WO2008075528A1 - Utilisation de thé de h. macrophylla - Google Patents
Utilisation de thé de h. macrophylla Download PDFInfo
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- WO2008075528A1 WO2008075528A1 PCT/JP2007/072571 JP2007072571W WO2008075528A1 WO 2008075528 A1 WO2008075528 A1 WO 2008075528A1 JP 2007072571 W JP2007072571 W JP 2007072571W WO 2008075528 A1 WO2008075528 A1 WO 2008075528A1
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- 230000014759 maintenance of location Effects 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 239000000401 methanolic extract Substances 0.000 description 1
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- 238000002156 mixing Methods 0.000 description 1
- 230000012666 negative regulation of transcription by glucose Effects 0.000 description 1
- 235000020925 non fasting Nutrition 0.000 description 1
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- 239000003960 organic solvent Substances 0.000 description 1
- 235000020830 overeating Nutrition 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N phenol group Chemical group C1(=CC=CC=C1)O ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 1
- 229960005095 pioglitazone Drugs 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229920001592 potato starch Polymers 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
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- 238000012545 processing Methods 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- 238000003762 quantitative reverse transcription PCR Methods 0.000 description 1
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- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
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- 150000003548 thiazolidines Chemical class 0.000 description 1
- 150000003549 thiazolines Chemical class 0.000 description 1
- 238000004809 thin layer chromatography Methods 0.000 description 1
- COBORSXHAXSETP-UHFFFAOYSA-N thunberginol B Natural products Oc1ccc(cc1)C2=Cc3cc(O)cc(O)c3C(=O)O2 COBORSXHAXSETP-UHFFFAOYSA-N 0.000 description 1
- CFXQRFYFWXTZOJ-QPEQYQDCSA-N thunberginol F Chemical compound O1C(=O)C=2C(O)=CC=CC=2\C1=C\C1=CC=C(O)C(O)=C1 CFXQRFYFWXTZOJ-QPEQYQDCSA-N 0.000 description 1
- NHFGEHLUROYMEB-UHFFFAOYSA-N thunberginol b Chemical compound C=1C(O)=CC(O)=C(C(O2)=O)C=1C=C2C1=CC=C(O)C(O)=C1 NHFGEHLUROYMEB-UHFFFAOYSA-N 0.000 description 1
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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
- A23F—COFFEE; TEA; THEIR SUBSTITUTES; MANUFACTURE, PREPARATION, OR INFUSION THEREOF
- A23F3/00—Tea; Tea substitutes; Preparations thereof
- A23F3/34—Tea substitutes, e.g. matè; Extracts or infusions thereof
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
- A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A23V2300/00—Processes
- A23V2300/20—Freezing
Definitions
- the present invention relates to an antidiabetic composition
- an antidiabetic composition comprising, as an active ingredient, an extract obtained by extracting candy tea with water, a lower alcohol or a mixture thereof.
- the present invention relates to a compound or a salt thereof contained in sweet tea prepared by processing and preparing Amatya or Amagyamachia belonging to the genus Hydrangeaceae Hydrangea in a tea production process including a fermentation process.
- the present invention relates to an antidiabetic composition to be contained.
- adiponectin has been found as a hormone secreted from adipose tissue, and when the hormone is normal, it has the main effects of preventing arteriosclerosis and enhancing insulin sensitivity, but excessive obesity. If abdominal visceral fat accumulates, the secretion of this adiponectin is suppressed, which is an important cause of metabolic syndrome, cardiovascular disease and type 2 diabetes.
- Non-patent document 1 Non-patent document 1).
- diabetes develops regardless of age or sex, and the number of patients and the possibility of diabetes cannot be denied! / The number of people has increased rapidly! /.
- thiazolidine derivatives such as troglitazone and pioglitazone, which are used as diabetes drugs, are potent agonists of the nuclear receptor PPAR ⁇ . Yes, it is thought to improve insulin resistance mainly by acting on PPARy in fat cells. In particular, it has been clarified that these drugs increase blood adiponectin concentration, which leads to improvement of abnormal sugar metabolism (for example, Non-Patent Document 2).
- Hydrangea macrophylla Sen. var. Amgiana Makino is a plant of the genus Saxifragaceae Hydrangea. )), But the plant has sweetness and has been processed and prepared by the tea production process including the fermentation process and used as sweet tea.
