CN103108556A - Ingredients derived from sphaeranthus indicus - Google Patents

Ingredients derived from sphaeranthus indicus Download PDF

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CN103108556A
CN103108556A CN2011800435489A CN201180043548A CN103108556A CN 103108556 A CN103108556 A CN 103108556A CN 2011800435489 A CN2011800435489 A CN 2011800435489A CN 201180043548 A CN201180043548 A CN 201180043548A CN 103108556 A CN103108556 A CN 103108556A
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lactone
extract
composition
yetai
energy
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冈加·拉吉·古卡拉吉
拉玛·拉吉·古卡拉吉
文卡塔·肯纳卡·兰加·拉吉·古卡拉吉
崔姆尔土卢·古兰扣提
吉兰·布帕蒂拉吉
文卡塔·克里斯南·拉吉·阿汝李
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Laila Nutraceuticals
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Abstract

The invention discloses herbal ingredients derived from Sphaeranthus indicus standardized to at least one frullanolide/eudesmanoid sesquiterpene compound and their compositions as natural energy enhancer to provide an onset and steady maintenance of energy and mental alertness in a mammal. The invention further includes the use of ingredients and compositions for food ingredient formulations such as dietary supplement, food ingredient, beverage, snack or energy drink containing the above said herbal ingredient(s) for enhancing physical activity, physical fitness, mental alertness, enhancing energy levels, stamina levels, circulatory health, blood vessel health and for better mental health in warm blooded animal.

Description

Herba Sphaeranthi indici derives composition
Invention field
The invention discloses a kind of medicinal herb components or its composition, be selected from extract and cut derived from least a Er Yetai lactone of being standardized as of Herba Sphaeranthi indici/folium eucalypti lactone sesquiterpenoids, provide the maintenance of energy and the maintenance of brains dexterity as natural energy reinforcing agent in morbidity and stable state in mammal.
The invention further relates to the food composition Formulation Example such as beverage, dietary ingredient formula, snack and the energy drink that comprise above-mentioned medicinal herb components or its composition, be used in morbidity and stable state maintenance energy and brains dexterity, for example strengthen the health, vascular health of physical exertion, healthy, brains dexterity, energy level, endurance level, the circulatory system or more good body and mental health.
Background of invention
Physical exertion as motion, particularly at high temperature, needs the storage of human body carbohydrate, for example muscle glycogen, hepatic glycogen, blood sugar.The loss of water, reallocation and electrolyte loss, and the exhaustion of endogenous carbohydrate deposit be the main cause of the fatigue that affects a personal work ability/fatigue.In order to keep the physiological function of human body, it is very important water, electrolyte, carbohydrate in time and by rights being provided, reaching other nutriments.Fluid infusion in the physical exertion process is in case anti-avulsion water and Gao Re have been proved to be effectively.
The existence that basic strength after all movable backs in people's life and condition are exactly energy.The energy is the most important principle that sustains life, and it the every aspect that exists be all what to need-each behavior needs the energy-thought, sensation, walks, has a meal, drinks water, daydream, breath light.Energy is felt and is experienced on the basis that consumes.Be at table energy that we experience at once after (for example sweet food), the propagation that we obtain after consuming coffee is all the consumption that comes from the body energy storage, rather than comes from its accumulation.Age, fatigue and pressure allow people's anaesthesia vigor.The obstruction of energy can affect people's brains dexterity usually.Suitably solve the body energy demand and can increase a people in place of working and the efficient in personal management.
The people of physical exertion or weakly people strengthen their health performance with dietary supplements, improve the health, and improve their health, reduce the negative consequences of physical exertion, for example the immunologic function of damage and confirmed fatigue or inhibition.
There are at present many energy drinks, nutritious supplementary pharmaceutical and food composition formula on sale on market.Yet, these all be added with disaccharides, carbohydrate compound, protein, amino acid and vitamin and with many other reagent.Many such formulas all show to provide too quickly the instant energy and can not keep and continue for some time.In addition, these formulas all tend to sharply increase blood sugar level, and then being accompanied by is their quick consumption.This may cause the generation of complication sometimes.The natural replenishers that therefore can increase vigorous sensation, general agility, endurance and brains dexterity are in demand.Many research groups in the whole world are devoted to be opened to the research well afoot of the better product that can solve the demand.
Therefore, the present invention is by providing composition or composition that energy and/or brains dexterity can be provided to solve the existing demand in this area.Therefore, the invention provides and to strengthen composition and/or the composition of mammiferous energy level within longer a period of time, strengthen energy level and brains dexterity and solve thus these demands.
Summary of the invention
In a main embodiment, the invention discloses medicinal herb components or its composition, be selected from least a extract and the cut in Er Yetai lactone/folium eucalypti lactone sesquiterpenoids of being standardized as derived from Herba Sphaeranthi indici, be used for maintenance and brains dexterity at morbidity and stable state maintenance energy.The composition that Dai Xingcao is derivative and composition thereof be for the health of the physical exertion that strengthens mammal, healthy, brains dexterity, energy level, endurance level, the circulatory system, vascular health or more good body and mental health.
In another embodiment, the present invention relates to comprise dietary supplements, food composition Formulation Example such as beverage, snack and the energy drink of above-mentioned medicinal herb components or its composition, be used for keeping energy and brains dexterity in morbidity and stable state.This formula is for the health of strengthening physical exertion, healthy, brains dexterity, energy level, endurance level, the circulatory system, vascular health or in better health and the mental health of mammal.
In a further embodiment, extract or cut are standardized as 7-hydroxyl Er Yetai lactone, its analog or its composition, for keeping of energy under sick and stable state; The brains dexterity and be used for to strengthen that physical exertion, healthy, brains dexterity, energy level, endurance level, circulation are healthy, vascular health or be used in the needed better mental health of warm-blooded animal.
In another embodiment, the invention provides composition, comprised be selected from derived from Herba Sphaeranthi indici be standardized as at least a at least a medicinal herb components in Er Yetai lactone/folium eucalypti lactone sesquiterpenoids in conjunction with at least a proof that is selected from extract, cut, reactive compound, phytochemicals the composition derived from plant, animal or microorganism of effective health benefit; Acceptable reagent, active component, vitamin, amino acid and mineral matter pharmaceutically or on diet.
