WO2022131724A1 - Cognitive function enhancing composition comprising hemp peel extract - Google Patents
Cognitive function enhancing composition comprising hemp peel extract Download PDFInfo
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- WO2022131724A1 WO2022131724A1 PCT/KR2021/018893 KR2021018893W WO2022131724A1 WO 2022131724 A1 WO2022131724 A1 WO 2022131724A1 KR 2021018893 W KR2021018893 W KR 2021018893W WO 2022131724 A1 WO2022131724 A1 WO 2022131724A1
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- Prior art keywords
- hemp
- extract
- extraction
- cognitive function
- bark extract
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- 229960002675 xylitol Drugs 0.000 description 1
Images
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2200/00—Function of food ingredients
- A23V2200/30—Foods, ingredients or supplements having a functional effect on health
- A23V2200/322—Foods, ingredients or supplements having a functional effect on health having an effect on the health of the nervous system or on mental function
Definitions
- the present invention relates to a composition for improving cognitive function, and more particularly, to a composition for improving cognitive function comprising a hemp bark extract.
- dementia As we enter an aging society, the number of dementia patients increases, resulting in an increase in health and social costs. Therefore, dementia is gradually emerging as a national problem rather than an individual problem. Dementia is a pathological phenomenon to be distinguished from normal aging, and depending on its cause, Alzheimer's disease, vascular dementia, other alcoholism, trauma, dementia caused by sequelae of Parkinson's disease, etc. It is known that more than 60% are Alzheimer's dementia. In dementia patients, intellectual functions such as memory, judgment, and language ability decline, or daily living ability decreases, and clinical features such as personality or behavioral disorders appear.
- Alzheimer's dementia the pathogenesis of Alzheimer's dementia is not clearly known, but the toxicity of the neurotoxic protein beta-amyloid protein is suggested as the most important cause. This substance is known to be produced due to incorrect metabolism of amyloid precursor protein (APP), and it is reported that the normal metabolite of APP has a neuroprotective action. Recent research results using genetic engineering methods have revealed that toxic proteins such as beta-amyloid accumulate in cells and blood vessels and cause toxicity to nerve cells, resulting in impairment of brain function.
- APP amyloid precursor protein
- acetylcholine precursor or a drug that inhibits the degradation of acetylcholine.
- Representative drugs include tacrine, donepezil, rivastigmine, and galantamine.
- the dementia treatment drugs as described above currently used are acetylcholinesterase inhibitor-based compounds, and are known to have side effects of the digestive system such as nausea, vomiting, loss of appetite, and abdominal pain.
- inhibition of acetylcholinesterase activity as well as butyrylcholinesterase activity in order to more effectively treat Alzheimer's dementia as the activity of butyrylcholinesterase is relatively dramatically increased in Alzheimer's dementia The development of simultaneous inhibitors is urgently required.
- the problem to be solved by the present invention is to provide a naturally-derived substance that simultaneously inhibits acetylcholinesterase activity and butyrylcholinesterase activity to more effectively improve cognitive dysfunction, such as Alzheimer's dementia.
- a pharmaceutical composition for improving cognitive function comprising a hemp bark extract.
- the hemp husk may be the husk of a hemp stem.
- the hemp bark extract may be a C 1 to C 3 alcohol extract, preferably an ethanol extract.
- the hemp bark extract may be extracted using one or more methods selected from the group consisting of hot water extraction, solvent extraction, ultra-high pressure extraction, supercritical extraction, and ultrasonic extraction.
- the cognitive function improvement may be for treatment or prevention of dementia.
- a food composition for improving cognitive function comprising a hemp bark extract.
- the hemp husk may be the husk of a hemp stem.
- the hemp bark extract may be a C 1 to C 3 alcohol extract, preferably an ethanol extract.
- the hemp bark extract may be extracted using one or more methods selected from the group consisting of hot water extraction, solvent extraction, ultra-high pressure extraction, supercritical extraction, and ultrasonic extraction.
- the cognitive function improvement may be for treatment or prevention of dementia.
- the hemp bark extract of the present invention has been confirmed to exhibit not only acetylcholinesterase inhibitory effect but also butyrylcholinesterase inhibitory effect, thereby reducing acetylcholine levels in brain tissue and lowering blood butyrylcholine levels seen in dementia patients. It has been found that the side effects in the treatment of dementia can be reduced at the same time by reducing the dose of each drug.
- the pharmaceutical composition and food composition for improving cognitive function comprising the hemp bark extract of the present invention are substances that simultaneously inhibit acetylcholinesterase and butyrylcholinesterase, and are substances for improving cognitive function in the pharmaceutical and health functional food fields can be usefully used as
- 1 is a graph showing the effect of hemp bark extract on inhibiting acetylcholinesterase activity (AChE activity) according to the concentration.
- Figure 2 is a graph showing the efficacy of hemp bark extract to inhibit butyrylcholinesterase activity (BuChE activity) according to the concentration.
- the present invention provides a pharmaceutical composition for improving cognitive function comprising a hemp bark extract.
- Hemp is an annual herb belonging to the Hemp family, hemp (hemp, hemp, scientific name Cannabis sativa ), also called hemp or hemp, and grows to a height of 1-2.5 m.
- the stem extends straight in the shape of a square column, and hairs are all over the surface, and the inside is hollow.
- the surface of the stem is corrugated vertically, and in the cross section, there is a hypodermis with several layers of chlorophyll inside the epidermal cells, with parenchyma on the inside and bast fibers on the inside.
- the length of the fiber is about 10 cm long, and it is usually 3-4 cm long.
- the bast fiber of the hemp stem is hemp yarn, which is used as a raw material for weaving hemp or rope, net, mosquito net, or tent.
- the extract included as an active ingredient in the pharmaceutical composition of the present invention may be an extract of hemp bark, preferably an extract of hemp stem bark.
- the extraction process may be performed by an extraction method commonly used in the technical field to which the present invention pertains, and preferably may be performed by the following process, but is not limited thereto.
- a C 1 to C 3 alcohol may be used as an extraction solvent of the hemp, preferably a mixed solvent of C 1 to C 3 alcohol and water, and more preferably 50 to 80 % (v/v) Ethanol, most preferably 70% (v/v) ethanol, can be used.
- the extraction process may be performed by pulverizing the hemp husks and mixing with an extraction solvent, and the extraction solvent may be mixed in a ratio suitable for extraction of the hemp husks, preferably at a weight of the hemp husks. It can be extracted by mixing 1 to 50 times, more preferably 1 to 20 times, and most preferably 1 to 10 times.
- the hemp bark extract may be used without limitation as long as it is an extraction method commonly used in the field of extraction of natural products, but preferably from the group consisting of hot water extraction, solvent extraction, ultra-high pressure extraction, supercritical extraction and ultrasonic extraction. It may be performed using one or more selected methods.
- the ultrasonic extraction may be performed with an appropriate level of intensity (eg, 10% to 50% amplitude), but is not limited thereto.
- the ultrasonic irradiation time may be performed for a time suitable for extraction (eg, about 1 to 120 minutes), but is not limited thereto.
- the extraction process may be repeated a sufficient number of times for extracting the hemp husk, and the supernatant of the finally obtained extract may be filtered and used as necessary.
- the solvent contained in the final extract may be removed by an appropriate method (eg, reduced pressure concentration method, etc.) if necessary to finally obtain a hemp husk extract.