- the above-mentioned sweet tea is also known to contain phyllodulcin as a sweetening ingredient (for example, Non-Patent Document 3), and it is also used as a flavoring agent for pharmaceuticals, an oral refresher and a sweetener for diabetics! /, Ru (non-patent document 4).
- phyllodulcin as a sweetening ingredient
- Non-Patent Document 3 Non-Patent Document 3
- Ru non-patent document 4
- Non-Patent Document 1 Kadowaki T. & Yamauchi Satoshi, Endocrine Reviews 2005, 26, 439
- Non-patent document 2 Takashi Kadowaki, Molecular biology of diabetes pathology, Nanzan-do, Tokyo, 2004
- Non-patent document 3 Asahina et al., Pharmaceutical Journal, 54, 314 (1934)
- Non-Patent Document 4 Yoshikawa, Food and Science, 1999, 11, pp. 38-43
- Non-Patent Document 5 Yoshikawa et al., Pharmaceutical Journal, 114, 176-181
- Non-Patent Document 6 Asahina et al., Chem. Pharm. Bull., 63, pp. 429-442 (1930)
- Non-Patent Literature 7 Tsuyoshi Yoshikawa et al., Chem. Pharm. Bull., 42, 225-2230 (1994)
- Non-Patent Literature 8 Tsuji Yoshikawa et al., Heterocycles, 50, 411-418 (1999)
- Non-Patent Document 9 Yagi et al., Chem. Pharm. Bull., 20, 1755-1761 (1972)
- An object of the present invention is to develop a new use of sweet tea.
- the present inventor has focused on the fact that PPAR yagonist promotes the differentiation of adipocyte 3T3-L1 into adipocytes and increases the production of adiponectin, and has been conventionally used as a sweetener for diabetic patients. Began developing new uses for Amacha.
- the present inventor has philozulcin (1), hydrangenol (2), humberginol A (3), humberginol B (4), humberginol F (5), 8- ⁇ _G lc- Regarding the anti-diabetic effect of phyllozulcin (6) or hydrangea acid (7), the accumulation of intracellular neutral lipid (TG) in 3T3-L1 cells was examined as an indicator of differentiation.
- TG intracellular neutral lipid
- any of the above-mentioned compounds (1) to (7) contained in Amazha more particularly, the main components phyllozulcin (1) and hydrangenol (2) have excellent antidiabetic activity. I found out.
- hydrangenol (2) which has been found to have particularly strong activity, has adiponectin concentration in medium and related gene expression and hypoglycemic action in type 2 diabetic mice (KK-A y mice). Was completed.
- an extract obtained by extraction of sweet tea water or lower alcohol or a mixture thereof as an active ingredient, or a processed product thereof, and a pharmaceutically acceptable excipient is provided.
- an antidiabetic composition comprising a carrier is provided.
- an extract of sweet tea or a processed product thereof is provided as an active ingredient for anti-diabetes and can be used safely.
- the sweet tea according to the present invention is a plant belonging to the genus Saxifragaceae hydrangea, which contains the phyllozoresin as a sweetening ingredient (Hydrangea macrophylla Seri nge var. var. amgiana Makino) means a sweet tea that is processed and prepared in a tea-making process including the fermentation process, and is used for beverages.
- the plant that is the raw material of sweet tea includes varieties obtained by these varieties or cultivars that exhibit sweetness in plants that are not limited to Amatya and Amagyamachia containing the above phyllozulcin or its glycoside. Including plants that are
- the above-mentioned sweet tea can be used as it is or after being shredded or pulverized.
- Examples of the solvent used in the preparation of the sweet tea extract or the processed product thereof according to the present invention include water, lower aliphatic alcohols, or a mixture thereof.
- Examples of the lower alcohol other than water include alcohols having 1 to 4 carbon atoms. Specifically, methanol, ethanol, n-propanol, isopropanol, n-butanol, isobutanol or t-butanol or a mixed solution thereof can be used.
- Examples of the mixed solution of water and lower alcohol include the ability to include a mixed solution in an arbitrary ratio thereof, and the above alcohols having a water content of up to 30% by volume are preferable. Of these, methanol, ethanol, or a mixture of these alcohols and water is preferably used.
- one feature of the present invention is that it can be extracted from Amacha using only water.
- the extraction temperature can be arbitrarily set between the boiling points of room temperature and solvent.
- the extraction material is immersed in the extraction solvent and shaken at a temperature from 50 ° C to the boiling point of the extraction solvent.