In another embodiment, one or more medicinal herb componentses or its composition derived from Herba Sphaeranthi indici is keeping for energy under sick or stable state; Brains dexterity and physical exertion, healthy, brains dexterity, energy level, endurance level, circulation are healthy in order to strengthen, vascular health or be used in the needed better mental health of warm-blooded animal.
In another embodiment, the invention provides a kind of method that strengthens natural energy source with mammal is provided at sick and stable state under energy keep and the brains dexterity, wherein the method comprises and replenishes or give at least a medicinal herb components that is selected from extract, cut, compound to described mammal; Extract or cut are standardized as derived from the reactive compound of Herba Sphaeranthi indici or its composition.
Description of drawings
Figure I: described the energy sustainability of LI12508 to the swimming parameter in figure.Strip represents time of having a rest, slow traveling time and the number of seconds of fast moving time.Numerical value is with mean value ± standard error, n=6, * P<0.05 and * * p<0.01, (tukey's test and variance analysis) compared with the control.
Figure II: the percentage of having described the energy sustainability of LI2508 in figure.Strip represents the percentage of time of having a rest, slow traveling time and the number of seconds of fast moving time.
Figure III: described energy sustainability-average moving distance (mm) in figure.Strip represents control group and replenishes the average moving distance of the processed group of 100mg/kg body weight or 250mg/kg body weight to animal.Digital with mean value ± standard error, n=6, * * p<0.01, (tukey's test and variance analysis) compared with the control.
Figure IV: described the energy sustainability in figure.The strip representative is by control group and animal processed group (100mg/kg body weight or 250mg/kg body weight).Numerical value is with mean value ± standard error, n=6, * P<0.05, (tukey's test and variance analysis) compared with the control.
Detailed Description Of The Invention
For purpose of the present invention, the phrase that uses in specification of the present invention and claim " medicinal herb components " or " medicinal herb componentses " or " described medicinal herb componentses " refer to extract, cut; At least a extract or cut or its composition in Er Yetai lactone/folium eucalypti lactone sesquiterpenoids of being standardized as derived from Herba Sphaeranthi indici.Phrase " medicinal herb components " or " medicinal herb componentses " can use interchangeably in whole specification and as those of skill in the art understand.
What word " composition " or " compositions " or " mixture " or " mixtures " limited is the combination that is selected from one or more compositions or the other biological active component of extract, cut or compound derived from Herba Sphaeranthi indici.
Phrase " bioactive ingredients " or " bioactive ingredients " refer to for the preparation of other components of composition or are selected from other components derived from the effective healthy extract that is worth of having proved of plant, animal or microorganism, cut, reactive compound, phytochemicals, powder; Acceptable active component, vitamin, amino acid or mineral matter pharmaceutically or on diet.
Phrase " weakling " refers to the individuality that those may suffer or may not suffer disease, and weakness can be physiology or psychological.
Word " main body " or " main bodys " represent the mankind or the mammal of warm-blooded animal, cold-blooded animal, bird, horse, any sex.
The inventor carries out in vitro test and has screened a large amount of plant extracts that are used for the trans fat activity in adipocyte before 3T3-L1 in to the research process of new anti-fat replenishers, and find that the performance of Herba Sphaeranthi indici extract is active except potent trans fat.Studies show that subsequently, Herba Sphaeranthi indici can be improved directly related with obesity, diabetes, angiocardiopathy and other metabolic diseases widely metabolism protein mark consumingly.During studying in vivo, the anti-obesity effect of Herba Sphaeranthi indici is proved in the metabolic syndrome model of the SD big white mouse of fat in diet induced of diet induced.The details of above-mentioned experiment and result of study are in the Indian patent application before the inventor and accordingly in the PCT application 224/CHE/2009 that submitted on February 2nd, 2009; Be described in the PCT/IN2010/000053 that on February 1st, 2010 submitted to.
In the present invention, utilize the standardized 5%7-hydroxyl of Herba Sphaeranthi indici extract Er Yetai lactone (LI12508) and include the standardized 5%7-hydroxyl of Herba Sphaeranthi indici extract Er Yetai lactone in conjunction with the composition (LI12507F) of standardized 10% α of mangosteen extract-mangostin (LI80018) study to assess they in obese people's main body in the double-blind placebo-controlled comparative study as the effect of anti-fat replenishers.Include six fat main body (27.6% male sex in random, double blinding, placebo-controlled study; 72.4% male sex; Age is between 22-50 year) continue 56 days.Participant (BMI30 to 40) is divided into three groups randomly; Placebo, LI12508 group and LI12507F group.The LI12508 of the 600mg/ that the participant takes or two are individually dosed days and the LI12507F preparation of 800mg or two identical Cebo-Capses, and they keep heat keep on a diet (200 card/day) and walking in 30 minutes within the time in 8 weeks.Various parameters comprise physiology, spirit, biochemistry and based on the survey of the assessment that comprises quality of life.Herba Sphaeranthi indici extract (LI12508) and preparation (LI12507F) thereof have significantly reduced body weight and have also shown its latent promise in use at the control serum triglyceride level in two treatment groups.In addition, compare with the placebo treatment group, LI12508 and LI12508 also show except beyond thought and improve quality of life and improve energy, locomitivity and the treatment main body is replenished persistence.This has comprised mobility, has improved walking speed, has increased walking distance, has not thought tired, has felt not tired, feeling relaxed and active.