- the hemp bark extract included in the pharmaceutical composition of the present invention exhibits excellent acetylcholinesterase inhibitory effect as well as excellent butyrylcholinesterase inhibitory effect, so that patients with dementia It was confirmed that it can simultaneously lower and improve the concentration of acetylcholine in brain tissue and butyrylcholine in blood. Therefore, the hemp bark extract contained in the pharmaceutical composition of the present invention may be used for improving cognitive function, and the use for improving cognitive function may include treatment or prevention of dementia.
- the pharmaceutical composition of the present invention may contain a pharmaceutically acceptable carrier or diluent, and each of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols, etc., oral dosage forms, external preparations, It may be formulated in the form of suppositories and sterile injectable solutions.
- the pharmaceutically acceptable carrier is lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, gum acacia, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methylcellulose, microcrystalline cellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil and the like. It also includes diluents or excipients such as fillers, bulking agents, binders, wetting agents, disintegrating agents, surfactants, and the like.
- Solid preparations for oral use include tablets, pills, powders, granules, capsules, and the like, and such solid preparations include at least one excipient, for example, starch, calcium carbonate, sucrose, or lactose. ), gelatin, and the like, and lubricants such as magnesium stearate and talc.
- Liquid formulations for oral use include suspensions, solutions, emulsions, syrups, and the like, and may include water, diluents such as liquid paraffin, wetting agents, sweeteners, fragrances, and preservatives.
- Parenteral preparations include sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, creams, freeze-dried preparations, and suppositories.
- Non-aqueous solvents and suspensions include propylene glycol, polyethylene glycol, and vegetable oils such as olive oil. oil, injectable esters such as ethyl oleate, and the like.
- As the base of the suppository witepsol, macrogol, tween 61, cacao butter, laurin, glycerogelatin, and the like can be used.
- the dosage of the active ingredient contained in the pharmaceutical composition of the present invention varies depending on the patient's condition and weight, the degree of disease, the form of the active ingredient, the route and period of administration, and may be appropriately adjusted according to the patient.
- the active ingredient may be administered at a dose of 0.0001 to 1000 mg/kg per day, preferably 0.001 to 100 mg/kg, and the administration may be administered once or in several divided doses per day.
- the pharmaceutical composition of the present invention may include the active ingredient in a weight percentage of 0.001 to 90% based on the total weight of the composition.
- the pharmaceutical composition of the present invention can be administered to mammals such as rats, mice, livestock, and humans by various routes, for example, oral, skin, abdominal cavity, rectal or intravenous, muscle, subcutaneous, intrauterine dura mater or intracerebroventricular (intracerebroventricular). It may be administered by injection.
- mammals such as rats, mice, livestock, and humans by various routes, for example, oral, skin, abdominal cavity, rectal or intravenous, muscle, subcutaneous, intrauterine dura mater or intracerebroventricular (intracerebroventricular). It may be administered by injection.
- the present invention also provides a food composition for improving cognitive function comprising a hemp bark extract.
- the hemp husk may be a husk of a hemp stem.
- the hemp bark extract may be a C 1 to C 3 alcohol extract, preferably an ethanol extract.
- the hemp bark extract may be extracted using one or more methods selected from the group consisting of hot water extraction, solvent extraction, ultra-high pressure extraction, supercritical extraction, and ultrasonic extraction.
- the extraction process and cognitive function improvement effect of the hemp husk extract contained in the food composition for improving cognitive function of the present invention are as described above.
- the effect of the hemp bark extract contained in the food composition for improving cognitive function of the present invention is as described above. That is, in one embodiment, the use for improving cognitive function may be for treatment or prevention of dementia.
- the food composition of the present invention can be used as a health functional food.
- health functional food means a food manufactured and processed using raw materials or ingredients useful for the human body in accordance with the Health Functional Food Act, and "functionality” refers to the structure and function of the human body. It refers to ingestion for the purpose of obtaining useful effects for health purposes such as regulating nutrients or physiological effects.
- the food composition of the present invention may contain conventional food additives, and the suitability as the "food additive” is determined according to the general rules and general test methods of food additives approved by the Ministry of Food and Drug Safety, unless otherwise specified. It is judged according to the standards and standards related to the item.
- Food Additives Code include, for example, chemical compounds such as ketones, glycine, potassium citrate, nicotinic acid, and cinnamic acid; and mixed preparations such as sodium L-glutamate preparations, noodles-added alkalis, preservatives, and tar dye preparations.
- the food composition of the present invention may include 0.01 to 95%, preferably 1 to 80% weight percentage of the hemp bark extract based on the total weight of the composition for the purpose of improving cognitive function, particularly preventing and/or improving dementia. have.
- it may be manufactured and processed in the form of tablets, capsules, powders, granules, liquids, pills, and the like.
- the health functional food in tablet form is granulated with a mixture of the hemp bark extract, excipients, binders, disintegrants, and other additives in a conventional manner, and then compression-molded by putting a lubricant, etc., or The mixture can be compression molded directly.
- the health functional food in the form of tablets may contain a mating agent, etc., if necessary, and may be coated with a suitable skinning agent if necessary.
- hard capsules can be prepared by filling conventional hard capsules with a mixture of the hemp bark extract and additives such as excipients, or their granules or skinned granules. It can be prepared by filling a mixture with additives such as extracts and excipients in a capsule base such as gelatin.
- the soft capsules may contain a plasticizer such as glycerin or sorbitol, a colorant, a preservative, and the like, if necessary.
- the health functional food in the form of granules may be prepared in a granular form by a suitable method of a mixture of the hemp bark extract, excipients, binders, disintegrants, and the like, and may contain flavoring agents, flavoring agents, etc. as needed.
- excipients binders, disintegrants, lubricants, flavoring agents, and the like of the present invention are those described in documents known in the art and include those having the same or similar functions.
- the dried hemp roots (30 g), stems (30 g), and stem bark (10 g) were each finely pulverized using a grinder.
- 70% (v/v) ethanol was added to the sample so as to be 10 times the weight of the pulverized sample, and extracted for 15 minutes (75.415 kJ) at an intensity of 20% amplitude using ultrasound at room temperature. After immersing the extract, the supernatant was collected separately, and 70% (v/v) ethanol was added to the residue to obtain a supernatant through repeated extraction twice.
- the obtained supernatant was filtered under reduced pressure with filter paper (ADVANTEC, No. 2 & No.
- Dithionitrobenzoic acid (DTNB) was prepared at 1.2 mg/ml, and then 50 ⁇ l was added to a 96-well plate and left for 10 minutes.
- the absorbance value by the extract was corrected by adding a phosphate buffer instead of acetylthiocholine or butyrylthiocholine (positive control rivastigmine).
- acetylcholinesterase (AChE) inhibitory efficacy measured as described above is shown in FIG. 1
- the butyrylcholinesterase (BuChE) inhibitory efficacy is shown in FIG. 2, and the IC 50 values of each extract are summarized in Table 1 below. and described.
- the hemp bark extract exhibited superior acetylcholinesterase inhibitory activity and butyrylcholinesterase inhibitory activity than the hemp root extract and hemp stem extract.
- the hemp bark extract not only exhibited superior acetylcholinesterase inhibitory efficacy (IC 50 0.553 mg/mL) than rivastigmine, a positive control, but also showed superior butyrylcholinesterase inhibitory efficacy (IC 50 50 mg/mL) than rivastigmine. 0.012 mg/mL), which is expected to be usefully used as a cognitive function improving substance.
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Abstract
The present invention provides a cognitive function enhancing pharmaceutical composition comprising a hemp peel extract, and a cognitive function enhancing food composition comprising a hemp peel extract. The cognitive function enhancing pharmaceutical composition and food composition comprising a hemp peel extract inhibit both acetylcholinesterase and butyrylcholinesterase and can be utilized as a cognitive function enhancing substance in the field of medicine and health functional food.
