TW200533366A - Agonist to human beta3 adrenaline receptor - Google Patents

Abstract

It is intended to provide an agonist to human beta3 adrenaline receptor originating in a natural substance which is a safe material having taken by humans, and a drug for preventing and/or ameliorating life style-related diseases such as fatness, obesity, diabetes, hyperlipemia, hypertension and gout. Namely, an agonist to human beta3 adrenaline receptor which comprises, as the active ingredient, at least one substance selected from among Tropaeolum majus extract, Dioscorea batatas extract, Cyperaceae Scirpus yagara extract and Tinospora capillipes Gagnep. extract. This agonist to human beta3 adrenaline receptor is efficacious as a drug for preventing and/or ameliorating life style-related diseases such as fatness, obesity, diabetes, hyperlipemia, hypertension and gout.

Description

200533366 IX. Description of the invention: [Technical field to which the invention belongs] The present invention relates to human y? 3 adrenal glands, ancient and ancient Chinese swords, and contains the special obesity, obesity, diabetes, Huanchuan and gout Preventive and / or improve agents for lifestyle-related diseases. Intersexual hemorrhage, [prior art] Prisoners are overeating, overnourished, and the population is growing. Obesity, especially obesity caused by internal organs

Obese people with fat obesity will be complicated by lifestyle diseases such as sugar and visceral fat gout with fat accumulation, which will cause a large community: Second disease, hypertension, weight loss can be reduced, 5 ~ 10%, it can be relieved. In addition, if the obese person Yu_ 广 — j ru solves or improves the concurrent life, white = symptom, prevention and / or improvement of obesity is related to prevention and / or improvement of life. Epinephrine receptors are catechin agonists that bind to T-receptors, such as adrenaline or noradrenalne, which are free from the sympathetic nerves. According to the susceptibility to catecholamine agonists, it can be divided into "Lu X body and mitochondria. That is, 0: the sensitivity of the adrenergic receptor to each substance is n-epinephrine epinephrine> dopamine> isopropyl Adrenaline, and the sensitivity of the stone adrenaline receptors is in order isopropyl adrenaline> adrenaline 1 or adrenaline> dopamine. / 3 month Adrenaline receptors have 51/1, cold 2 and 厶 3 receptors, in recent years In the future, the existence of Shi 4 stylistics has also been proposed. Corresponding to the role of each receptor agonist, it is known that '/ 3 1 adrenergic receptor agonist has the effect of increasing the number of heartbeats, and / 5 2 epinephrine receptor The body agonist has the effect of relaxing tracheobronchial smooth muscle, 2230-6842- PF 5 200533366/3 March. The adrenergic receptor agonist has the effect of activating heat production and promoting lipolysis. From the above, it can be known that 'stone 3 adrenaline receptor The agonist is effective for preventing and / or improving lifestyle diseases such as obesity.

The stone 3 adrenergic receptor agonist was first discovered in 1984. It has been confirmed in animal experiments that it has anti-obesity and anti-diabetic effects such as thermogenesis and lipolysis. However, the role of 々3 adrenergic receptor agonists in the human body is weak. It was not until 1989 that the cause of the poor effect was due to the difference in the chemical structure of the rodent 3 adrenergic receptor between rodents such as mice and rats (see Patent Documents 1 and 2). It can be understood from the above that "the selectivity for the adrenergic receptors is higher than that of the adrenergic receptors and the adrenergic receptors for the human stone 3 adrenergic receptors, that is, the selectivity of $ 3 Adrenergic receptor agonists are effective for preventing and / or improving lifestyle habits such as obesity, diabetes, and the like, and their development is expected. Recently, several compounds have been known to be used for selective human spot 3 adrenergic receptor agonist testing (refer to non-specialized donations, and clinical trials have confirmed their effectiveness as anti-fertility anti- # or anti-diabetic drugs. But At present, the human stone 3 adrenergic receptor agonist derived from natural materials with edible experience is still unknown. Nasturtium is a plant of the genus Trollius of the family Ranunculaceae, and there are more than 10 species of golden plum in China. The closely related species of nasturtium, the flower, has a detoxifying effect or has a creeping effect on amygdala, and is used as a flower for making tea (Patent Document 3). / Well 3's plant, its succulent roots are used by folks for nocturia, and the yam is Dioscorea. Since ancient times, it has been known to have strong and nourishing effects.