Be subject to the inspiration of this wonderful result, the inventor has assessed this research product LI12508 and LI12507F for improve the ability of ATP level in cell model.In cell in the cell of processing with LI12508 and LI12507F, the ATP level is to detect for the luminesceence analysis that detects analytical system ATP scaled-down version (Perkinelmer Inc., Waltham, Massachusetts) based on ATP.Briefly, the L6 rat myocyte of equal number is inoculated in each holes of 96 porocyte culture plates and in the DMED that 10%FBS replenishes and cultivates.Cell is processed with specimen (LI12508 and LI12507F) 50pg/ml.Intracellular ATP level is come quantitative assay by the calibration curve of drawing with flat light emission and ATP concentration known, and this result compares with the result that the control treatment sample obtains, such as in table 1 summary.Compared with the control, the standardized 5%7-HF(LI12508 of Herba Sphaeranthi indici extract) and composition (LI12507F) increased significantly ATP level in the rat myocyte.
Energy persistence potential after oral LI12508 is estimated in male and female Switzerland albefaction mouse further.Select the Switzerland albefaction mouse in 20 weeks and check health status, then being divided into three groups, each group comprises 6 (3 male and 3 female).Control animals is processed with oral 0.5%CMC, and processed group is processed a week with day-to-day test compound L I12508100mg/kg or 250mg/kg body weight.At the 7th day, in processing rear 1 hour, adopt SMART video frequency tracking system (Panlab.S.L.U) to utilize to be forced to swim test animal is carried out the test of energy persistence.Time of having a rest and percentage thereof, slowly move and percentage, fast moving and percentage thereof, total swimming path and average speed all utilizes SMART video frequency tracking software to analyze and data are summarised in table 2.
Based on the result that obtains, animal replenish to 100 or the test substrate LI12508 of 250mg/kg in the dose dependent that has for the average time of having a rest reduce.Compared with the control, be significance,statistical to the decreased average to the time of having a rest of observing in processed group.In addition, as in Fig. 1 to 3, compare with control group, the average increase of the slow swimming time in replenishing to two processed group of LI12508 in (100mg/kg and 250mg/kg), quick swimming time and average distance is all also significant.Described in Fig. 4, to compare with control group, the conspicuousness increase of the average speed in the animal that oral 250mg/kg processes is also observed.Average slowly swimming time and the average increase of swimming time fast also show, process the animal of (100mg/kg and 250mg/kg) with LI12508 and more are ready to swim one longer period, but not process at blank the rest of observing in animal.Compare with other two groups, the increase of the average distance that the animal in shorter time relates to has been supported in the increase of the average swimming rate of observing in the animal that 250mg/kgLI12508 processes further.This shows, compare with the control group that 0.5%CMC processes, the animal of processing with LI12508 15 minutes to be forced to during swimming be to enliven very much with energetic, and tend to or swim slowly or rapidly maximum time rather than rest.The longer distance that relates in higher speed and shorter time of having a rest of observing in the animal that LI12508 processes shows, LI12508 raising ability and persistence.Therefore, replenish that the Herba Sphaeranthi indici extract can increase ability level and potential endurance is obviously.
Aforementioned showing, the standardized 5%7-hydroxyl of Herba Sphaeranthi indici Er Yetai lactone and be that strong natural replenishers provide the keeping of the energy of human and animal under sick and stable state, physiological endurance and brains dexterity in conjunction with the composition (LI12507F) of standardized 10% α of mangosteen extract-mangostin.
Therefore, in a main embodiment, the invention discloses medicinal herb components, be selected from derived from least a extract that is standardized as Er Yetai lactone/folium eucalypti lactone sesquiterpenoids of Herba Sphaeranthi indici and cut or its composition and be used for maintenance and brains dexterity at morbidity and stable state maintenance energy.The composition that Dai Xingcao is derivative and composition thereof are for the health that strengthens physical exertion, healthy, brains dexterity, energy level, endurance level, the circulatory system, vascular health or in more good body and the mental health of mammal.
in another embodiment, the invention discloses the composition that is formed in conjunction with at least a bioactive ingredients by the derivative medicinal herb components of Herba Sphaeranthi indici, alternatively with excipient, the composition of diluent or carrier combination, with provide warm-blooded animal or mammal under sick and stable state needed energy keep and brains dexterity bioactive ingredients is selected from the mangosteen pericarp extract, the osmium Ocimum sanctum P.E, the stir-baked CORTEX MAGNOLIAE OFFICINALIS with rhizoma zingiberis recens juice extract, Tribulus terrestris, vitamin, amino acid, taurine, ginkgo biloba p.e, gadol extract and guarana extract.
In another embodiment, the present invention relates to the derivative medicinal herb components of at least a Herba Sphaeranthi indici, be selected from extract or cut and be standardized as 7-hydroxyl Er Yetai lactone, its analog or its mixture as natural energy reinforcing agent, be used for providing the health of enhancing or psychological behavior, energy keeps and the brains dexterity of mammal under sick and stable state.
in also having another embodiment, the present invention relates to a kind of composition, comprise to be selected from and be standardized as at least a combination in medicinal herb components in Er Yetai lactone/folium eucalypti lactone sesquiterpenoids derived from the extract of Herba Sphaeranthi indici or cut and be selected from extract derived from mangosteen, at least a composition in cut or compound, further comprise alternatively and be selected from excipient, diluent, at least a composition in vitamin or amino acid, be used for strengthening health or psychological behavior as natural energy reinforcing agent, under sick or stable state, energy keeps the enhancing physical exertion, healthy, the brains dexterity, energy level, the persistence level, circulation is healthy, vascular health or be used in the better mental health of mammal.
In also having another embodiment, the invention provides composition, comprise that at least a medicinal herb components in extract, cut or the compound that is selected from derived from Herba Sphaeranthi indici is in conjunction with at least a composition in the extract, cut or the compound that are selected from derived from mangosteen, comprise alternatively at least a composition that is selected from excipient, diluent, vitamin or amino acid, be used for to strengthen health or psychological behavior, the keeping and the brains dexterity of mammal of energy under sick or stable as natural energy reinforcing agent.
in another embodiment, the invention provides a kind of composition, comprise be selected from derived from the extract of Herba Sphaeranthi indici or the standardized Er Yetai lactone of cut/folium eucalypti lactone sesquiterpenoids for example at least a medicinal herb components at least a in 7-hydroxyl Er Yetai lactone (1) in conjunction with the standardized α-mangosteen of mangosteen extract (2) or γ-mangosteen (3), health or the psychological behavior of reinforcement also further are provided as natural energy reinforcing agent in conjunction with suitable excipient alternatively, under sick and stable state, energy keeps, the brains dexterity, be used for strengthening physical exertion, healthy, energy level, endurance level, circulation is healthy, vascular health or be used in the better mental health of mammal.
