Compositions Containing Cistanche Y.c.ma Extract Shown To Enhance Axonal Growth Activity And Neurotrophic Effects Ⅱ
Jul 28, 2022
Cistanche Y.C.MA belongs to the family Orobanchaceae and is distributed in alkaline soil, dry riverbed and sandy land. It is used as a tonic Chinese medicinal material and has been reported to contain some enzymes, fatty lipids, trace alkaloids and crystalline neutral substances (Chung B.S. and Shin M.K.; Hyangyak Daesacheon, Youngrimsa., 888-889, 1998).
It reports that it consist of cistanoside, cistanoside F, tubuloside A, tubuloside B, 2'-acetylergosteroside, echinoside, 3 '-α-rhamnopyranoside, isoergosteroside, ergosteroside, syringalide A (Wang YM et al., Acta Pharmaceutics, 35(11), 839-842, 2000) components.
However, the therapeutic effect of Cistanche Y.C.MA on cerebral diseases is not reported or disclosed in any of the above-cited documents, and the contents disclosed in the above-mentioned documents are hereby incorporated by reference.
The effects of Cistanche Y.C.MA on the growth and differentiation of neurons were studied through some biochemical experiments, and it was determined that crude extracts and soluble extracts of non-polar solvents were in inhibiting neuronal apoptosis, the main cause of degenerative brain diseases, and Whether it plays an important role in promoting NGF induction, the inventors have conducted some molecular biological experiments in depth and made microscopic observations through cell line culture to confirm that crude extracts and soluble extracts of non-polar solvents inhibit neuronal apoptosis, promote the generation of NGFs and have neuron cell protection activity, and finally complete the present invention.
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These and other objects of the present invention will be apparent from the detailed disclosure of the invention provided hereinafter.
SUMMARY OF THE INVENTION
The present invention provides a pharmaceutical composition containing an effective amount of a crude extract of Cistanche Y.C.MA as an active ingredient for treating and preventing degenerative brain diseases by protecting neuronal cells.
The present invention also provides the use of the above extract in the preparation of a pharmaceutical composition for treating and preventing degenerative brain diseases in mammals or humans by protecting neuronal cells.
The present invention also provides a healthy food or food additive containing the above extract for preventing or alleviating degenerative brain diseases by protecting neuronal cells.
DISCLOSURE OF THE INVENTION
Therefore, the object of the present invention is to provide a crude extract, polar solvent or non-polar solvent soluble extract containing Cistanche deserticola Y.C.MA as an active ingredient for the treatment and prevention of degenerative brain diseases by protecting neuronal cells pharmaceutical composition of the substance.
The above-mentioned crude extracts include extracts prepared by extracting plant materials with water, lower alcohols such as methanol, ethanol, preferably methanol, etc., or a mixture thereof.
The above polar solvent-soluble extract can be prepared by extracting the above crude extract with a polar solvent, such as water, a lower alcohol such as methanol, ethanol, preferably butanol, etc., or a mixture thereof.
The above non-polar solvent soluble extract can be prepared by extracting the above crude extract with a non-polar solvent such as hexane, ethyl acetate or dichloromethane, preferably ethyl acetate.
The object of the present invention is to provide crude extract, polar solvent-soluble or non-polar solvent-soluble extract of Cistanche deserticola Y.C.MA in preparation for the treatment and prevention of degenerative brain diseases by protecting neuronal cells in humans or mammals use of therapeutic agents.
The object of the present invention is to provide a method for treating or preventing degenerative brain diseases by protecting neuronal cells in mammals, comprising applying an effective amount of a crude extract of Cistanche deserticola Y.C.MA, a polar solvent soluble or Non-polar solvent soluble extracts and pharmaceutically acceptable carriers thereof.
Another object of the present invention is to provide a health food or food additive containing the above extract and nutritionally acceptable additives for preventing and improving degenerative brain diseases by protecting neuronal cells.
The above-mentioned degenerative brain diseases include stroke, Alzheimer's disease (AD), Parkinson's disease (PD), senile dementia, and the like.
The above crude extract can be extracted from any Cistanche plant such as Cistanche Tubulosa, C. deserticola, C. ambigua.
The pharmaceutical composition of the present invention contains about 0.01-50% by weight of the above-mentioned extract based on the total weight of the composition.
The health food of the present invention contains about 0.01-80% by weight, preferably 1-50% by weight of the above-mentioned extract based on the total weight of the composition.
The above-mentioned health food can be added to health food, health drink, etc., and can be used in the form of powder, granule, tablet, chewable tablet, capsule, drink and the like.
An inventive extract isolated from Cistanche tubulosa Y.C.MA can be prepared according to the following preferred embodiments.
The present invention is described in detail below.