Description
본 발명은 인지기능 개선용 조성물에 관한 것으로, 더욱 상세하게는 헴프 껍질 추출물을 포함하는 인지기능 개선용 조성물에 관한 것이다.The present invention relates to a composition for improving cognitive function, and more particularly, to a composition for improving cognitive function comprising a hemp bark extract.
고령화 사회에 접어들게 됨에 따라 치매 환자가 증가하면서 이에 따른 건강 및 사회적 비용이 증가하고 있다. 따라서, 점차적으로 치매는 개인의 문제가 아닌 국가적인 과제로 대두되고 있는 실정이다. 치매(dementia)는 정상적인 노화와는 구분해야 할 병적인 현상이며, 그 원인에 따라 알츠하이머성 치매(Alzheimer's disease), 혈관성 치매(vascular dementia), 기타 알콜 중독, 외상, 파킨슨병의 후유증으로 오는 치매 등으로 구별되며, 60% 이상이 알츠하이머성 치매인 것으로 알려져 있다. 치매 환자에서는 기억·판단·언어 능력 등의 지적인 기능이 감퇴하거나, 일상생활 능력이 저하되고, 인격 또는 행동 장애 등의 임상적인 특징이 나타난다.As we enter an aging society, the number of dementia patients increases, resulting in an increase in health and social costs. Therefore, dementia is gradually emerging as a national problem rather than an individual problem. Dementia is a pathological phenomenon to be distinguished from normal aging, and depending on its cause, Alzheimer's disease, vascular dementia, other alcoholism, trauma, dementia caused by sequelae of Parkinson's disease, etc. It is known that more than 60% are Alzheimer's dementia. In dementia patients, intellectual functions such as memory, judgment, and language ability decline, or daily living ability decreases, and clinical features such as personality or behavioral disorders appear.
치매 분류 중, 알츠하이머성 치매의 발병 기전은 명확히 알려져 있지 않으나, 신경독성단백질인 베타-아밀로이드(β-amyloid protein)의 독성이 가장 중요한 원인으로 제시되고 있다. 이 물질은 아밀로이드 전구단백질(APP: amyloid precursor protein)의 잘못된 대사로 인해 생성되는 것으로 알려져 있고, APP의 정상 대사물은 신경세포 보호작용이 있는 것으로 보고되고 있다. 최근 유전공학적 방법을 이용한 연구 결과에서는 베타아밀로이드(β-amyloid) 등의 독성 단백질이 세포와 혈관에 쌓여 신경세포에 독성을 미침으로써 결과적으로 뇌기능에 장애가 초래된다는 사실이 밝혀졌다.Among the classifications of dementia, the pathogenesis of Alzheimer's dementia is not clearly known, but the toxicity of the neurotoxic protein beta-amyloid protein is suggested as the most important cause. This substance is known to be produced due to incorrect metabolism of amyloid precursor protein (APP), and it is reported that the normal metabolite of APP has a neuroprotective action. Recent research results using genetic engineering methods have revealed that toxic proteins such as beta-amyloid accumulate in cells and blood vessels and cause toxicity to nerve cells, resulting in impairment of brain function.
현재까지 치매 치료를 위한 약물 치료는 아세틸콜린 전구체를 투여하거나 아세틸콜린의 분해를 저해하는 약물을 투여하여 뇌의 아세틸콜린 농도를 높여 주는 치료 방법이 사용되어 왔다. 대표적인 약물로는 타크린(tacrine), 도네페질(donepezil), 리바스티그민(rivastigmine), 갈란타민(galantamine) 등이 있다.Until now, drug treatment for the treatment of dementia has been used to increase the concentration of acetylcholine in the brain by administering an acetylcholine precursor or a drug that inhibits the degradation of acetylcholine. Representative drugs include tacrine, donepezil, rivastigmine, and galantamine.
현재 사용되고 있는 상기와 같은 치매 치료 약물은 아세틸콜린에스테라제 저해제 기반의 화합물로서, 오심, 구토, 식욕감퇴, 복통 등 소화기 계통의 부작용이 있는 것으로 알려져 있다. 또한, 알츠하이머성 치매에서는 상대적으로 부티릴콜린에스테라제의 활동성이 비약적으로 증가됨에 따라 알츠하이머성 치매를 보다 효과적으로 치료하기 위하여는 아세틸콜린에스테라제 활성의 저해뿐만 아니라 부티릴콜린에스테라제 활성도 저해하는 동시 저해제 개발이 절실하게 요구된다.The dementia treatment drugs as described above currently used are acetylcholinesterase inhibitor-based compounds, and are known to have side effects of the digestive system such as nausea, vomiting, loss of appetite, and abdominal pain. In addition, inhibition of acetylcholinesterase activity as well as butyrylcholinesterase activity in order to more effectively treat Alzheimer's dementia as the activity of butyrylcholinesterase is relatively dramatically increased in Alzheimer's dementia The development of simultaneous inhibitors is urgently required.
본 발명이 해결하고자 하는 과제는 아세틸콜린에스테라제 활성과 부티릴콜린에스테라제 활성을 동시에 억제하여 보다 효과적으로 알츠하이머성 치매 등의 인지기능 장애를 개선시키는 천연 유래 물질을 제공하는 것이다.The problem to be solved by the present invention is to provide a naturally-derived substance that simultaneously inhibits acetylcholinesterase activity and butyrylcholinesterase activity to more effectively improve cognitive dysfunction, such as Alzheimer's dementia.
본 발명이 해결하고자 하는 과제는 이상에서 언급한 해결 과제로 제한되지 않으며, 언급되지 않은 또 다른 기술적 과제들은 아래의 기재로부터 본 발명이 속하는 기술 분야에서 통상의 지식을 가진 자에게 명확하게 이해될 수 있을 것이다.The problem to be solved by the present invention is not limited to the above-mentioned problems, and other technical problems not mentioned can be clearly understood by those of ordinary skill in the art to which the present invention belongs from the description below. There will be.
상기 해결 과제를 달성하기 위하여, 본 발명의 일 측면에 따라, 헴프 껍질 추출물을 포함하는 인지기능 개선용 약학 조성물이 제공된다.In order to achieve the above object, according to an aspect of the present invention, there is provided a pharmaceutical composition for improving cognitive function comprising a hemp bark extract.
일 구현예에서, 상기 헴프 껍질은 헴프 줄기의 껍질일 수 있다.In one embodiment, the hemp husk may be the husk of a hemp stem.
일 구현예에서, 상기 헴프 껍질 추출물은 C1 내지 C3 알코올 추출물일 수 있으며, 바람직하게는 에탄올 추출물일 수 있다.In one embodiment, the hemp bark extract may be a C 1 to C 3 alcohol extract, preferably an ethanol extract.
일 구현예에서, 상기 헴프 껍질 추출물은 열수 추출, 용매 추출, 초고압 추출, 초임계 추출 및 초음파 추출로 이루어진 군으로부터 선택된 1 이상의 방법을 이용하여 추출될 수 있다.In one embodiment, the hemp bark extract may be extracted using one or more methods selected from the group consisting of hot water extraction, solvent extraction, ultra-high pressure extraction, supercritical extraction, and ultrasonic extraction.
일 구현예에서, 상기 인지기능 개선용은 치매 치료 또는 예방용일 수 있다.In one embodiment, the cognitive function improvement may be for treatment or prevention of dementia.