- the extraction operation may be performed only once for the same material, but the force of repeating multiple times, for example, about 2 to 5 times, is preferable from the viewpoint of extraction efficiency.
- the extract obtained by filtering the solid after the extraction may be concentrated by an ordinary method to obtain an extract. Concentration is preferably performed under reduced pressure. Concentration may be performed until the extract is dry.
- the extract may be used as it is to prepare the composition of the present invention, but may also be used as a powder or a freeze-dried product. A method known in the art can be adopted as a method for obtaining these solids.
- the extract or treated product in the present invention means any of an extract, an extract, a concentrated dried product or a freeze-dried product, but the extract according to the present invention is not purified. It can be used as it is, and constitutes a part of the present invention.
- the extract obtained by concentrating the extract is subjected to partition extraction using a solvent as a processed product, that is, partition extraction using water and water and a non-miscible organic solvent one or more times. It can also be used as an organic solvent-soluble fraction and a water-soluble fraction.
- the above-mentioned extract or its treated product can be subjected to a depressurization-concentration treatment or a purification treatment before or after it at any of the above stages.
- examples of the chromatographic method described above include alumina, normal phase or reverse phase silica gel.
- purification conditions such as the carrier and the elution solvent can be appropriately selected according to various chromatographies.
- the extract of the present invention has the general formula (I):
- R and R are independent of each other, and are the same or different and each represents a hydrogen atom or a hydroxy group.
- R is a carboxy group, or the carboxy group is bonded to the ⁇ -position or ⁇ -position of the phenethyl group or styryl group to form a rataton ring,
- R is a hydroxy group or a gnorecopyranosinoxy group
- R is an elemental hydrogen or a hydroxy group
- An antidiabetic composition comprising a compound represented by the formula or a salt thereof as an active ingredient is provided.
- the extract is a compound of the general formula (I),
- R is R force S methoxy group
- R force S hydroxy group is phenethyl group
- R is force nore
- a oxy group forms a Rataton ring with the ⁇ -position of this phenethyl group, and R is a hydroxy group.
- R is a hydrogen atom
- R is an R force S hydroxy group
- R is a phenethyl group that is a hydrogen atom
- R is a force nore
- a oxy group forms a Rataton ring with the ⁇ -position of this phenethyl group, and R is a hydroxy group.
- R is a hydrogen atom, formula (2):
- R is a styryl group in which R and R are both hydroxy groups, and R is a carboxy group
- R is a styryl group in which R and R are both hydroxy groups, and R is a carboxy group
- R is a styryl group in which R and R are both hydroxy groups, and R is a carboxy group
- R is R force S methoxy group
- R force S hydroxy group is phenethyl group
- R is force nore
- the oxy group forms a rataton ring with the ⁇ -position of this phenethyl group.
- R is an R force S hydroxy group
- R is a styryl group that is a hydrogen atom
- R is a carbo
- An anti-diabetic composition comprising at least one selected compound as an active ingredient is provided.
- the said compound formed by a conventional method has And a salt of a phenolic hydroxy group or carboxy group with an alkali metal such as sodium or potassium.
- the present inventors focused on the fact that PPAR ⁇ agonists promote differentiation of adipocyte 3T3-L1 into adipocytes and increase production of adiponectin. Intracellular neutral lipids in 3T3-L1 cells When searching for anti-diabetic substances using the accumulation of (TG) as an index of differentiation, surprisingly, the above compounds (1) to (7) contained in sweet tea that has been used as a sweetener for diabetics. It has been found that most of them have an antidiabetic action.
- one or more compounds selected from the group consisting of the compounds of the above formulas (1) to (7) are effective.
- a human or veterinary medicine or health food comprising the composition comprising an extract of sweet tea contained as an ingredient or a processed product thereof and a pharmaceutically acceptable excipient or carrier.
- the extract as described above or a processed product or compound thereof (1) to (7) is used as it is, individually or as a mixture, or diluted with an appropriate medium to produce a pharmaceutical product or the like.
- an appropriate medium may be added.
- vehicles include pharmaceutically acceptable excipients such as binders (e.g. syrup, gum arabic, gelatin, sorbitol, tragacanth or polybulurpyrrolidone), fillers (e.g. lactose, sugar, corn starch, Calcium phosphate, sorbitol or glycine), tablet lubricants (eg magnesium stearate, talc, polyethylene glycol or silica), disintegrants (eg potato starch) or wetting agents (eg sodium lauryl sulfate).
