kind of β-ecdysterone according to claim 1 is characterized in that: the medicine of described cerebral ischemia diseases also comprises the medicine of anticoagulant effect.
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CN 01113995 CN1323583A (en) | 2001-05-28 | 2001-05-28 | Medicinal use of beta-ecdysterone |
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CN 01113995 CN1323583A (en) | 2001-05-28 | 2001-05-28 | Medicinal use of beta-ecdysterone |
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Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104093409A (en) * | 2011-12-13 | 2014-10-08 | 比奥菲蒂斯研究所简单股份有限公司 | Phytoecdysones for use in improving the muscle quality of obese and/or sarcopenic mammals |
WO2020143333A1 (en) * | 2019-01-10 | 2020-07-16 | 河南中医药大学 | Use of taraxasterol for preparing drug for preventing and treating alzheimer's disease |
US11464876B2 (en) | 2016-08-31 | 2022-10-11 | Biocytogen Pharmaceuticals (Beijing) Co., Ltd. | Genetically modified mouse comprising a chimeric TIGIT |
-
2001
- 2001-05-28 CN CN 01113995 patent/CN1323583A/en active Pending
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104093409A (en) * | 2011-12-13 | 2014-10-08 | 比奥菲蒂斯研究所简单股份有限公司 | Phytoecdysones for use in improving the muscle quality of obese and/or sarcopenic mammals |
CN104093409B (en) * | 2011-12-13 | 2017-06-30 | 比奥菲蒂斯公司 | Plant ecdysone for improving the meat quality of fat and/or amyotrophic mammal |
US11464876B2 (en) | 2016-08-31 | 2022-10-11 | Biocytogen Pharmaceuticals (Beijing) Co., Ltd. | Genetically modified mouse comprising a chimeric TIGIT |
US11534502B2 (en) | 2016-08-31 | 2022-12-27 | Biocytogen Pharmaceuticals (Beijing) Co., Ltd. | Genetically modified non-human animal with human or chimeric TIGIT |
WO2020143333A1 (en) * | 2019-01-10 | 2020-07-16 | 河南中医药大学 | Use of taraxasterol for preparing drug for preventing and treating alzheimer's disease |
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