2230-6842-PF 6 200533366 Essence, night sweats, etc. (refer to Non-Patent Document 4). The two-rowed plant is a plant of the genus Sparganium, which can be classified into the three-winged plant and the three-winged plant. Its rhizomes are in the rhizomes of the closely related species Sparganium stenophyllum Maxim, S. simplex Huds., And S. minimum Hi 11 in Northeast China. It is called Jing Sanling. In addition, Jing Sanling originally referred to the root of the Scirpus yagara Ohwi of the Cyperaceae. These are used as one of menstruation and prolactin (see Non-Patent Document 4). Φ Golden Fruit Sandalwood is a plant of the genus Ti nos pora of the family Tetrapodaceae. The water or ethanol extracts of its roots are administered orally to rabbits and mice, and have thymus atrophy effect, antiparanephric hormone-like effects, and anti-tuberculosis effect. According to Chinese clinical reports, it has antipyretic, anti-inflammatory and analgesic effects on fever caused by influenza, acute tonsillitis, pneumonia, biliary tract infections, and skin suppuration infections, with few side effects. And, Jin Guo Lan is used for acute and chronic tonsillitis, acute pharyngitis, stomatitis, subauritis, mastitis, cecumitis, acute and chronic enteritis, gastritis, blister, etc._Antipyretic, Antidote . It is also used for veterinary medicine such as double goose disease, pink bloat, and anthracnose (see Non-Patent Document 4). However, it is still unknown whether nasturtium, yam, Sanling, and Golden Fruit have human cold 3 adrenergic receptor effects and are effective for preventing and / or improving human lifestyle diseases such as obesity and diabetes. [Non-Patent Literature 1] Takakura Yasunori, Yoshida Junxiu, Japanese Pharmacological Journal, 118, 315 ~ 320, 2001 [Non-Patent Literature 2] C. Weyer, et al., Diabetes &

2230-6842-PF 7 200533366

Metabolism, 25, 11 ~ 21, 1999 [Non-Patent Document 3] Shibata Man (Editor's Representative), World Botanical Textbook, Ping Fansha [Non-Patent Document 4] Mihashi Hiroshi, Primary Color Makino and Han Herbs, Illustrated Book, Beilong Pavilion [ SUMMARY OF THE INVENTION [Disclosure of the invention] (Problems to be solved by the invention) _ The purpose of the present invention is to provide humans with 3/3 adrenergic receptor agonists derived from natural materials with edible experience, and obesity and obesity containing these. Preventive and / or improvement agent for lifestyle-related diseases such as diabetes, diabetes, hyperlipidemia, hypertension, and gout. (Means for solving problems)

The present inventors conducted diligent research in order to solve the above-mentioned problems, and as a result, they found that the nasturtium, yam, Sanling, and Golden Fruit were extracted with a solvent (especially: a solvent having a water-soluble organic solvent) (nasturtium The extract, the yam extract, the triangular prism extract, and the Golden Fruit extract have the effect of human 々3 adrenergic receptor agonist, and completed the present invention. That is, the present invention relates to a human-type 3 adrenergic receptor-promoting scraper, which is at least effective in a group consisting of extracts of nasturtium extract, yam extract, triangular prism extract, and golden fruit locust extract. Composition of ingredients. Furthermore, the present invention relates to a preventive and / or ameliorating agent for lifestyle-related diseases containing the aforementioned human β 3 adrenergic receptor-enhancing J. The present invention relates to administering the above-mentioned human " 3 adrenergic receptor

2230-6842-PF 8 200533366 Method for preventing and / or improving lifestyle-related diseases ′ The present invention is described in detail. 1 The human Θ 3 f adrenergic receptor agonist in February is composed of at least one selected from the group of Golden lotus :: substance, yam extract, triangular prism extract, and golden fruit extract as an active ingredient.人 The human adrenergic receptor agonist of the present invention can be an extract. This can also be a conventional carrier or adjuvant added to the extract, a food and beverage factory, and other pharmaceutical materials that are allowed by pharmacology. Composition of the composition.