- binders e.g. syrup, gum arabic, gelatin, sorbitol, tragacanth or polybulurpyrrolidone
- fillers e.g. lactose, sugar, corn starch, Calcium phosphate, sorbitol or glycine
- tablet lubricants eg magnesium stearate, talc, polyethylene glycol or silica
- disintegrants
- the tablets may be coated by methods well known in normal pharmaceutical practice.
- Liquid formulations may be in the form of, for example, aqueous or oily suspensions, solutions, emulsions, syrups or elixirs and may be provided as dry products that are mixed with water or other suitable excipients before use. Good.
- Such liquid preparations may contain conventional additives such as suspending agents (for example, sorbitol, syrup, methylcellulose, glucose syrup, gelatin, water-added edible fat), edible fats! /, Emulsifiers (for example, Lecithin, sorbitan monooleate or gum arabic), non-aqueous excipients (e.g.
- almond oil fractionated coconut oil or glycerin, oily esters such as propylene glycol or ethylene glycol), preservatives (e.g. p-hydroxy Methyl propyl benzoate or sorbic acid) and, if desired, colorants or fragrances.
- oily esters such as propylene glycol or ethylene glycol
- preservatives e.g. p-hydroxy Methyl propyl benzoate or sorbic acid
- colorants or fragrances e.g. p-hydroxy Methyl propyl benzoate or sorbic acid
- the above health food means a food that is more active than ordinary food, and is intended for health, health maintenance and promotion, for example, liquid or semi-solid, solid products, specifically Examples include powders, granules, tablets, capsules, liquids, and other forms of confectionery such as cookies, rice crackers, jelly, yokan, yogurt, and manju, soft drinks, teas, nutritional drinks, and soups.
- the above extract or a processed product thereof or the compound (1) to (7) is added by mixing, coating, spraying or the like to obtain a health food. I can do it.
- composition according to the present invention can be effectively used as a sugar substitute for humans corresponding to the metabolic syndrome of diabetic patients.
- the amount of the extract or the processed product or compound (1) to (7) used depends on the purpose of use, the degree of the target disease, subjective symptoms, etc. It can be adjusted according to weight, age, etc. For example, in the case of an adult, an extract or extract may contain about 0.01 to 5 g depending on the degree of purification, water content, etc., and about 0.1 mg to about 1 lg for compounds.
- Mouse fibroblasts 3T3-Ll (5 X 10 4 cells / 150 ⁇ L / well) seeded on 48-well plates (Sumilon Celtite C-1 plate 48F, Sumitomo Bakelite Co., Ltd.), 10% bovine fetus The cells were cultured in DMEM medium containing serum (FCS) for 24 hours (37 ° C, 5% CO 2 / air).
- FCS serum
- DMEM high dalcose
- differentiation medium differentiation medium
- DMEM high glucose
- FCS maintenance medium
- test samples compounds
- the culture medium of the above cultured cells is removed, 200 L of purified water is added, the cells are ultrasonically disrupted, and the TG concentration in the disrupted liquid is determined by the enzymatic method (Triglycerase The following table shows the results measured with E test Wako).
- the culture medium of 3T3-L1 cells in Preparation Example 1 was replaced with a maintenance medium, and the concentration of adiponectin released into the medium after 48 hours was measured using a commercially available ELISA kit (R & D). It is shown in the table.
- troglitazone which is a thiazoline derivative and an insulin sensitizer, was used as a control.
- the gene expression analysis was performed using a quantitative RT-PCR apparatus (MiniOptico, Bio-Rad). That is, 3T3-L 10 6 cells / 2 mL / well) were seeded on a 6-well plate, and after 24 hours, changed to a differentiation medium and cultured for 3 days. This medium was replaced with a retention medium, and total RNA was extracted 48 hours later.
- mRNA was synthesized and cDNA was synthesized.
- the following table shows a primer pair of the related gene.