본 발명의 다른 측면에 따라, 헴프 껍질 추출물을 포함하는 인지기능 개선용 식품 조성물이 제공된다.According to another aspect of the present invention, there is provided a food composition for improving cognitive function comprising a hemp bark extract.
일 구현예에서, 상기 헴프 껍질은 헴프 줄기의 껍질일 수 있다.In one embodiment, the hemp husk may be the husk of a hemp stem.
일 구현예에서, 상기 헴프 껍질 추출물은 C1 내지 C3 알코올 추출물일 수 있으며, 바람직하게는 에탄올 추출물일 수 있다.In one embodiment, the hemp bark extract may be a C 1 to C 3 alcohol extract, preferably an ethanol extract.
일 구현예에서, 상기 헴프 껍질 추출물은 열수 추출, 용매 추출, 초고압 추출, 초임계 추출 및 초음파 추출로 이루어진 군으로부터 선택된 1 이상의 방법을 이용하여 추출될 수 있다.In one embodiment, the hemp bark extract may be extracted using one or more methods selected from the group consisting of hot water extraction, solvent extraction, ultra-high pressure extraction, supercritical extraction, and ultrasonic extraction.
일 구현예에서, 상기 인지기능 개선용은 치매 치료 또는 예방용일 수 있다.In one embodiment, the cognitive function improvement may be for treatment or prevention of dementia.
본 발명의 헴프 껍질 추출물은 아세틸콜린에스테라제 저해 효능뿐만 아니라 부티릴콜린에스테라제 저해 효능을 나타내는 것으로 확인되어, 치매 환자들에게서 나타나는 뇌조직 내의 아세틸콜린 수준 저하 및 혈중 부티릴콜린 수준 저하를 동시에 개선시킬 수 있으며, 이에 따라, 각각의 약물 복용양을 감소시켜 치매 치료시의 부작용을 낮출 수 있다는 것이 밝혀졌다.The hemp bark extract of the present invention has been confirmed to exhibit not only acetylcholinesterase inhibitory effect but also butyrylcholinesterase inhibitory effect, thereby reducing acetylcholine levels in brain tissue and lowering blood butyrylcholine levels seen in dementia patients. It has been found that the side effects in the treatment of dementia can be reduced at the same time by reducing the dose of each drug.
따라서, 본 발명의 헴프 껍질 추출물을 포함하는 인지기능 개선용 약학 조성물 및 식품 조성물은 아세틸콜린에스테라제 및 부티릴콜린에스테라제를 동시에 저해하는 물질로 의약 및 건강기능식품 분야에서 인지기능 개선 물질로서 유용하게 사용될 수 있다.Therefore, the pharmaceutical composition and food composition for improving cognitive function comprising the hemp bark extract of the present invention are substances that simultaneously inhibit acetylcholinesterase and butyrylcholinesterase, and are substances for improving cognitive function in the pharmaceutical and health functional food fields can be usefully used as
본 발명의 효과는 상기한 효과로 한정되는 것은 아니며, 본 발명의 설명 또는 특허청구범위에 기재된 발명의 구성으로부터 추론 가능한 모든 효과를 포함하는 것으로 이해되어야 한다.The effects of the present invention are not limited to the above-described effects, and it should be understood to include all effects that can be inferred from the configuration of the invention described in the description or claims of the present invention.
도 1은 헴프 껍질 추출물이 농도에 따라 아세틸콜린에스테라제 활성(AChE activity)을 저해하는 효능을 나타낸 그래프이다. 1 is a graph showing the effect of hemp bark extract on inhibiting acetylcholinesterase activity (AChE activity) according to the concentration.
도 2는 헴프 껍질 추출물이 농도에 따라 부티릴콜린에스테라제 활성(BuChE activity)을 저해하는 효능을 나타낸 그래프이다. Figure 2 is a graph showing the efficacy of hemp bark extract to inhibit butyrylcholinesterase activity (BuChE activity) according to the concentration.
본 발명은 헴프 껍질 추출물을 포함하는 인지기능 개선용 약학 조성물을 제공한다.The present invention provides a pharmaceutical composition for improving cognitive function comprising a hemp bark extract.
헴프는 삼과에 속하는 1년생 초본인 삼(헴프, hemp, 학명 Cannabis sativa)으로서, 대마(大麻) 또는 마(麻)라고도 지칭되며, 높이 1~2.5 m로 자란다. 줄기는 사각주(斜角柱)상으로 곧게 뻗으며, 표면(表面)에는 전체에 유모(柔毛)가 나 있고, 속이 비어 있다. 줄기의 표면에는 세로로 골이 져 있고 횡단면은 표피세포 안쪽에 여러 층의 엽록소(葉綠素)를 가진 하피(下皮)가 있으며 그 안쪽에 유조직이 있고 안쪽에 인피섬유(靭皮纖維)가 있다. 섬유의 길이는 긴 것이 10cm 정도이고 대개는 3~4cm이다. 대마 줄기의 인피섬유는 삼실[麻絲]로서 삼베를 짜거나 로프, 그물, 모기장 또는 천막 등의 원료로 쓰인다.Hemp is an annual herb belonging to the Hemp family, hemp (hemp, hemp, scientific name Cannabis sativa ), also called hemp or hemp, and grows to a height of 1-2.5 m. The stem extends straight in the shape of a square column, and hairs are all over the surface, and the inside is hollow. The surface of the stem is corrugated vertically, and in the cross section, there is a hypodermis with several layers of chlorophyll inside the epidermal cells, with parenchyma on the inside and bast fibers on the inside. The length of the fiber is about 10 cm long, and it is usually 3-4 cm long. The bast fiber of the hemp stem is hemp yarn, which is used as a raw material for weaving hemp or rope, net, mosquito net, or tent.
본 발명의 약학 조성물에 유효성분으로서 포함되는 추출물은 헴프 껍질의 추출물로서, 바람직하게는 헴프 줄기 껍질의 추출물일 수 있다. 추출 과정은 본 발명이 속하는 기술 분야에서 통상적으로 사용되는 추출 방법에 의해 수행될 수 있으며, 바람직하게는 하기 공정에 의해 수행될 수 있으나, 이에 제한되지 않는다.The extract included as an active ingredient in the pharmaceutical composition of the present invention may be an extract of hemp bark, preferably an extract of hemp stem bark. The extraction process may be performed by an extraction method commonly used in the technical field to which the present invention pertains, and preferably may be performed by the following process, but is not limited thereto.
추출 과정에서는 헴프 껍질의 추출 용매로서 C1 내지 C3 알코올을 사용할 수 있으며, 바람직하게는 C1 내지 C3 알코올 및 물의 혼합 용매를 사용할 있으며, 더욱 바람직하게는 50 ~ 80 %(v/v) 에탄올, 가장 바람직하게는 70 %(v/v) 에탄올을 사용할 수 있다. 필요한 경우에 헴프 껍질을 분쇄한 후 추출 용매와 혼합하여 추출 공정을 수행할 수 있으며, 추출 용매는 헴프 껍질의 추출이 수행되기에 적절한 정도의 비율로 혼합할 수 있으며, 바람직하게는 헴프 껍질 중량의 1~50배, 더욱 바람직하게는 1~20배, 가장 바람직하게는 1~10배로 혼합하여 추출할 수 있다.In the extraction process, a C 1 to C 3 alcohol may be used as an extraction solvent of the hemp, preferably a mixed solvent of C 1 to C 3 alcohol and water, and more preferably 50 to 80 % (v/v) Ethanol, most preferably 70% (v/v) ethanol, can be used. If necessary, the extraction process may be performed by pulverizing the hemp husks and mixing with an extraction solvent, and the extraction solvent may be mixed in a ratio suitable for extraction of the hemp husks, preferably at a weight of the hemp husks. It can be extracted by mixing 1 to 50 times, more preferably 1 to 20 times, and most preferably 1 to 10 times.