The structure of 7-hydroxyl Er Yetai lactone (1), α-mangosteen (2) and γ-mangosteen (3)
Figure 83767DEST_PATH_IMAGE001
Also having another embodiment, the invention provides a kind of composition, comprise be selected from derived from the extract of Herba Sphaeranthi indici or at least a medicinal herb components in the standardized 5%7-hydroxyl of cut Er Yetai lactone and standardized 10% α of mangosteen extract-mangosteen and suitable excipient be combined provide as natural energy reinforcing agent energy under the muscle power of reinforcement or physiological behavior, sick and stable state keep and mammal in the brains dexterity.
In another important embodiment, the embodiment of the physical behavior of reinforcement comprises the increase of speed, intensity, power, endurance, pliability, agility, balance, emphasis cooperation, reaction time, fatigue recovery and the property endurance of the persistence of increase and increase.The psychological behavior of strengthening comprise improve definition, notice scope, brains dexterity, cognitive function, be heightened in spirits, mental fatigue recovers or reduce (for example following high-intensity physical training).
In another embodiment, the present invention includes mentioned component or its composition dietary supplements, COF Formulation Example such as beverage, snack and energy drink physical exertion, healthy, brains dexterity, energy level, endurance level, circulation are healthy for the preparation of strengthening, vascular health or be used in the needed better mental health of warm-blooded animal.
At another embodiment, the invention provides at least a medicinal herb components in the standardized reactive compound of the extract, cut, compound, extract or the cut that are selected from derived from Herba Sphaeranthi indici/7-hydroxyl Er Yetai lactone or its analog and composition as the natural reinforcing agent of energy stabilization, needed physical behavior in warm-blooded animal.
In another embodiment, extract and/or cut are standardized as 7-hydroxyl Er Yetai lactone, its analog or their composition and are used to strengthen physical exertion or energy level in warm-blooded animal.
In also having another embodiment, the invention provides composition, comprise that bioactive ingredients is in conjunction with being selected from extract, cut, reactive compound, phytochemicals, derived from the powder that has proved effective health benefits of plant, animal or microorganism, one or more compositions in acceptable reagent, active component, microorganism, amino acid or mineral matter pharmaceutically or on diet.
In another embodiment; the invention discloses composition; include the standardized 7-hydroxyl of Herba Sphaeranthi indici extract or cut Er Yetai lactone or its analog in conjunction with at least a bioactive ingredients, be selected from mangosteen extract, osmium Ocimum sanctum P.E, stir-baked CORTEX MAGNOLIAE OFFICINALIS with rhizoma zingiberis recens juice extract, Tribulus terrestris, Cobastab, vitamin C, vitamin E, taurine, ginkgo biloba p.e, rhodiola root and guarana extract.
In another embodiment; the invention discloses composition; by the derivative medicinal herb components of Herba Sphaeranthi indici in conjunction with at least a bioactive ingredients that is selected from mangosteen pericarp extract, osmium Ocimum sanctum P.E, stir-baked CORTEX MAGNOLIAE OFFICINALIS with rhizoma zingiberis recens juice extract, Tribulus terrestris, vitamin, amino acid, taurine, ginkgo biloba p.e, rhodiola root and guarana extract; alternatively in conjunction with excipient, diluent or carrier, as natural energy reinforcing agent provide in warm-blooded animal or in mammal the energy under needed life and stable state keep and the brains dexterity.
In another embodiment, the invention discloses composition, wherein the mangosteen pericarp extract is that at least a combination in standardized α mangostin or γ mangostin or both and optional region excipients/diluents provides keeping of needed energy and brains dexterity as natural energy reinforcing agent in warm-blooded animal or mammal.
In further exemplary embodiment, bioactive ingredients for the preparation of composition in the present invention can further comprise one or more non-limiting components, for example be selected from the vitamin of B family vitamin, comprise thiamine, riboflavin, nicotinic acid, pyridoxol, pantothenic acid, biotin, cyanocobalamin, choline and/or folic acid, the folic acid that comprises the reduction form is such as but not limited to folinic acid, Calciumlevofolinate and methyl tetrahydrofolate.Vitamin B compound is also water soluble vitamin, and it helps carbohydrate breakdown to provide energy for glucose, and the decomposition of fat and protein helps the muscle tone of neural normal operation and stomach and enteron aisle.The particular form of B family vitamin can comprise D-VB5 calcium, niacinamide, pyridoxine hydrochloride, thiamine mononitrate in composition, or amino acid.
In another embodiment, being selected from the derivative medicinal herb components of the Herba Sphaeranthi indici of the standardized 7-hydroxyl of extract or cut Er Yetai lactone or its analog or mixture and/or its composition has increased circulation, metabolic efficiency, adjusting neurotransmitter and has been lifted at oxygen levels in brain.The benefit that increases circulation in brain comprise improvement short-term and long-term memory, increase the reaction time and improve thinking clear.
In also having another embodiment, described medicinal herb components or their composition are for increasing energy level, brains dexterity, endurance level, circulation health and vascular health and are used for providing nutritional support.It also can be as the energy supporting agent in required patient, for example cancer patient or aids patient.In addition, it is used for improving the athletic performance of humans and animals such as Malaysia and China.
In another embodiment, described medicinal herb components and/or their composition can be by the diseases that endurance and composite sports, old and ill people use to increase psychology and health efficient and suppress in the mode of nature easily to suffer from of being engaged in as the elite, as flu, bacterium and virus infections.This composition and composition can be configured to can be used as breakfast or as " healthy beverage " of the conc forms of the conventional beverage that uses.