- Antisense 5 -TATGGGTAGTTGCAGTCAGTTGG-3 '(SEQ ID NO: 2)
- PPARr 2 sense 5, -GGTGAAACTCTGGGAGATTC-3 '(SEQ ID NO: 3)
- Antisense 5 -CAACCATTGGGTCAGCTCTTG-3 '(SEQ ID NO: 4)
- GLUT4 sense 5 '-CCTGAGAGCCCCAGATACCTCTAC-3' (SEQ ID NO: 7)
- Antisense 5 '-GTCGTCCAGCTCGTTCTACTAAG-3' (SEQ ID NO: 8) ⁇ -1000 Sensense 5, -ATGGGTCAGAAGGACTCCTACG-3 '(SEQ ID NO: 9)
- Antisense 5'-AGTGGTACGACCAGAGGCATAC-3 5 (SEQ ID NO: 10) [0072] Regarding the primer pair 1 listed in the above table, adiponectin was determined based on G ENEBANK accession number NM009605, and PPARy 2 was determined by Tontonoz P et al., Genes Dev., 1994, May 15 8 (10), 1224-1234, for IL-6 and / 3-actin, Ajuon KM et al., Am. J. Physiol. Regul. Integr. Comp. Physiol., 2005, May; 288 (5), R1220-R1225, and GLUT4 was determined based on McClain DA et al., Am. J. Physiol. Endocrinol Metab., 2005, May; 288 (5), E973-E97 9.
- RT-PCR quantitative reverse transcription PCR
- Compound (2) increases the expression of adiponectin mRNA and PPAR ⁇ 2 mRNA and decreases the expression of IL-6 mRNA, which is one of the adipocytes.
- Compound (2) was also found to have a tendency to increase the expression of insulin receptor GLUT4.
- compound (2) exhibited a gene expression pattern different from that of troglitazone, which is a PPARy agonist, it is presumed that it has a mechanism of action different from that of agonist.
- NIPPON CLEA Co., Ltd. as an in vivo test Compound (2) was administered once a day for 2 weeks to KK-A y mice with a weight of 27-30 g, which were purchased at 5 weeks of age, and orbital veins under ether anesthesia every week The blood was collected using a capillary tube, and blood glucose level, blood neutral fat and blood free fatty acid concentrations at non-fasting were measured.
- Glucose CII test KO (Wako Pure Chemical Industries, Ltd.) was used for blood glucose measurement, and triglyceride E test KO (Wako Pure Chemical Industries, Ltd.) was used for blood neutral fat concentration measurement.
- NEFAC test KOKO (Wako Pure Chemical Industries, Ltd.) was used to determine the free fatty acid concentration in the blood.
- Control 14 360.6 + 18.0 480.0 ⁇ 38.2 538.8 ⁇ 34.7 2) 100 13 332.1 + 21.2 429.3 ⁇ 24.0 483,9 ⁇ 28.4
- the extract of sweet tea according to the present invention containing the compounds (1) to (7) as an active ingredient or a processed product thereof has an anti-diabetic action and is also effective against metabolic syndrome. Turned out to be.
- 1 part by weight of water extract of sweet tea obtained according to a method known in the art is mixed with 3 parts by weight of lactose to obtain a mixture lOOg, filled into gelatin capsules, and gelatin containing 1 500 parts of extract strength S500 mg Capsules were obtained.
- Example 1 1 part by weight of the water extract described in Example 1 was mixed with 3 parts by weight of lactose to obtain a granule lOOg according to a method known in the art.
- a granule lOOg was obtained in the same manner as in Example 2 except that dextrin was used instead of the lactose described in Example 2.
- Granules lOOg was obtained in the same manner as in Example 2 except that crystalline cellulose was used instead of the lactose described in Example 2.
- Example 5 100 g of granules were obtained in the same manner as in Example 2 except that anhydrous glucose was used instead of the lactose described in Example 2.
- Example 1 The water extract described in Example 1 was freeze-dried according to a conventional method to obtain a freeze-dried sweet tea extract.
- the present invention comprises a sweet tea water or lower alcohol as an active ingredient or an extract obtained by extraction with a mixed solution thereof or a processed product thereof, and a pharmaceutically acceptable excipient or carrier.
- An antidiabetic composition is provided and can be used safely.
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Abstract
Le but de l'invention est de développer une nouvelle utilisation du thé d'Hydrangea macrophylla de la variété thunbergii. L'invention concerne une composition anti-diabétique qui comprend un extrait éventuellement traité d'Hydrangea macrophylla de la variété thunbergii avec de l'eau, un alcool inférieur ou un mélange de ces composés en tant qu'ingrédient actif ainsi qu'un excipient ou un véhicule pharmaceutiquement acceptable.