As described above, the human / 3 adrenergic receptor agonist is derived from natural materials with experience in use. The golden lotus cesium used in this month is the flower of a plant belonging to the genus Tropoaceae (Tr〇 11 i us). In the present invention, any variety of the genus Globeflower can be used, but a flower of the flower Trollius (Trol i ius chinensi s Bge ·) is preferred. The yam name used in the present invention is Huaishan, which belongs to Dioscoreaceae

The effective agent is the succulent root of the plant (Dioscorea). Any variety of yam can be used in the present invention, but a fleshy root of Dioscorea "ρ〇ηί" Thunb. Is preferred. The rhizomes of the plants of the present invention, Sparganium, are used in the present invention. Sparganium stenophyllum Maxim, s simplex Huds · ), Short black triangular (s. Minimum Hi 丨 丨), long leaf black triangular (s. I〇ngif〇iiumTurcz ·), cyperaceae (Scirpus yagara Ohwi) and other varieties , But preferably S. simplex Huds. 2230-6842-PF 9 200533366 The golden fruit locust used in the present invention is the root of a plant of the genus Tinospora. In the present invention, any variety of the genus Pallidus can be used, but the root tuber of the variety is preferably Tingo Spora capillipes (卯 邛). The nasturtium extract, yam extract, tri-angle extract, and golden fruit extract used in the present invention can be obtained by extracting the above nasturtium, yam, and golden fruit extract with a solvent. Further, in the present invention, if the extract contains no impurities unsuitable for beverages or pharmaceuticals, it can be used as an extract, a crude extract, or a semi-refined extract. When solvent extraction is performed, the burial glands can also be buried. Λ 人 ## tj 由, for example, the flower of Jinda flower, the root of yam, the rhizome of Triangular ridge, and the roots of Golden Fruit Palm are directly or crushed into 1 ~ 2 (^ quantity (weight basis), preferably !: 10 wide in the following extraction solvent, and by giving and / or placing with :, and then filtering or centrifugation to obtain the extract. It may be concentrated to dry The method consists of the following: + / / chen ^ and / to the extract. The solvent can be obtained by removing the solvent from the extraction solution. ^ I is preferably a solvent containing a water-soluble organic solvent. S The solvent with an organic solvent is better. It is only composed of water-soluble, water-soluble, or water-soluble, or a mixture of water-soluble organic solvents and organic solvents. The water-soluble organic solvent is lower than methanol, ethanol, 1-propanol, and 2 = lower grade. Alcohols (for example, especially ethanol is better. ”From the viewpoint of the safety of residual solvents, it is better to measure the percentage of water-soluble organic solvents above ％. Above% is particularly good. That is, from thick