In another embodiment, naturally, synthetic or semisynthetic 7-hydroxyl Er Yetai lactone or its analog can be used for strengthening health or psychological behavior.
in another embodiment, the one or more analogs that can be used for preparing the 7-hydroxyl Er Yetai lactone of composition comprise the Er Yetai lactone, ll α, 13-dihydro-3 α, 7 alpha-dihydroxy-s-4,5-epoxy-6 β, 7-eudesmanolide, 1l α, 13-dihydro-7 α-acetoxy-3 beta-hydroxy-6 β, 7-eucalyptol-4-lactone, 3-ketone-sagittol, 11 α, 13-dihydro-3 α, 7 alpha-dihydroxy-eucalyptus alkane-4-alkene-6 α, 12-lactone, ll α, 13-dihydro-3 α, 7 alpha-dihydroxy-Er Yetai lactones, 1l α, 13-dihydro-7 α, 13-dihydroxy Er Yetai lactone, ll α, 13-dihydro-7 Alpha-hydroxies-13-methoxyl group Er Yetai lactone, 2 α, 7 alpha-dihydroxy-s-4-alkene-ll, 13-dihydroxy eucalyptol-6,12-lactone, 2 Alpha-hydroxy costic acids, 3-ketone-7 Alpha-hydroxy eucalyptol-4-alkene-6,12-lactone (cryptomeridiol), 4-shows cryptomeriol, the Herba Sphaeranthi indici lactone glycoside, 2 α-hydroxyl Herba Sphaeranthi indici lactone, 2 α-acetoxyl group Herba Sphaeranthi indici lactone, 2 α, 7 alpha-dihydroxy-Herba Sphaeranthi indici lactones, the different Herba Sphaeranthi indici lactone of 2 α-acetoxyl group-7 Alpha-hydroxy Herba Sphaeranthi indici lactone and 2 α-acetoxyl group-5 Alpha-hydroxy.
Derivative 7-hydroxyl Er Yetai lactone or the Er Yetai lactone/folium eucalypti lactone sesquiterpenoids of Herba Sphaeranthi indici in the present invention divides other concentration or total concentration to change in the 0.01%-99.99% scope.
Composition wherein, the concentration of mangosteen pericarp extract, α-mangosteen and γ-mangosteen are respectively or together to change from 0.01% to 99.99%.
In another embodiment, medicinal herb components of the present invention or composition are for strengthening aerobic exercise behavior and ability by lactic acid metabolism and reduction fatigue, and the one or more bio-energy labels of mitigation, include but not limited to ATP level/generation, nitric oxide levels, NADH balance, leptin level, the adipocyte derived peptide.
In another embodiment, medicinal herb components is combined with a plurality of bioactive ingredients further, comprises anti-diabetic, hyperlipidemia disease, anti-obesity, anti-hypertension, antiplatelet aggregative activity, anti-infective, antiatherosclerosis, anti-inflammatory, anti-oxidant and Bioaugnentation is active.
In further exemplary embodiment, said composition can contain a kind of effervescent agent.Be appreciated that effervescent agent is contain the independent of one or more compounds or combine to contact with water the reagent of emitting gas.The gas of emitting is generally oxygen or the most frequently used, carbon dioxide.Preferred effervescent agent is included in acid ingredient and the alkali composition of reaction generation carbon dioxide in water.Acidic components comprise one or more acid, and basic component comprises one or more alkali.Preferably, alkaline constituents comprises alkali metal or alkaline earth metal carbonate or bicarbonate, and acidic components comprise aliphatic carboxylic acid.The non-limiting example that is used for the suitable alkali of alkaline constituents comprises carbonate (for example calcium carbonate), bicarbonate (for example sodium acid carbonate), sesquicarbonate and their mixture.Sodium acid carbonate is preferred alkali.
The non-limiting example of the suitable acid of using in acidic components comprises acid anhydrides, these sour hydrochlorates of citric acid, lactic acid, glutaric acid, phosphoric acid, acetic acid, tartaric acid, malic acid, fumaric acid, adipic acid, butanedioic acid, oxaloacetic acid, this class acid, and their mixture.Citric acid is preferred acid.
In further exemplary embodiment, composition can comprise sweetener.The preferred sweetener that uses in the present invention is Saccharide and saccharide alcohols, for example corn-syrup solids of sucrose, fructose, glucose, maltose, lactose, high fructose, invert sugar, and sugar alcohol comprises D-sorbite, and the mixture of these Saccharide and saccharide alcohols.For the solid of reduced levels is provided, preferably use the more sweetener of the Saccharide and saccharide alcohols of strong sweetness in every dosage.These high intensity sweetners comprise asccharin, cyclamate, acesulfame potassium, L-aspartyl-L-phenylalanine lower alkyl ester sweetener (for example aspartame), L-aspartoyl-D-alanine acid amides, L-aspartoyl-D-Ser acid amides, L-aspartoyl-L-1-hydroxymethyl alkane amide sweetener, L-aspartoyl-1-hydroxyethyl alkane amide sweetener and L-aspartoyl-D-PG ester and acid amides sweetener.The further sweetener that plan disclosed herein is used for composition comprises sweetener derived from stevia rebaudianum, from the sweetener of Momordica grosvenori with from the sweetener of mogroside.A particularly preferred sweetener system is the combination of acesulfame potassium and corn-syrup solids and Sucralose.
In another exemplary embodiment, composition can be dissolved in the liquid that water or other suitable mankind eat
In another embodiment of the present invention, can for the preparation of extract and cut or extraction or cut herbal medicine for example the various suitable solvent of Herba Sphaeranthi indici, mangosteen include but not limited to that C1-C5 alcohol is as ethanol, methyl alcohol, water and their mixture, C1-C7 hydro carbons such as hexane, ester class such as ethyl acetate and analog and their mixture.
In another embodiment, composition of the present invention and composition can be with dried forms, liquid form, food product, dietary supplements or any form for example tablet, capsule or soft masticatories.
