JPH06199690A - Agent for promoting cerebral metabolism and improving cerebral function - Google Patents

Abstract

PURPOSE:To provide the subject agent containing a substance having superoxide dismutase-like activity and antioxidation activity, a phenolic compound and a sugar compound, effective for activating the cerebral metabolism to improve the memory and cerebral function, free from side action and useful for the treatment of cerebral and neurologic diseases. CONSTITUTION:The objective agent is effective for promoting cerebral metabolism and improving cerebral function and activating the cerebral function of mammals including human to improve the memory and cerebral function and capable of treating or ameliorating cerebral and neurologic diseases such as senile dementia and Parkinson's disease without causing side effect. The agent can be prepared by compounding a substance having superoxide dismutase(SOD)-like activity and/or antioxidation activity (including scavenger function) (e.g. fat-soluble ascorbic acid), a phenolic compound such as guaiacol, phenol, eugenol phenylethanol, a glycoprotein such as asparatin, orientin (lutexin), cisorientin (lutonaletin), isoquercitin and rutin and a sugar compound such as saccharified flavonoid.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a therapeutic agent for promoting brain metabolism and improving brain function.

[0002]

2. Description of the Related Art Aban (Takeda Pharmaceutical Co., Ltd.), L-Dopa and the like have been known as therapeutic agents for promoting cerebral metabolism and improving cerebral function related to cerebral function such as senile dementia and Parkinson's disease.

[0003]

However, although senile dementia improving agents such as Avan and Parkinson's disease improving therapeutic agents such as L-dopa promote brain metabolism in the short term, they are fundamentally associated with cerebral metabolism. It has not improved. As side effects of Avan and L-Dopa, nervous system disorders such as numbness of limbs, dizziness, lightheadedness and headache, and agitation, delirium, restlessness, mental disorders such as insomnia, loose stools, diarrhea,
Disorders of the digestive system such as nausea, loss of appetite, stomachache, and abdominal discomfort are known.

Further, it is difficult to treat senile dementia and Parkinson's disease, and the effect is weak or it takes a long time. Therefore, no one having sufficient effect has been known.

The present invention provides a cerebral metabolism promoter and a therapeutic agent for improving cerebral function, which has few side effects and activates cerebral metabolism in elderly people such as metabolism of neurotransmitters and protein metabolism to improve memory and brain function. The purpose is to

Therefore, as a result of intensive studies to solve the above-mentioned object, the present inventors have found that superoxide dismutase (SOD) -like activity for removing active oxygen in the body and / or antioxidant ability (superoxide radical). (Including a scavenger function of capturing active oxygen) such as, and a phenol compound and glycoprotein,
The present inventors have found that a composition containing a sugar compound such as a glycated flavonoid is effective for promoting cerebral metabolism and treating cerebral function improvement without side effects, and completed the present invention.

[0007] SOD-like activity refers to a substance having an activity (physiological function) similar to the SOD activity for converting superoxide radicals into hydrogen peroxide, and as a substance having SOD-like activity, amino acids and peptides such as copper (II) are used. ) Complex,
Low molecular weight compounds such as manganese complex, fat-soluble ascorbic acid, porphyrin metal complex, polyamine metal complex, etc. are mentioned, and those having antioxidant ability are vitamin C, vitamin E, uric acid, glutathione, β-carotene, calatase, glutathione peroxin. Examples include dase.

Examples of the phenol compound include one selected from the group of guaiacol, phenol, eugenol, phenylethanol and the like, or a mixture thereof.

Examples of sugar compounds such as glycoproteins and glycated flavonoids include one selected from the group consisting of aspalathin, orientin (lutexin), cis-orientin (lutonaretin), isoquercitin, rutin or a mixture thereof.

The present invention also provides phosphorus, iron, calcium,
The effect is more excellent if one or more kinds of minerals such as sodium, potassium, magnesium, copper, zinc, manganese, quercetin, selenium, etc. or a mixture thereof is mixed.

All of the constituents of the present invention are non-toxic and meet the pharmacological criteria. There are no deaths in the acute toxicity test for rats, and no biochemical blood test or histopathological test is performed. No abnormality was found.

The present invention exhibits an excellent effect for the first time by containing a substance having SOD-like activity and / or antioxidant ability, a glycated flavonoid and a phenol compound, and a mineral added as necessary. The composition has a titer of SOD-like activity and / or antioxidant ability of 10,000 to 100,000 units / g, sugar compound 2 to
20 mg / g, 1 to 30 mg / g of a proteinaceous substance, 1 to 20% of a phenol compound, and when adding minerals, it is necessary to contain 10 to 500 mg / g.