2230-6842-PF

From the viewpoint of 200533366 degrees, it is better to use an aqueous solution on the heart, and the solvent is a water-soluble organic solvent. Capacity > y # # A water solution containing 50% by volume or more of a water-soluble organic solvent is preferred, and a person, ^ li / 0 from above < In addition, it is preferable that the water-soluble organic solvent has a capacity of 9G% by volume or more and 100% by volume or less. + The limit is different. The extraction temperature is extremely high. First, the temperature is usually limited to -2 ～ 0 ～ 10rc, preferably 1 ～ 80C, more preferably 2 ～ 6 (rc. The extraction time is not special. The limitation is usually 0 "hours to i months, and preferably 0.5 hours to 7 days. The evaluation method for the action of human point 3 adrenergic receptor agonists in Benmemin is not particularly limited. For example," can be used " Cells expressing human $ 3 adrenergic receptors were evaluated. That is, human / 3 3 adrenergic receptors were stably expressed in CH0 cells in vitro (lnvitr0) (origin of Chinese hamster ovary) Culture cells) and other animal cells, the extract was added to the cells, and the increase in the concentration of Cyclic ic AMp in the cells was measured for evaluation (A · A · Konkar, etal ·, J. Pharmac 〇1 · Eχρ · Ther ·, 291, 875 ~ 883, 1999; T. Kiso, etal ·, Biol · Parm · Bull ·, 22, 1073 ~ 1078, 1999). Alternatively, human coldness can be expressed in a stable manner as described above. 3 After the adrenoceptor cells were transfected with the cre-LUC reporter gene, the extract was added and the hair was measured. Enzyme activity was evaluated (w. Zheng, etal ·, J. Med. Chem ·, 42, 2287 ~ 2994, 1999; S · S · Vansal & D. R · Feller, Biochem. Pharmacol ·, 58, 807 ~ 810, 1 999). Furthermore, CRE-LUC is a reporter gene obtained by combining luminase (LUC) with cyclic adenosine monophosphate and responsin factor (CRE), which is due to the intracellular 2230-6842-PF 11 200533366% Increase in the concentration of mono-disc acid gland ridges to express luminescent enzymes. Also, 'in the above experimental system, if the cells expressing human θ 1 or / 3 2 adrenaline forks were replaced by those expressing human point 3 adrenaline receptors, Then you can compare the difference between / 5 1, 3, 2 and 3, and you can evaluate the selectivity. Secondly, the preventive and / or ameliorating agent of the lifestyle disease of the present invention contains the above-mentioned human / 3 3 adrenergic receptor agonist The above-mentioned human 5.3 adrenergic receptor agonist of the present invention has a thermogenic activation effect and a lipolytic effect, and can be used as a lifestyle habit of obesity, obesity, diabetes, same-month blood pressure, hypertension, gout and the like. Preventive and / or ameliorative agent for disease. ° Furthermore, the human yj 3 adrenal gland of the present invention Receptor agonists can be selected from at least one of the following symptoms: high body fat rate, high blood pressure, high blood sugar, hypercholesterolemia, hypertriglyceridemia, hypertension, and hyperuricemia. Preventive and / or improver.

The obesity and obesity referred to here are determined based on the obesity: diagnosis criteria of the Japan Obesity Association. In other words, obesity is defined as a person with a mass index of “Mass Index” (body weight index / height On) of 25 or higher. Obesity ^ Fatty fats become poorly healthy or visceral fat type. Visceral fat type Obesity is judged as waist circumference (circle umbilical diameter) is more than 81 for men and more than 90cm for women, or visceral volume of the abdominal beta CT examination of the fly is greater than -IGGcm. Also, the obesity caused The adverse health effects are selected from (") type 2 diabetes, glucose tolerance, lipid metabolism [interstitial urine, gout, gout, (5) coronary artery disease (myocardial infarction, stenosis), and cerebral infarction ( Stroke and transient brain deficiency

2230-6842-PF 12 200533366 (7) Asthenia (Pickwick syndrome) during sleep, (8) Fatty liver (9) Diseases of orthopedics (deformable joint disease, lumbar spondylosis), (10) Menstruation At least one species in the anomalous group. In addition, the above-mentioned obesity includes a state of local body fat ratio of 25% or more for males and 30% or more for females. The type 2 diabetes and glucose tolerance disorders include conditions such as hyperglycemia and hyperinsulinemia. The above-mentioned abnormal lipid metabolism includes states such as hypercholesterolemia, hypertriglyceridemia, hypermuscular cholesterolemia, and low HDL cholesterolemia.