In another embodiment, medicinal herb components or composition can be controlled the polymer that discharges by the technology utilization that comprises nanometer technology, microcapsules, colloidal carrier system, other drug induction system and provide for the form of controlling release tablet that is coated with on basis.
as, in another embodiment, the invention provides the composition of medicinal herb components or their nutrition/dietary supplements, can/preparation predetermined with the dosage form of healthy food or as the ground use of specific health food for example, solid food such as chocolate or nutrition bar, semisolid food such as cream or jam or gel, also have beverage and analog such as cold drink, sour milk beverage, drops, candy, chewing gum, the candy of viscosity, sour milk, ice cream, pudding, soft red bean jelly, jelly, biscuit, tea, soft drink, fruit juice, milk, coffee, oatmeal, fast food restaurant and analog.
Flavorant in this composition and invention theory disclosed herein are incoherent, and those skilled in the art is that these widely used flavorants are known in non-Changshu.Therefore, natural and/or combination artificial any flavorant or flavorant is all in the scope of the present disclosure.
In another exemplary embodiment, described composition can comprise further that food color is to improve the visual appearance with the beverage of said composition preparation.
Flavor enhancement or reagent can provide fruity, laughable flavor, vanilla flavored or chocolate flavoured, by way of example rather than by the restriction mode.Sweetener, natural or synthetic, as sweet in sucrose, Aspartame, Sucralose and/or acesulfame potassium, knob, dextrosan, glycerine, D-sorbite, xylitol can use, by way of example, rather than the mode by restriction.Also can add colouring agent.Reagent such as citric acid, fumaric acid, adipic acid, tartaric acid, and lactic acid in some cases can add to adjust tart flavour.
Other compositions in the form of anodyne (for example aspirin), above-mentioned except caffeine slight excitant (as green tea) or loosen agent (as melatonin) and can add in specific product uses.
In other embodiment, medicinal herb components of the present invention and composition are the mitochondrial defects that is used for the treatment of in the human and animal.It also can be used for strengthen or keep health or psychological behavior, the sportsman who reduces physical pressure or non athlete from the infectious disease of the physical exertion of fierceness.In addition, it can be the activator of deacetylase.
in a further exemplary embodiment, on biology acceptable composition or composition can be further with one or more pharmacy or diet on acceptable excipient, carrier and diluent combination comprise glucose, fructose, sucrose, maltose, yellow starch gum, white dextrin, superfine silica gel powder, microcrystalline cellulose, the stearic acid calcium silicates, dolomol, D-sorbite, stevioside, corn syrup, lactose, citric acid, tartaric acid, malic acid, butanedioic acid, lactic acid, L-AA, DL-alpha-tocopherol, glycerine, propane diols, fatty acid glyceride, polyglyceryl fatty acid ester, sucrose fatty ester, sorbitan fatty acid ester, methyl glycol fatty acid ester, Arabic gum, carragheen, casein, gelatin, pectin, agar, the B family vitamin, niacinamide, calcium pantothenate, amino acid, calcium salt, pigment, spices, anticorrisive agent, distilled water, physiological saline, D/W, alcohol, propane diols and polyethylene glycol, various animal oil and vegetable oil, paraffinum molle alba, paraffin and wax.
In another embodiment, the present invention has described a method that improves health or psychological behavior in the mankind and animal, stably keeps energy, physical endurance and brains dexterity especially, and wherein the method comprises at least a medicinal herb components and the composition thereof in the standardized reactive compound of extract, cut, compound, extract or cut derived from Herba Sphaeranthi indici/7-hydroxyl Er Yetai lactone of being selected from from effective dose to the main body of needs that take.The embodiment that improves the health behavior comprises increases endurance and raising speed, intensity, strength, persistence, pliability, flexibility, balance, attention coordination, reaction time, fatigue recovery, reach increasing property endurance.The embodiment that improves psychological behavior comprise improve definition, notice scope, brains dexterity, cognitive function, be heightened in spirits, mental fatigue recovers or reduce (for example following high-intensity physical training).By suitably taking composition or composition, the health of main body or psychological behavior can greatly be strengthened and be with no harmful side-effects.
In another embodiment, the present invention has described especially the extract, cut, compound, extract or the cut that are selected from derived from Herba Sphaeranthi indici and has been standardized as at least a medicinal herb components in reactive compound/7-hydroxyl Er Yetai lactone and the body movement that makes to strengthen warm-blooded animal or the mankind or animal of composition, healthy, brains dexterity, strengthens that energy level, endurance level, circulation are healthy, vascular health and be used for better mental health.
In another other embodiment, be selected from that extract, cut, compound, extract or cut derived from Herba Sphaeranthi indici is standardized as at least a medicinal herb components in reactive compound/7-hydroxyl Er Yetai lactone and composition thereof health in the mankind and animal or psychological behavior, stable energy are kept for the preparation of can be used for strengthening, the use of the medicine of physical endurance and brains dexterity.
These those of ordinary skill in this area should be appreciated that, the example that is applied to these enforcements recited above changes and do not exceed wide in range scope of the present invention.Therefore, be interpreted as, the present invention does not limit disclosed these specific embodiments or example, but is to cover purpose and the interior modification of scope that is included in specification definition of the present invention.
Embodiment 1
The Herba Sphaeranthi indici methanolic extract(LI12500): Herba Sphaeranthi indici fresh idea (1 kg) is put into a round-bottomed flask, and with methyl alcohol (8 L) lixiviate 2 hours at the temperature of 60-65 ℃.Extracting liquid filtering repeats to extract twice to the raw material with mistake with methyl alcohol (2x6 L) under identical condition.Merge extract and fine filtering, and concentrate and obtain residue (110g) in a climbing film evaporator.Show that with HPLC analytical method this methanolic extract (LI12500) contains 11% 7-hydroxyl Er Yetai lactone.
The standardized 5%7-hydroxyl of Herba Sphaeranthi indici methanolic extract Er Yetai lactone
The standardized 5%7-hydroxyl of the Herba Sphaeranthi indici methanolic extract Er Yetai lactone that the above obtains utilizes microcrystalline cellulose and dolomol and 2% weight silica to dilute the standardized 5%7-hydroxyl of the methanolic extract that obtains Herba Sphaeranthi indici powder Er Yetai lactone (LI12508).