An inventive extract of Cistanche Y.C.MA can be prepared according to the following method in detail, and the crude extract of the invention of Cistanche Y.C.MA is prepared as follows: drying, shearing, and crushing Cistanche Y.C.MA, and 5-25 times, preferably About 10 times the volume of distilled water, lower alcohols such as methanol, ethanol, butanol, etc. or their mixtures, preferably methanol phase mixing; continuous extraction by hot water, cold water, reflux extraction or ultrasonic extraction 1-5 times, preferably 2-3 times of extraction method, the solution is treated with hot water with a temperature range of 20-100°C, preferably 60-100°C for 1-24h; the residue is filtered to obtain a supernatant, at a temperature range of 20-100°C, preferably 50-70°C Concentrated with a rotary evaporator at ℃, and then vacuum freeze-drying, hot-air drying or spray-drying to obtain dry Cistanche deserticola Y.C.MA crude extract powder, which can be dissolved in water, lower alcohol or their mixture.
In addition, the polar solvent-soluble and non-polar solvent-soluble extracts of the present invention can be prepared by the following methods; the crude extract prepared by the above method is suspended in water, and then mixed 1-100 times, preferably 1-5 times Volume of non-polar solvents such as ethyl acetate, chloroform, hexane, etc. are mixed; the non-polar solvent-soluble layer is collected to obtain the non-polar solvent-soluble extract of the present invention, and the residual polar solvent-soluble layer is collected to The polar solvent-soluble extract of the present invention is obtained, which is soluble in water, lower alcohol or a mixture thereof. The above method can also be modified or filtered through other steps by conventional methods well known in the art such as those disclosed in the literature (Harbone J.B. Phytochemical Methods: A Guide to Modern Plant Analysis Methods, 3rd Edition, 6-7, 1998). Or separate more efficient fractions or compounds.
The effect of Cistanche deserticola Y.C.MA on neuronal growth and differentiation was investigated by some biochemical experiments, and microscopic observation by cell line culture confirmed that crude extracts and non-polar soluble extracts inhibit the main neuronal cells of degenerative brain diseases and Whether it plays an important role in apoptosis and in promoting NGF induction, it was determined that crude extracts, polar solvent-soluble and non-polar solvent-soluble extracts inhibit neuronal apoptosis, promote NFs generation and have neuronal cytoprotective activity .
According to another aspect of the present invention, there is provided a crude extract, polar solvent-soluble or non-polar solvent of Cistanche deserticola Y.C.MA prepared by the above method for treating and preventing degenerative brain diseases by protecting neuronal cells Pharmaceutical compositions with soluble extracts as active ingredients.
Another aspect of the present invention provides a method of treatment and prevention comprising applying a pharmaceutical composition containing the extract prepared by the above method to the degenerated brain of mammals including humans.
The inventive composition for treating and preventing degenerative brain diseases by protecting neuronal cells may contain 0.01-50% by weight of the above-mentioned extract based on the total weight of the composition.
The compositions of the invention may also contain conventional carriers, adjuvants or diluents according to methods of application well known in the art. According to the method of use and application, the carrier is preferably used as a suitable substance, but is not limited thereto. Suitable diluents are listed in Remington's Pharmaceutical Sciences written text (Mack Publishing Company, Easton PA).
In the following, the following formulation methods and excipients are for illustration only and do not limit the invention in any way.
The composition of the present invention may be provided as a pharmaceutical composition containing a pharmaceutically acceptable carrier, adjuvant or diluent such as lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol halitol, maltitol, starch, gum arabic, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methylcellulose, polyvinylpyrrolidone, water, hydroxymethylbenzoate, hydroxypropyl benzoate, talc, magnesium stearate and mineral oil. Formulations may also include fillers, anticoagulants, lubricants, wetting agents, flavoring agents, emulsifiers, preservatives, and the like. The compositions of the present invention may be formulated to provide rapid, sustained or delayed release of the active ingredient after application to a patient by any method well known in the art.
For example, the compositions of the present invention may be dissolved in oils, propylene glycol or other solvents commonly used in the preparation of injectables. Suitable carriers include, but are not limited to, physiological saline, polyethylene glycol, ethanol, vegetable oils, isopropyl myristate, and the like. For topical application, the extracts of the present invention can be formulated into ointments and creams.
The pharmaceutical formulation containing the composition may be prepared in any form, such as oral dosage form (powder, tablet, capsule, softgel, potion, syrup, pill, powder, sachet, granule), or topical formulation (cream, ointment, lotion, gel, patch, ointment, spray solution, aerosol, etc.), or injection (solution, suspension, emulsion).
The compositions of the present invention in the form of pharmaceutical preparations can be used in the form of their pharmaceutically acceptable salts, either alone or in suitable combinations and in combination with other pharmaceutically active compounds.
Appropriate doses of the inventive extract or composition vary depending on the subject's pathological state and body weight, severity, pharmaceutical form, route of application and period, and can be selected by those skilled in the art. However, in order to obtain the desired effect, it is generally recommended that the inventive extract or composition be applied in an amount in the range of 10 g/kg, preferably 1-3 g/kg body weight/day. The dose is applied once or in divided doses per day. As for the composition, the inventive extract should be contained in an amount of 0.01-50% by weight, preferably 0.5-40% by weight, based on the total weight of the composition.