There are preventive and / or ameliorating agents for lifestyle-related diseases such as obesity, obesity, diabetes, hyperlipidemia, hypertension, gout, and the like in humans according to the invention. 3 Prevention of at least one symptom of high body fat rate, high blood M, hyperinsulinemia, hypercholesterolemia, hypertriglyceridemia, hyperlipidemia, and hyperuricemia in adrenaline receptor agonists And / or improving agent (hereinafter referred to as the preventive capping agent of the present invention), which can be used for diet or medicine, and its form is not limited. For example, it can be made into health functional foods (specific foods and nutritional functional foods), health Food, nutritional supplements, functional foods and other food and beverage products, or — ^ '(over-the-counter drug: 0TC) f ^ ¢.

When the preventive and improving agent of the present invention is used as a food or drink, it can be ingested directly, or additives such as conventional carriers or auxiliaries can be used, and they can be used after being formed into an easy-to-take form such as capsules, tinctures, and granules. A // The content of the preventive improving agent of the present invention in these molding agents is preferably 0.1% by weight, more preferably 2 to 95% by weight, and even more preferably 10 to 90% by weight. 2230-6842-PF 13 • 200533366 The preventive and improving agent of the present invention can be mixed with food and beverage materials to make chewing gum, chocolate, candy, fruit bunches, biscuits, crispy biscuits and other snacks; ice cream, iced fruit ice cream Violation s # Hesi water ° σ; tea, refreshing beverages, nutrition drinks, beauty drinks and other beverages; udon noodles, Chinese noodles, Italian noodles, instant noodles and other noodles; fish plate, bamboo wheels, fish cakes and other training products; Oils such as milk marlin and butter; bread, Chinese food, and other food products such as frozen food, frozen food, etc. When the preventive improver of the present invention is ingested in the form of food, its intake is converted into an extract. Per-position λ! Ingestion of 0.00H_mg / kg weight, more preferably Q weight weight. When used as a pharmaceutical, its dosage form is not particularly limited. For example, capsules, tablets, granules, injections, Formulations, patches, etc. When formulated, other pharmacologically acceptable formulation materials can be appropriately added, for example, excipients, disintegrating agents, lubricants, binding agents, antioxidants, colorants, and anticoagulants. Aggregation, absorption Accelerators, dissolution aids, stabilizers, etc. The dosage of these preparations is converted into extracts, preferably UHooomg / kg is administered once per day per adult or divided into several times as follows: 1 ~ 100mg / kg weight ... Use as a quasi-medicine, other additives can be added as needed, for example, ointment, lotion, aerosol, cream, fat 4, face wash ~, cold milk, lotion, A lotion, a bathing agent, etc. are used for local use. The method of preventing and / or improving the lifestyle-related disease of the present invention is described as a human stone 3 adrenergic receptor agonist. In the method, human W Adrenergic receptor agonists can be administered in the form and description of foods, pharmaceuticals, and quasi-drugs.

2230-6842-PF 14 200533366 (Effect of the invention) According to the present invention, a human 30-epinephrine receptor agonist can be obtained from a natural material having experience of ㈡g use. The composition containing ^ ^ 3 is useful as a preventive and / or ameliorating agent for lifestyle-related diseases such as obesity, obesity, diabetes, diabetic hemorrhage, hypertension, pain bugs and the like. [Embodiment] (The best form in which the invention is implemented) Hereinafter, the present invention will be specifically described with examples. ♦ Qiming ', but the present invention is not limited to this specific embodiment. (Example 1) After nasturtium flower (Shinwasan Co., Ltd.) I β ~ Degree A y J was cut into fine chips, it was pulverized with a pulverizer, and 2 g of the pulverized product was 99 5 oh ^ g⑽ · 5 valley 7mg。 %% ethanol / water extraction (room temperature (23 ~ 24 ° C), placed in a dark place for 3 a ,, and / day), filtered, concentrated to dryness, to get nasturtium extract 87. 7mg (Example 2) Extraction of yam's succulent root (Shinwasan Co., Ltd.) powder 2gu 99 5 volume% ethanol / water 10ml (room temperature (23 ~ stage), left in the dark for 3 days), filtered, concentrated Dry solid to obtain yam extract i4 mg. (Example 3) Triangular rhizomes (Shinwa Sansan Co., Ltd.) were cut into fine chips, and then pulverized with a pulverizer, and 2 g of the pulverized product was subjected to QQ R. 0 / Extraction of 10% g 乂 yy · b ethanol in ethanol / water (room temperature (23 ~ 24 ° C), put qg in the dark, and place the valley for d days), filter, concentrate and dry 9mg。 Triangle extract was obtained 17.9mg.