The substance having an SOD-like activity and / or antioxidant ability, the sugar component and the phenol compound used in the present invention are mixed alone and directly administered in any form such as solution, powder granules, tablets, emulsions and jellies. Alternatively, it can be mixed with other foods and drinks.

Although the dose varies depending on the kind and degree of the target disease, it is preferably used within the range of 2 to 40 mg / kg / day, and when used as a beverage, 0.1 to
It is preferable to eat and drink the 3.0% solution at 100 ml to 500 ml / day.

[0015]

[Action] Parkinson's disease is a disease caused by a decrease in the amount of dopamine in the brain, and administration of L-dopa has been known so far, but side effects are strong. Although senile dementia is known to be cerebrovascular dementia and Alzheimer's dementia, there are many unclear points regarding the cause of the latter dementia, and therapeutic agents are limited. The composition of the present invention is an SOD having an action of removing active oxygen such as superoxide radicals.
It is considered that the combination of the substance having a similar activity and the component of the sugar compound having an antioxidant action is due to the increase of blood flow due to vasodilation, the promotion of cerebral metabolism and the like.

[0016]

[Effect] The present invention can activate or improve brain metabolism of mammals including humans to improve memory and brain function, and treat or improve cerebral / neurological diseases such as senile dementia and Parkinson's disease without side effects. . In addition, since there are no side effects, it is possible to rapidly improve and treat the brain function by taking it by eating or drinking.

[0017]

【Example】

Production Example Glycated flavonoids 1 to 50 mg / g, protein 2 to 20%, and phenol 3 to 15% as a sugar compound are mixed in a solution state, and a titer of 20,000 units / g as SOD-like activity and / or antioxidant ability is mixed. It was prepared as described above. Distilled water was added to the obtained composition to obtain a solution containing 0.25% of the composition.

Example 1 [Cerebral metabolism promoting experiment] Rats (SD system, male) were administered the solution obtained in the production example instead of the water which they ingest daily, and a solution administration group and rats to which normal water was given. It is divided into (control group), and a guide cannula for microdialysis tube is surgically implanted in the brain of rat, and after the operation, the microdialysis tube is inserted 20 hours or more after the operation, and the neurotransmitter (neurotransmission) in the brain is dialyzed. Substance) was taken out and connected to high performance liquid chromatography (HPLC) to detect the state of cerebral metabolism promotion by an electrochemical detector. The results are shown in Table 1.

[Table 1] From Table 1, it was revealed that in the extract-administered group, dopamine metabolites and the like increased and brain metabolism was promoted.

Example 2 [Experiment for improving dementia symptom] Dry powder (1 g; equivalent to 3 g of dry leaf) obtained by drying the extract obtained in the production example with a freeze dryer was used without any appetite and forgot to take a walk.
It was administered to five elderly dogs who were in a daze, and the improvement in symptoms was examined. The results are shown in Table 2.

[Table 2] After the administration, 4 out of 5 aged dogs recovered their energy and became appetite and wanted to go for a walk.

Example 3 Using the solution obtained in the production example, the active oxygen removing / eliminating action depending on the amount of the solution added in a test tube was examined. The result is shown in FIG. According to FIG. 1, ESR in a test tube
A large signal (waveform) indicates the presence of active oxygen, and it can be seen that the amount of active oxygen decreases as the amount of solution added increases.

Then, the solution obtained in Preparation Example was fed to rats for 8 weeks instead of water to examine the amount of active oxygen in adipose tissue. The result is shown in FIG.

[Brief description of drawings]

FIG. 1 is a diagram showing changes in active oxygen according to the amount of a solution added in a test tube.

FIG. 2 is a view showing changes in ESR signal in abdominal adipose tissue.

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁵ Identification code Internal reference number FI Technical indication location A61K 31/375 7431-4C 31/70 8314-4C (72) Inventor Masatoshi Nakano New Chiryu City, Aichi Prefecture 36-16 Chano, Hayashi-cho

Claims (3)

[Claims] 1. Superoxide dismutase (SO
D) A therapeutic agent for promoting cerebral metabolism / improving cerebral function, which comprises a substance having a similar activity and / or antioxidant ability (including scavenger function), a phenol compound, and a saccharide compound such as glycoprotein and glycated flavonoid. 2. The therapeutic agent for promoting cerebral metabolism / improving cerebral function according to claim 1, wherein the phenol compound is one selected from the group consisting of guaiacol, phenol, eugenol, phenylethanol and the like, or a mixture thereof. . 3. The glyco compound such as glycoprotein and glycated flavonoid is one or a mixture thereof selected from the group consisting of aspalathin, orientin (lutexin), cis-orientin (lutonaretin), isoquercitin, rutin and the like. The therapeutic agent for promoting brain metabolism and improving brain function according to claim 1.