일 구현예에서, 상기 헴프 껍질 추출물은 천연물의 추출 분야에서 통상적으로 사용되는 추출 방법이라면 제한 없이 사용될 수 있으나, 바람직하게는 열수 추출, 용매 추출, 초고압 추출, 초임계 추출 및 초음파 추출로 이루어진 군으로부터 선택된 1 이상의 방법을 이용하여 수행될 수 있다.In one embodiment, the hemp bark extract may be used without limitation as long as it is an extraction method commonly used in the field of extraction of natural products, but preferably from the group consisting of hot water extraction, solvent extraction, ultra-high pressure extraction, supercritical extraction and ultrasonic extraction. It may be performed using one or more selected methods.
일 구현예에서, 초음파 추출을 이용하여 추출되는 경우에는 초음파 추출이 수행되기에 적절한 정도의 강도(예를 들어, 10%~50% 진폭(amplitude))로 수행될 수 있으나, 이에 제한되지 않는다. 초음파의 조사 시간은 추출이 수행되기에 적절한 정도의 시간 동안(예를 들어, 1~120분 정도) 수행될 수 있으나, 이에 제한되지 않는다. 추출 과정은 헴프 껍질 추출에 충분한 정도의 횟수로 반복하여 수행될 수 있으며, 최종 얻은 추출물의 상등액은 필요에 따라 여과하여 사용할 수 있다. 최종 추출물에 포함된 용매는 필요에 따라 적절한 방법(예를 들어, 감압농축법 등)으로 제거하여 최종적으로 헴프 껍질 추출물을 얻을 수 있다.In one embodiment, when the extraction is performed using ultrasonic extraction, the ultrasonic extraction may be performed with an appropriate level of intensity (eg, 10% to 50% amplitude), but is not limited thereto. The ultrasonic irradiation time may be performed for a time suitable for extraction (eg, about 1 to 120 minutes), but is not limited thereto. The extraction process may be repeated a sufficient number of times for extracting the hemp husk, and the supernatant of the finally obtained extract may be filtered and used as necessary. The solvent contained in the final extract may be removed by an appropriate method (eg, reduced pressure concentration method, etc.) if necessary to finally obtain a hemp husk extract.
본 발명의 약학 조성물에 포함되는 헴프 껍질 추출물은 표 1, 도 1 및 도 2에 나타난 바와 같이, 우수한 아세틸콜린에스테라제 저해 효능뿐만 아니라 우수한 부티릴콜린에스테라제 저해 효능을 나타내어, 치매 환자들에게서 나타나는 뇌조직 내의 아세틸콜린 농도 및 혈중 부티릴콜린 농도를 동시에 저하, 개선시킬 수 있는 것으로 확인되었다. 따라서, 본 발명의 약학 조성물에 포함되는 헴프 껍질 추출물은 인지기능 개선용으로 사용될 수 있으며, 이러한 인지기능 개선 용도에는 치매 치료 또는 예방 용도 등이 포함될 수 있다.As shown in Table 1, FIGS. 1 and 2, the hemp bark extract included in the pharmaceutical composition of the present invention exhibits excellent acetylcholinesterase inhibitory effect as well as excellent butyrylcholinesterase inhibitory effect, so that patients with dementia It was confirmed that it can simultaneously lower and improve the concentration of acetylcholine in brain tissue and butyrylcholine in blood. Therefore, the hemp bark extract contained in the pharmaceutical composition of the present invention may be used for improving cognitive function, and the use for improving cognitive function may include treatment or prevention of dementia.
본 발명의 약학 조성물은 약제학적으로 허용가능한 담체 또는 희석제를 포함할 수 있으며, 각각 통상의 방법에 따라 산제, 과립제, 정제, 캡슐제, 현탁액, 에멀젼, 시럽, 에어로졸 등의 경구형 제형, 외용제, 좌제 및 멸균 주사용액의 형태로 제제화될 수 있다. 상기 약제학적으로 허용가능한 담체는 락토즈, 덱스트로즈, 수크로스, 솔비톨, 만니톨, 자일리톨, 에리스리톨, 말티톨, 전분, 아카시아 고무, 알지네이트, 젤라틴, 칼슘 포스페이트, 칼슘 실리케이트, 셀룰로즈, 메틸셀룰로즈, 미정질 셀룰로스, 폴리비닐 피롤리돈, 물, 메틸히드록시벤조에이트, 프로필히드록시벤조에이트, 탈크, 마그네슘 스테아레이트 및 광물유 등을 포함한다. 또한, 충진제, 증량제, 결합제, 습윤제, 붕해제, 계면활성제 등의 희석제 또는 부형제를 포함한다. 경구용 고형 제제는 정제, 환제, 산제, 과립제, 캡슐제 등을 포함하며, 이러한 고형제제는 적어도 하나 이상의 부형제 예를 들면, 전분, 칼슘카보네이트(calcium carbonate), 수크로스(sucrose) 또는 락토오스(lactose), 젤라틴 등을 포함할 수 있으며, 마그네슘 스테아레이트, 탈크 같은 윤활제 등을 포함할 수 있다. 경구용 액상 제제는 현탁제, 내용액제, 유제, 시럽제 등을 포함하며, 물, 리퀴드 파라핀 등의 희석제, 습윤제, 감미제, 방향제, 보존제 등을 포함할 수 있다. 비경구용 제제는 멸균된 수용액, 비수성용제, 현탁제, 유제, 크림제, 동결건조 제제, 좌제를 포함하며, 비수성 용제, 현탁제로는 프로필렌글리콜(propylene glycol), 폴리에틸렌 글리콜, 올리브 오일과 같은 식물성 기름, 에틸올레이트와 같은 주사 가능한 에스테르류 등을 포함한다. 좌제의 기제로는 위텝솔(witepsol), 마크로골, 트윈(tween) 61, 카카오지, 라우린지, 글리세로젤라틴 등이 사용될 수 있다.The pharmaceutical composition of the present invention may contain a pharmaceutically acceptable carrier or diluent, and each of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols, etc., oral dosage forms, external preparations, It may be formulated in the form of suppositories and sterile injectable solutions. The pharmaceutically acceptable carrier is lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, gum acacia, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methylcellulose, microcrystalline cellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil and the like. It also includes diluents or excipients such as fillers, bulking agents, binders, wetting agents, disintegrating agents, surfactants, and the like. Solid preparations for oral use include tablets, pills, powders, granules, capsules, and the like, and such solid preparations include at least one excipient, for example, starch, calcium carbonate, sucrose, or lactose. ), gelatin, and the like, and lubricants such as magnesium stearate and talc. Liquid formulations for oral use include suspensions, solutions, emulsions, syrups, and the like, and may include water, diluents such as liquid paraffin, wetting agents, sweeteners, fragrances, and preservatives. Parenteral preparations include sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, creams, freeze-dried preparations, and suppositories. Non-aqueous solvents and suspensions include propylene glycol, polyethylene glycol, and vegetable oils such as olive oil. oil, injectable esters such as ethyl oleate, and the like. As the base of the suppository, witepsol, macrogol, tween 61, cacao butter, laurin, glycerogelatin, and the like can be used.