(Example 4) 2230-6842-PF 15 200533366 After cutting the roots of Jinguo Lan (Shinwasan Co., Ltd.) into fine chips, it was pulverized with a pulverizer, and 2 g of the pulverized product was 109.5% by volume ethanol / water 10ml. 3mg。 Extraction (room temperature (23 ~ 24 ° C), placed in the dark for 3 days), filtered, concentrated and dried 'Pay to Jinguolian extract 69.3mg. (Example 5) Human dot 3 adrenergic receptor agonist activity On CHO-K1 cells (cultured cells derived from Chinese hamster ovary), transfection of human / 33 epinephrine receptor gene using lipofectamineTM 2000 (Invitrogen) Plastids were used for the expression of somatic genes to obtain cells that express human adrenergic receptors (hereinafter referred to as / 5 3 / CH0 cells). Experiment day 1: / 3 3 / CH0 cells were implanted into a 96-well culture plate to a concentration of 3 × 104ceiis / well, and cultured at 37 ° C and 5% co2 for about 24 hours. As the medium, an HD medium containing 5% FBS (fetal bovine serum) was used. In addition, the HD medium was composed of Ham F-12 (SIGMA) 5.35 g / L, DMEM (GIBC0) 4.75 g / L, and L-glutamine (Wako Pure Chemical Industries) 0.59 g / L, CaCl2 Compositional composition of 2H20 (Wako Pure Chemical Industries, Ltd.), 44 g / L, and sodium bicarbonate (GIBC0, GIBC0) 1.27 g / L. Lab 2nd day: pCRE-luc (STRATAGEN) was transfected into cells using iipfectamineTM 2000 (Invitrogen). After 6 hours, the medium was changed and cultured overnight. In addition, pCRE-luc is a report plastid obtained by binding a luciferase gene to a cyclic adenosine monophosphate Riespons factor (CRE). Experiment day 3: The medium containing the sample (the scoop obtained from each of the above Examples 1 to 4) was replaced and cultured for 6 hours. Culture of the above-mentioned sample