Embodiment 2
The Herba Sphaeranthi indici ethanol extract: Herba Sphaeranthi indici fresh idea (1 kg) is put into a RB flask, and with ethanol (8 L) lixiviate 2 hours at the temperature of 60-65 ℃.Extracting liquid filtering repeats to extract twice to the raw material with mistake with ethanol (2x6 L) under identical condition.Merge extract and fine filtering, and concentrate and obtain residue (98g) in a climbing film evaporator.Show that with the HPLC method this ethanol extract contains 12% 7-hydroxyl Er Yetai lactone.
Embodiment 3
Mangosteen pericarp methanolic extract (LI80013):The mangosteen pericarp (1Kg) that dries is ground into corase meal, with 90% methyl alcohol (5L) lixiviate 2 hours at the temperature of 60-65 ℃.By filtering, solvent is separated with raw material.With 90% methyl alcohol (2x3 L ﹠amp; 1x2 L) repeat leaching process 3 times.Merge extract and fine filtering, vacuumize under condition concentrated, and precipitation at room temperature.The isolated by filtration solid obtains dried powder (150g, α-mangostin: 21% and γ-mangostin: 2.5%).
Embodiment 4
Standardized 10% α of mangosteen methanolic extract-mangostin
The mangosteen methanolic extract (embodiment 3) that utilizes microcrystalline cellulose and dolomol and 2% weight silica to dilute the α of including obtained above-mangostin obtains standardized 10% α of mangosteen methanolic extract-mangostin (LI80018).
Embodiment 5
Mangosteen pericarp ethanol extract:The mangosteen pericarp (1Kg) that dries is ground into corase meal, with 90% ethanol (5L) lixiviate 2 hours at the temperature of 60-65 ℃.By filtering, solvent is separated with raw material.With 90% ethanol (2x3 L ﹠amp; 1x2 L) repeat leaching process 3 times.Merge extract and fine filtering, vacuumize under condition concentrated, and precipitation at room temperature.The isolated by filtration solid obtains dried powder (136g, α-mangostin: 22%).
Embodiment 6
Composition LI12506F: prepare composition LI12506F by being combined with the ratio of 3:1 with 90% methanolic extract (LI80013) of mangosteen as the methanolic extract (LI12500) of top prepared Herba Sphaeranthi indici.
Embodiment 7
Preparation LI12507F(Merastin): with the 5%7-hydroxyl Er Yetai lactone (LI12508) of the top prepared standardized minimum of Herba Sphaeranthi indici powder extracts and standardized 10% α of mangosteen methanolic extract-mangostin (LI80018) with the ratio of 3:1 in conjunction with and suitably be mixed to get LI12507F.
Embodiment 8
Composition LI12571F:
Prepare composition LI12517F by the following component of mixing UD:
A Herba Sphaeranthi indici ethanol extract (1g) reaches
Three parts of mangosteen 90% ethanol extracts (3g).
Embodiment 9
Utilize the standardized 5%7-hydroxyl of Herba Sphaeranthi indici extract Er Yetai lactone (LI12508) and contain the standardized 5%7-hydroxyl of Herba Sphaeranthi indici extract Er Yetai lactone in conjunction with standardized 10% α of mangosteen extract-mangostin composition (LI12507F) study, assess they in the double-blind placebo-controlled comparative study in the obese people main body as the effect of anti-fat replenishers.Include six fat main body (27.6% male sex in random, double blinding, placebo-controlled study; 72.4% male sex; Age is between 22-50 year) continue 56 days.Participant (BMI30 to 40) is divided into three groups randomly; Placebo, LI12508 group and LI12507F group.The LI12508 of the 600mg/ that the participant takes or two are individually dosed days and the LI12507F preparation of 800mg or two identical Cebo-Capses, and they keep heat keep on a diet (200 card/day) and walking in 30 minutes within the time in 8 weeks.Various parameters are studied, comprise physiology, spirit, biochemistry and based on the survey of the assessment that comprises quality of life.Herba Sphaeranthi indici extract (LI12508) and preparation (LI12507F) thereof have significantly reduced body weight and have also shown its latent promise in use at control serum triglyceride level processed in two treatment groups.
The impact of the body weight on the quality of life survey scaled-down version (IWQOL scaled-down version) that contains the main body feedback is all observed in each evaluation point all main bodys, comprises 0,14,28 and 56 day.Main body has been expressed the improvement of various parameters, and comprising has increased mobility, has increased walking speed, has increased walking distance and time, feels not tired, feeling relaxed and dynamic.Compare with placebo, the main body quantity of expressing this physical ability and persistent improvement is more in supplementation group.
Compare with placebo, LI12508 and LI12507F show except the quality of life of beyond thought improvement in the processed group of the main body of having carried out replenishing and have strengthened energy, locomitivity and persistence.This comprises has increased mobility, increased walking speed, increase flesh A Le walking distance, do not think tired, feel not tired, feeling relaxed and vigor.
Embodiment 10
In cell in the cell of processing with LI12508 and LI12507F, the ATP level is by detect analytical system ATPlite(Perkinelmer Inc., Waltham, Massachusetts based on ATP) luminesceence analysis detect.Briefly, the L6 rat myocyte of equal number is inoculated in each holes of 96 porocyte culture plates and in the DMED that 10%FBS replenishes and cultivates.Cell was processed 4 hours with the specimen (LI12508 and LI12507F) of variable concentrations, then, added the cell lysis buffer solution of 50 μ l in every hole.Add 0.2% DMSO(v/v in the blank cultured cell).At last, add 50 μ l substrate solutions and at room temperature hatched on oscillator plate 5 minutes in every hole.After 10 minutes, read luminous at dark adaptation in luminometer (multimode reader, Tener Biosys Corp., California Sani Wei Er).With 1*10 -5ATP standard liquid to blank a series of dilutions is applied to the analysis flat board.Intracellular ATP level is come quantitative assay by the calibration curve of drawing with flat light emission and ATP concentration known.