본 발명의 약학 조성물에 함유되는 유효성분의 투여량은 환자의 상태 및 체중, 질병의 정도, 유효성분 형태, 투여 경로 및 기간에 따라 다르며, 환자에 따라 적절하게 조절될 수 있다. 예를 들면, 상기 유효성분은 1일 0.0001 내지 1000 mg/kg으로, 바람직하게는 0.001 내지 100 mg/kg의 용량으로 투여할 수 있으며, 상기 투여는 하루에 한번 또는 수회 나누어 투여할 수도 있다. 또한, 본 발명의 약학 조성물은 조성물 총 중량에 대하여 상기 유효성분을 0.001 내지 90 % 중량백분율로 포함할 수 있다.The dosage of the active ingredient contained in the pharmaceutical composition of the present invention varies depending on the patient's condition and weight, the degree of disease, the form of the active ingredient, the route and period of administration, and may be appropriately adjusted according to the patient. For example, the active ingredient may be administered at a dose of 0.0001 to 1000 mg/kg per day, preferably 0.001 to 100 mg/kg, and the administration may be administered once or in several divided doses per day. In addition, the pharmaceutical composition of the present invention may include the active ingredient in a weight percentage of 0.001 to 90% based on the total weight of the composition.
본 발명의 약학 조성물은 랫트, 마우스, 가축, 인간 등의 포유동물에 다양한 경로로, 예를 들면, 경구, 피부, 복강, 직장 또는 정맥, 근육, 피하, 자궁 내 경막 또는 뇌혈관 내(intracerebroventricular) 주사에 의해 투여될 수 있다.The pharmaceutical composition of the present invention can be administered to mammals such as rats, mice, livestock, and humans by various routes, for example, oral, skin, abdominal cavity, rectal or intravenous, muscle, subcutaneous, intrauterine dura mater or intracerebroventricular (intracerebroventricular). It may be administered by injection.
본 발명은 또한, 헴프 껍질 추출물을 포함하는 인지기능 개선용 식품 조성물을 제공한다. The present invention also provides a food composition for improving cognitive function comprising a hemp bark extract.
본 발명의 인지기능 개선용 식품 조성물에 포함되는 헴프 껍질 추출물의 추출 과정은 앞서 설명한 바와 같다. 즉, 일 구현예에서, 상기 헴프 껍질은 헴프 줄기의 껍질일 수 있다. 또한, 일 구현예에서, 상기 헴프 껍질 추출물은 C1 내지 C3 알코올 추출물일 수 있으며, 바람직하게는 에탄올 추출물일 수 있다. 일 구현예에서, 상기 헴프 껍질 추출물은 열수 추출, 용매 추출, 초고압 추출, 초임계 추출 및 초음파 추출로 이루어진 군으로부터 선택된 1 이상의 방법을 이용하여 추출될 수 있다.The extraction process of the hemp husk extract contained in the food composition for improving cognitive function of the present invention is the same as described above. That is, in one embodiment, the hemp husk may be a husk of a hemp stem. Also, in one embodiment, the hemp bark extract may be a C 1 to C 3 alcohol extract, preferably an ethanol extract. In one embodiment, the hemp bark extract may be extracted using one or more methods selected from the group consisting of hot water extraction, solvent extraction, ultra-high pressure extraction, supercritical extraction, and ultrasonic extraction.
본 발명의 인지기능 개선용 식품 조성물에 포함되는 헴프 껍질 추출물의 추출 과정 및 인지기능 개선 효과는 앞서 설명한 바와 같다. The extraction process and cognitive function improvement effect of the hemp husk extract contained in the food composition for improving cognitive function of the present invention are as described above.
본 발명의 인지기능 개선용 식품 조성물에 포함되는 헴프 껍질 추출물의 효과는 앞서 설명한 바와 같다. 즉, 일 구현예에서, 상기 인지기능 개선용은 치매 치료 또는 예방용일 수 있다.The effect of the hemp bark extract contained in the food composition for improving cognitive function of the present invention is as described above. That is, in one embodiment, the use for improving cognitive function may be for treatment or prevention of dementia.
본 발명의 식품 조성물은 건강기능식품으로서 사용될 수 있다. 상기 "건강기능식품"이라 함은 건강기능식품에 관한 법률에 따른 인체에 유용한 기능성을 가진 원료나 성분을 사용하여 제조 및 가공한 식품을 의미하며, "기능성"이라 함은 인체의 구조 및 기능에 대하여 영양소를 조절하거나 생리학적 작용 등과 같은 보건 용도에 유용한 효과를 얻을 목적으로 섭취하는 것을 의미한다.The food composition of the present invention can be used as a health functional food. The term "health functional food" means a food manufactured and processed using raw materials or ingredients useful for the human body in accordance with the Health Functional Food Act, and "functionality" refers to the structure and function of the human body. It refers to ingestion for the purpose of obtaining useful effects for health purposes such as regulating nutrients or physiological effects.
본 발명의 식품 조성물은 통상의 식품 첨가물을 포함할 수 있으며, 상기 "식품 첨가물"로서의 적합 여부는 다른 규정이 없는 한, 식품의약품안전처에서 승인된 식품 첨가물 공전의 총칙 및 일반시험법 등에 따라 해당 품목에 관한 규격 및 기준에 의하여 판정한다.The food composition of the present invention may contain conventional food additives, and the suitability as the "food additive" is determined according to the general rules and general test methods of food additives approved by the Ministry of Food and Drug Safety, unless otherwise specified. It is judged according to the standards and standards related to the item.
상기 "식품 첨가물 공전"에 수재된 품목으로는 예를 들어, 케톤류, 글리신, 구연산칼륨, 니코틴산, 계피산 등의 화학적 합성물, 감색소, 감초추출물, 결정셀룰로오스, 고량색소, 구아검 등의 천연첨가물, L-글루타민산나트륨제제, 면류첨가알칼리제, 보존료제제, 타르색소제제 등의 혼합제제류 등을 들 수 있다.The items listed in the "Food Additives Code" include, for example, chemical compounds such as ketones, glycine, potassium citrate, nicotinic acid, and cinnamic acid; and mixed preparations such as sodium L-glutamate preparations, noodles-added alkalis, preservatives, and tar dye preparations.
본 발명의 식품 조성물은 인지기능 개선, 특히 치매의 예방 및/또는 개선을 목적으로, 조성물 총 중량에 대하여 상기 헴프 껍질 추출물을 0.01 내지 95 %, 바람직하게는 1 내지 80 % 중량백분율로 포함할 수 있다. 또한, 치매의 예방 및/또는 개선을 목적으로, 정제, 캅셀, 분말, 과립, 액상, 환 등의 형태로 제조 및 가공할 수 있다.The food composition of the present invention may include 0.01 to 95%, preferably 1 to 80% weight percentage of the hemp bark extract based on the total weight of the composition for the purpose of improving cognitive function, particularly preventing and/or improving dementia. have. In addition, for the purpose of preventing and / or improving dementia, it may be manufactured and processed in the form of tablets, capsules, powders, granules, liquids, pills, and the like.
예를 들어, 상기 정제 형태의 건강기능식품은 상기 헴프 껍질 추출물, 부형제, 결합제, 붕해제, 및 다른 첨가제와의 혼합물을 통상의 방법으로 과립화한 다음, 활택제 등을 넣어 압축성형하거나, 상기 혼합물을 직접 압축성형할 수 있다. 또한, 상기 정제 형태의 건강기능식품은 필요에 따라 교미제 등을 함유할 수 있으며, 필요에 따라 적당한 제피제로 제피할 수도 있다.For example, the health functional food in tablet form is granulated with a mixture of the hemp bark extract, excipients, binders, disintegrants, and other additives in a conventional manner, and then compression-molded by putting a lubricant, etc., or The mixture can be compression molded directly. In addition, the health functional food in the form of tablets may contain a mating agent, etc., if necessary, and may be coated with a suitable skinning agent if necessary.