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Cited By (5)
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EP2801357A1 (fr) * | 2013-05-10 | 2014-11-12 | IMD Natural Solutions GmbH | Stilbènes carboxylés destinés à activer l'AMPK et des sirtuines |
KR101662498B1 (ko) | 2015-11-24 | 2016-10-05 | 세종대학교산학협력단 | 수국차 잎으로부터 천연 고감미료인 필로둘신을 수득하는 방법 |
US20190365760A1 (en) * | 2016-11-14 | 2019-12-05 | Keio University | A therapeutic or prophylactic agent for ischemic disease, glaucoma, optic nerve disease, retinal degenerative disease, angiogenic retinal disease, cancer, neurodegenerative or autoimmune disease, and a hypoxia inducing factor inhibitor |
WO2020013397A1 (fr) * | 2018-07-11 | 2020-01-16 | 코스맥스바이오 주식회사 | Composition pour la prévention et le traitement de maladies musculaires, l'amélioration de la fonction musculaire ou l'amélioration de la capacité motrice, ayant un extrait d'hydrangénol ou d'hydrangea en tant que principe actif |
KR20200098042A (ko) * | 2019-02-11 | 2020-08-20 | 코스맥스바이오 주식회사 | 하이드란제놀을 유효성분으로 하는 지방형성 억제 및 체지방 감소용 조성물 |
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EP2801357A1 (fr) * | 2013-05-10 | 2014-11-12 | IMD Natural Solutions GmbH | Stilbènes carboxylés destinés à activer l'AMPK et des sirtuines |
KR101662498B1 (ko) | 2015-11-24 | 2016-10-05 | 세종대학교산학협력단 | 수국차 잎으로부터 천연 고감미료인 필로둘신을 수득하는 방법 |
US20190365760A1 (en) * | 2016-11-14 | 2019-12-05 | Keio University | A therapeutic or prophylactic agent for ischemic disease, glaucoma, optic nerve disease, retinal degenerative disease, angiogenic retinal disease, cancer, neurodegenerative or autoimmune disease, and a hypoxia inducing factor inhibitor |
WO2020013397A1 (fr) * | 2018-07-11 | 2020-01-16 | 코스맥스바이오 주식회사 | Composition pour la prévention et le traitement de maladies musculaires, l'amélioration de la fonction musculaire ou l'amélioration de la capacité motrice, ayant un extrait d'hydrangénol ou d'hydrangea en tant que principe actif |
KR20200006885A (ko) * | 2018-07-11 | 2020-01-21 | 코스맥스바이오 주식회사 | 하이드란제놀 또는 수국속 추출물을 유효성분으로 하는 근육 질환 예방 및 치료, 근기능 개선, 또는 운동수행능력 향상용 조성물 |
KR102113563B1 (ko) | 2018-07-11 | 2020-05-29 | 코스맥스바이오 주식회사 | 하이드란제놀을 유효성분으로 하는 근육 질환 예방 및 치료, 근기능 개선, 또는 운동수행능력 향상용 조성물 |
KR20200098042A (ko) * | 2019-02-11 | 2020-08-20 | 코스맥스바이오 주식회사 | 하이드란제놀을 유효성분으로 하는 지방형성 억제 및 체지방 감소용 조성물 |
WO2020166779A1 (fr) * | 2019-02-11 | 2020-08-20 | 코스맥스바이오 주식회사 | Composition pour l'inhibition de la formation de graisse et la réduction de la graisse corporelle, contenant de l'hydrangénol en tant que principe actif |
KR102173259B1 (ko) * | 2019-02-11 | 2020-11-03 | 코스맥스바이오 주식회사 | 하이드란제놀을 유효성분으로 하는 지방형성 억제 및 체지방 감소용 조성물 |
CN112533580A (zh) * | 2019-02-11 | 2021-03-19 | 科丝美诗生物有限公司 | 以绣球酚作为有效成分的用于抑制脂肪形成和减少体脂的组合物 |
JP2022508234A (ja) * | 2019-02-11 | 2022-01-19 | コスマックス バイオ カンパニー リミテッド | ヒドランゲノールを有効成分とする脂肪形成抑制用及び体脂肪減少用の組成物 |
CN112533580B (zh) * | 2019-02-11 | 2023-07-28 | 科丝美诗生物有限公司 | 以绣球酚作为有效成分的用于抑制脂肪形成和减少体脂的组合物 |
JP7336153B2 (ja) | 2019-02-11 | 2023-08-31 | コスマックス バイオ カンパニー リミテッド | ヒドランゲノールを有効成分とする脂肪形成抑制用及び体脂肪減少用の組成物 |
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