The pharmaceutical composition of the present invention can be applied to subject animals such as mammals (rats, mice, livestock or humans) through various routes. All modes of use are contemplated, eg by oral, rectal application or by intravenous, intramuscular, subcutaneous, intradermal, intramembranous, epidural or intracerebroventricular injection.
In addition, the present invention provides a health food and beverage composition for preventing and improving degenerative brain diseases by protecting neuronal cells, adding 0.01-80% by weight of the above extract, 0.001-5% by weight of amino acids, 0.001-2% by weight of amino acids of vitamins, 0.001-20% by weight of sugar, 0.001-10% by weight of organic acids, appropriate weights of sweeteners and flavors.
The above-mentioned Cistanche Y.C.MA extract can be added to foods and beverages for preventing and improving degenerative brain diseases by protecting neuronal cells.
In order to develop a health food, examples of the supplementable food containing the above-mentioned extract of the present invention are various foods, beverages, chewing gums, vitamin complexes, health-improving foods, etc., which can be used as powders, granules, tablets, chewable tablets, capsules or Use for beverages, etc.
In addition, the extract of the present invention can be used to prevent and improve allergic diseases or non-allergic inflammatory diseases by adding to infant food, such as improved milk powder, improved growth period milk powder, and improved growth period food.
The above-mentioned composition can be added to food, additive or beverage, wherein the content of the above-mentioned extract in food or beverage is generally about 0.1-80w/w% of the total weight of food in the health food composition, preferably 1-50w/w/ w%, and the proportion in 100ml health drink composition is 1-30g, preferably 3-10g.
As long as the health drink composition of the present invention contains the above-mentioned extract in a certain proportion as the main component, other liquid components are not particularly limited, wherein the other components may be various deodorants or natural carbohydrates such as conventional beverages. The aforementioned natural carbohydrates are monosaccharides such as glucose, fructose, etc.; disaccharides such as maltose, sucrose, etc.; ordinary sugars such as dextrin, cyclodextrin, etc.; and sugar alcohols such as xylitol, erythritol, and the like. As other deodorants in addition to the aforementioned, natural deodorants such as taumatin, stevia extracts such as levaudioside A, licorice saponin, etc., and synthetic deodorants such as saccharin, partyyl phenylalanine methyl ester, etc. are all Applicable. The content of the above-mentioned natural carbohydrates generally ranges from about 1-20 g, preferably 5-12 g, in 100 ml of the beverage composition.
Other ingredients than the aforementioned ingredients are various nutrients, vitamins, minerals or electrolytes, synthetic flavoring agents, colorants and improvers in the case of cream chocolate, etc., pectic acid and its salts, alginic acid and its salts , organic acids, binders for protective colloids, pH regulators, stabilizers, preservatives, glycerol, ethanol, carbonizing agents used in carbonated beverages, etc. In addition to the aforementioned other ingredients may be fruit juices, fruit juice beverages and vegetable beverages used to prepare natural fruit juices, wherein the ingredients may be used alone or in combination. The proportions of these ingredients are not very critical, but generally range from about 0-20% w/w% per 100 w/w% of the composition. Examples of the supplementable foods in which the aforementioned extracts are contained are various foods, beverages, chewing gums, vitamin complexes, health-improving foods, and the like.
The inventive composition may also contain one or more organic acids, such as citric acid, fumaric acid, adipic acid, lactic acid, malic acid; phosphates, such as phosphate, sodium phosphate, potassium phosphate, acid pyrophosphate, Polyphosphates; natural antioxidants such as polyphenols, catechol, alpha-tocopherol, rosemary extract, vitamin C, green tea extract, licorice root extract, chitosan, tannins, phytic acid Wait.
The above-mentioned extract of Cistanche Y.C.MA is in the form of 20-90% highly concentrated liquid, powder, or granules.
Similarly, the above-mentioned extract of Cistanche Y.C.MA may also contain one or more of lactose, casein, dextrose, glucose, sucrose and sorbitol.
Thus the inventive extract of the present invention has no toxicity and side effects; it can be used safely.
It will be apparent to those skilled in the art that various modifications and variations can be made in the compositions, uses and preparations of the present invention without departing from the spirit and scope of the invention.
DESCRIPTION OF THE DRAWINGS The above and other objects, features and advantages of the present invention will be more clearly understood from the following detailed description in conjunction with the accompanying drawings, in which: Figure 1 shows the inventive extract or NGF in a microscope at a magnification of x 200 Photographs of neurite outgrowth of treated PC12 cell line; Figure 2 shows the effect of neurite outgrowth treated with the inventive extract or NGF; Figure 3 shows the effects of different concentrations in a microscope at a magnification of ×200
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