캅셀 형태의 건강기능식품 중 경질캅셀제는 통상의 경질캅셀에 상기 헴프 껍질 추출물 및 부형제 등의 첨가제와의 혼합물 또는 그의 입상물 또는 제피한 입상물을 충진하여 제조할 수 있으며, 연질캅셀제는 상기 헴프 껍질 추출물 및 부형제 등의 첨가제와의 혼합물을 젤라틴 등 캅셀기제에 충진하여 제조할 수 있다. 상기 연질캅셀제는 필요에 따라 글리세린 또는 소르비톨 등의 가소제, 착색제, 보존제 등을 함유할 수 있다.Among health functional foods in the form of capsules, hard capsules can be prepared by filling conventional hard capsules with a mixture of the hemp bark extract and additives such as excipients, or their granules or skinned granules. It can be prepared by filling a mixture with additives such as extracts and excipients in a capsule base such as gelatin. The soft capsules may contain a plasticizer such as glycerin or sorbitol, a colorant, a preservative, and the like, if necessary.
과립 형태의 건강기능식품은 상기 헴프 껍질 추출물, 부형제, 결합제, 붕해제 등의 혼합물을 적당한 방법으로 입상으로 제조할 수 있으며, 필요에 따라 착향제, 교미제 등을 함유할 수 있다.The health functional food in the form of granules may be prepared in a granular form by a suitable method of a mixture of the hemp bark extract, excipients, binders, disintegrants, and the like, and may contain flavoring agents, flavoring agents, etc. as needed.
본 발명의 상기 부형제, 결합제, 붕해제, 활택제, 교미제, 착향제 등에 대한 용어 정의는 당업계에 공지된 문헌에 기재된 것으로 그 기능 등이 동일 내지 유사한 것들을 포함한다.The term definitions for the excipients, binders, disintegrants, lubricants, flavoring agents, and the like of the present invention are those described in documents known in the art and include those having the same or similar functions.
이하, 본 발명을 실시예 및 실험예를 통하여 더욱 상세히 설명한다. 그러나, 하기 실시예 및 실험예는 본 발명을 예시하기 위한 것으로, 본 발명의 범위가 이에 제한되는 것은 아니다.Hereinafter, the present invention will be described in more detail through Examples and Experimental Examples. However, the following Examples and Experimental Examples are for illustrating the present invention, and the scope of the present invention is not limited thereto.
실시예 1. 헴프 껍질 추출물의 제조Example 1. Preparation of Hemp Husk Extract
건조된 헴프의 뿌리(30 g), 줄기(30 g) 및 줄기의 껍질(10 g)을 각각 분쇄기를 이용하여 잘게 분쇄하였다. 70 %(v/v) 에탄올을 상기 분쇄된 시료 중량의 10배가 되도록 시료에 가하고, 상온에서 초음파를 이용해 20% 진폭(amplitude)의 강도로 15 분 동안(75.415 kJ) 추출하였다. 추출액을 침적시킨 후 상등액을 따로 포집하고, 잔여물은 다시 70%(v/v) 에탄올을 가하여 추가적으로 2회 반복 추출을 통해 상등액을 얻었다. 수득한 상등액은 여과지(ADVANTEC, No. 2 & No.1)로 감압 여과를 총 2회 수행하고, 여과된 상등액을 감압농축기를 이용하여 용매를 제거한 다음, 동결건조를 통해 건조시켜 냉장보관하였다. 헴프 뿌리의 추출물은 1.7 g (5.7%)를 수득하였고, 헴프 줄기의 추출물은 2.8 g (9.2%)를 수득하였고, 헴프 껍질의 추출물은 0.45 g (4.5%)를 수득하였다.The dried hemp roots (30 g), stems (30 g), and stem bark (10 g) were each finely pulverized using a grinder. 70% (v/v) ethanol was added to the sample so as to be 10 times the weight of the pulverized sample, and extracted for 15 minutes (75.415 kJ) at an intensity of 20% amplitude using ultrasound at room temperature. After immersing the extract, the supernatant was collected separately, and 70% (v/v) ethanol was added to the residue to obtain a supernatant through repeated extraction twice. The obtained supernatant was filtered under reduced pressure with filter paper (ADVANTEC, No. 2 & No. 1) twice in total, and the solvent was removed from the filtered supernatant using a vacuum concentrator, and then dried through freeze-drying and refrigerated. 1.7 g (5.7%) of the extract of hemp root was obtained, 2.8 g (9.2%) of the extract of hemp stem, and 0.45 g (4.5%) of the extract of hemp bark.
실험예 1. 헴프 껍질 추출물의 아세틸콜린에스테라제 및 부티릴콜린에스테라제 저해 효능 평가Experimental Example 1. Evaluation of acetylcholinesterase and butyrylcholinesterase inhibitory efficacy of hemp bark extract
헴프 껍질 추출물을 100 mg/mL이 되도록 DMSO에 용해한 다음, 0, 0.02, 0.05, 0.1, 0.2, 0.5, 1, 2 mg/mL이 되도록 인산염 완충액으로 희석하여 시료를 준비하고 50 μl를 96-웰 플레이트에 분주하였다. 아세틸콜린에스테라제 또는 부티릴콜린에스테라제를 0.5 U/ml로 제조하고, 50 μl를 96-웰 플레이트에 첨가하여 분주된 추출물과 혼합하고 10분간 방치하였다. 기질 물질인 아세틸티오콜린 또는 부티릴티오콜린을 0.4 mg/ml로 제조한 다음 96-웰 플레이트에 50 μl를 첨가하고 20분간 방치하였다. 디티오니트로벤조산(dithionitrobenzoic acid, DTNB)을 1.2 mg/ml로 제조한 다음 96-웰 플레이트에 50 μl를 첨가하고 10분간 방치하였다. 흡광도 공실험(blank)를 위해 아세틸티오콜린 또는 부티릴티오콜린 대신 인산염 완충액(phosphate buffer)을 첨가하여 추출물에 의한 흡광값을 보정하였다(양성대조군 리바스티그민(rivastigmine)).Prepare samples by dissolving hemp hull extract in DMSO to 100 mg/mL, then diluting it with phosphate buffer to 0, 0.02, 0.05, 0.1, 0.2, 0.5, 1,2, 2 mg/mL, and pour 50 μl into 96-well was dispensed on a plate. Acetylcholinesterase or butyrylcholinesterase was prepared at 0.5 U/ml, 50 μl was added to a 96-well plate, mixed with the aliquoted extract, and left for 10 minutes. A substrate material, acetylthiocholine or butyrylthiocholine, was prepared at 0.4 mg/ml, and then 50 μl was added to a 96-well plate and left for 20 minutes. Dithionitrobenzoic acid (DTNB) was prepared at 1.2 mg/ml, and then 50 μl was added to a 96-well plate and left for 10 minutes. For the absorbance blank experiment (blank), the absorbance value by the extract was corrected by adding a phosphate buffer instead of acetylthiocholine or butyrylthiocholine (positive control rivastigmine).