2230-6842-PF 16 200533366 was added at a volume ratio of 1/1. 00 of the culture medium, and the above-mentioned extracts were each dissolved in DMS0, so that the concentration was as described in Table 1. The untreated control was only DMS0, and the positive control was BRL37344 (TOCRIS) ', which is a selective / 3 3 adrenergic receptor agonist. The cells were washed with linoleic acid buffered saline (pbs +) containing Ca and Mg, and then the luminescence tester LucliteTM (Perkin-Elmer) was added, and the cells were counted in a TopcountTM micro-cold light / fluorescence counter ( perkin_Elmer) to determine the intensity of luminescent enzyme. The ratio of the luminous intensity of the luminescent enzyme to the untreated control φ is taken as the specific luminase activity of the sample. The measurement results of the extracts obtained in Examples 1 to 4 are shown in Table 1. [Table 1] Specific component luminase specific activity (mean + standard deviation, n = 4) Untreated control (DMS0) 0.1 ° / 〇1.00 + 0.05 Positive control (BRL37344) 3nM 1.65 + 0.04 * Example 1 Gold Lotus extract 10 // g / ml 1.67 + 0.22 * Example 2 yam extract 100 β g / ml 2.71 soil 0.21 * Example 3 Triangular extract 100 β g / ml 1. 45 + 0. 07 * Example 4 Golden Fruit Extract —------------ 100 β g / ml 1. 51 + 0.10 * * (P < 0.05) The positive control BRL37344 is considered as the specific activity of luminase Significantly increased. In other words, BRL37344 increased the concentration of adenosine monophosphate in cells through the human / 3 3 adrenergic receptor and expressed luminescent enzyme, which confirmed the human / 3 3 adrenergic receptor agonist action of BRL37344. 2230-6842-PF 17 200533366 Any of the nasturtium extract of Example 1, the yam extract of Example 2, the triangular extract of Example 3, and the golden fruit extract of Example 4 The positive control, BRL37344, is also considered to have a significant increase in specific luminase activity, and is believed to have a human y5 3 adrenergic receptor agonist effect. (Example 6) Binding activity of adrenergic receptors on human cold 1, cold 2, and 3 3 adrenaline receptors on human Wan 1, stone 2, and / 33 adrenaline receptors to inhibit the binding of RI-labeled ligands Tests (MDS Pharma Services # Company: Test Nos. 20401 0, 2041 10, 204200) were evaluated. Table 2 shows the measurement results of the extracts obtained in Examples 1 to 4. [Table 2] Concentration inhibition ratio of main component concentration β 2/33 Example 1 Golden lotus flower extract 50 g / ml 11 ° / 〇33% 71% Example 2 Yam extract bQ βg / ml 18% 0% 66 ° / 〇 Example 3 Triangular Extract 200 // g / ml 23% 4% 76% Example 4 Golden Fruit Extract 50 // g / ml 19 ° / 〇90% 39% 200 / zg / ml 46% 105 % 89% Regarding any of the nasturtium extract of Example 1, the yam extract of Example 2, and the triangular prism extract of Example 3, it is considered to be compared with human stone 1 and β 2 adrenaline receptors. It has strong inhibitory effect on the adrenergic receptor binding. In addition, the extract of Aquilegia officinalis in Example 4 is considered to have stronger binding inhibition to the adrenergic receptors of stone 2 and dot 3 than the adrenergic receptors to human / 51. From the above findings, we can understand the gold of Example 1.

2230-6842-PF 18 200533366 Lotus extract, Yam extract of Example 2, Triangular extract of Example 3, and Golden Fruit extract of Example 4 will bind to human stone 3 adrenaline receptors and present The role of agonists. (Example 7) 5 parts by weight of nasturtium extract, 1000 parts by weight of medium chain fatty acid triglyceride, and 1 part by weight of vitamin E were mixed in the same manner as in Example 1 to prepare gold. Flavoring oil of lotus extract. (Example 8) • 40 parts by weight of yam extract, 40 parts by weight of sodium carboxymethyl cellulose, 15 parts by weight of crystalline cellulose, and 5 parts by weight of vitamin C were mixed and pulverized in the same manner as in Example 2. , Filled in hard gelatin capsules to prepare edible hard capsules containing yam extract. (Example 9) The Triangular extract obtained in the same manner as in Example 3 ^ parts by weight, coconut: ¾ 150 parts by weight, 70% by weight of grape seed oil, and 5 parts by weight of vitamin E were mixed to prepare The second from the right is & 仏. In Table 3 there is an edible soft capsule with a sharp edge.

(Example 10) The weight fraction of the golden fruit extract obtained in the manner similar to that of Example 5 was obtained, 20 parts by weight of horn meal was cooked, and the above was used. 10 parts by weight of olive oil was refined and refined. 5 parts by weight of beeswax, 3 parts by weight of glycerol monostearic acid, 2 parts by weight of cetyl alcohol, 3 parts by weight of hardened polyethylene oxide ramie oil, 10 parts by weight of glycerin, 3 parts by weight of vitamin C, and purified water 42 The parts by weight are mixed and emulsified to prepare a skin cream containing golden fruit extract. [Industrial availability]

2230-6842-PF 19 200533366 According to the invention, the human stone 3 kidney material is used for life habits such as obesity, gout, etc. [Schematic illustration Ml

Can be obtained from natural materials with edible experience adenosine receptor agonists. It is useful to have a preventive and / or ameliorative agent for these constituents, such as obesity, diabetes, hyperlipidemia, hypertension, and disease. [Description of main component symbols]

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Claims (1)

200533366 10. Scope of patent application: ^ A human epinephrine receptor agonist, comprising at least one selected from the group consisting of Jinlianhua ten extracts, yam extracts, triangular prism extracts, and golden fruit extracts One as an active ingredient. 2. The human stone 3 adrenergic receptor agonist as described in item 1 of the scope of the patent application, beans φ | & μ ^ 8T Jinyunhua Pellets System uses nasturtium as a solvent containing a water-soluble organic solvent Extracted. 3. As described in item 1 of the scope of the patent application, the human adrenergic receptor agonist 'is obtained by extracting yam with a solvent containing a water-soluble organic solvent. 4. The human ^ 3 adrenergic receptor agonist as described in item 1 of the scope of patent application, the three materials of the towel are extracted from the three edges with a solvent containing a water-soluble organic solvent. 5. The human 03 epinephrine receptor agonist according to item 1 of the scope of the patent application, wherein the Golden Fruit Extract is obtained by extracting Golden Fruit with a solvent containing a water-soluble organic solvent. 6 · The human / 5 as described in any one of items 2 to 5 of the scope of the patent application. 3 Adrenergic receptor agonists, wherein the solvent containing a water-soluble organic solvent contains a lower alcohol having a carbon number of 1 to 3. 1 〇Capacity% or more. 7. The human dot 3 adrenergic agonist according to any one of items 2 to 6 of the scope of the patent application, wherein the water-soluble organic solvent is contained, and the container contains more than 10% by volume of ethanol. 8 · —A preventive and / or ameliorative agent for lifestyle diseases, which is characterized by containing human points as described in any one of claims 1 to 7 in the scope of patent application 3 soft month 2230-6842-PF 21 • 200533366 Adrenergic receptor agonist. 9. The improving agent described in item 8 of the scope of patent application, wherein the lifestyle disease is freedom of choice / prevention and disease of 1 shellfish disease, hyperlipidemia, hypertension, and obesity caused by gout, obesity , Diabetes I 〇. One kind of free high body fat rate, paleo at least one. Cholesterolemia, hypertriglyceridemia, hyperemia * "Symptoms, high at least in the group] [Prevention of symptoms: urinary dysemia Any one of item i to item 7 of the patent scope = two, which is characterized by containing a nootropic agent. Human Cardiac Adrenaline of 1 is subject to II. Prevention and / or Coverage of a Habitual Disease. Please refer to any of the patent scope items 1 to 7 for application of body stimulants. The method of preventing and / or improving the lifestyle-related diseases described in Item U of the patent scope of Item No. 12, wherein the lifestyle-related diseases are free obesity, obesity, diabetes, dysentery Lipidemia, hypertension, and gout constitute a small to medium group. V 13. —Selection of prevention and / or prevention of at least one symptom in a group consisting of high body fat rate, hyperglycemia, hyperinsulinism, cholesterol, hypertriglyceridemia, hypertension and hyperuricemia The improvement method is characterized by administering a human 30 adrenergic receptor agonist in any one of claims 1 to 7 of the scope of patent application. '2230-6842-PF 22 200533366 7. Designated representative map: (1) The designated representative map of this case is: None (II) The component symbols of this representative map are simply explained: No 8. If there is a chemical formula in this case, please reveal the best display Inventive chemical formula: None 2230-6842-PF 4