상기와 같이 측정한 아세틸콜린에스테라제(AChE) 저해 효능을 도 1에, 부티릴콜린에스테라제(BuChE) 저해 효능을 도 2에 나타내었고, 하기 표 1에 각 추출물의 IC50 값을 정리하여 기재하였다.The acetylcholinesterase (AChE) inhibitory efficacy measured as described above is shown in FIG. 1, and the butyrylcholinesterase (BuChE) inhibitory efficacy is shown in FIG. 2, and the IC 50 values of each extract are summarized in Table 1 below. and described.
| 추출물extract | IC50 (AChE 활성)IC50 (AChE activity) | IC50 (BuChE 활성)IC50 (BuChE activity) |
| 헴프 뿌리hemp root | >1.0 mg/mL>1.0 mg/mL | >1.0 mg/mL>1.0 mg/mL |
| 헴프 줄기hemp stem | 0.528 mg/mL0.528 mg/mL | 0.061 mg/mL0.061 mg/mL |
| 헴프 껍질hemp husk | 0.553 mg/mL0.553 mg/mL | 0.012 mg/mL0.012 mg/mL |
| 리바스티그민(rivastigmine)Rivastigmine | 1.579 mg/mL1.579 mg/mL | 0.015 mg/mL0.015 mg/mL |
상기 표 1에 기재된 바와 같이, 헴프 껍질 추출물은 헴프 뿌리 추출물, 헴프 줄기 추출물 보다 우수한 아세틸콜린에스테라제 저해 활성 및 부티릴콜린에스테라제 저해 활성을 나타내는 것으로 확인되었다. 특히, 헴프 껍질 추출물은 양성대조군인 리바스티그민보다 우수한 아세틸콜린에스테라제 저해 효능(IC50 0.553 mg/mL)을 나타낼 뿐만 아니라, 리바스티그민보다 우수한 부티릴콜린에스테라제 저해 효능(IC50 0.012 mg/mL)을 나타내어, 인지기능 개선 물질로 유용하게 사용될 수 있을 것으로 기대된다.As shown in Table 1, it was confirmed that the hemp bark extract exhibited superior acetylcholinesterase inhibitory activity and butyrylcholinesterase inhibitory activity than the hemp root extract and hemp stem extract. In particular, the hemp bark extract not only exhibited superior acetylcholinesterase inhibitory efficacy (IC 50 0.553 mg/mL) than rivastigmine, a positive control, but also showed superior butyrylcholinesterase inhibitory efficacy (IC 50 50 mg/mL) than rivastigmine. 0.012 mg/mL), which is expected to be usefully used as a cognitive function improving substance.
전술한 본 발명의 설명은 예시를 위한 것이며, 본 발명이 속하는 기술분야의 통상의 지식을 가진 자는 본 발명의 기술적 사상이나 필수적인 특징을 변경하지 않고서 다른 구체적인 형태로 쉽게 변형이 가능하다는 것을 이해할 수 있을 것이다. 그러므로 이상에서 기술한 실시예들은 모든 면에서 예시적인 것이며 한정적이 아닌 것으로 이해해야만 한다. 예를 들어, 단일형으로 설명되어 있는 각 구성 요소는 분산되어 실시될 수도 있으며, 마찬가지로 분산된 것으로 설명되어 있는 구성 요소들도 결합된 형태로 실시될 수 있다.The description of the present invention described above is for illustration, and those of ordinary skill in the art to which the present invention pertains can understand that it can be easily modified into other specific forms without changing the technical spirit or essential features of the present invention. will be. Therefore, it should be understood that the embodiments described above are illustrative in all respects and not restrictive. For example, each component described as a single type may be implemented in a dispersed form, and likewise components described as distributed may also be implemented in a combined form.
본 발명의 범위는 후술하는 청구범위에 의하여 나타내어지며, 청구범위의 의미 및 범위 그리고 그 균등 개념으로부터 도출되는 모든 변경 또는 변형된 형태가 본 발명의 범위에 포함되는 것으로 해석되어야 한다.The scope of the present invention is indicated by the following claims, and all changes or modifications derived from the meaning and scope of the claims and their equivalents should be construed as being included in the scope of the present invention.
Claims (12)
- 헴프 껍질 추출물을 포함하는 인지기능 개선용 약학 조성물.A pharmaceutical composition for improving cognitive function comprising a hemp bark extract.
- 제1항에 있어서, 상기 헴프 껍질이 헴프 줄기의 껍질인 것을 특징으로 하는 약학 조성물.The pharmaceutical composition according to claim 1, wherein the hemp husk is the husk of a hemp stem.
- 제1항에 있어서, 상기 헴프 껍질 추출물이 C1 내지 C3 알코올 추출물인 것을 특징으로 하는 약학 조성물.The pharmaceutical composition according to claim 1, wherein the hemp bark extract is a C 1 to C 3 alcohol extract.
- 제1항에 있어서, 상기 헴프 껍질 추출물이 에탄올 추출물인 것을 특징으로 하는 약학 조성물.The pharmaceutical composition according to claim 1, wherein the hemp bark extract is an ethanol extract.
- 제1항에 있어서, 상기 헴프 껍질 추출물이 열수 추출, 용매 추출, 초고압 추출, 초임계 추출 및 초음파 추출로 이루어진 군으로부터 선택된 1 이상의 방법을 이용하여 추출된 추출물인 것을 특징으로 하는 약학 조성물.The pharmaceutical composition according to claim 1, wherein the hemp bark extract is an extract extracted using at least one method selected from the group consisting of hot water extraction, solvent extraction, ultra-high pressure extraction, supercritical extraction, and ultrasonic extraction.
- 제1항에 있어서, 상기 인지기능 개선용이 치매 치료 또는 예방용인 것을 특징으로 하는 약학 조성물.The pharmaceutical composition according to claim 1, wherein the cognitive function improvement is for treatment or prevention of dementia.
- 헴프 껍질 추출물을 포함하는 인지기능 개선용 식품 조성물.A food composition for improving cognitive function comprising a hemp bark extract.
- 제7항에 있어서, 상기 헴프 껍질이 헴프 줄기의 껍질인 것을 특징으로 하는 식품 조성물.The food composition according to claim 7, wherein the hemp husk is the husk of a hemp stem.
- 제7항에 있어서, 상기 헴프 껍질 추출물이 C1 내지 C3 알코올 추출물인 것을 특징으로 하는 식품 조성물.The food composition according to claim 7, wherein the hemp bark extract is a C 1 to C 3 alcohol extract.
- 제7항에 있어서, 상기 헴프 껍질 추출물이 에탄올 추출물인 것을 특징으로 하는 식품 조성물.The food composition according to claim 7, wherein the hemp bark extract is an ethanol extract.
- 제7항에 있어서, 상기 헴프 껍질 추출물이 열수 추출, 용매 추출, 초고압 추출, 초임계 추출 및 초음파 추출로 이루어진 군으로부터 선택된 1 이상의 방법을 이용하여 추출된 추출물인 것을 특징으로 하는 식품 조성물.The food composition according to claim 7, wherein the hemp bark extract is an extract extracted using at least one method selected from the group consisting of hot water extraction, solvent extraction, ultra-high pressure extraction, supercritical extraction, and ultrasonic extraction.
- 제7항에 있어서, 상기 인지기능 개선용이 치매 치료 또는 예방용인 것을 특징으로 하는 식품 조성물.The food composition according to claim 7, wherein the cognitive function improvement is for treating or preventing dementia.
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| US20100239693A1 (en) * | 2006-01-18 | 2010-09-23 | Gw Pharma Limited | Cannabinoid-containing plant extracts as neuroprotective agents |
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