Table 1
Figure 876274DEST_PATH_IMAGE002
Embodiment 11:
Energy persistence ability to Chinese herbal medicine extract in the Switzerland small white mouse is assessed:
Select the Switzerland albefaction mouse in 20 weeks and check health status, conforming before beginning one's study a week.Animal is divided into three groups randomly, and each group comprises 6 (3 male and 3 female), detection material LI12508 and the blank of two dosage (100mg/kg and 250mg/kg body weight).The detection material LI12508 of the oral distribution of animal and one week of blank.Begin swimming exercise (15 minutes) and adhered to every day totally 7 days after processing 1 hour.Allow mouse to swim with the constant load (the fish lead pendant is tied up on tail) of its body weight 10% weight in filling the acrylic resin tank of water.At the 7th day, utilize SMART video frequency tracking system (Panlab.S.L.U) that swimming exercise was followed the trail of in 15 minutes.Utilize distance and the swimming rate of Trancking Software measurement swimming time or time of having a rest, process.Time of having a rest and percentage thereof, slowly move and percentage, fast moving and percentage thereof, total swimming path and average speed all utilizes SMART video frequency tracking software to analyze and data are summarised in table 2.
Such as in Fig. 1 to 2 summary, compare with the control treatment animal groups, 100mg/kg and 250mg/kgLI12508 processed group animal have significant reduction aspect the average time of having a rest, aspect the average distance of average slowly swimming time, average swimming time fast and process, significant increase are being arranged.In addition, as represented in Fig. 4, compare with control group, the animal of the oral processing of 250mg/kg shows except significant increase aspect average speed.
 
Table 2
The potential energy persistence of LI12508 in being forced to the swim test parameter
Figure 656011DEST_PATH_IMAGE003
Numerical value represents with mean value ± standard error, n=6.
* P<0.05 and * * p<0.01, (tukey's test and variance analysis) compared with the control

Claims (14)

1. the derivative medicinal herb components of a Herba Sphaeranthi indici, be selected from least a in the standardized Er Yetai lactone of extract and cut/folium eucalypti lactone sesquiterpenoids, keeping and the brains dexterity of energy under sick and stable state is provided in the warm-blooded animal of needs or mammal as natural energy reinforcing agent.
2. composition, contain the derivative medicinal herb components of at least a Herba Sphaeranthi indici in conjunction with at least a bioactive ingredients, medicinal herb components is selected from least a in extract and the standardized Er Yetai lactone of cut/folium eucalypti lactone sesquiterpenoids, bioactive ingredients is selected from the mangosteen pericarp extract, the osmium Ocimum sanctum P.E, the stir-baked CORTEX MAGNOLIAE OFFICINALIS with rhizoma zingiberis recens juice extract, Tribulus terrestris, vitamin, amino acid, taurine, ginkgo biloba p.e, gadol extract and guarana extract, also contain alternatively excipient, diluent or carrier provides keeping and the brains dexterity of energy under sick and stable state in the warm-blooded animal of needs and mammal as natural energy reinforcing agent.
3. composition, contain the derivative medicinal herb components of at least a Herba Sphaeranthi indici and make natural energy reinforcing agent in conjunction with the standardized α-mangosteen of mangosteen pericarp extract or γ-mangosteen or its both and at least a excipients/diluents keeping and the brains dexterity of energy under sick and stable state is provided in the warm-blooded animal of needs and mammal, medicinal herb components is selected from least a in extract and the standardized Er Yetai lactone of cut/folium eucalypti lactone sesquiterpenoids.
4. the derivative composition of the Herba Sphaeranthi indici of according to claim 1 to 3, wherein standardized compound is selected from 7-hydroxyl Er Yetai lactone, ll α, 13-dihydro-3 α, 7 alpha-dihydroxy-s-4,5-epoxy-6 β, 7-eudesmanolide, 1l α, 13-dihydro-7 α-acetoxy-3 beta-hydroxy-6 β, 7-eucalyptol-4-lactone, 3-ketone-sagittol, 11 α, 13-dihydro-3 α, 7 alpha-dihydroxy-eucalyptus alkane-4-alkene-6 α, 12-lactone, ll α, 13-dihydro-3 α, 7 alpha-dihydroxy-Er Yetai lactones, 1l α, 13-dihydro-7 α, 13-dihydroxy Er Yetai lactone, ll α, 13-dihydro-7 Alpha-hydroxies-13-methoxyl group Er Yetai lactone, 2 α, 7 alpha-dihydroxy-s-4-alkene-ll, 13-dihydroxy eucalyptol-6,12-lactone, 2 Alpha-hydroxy costic acids, 3-ketone-7 Alpha-hydroxy eucalyptol-4-alkene-6,12-lactone (cryptomeridiol), 4-shows cryptomeriol, the Herba Sphaeranthi indici lactone glycoside, 2 α-hydroxyl Herba Sphaeranthi indici lactone, 2 α-acetoxyl group Herba Sphaeranthi indici lactone, 2 α, 7 alpha-dihydroxy-Herba Sphaeranthi indici lactones, the different Herba Sphaeranthi indici lactone of 2 α-acetoxyl group-7 Alpha-hydroxy Herba Sphaeranthi indici lactone and 2 α-acetoxyl group-5 Alpha-hydroxy or its mixture.
5. the derivative composition of according to claim 1 with 2 Herba Sphaeranthi indici, be to obtain from least one plant part, is selected from leaf, fresh idea, stem, root, complete stool or its mixture or by chemical synthesis.
According to claim 1 to 3 desired Chinese herbal medicine extract or cut, wherein extract or the solvent of fractionation is selected from C1-C5 alcohol, C1-C7 hydrocarbon, ester class, water and composition thereof.
7. at least a in desired Herba Sphaeranthi indici extract or the standardized Er Yetai lactone of cut/folium eucalypti lactone sesquiterpenoids according to claim 1 with 2, wherein derived from the concentration of the extract of Herba Sphaeranthi indici and the 7-hydroxyl Er Yetai lactone in cut/other Er Yetai lactone/folium eucalypti lactone sesquiterpenoids for to change respectively or in total scope between 0.01% to 99.99%.
8. according to claim 2 with 3 desired compositions, wherein the concentration of reactive compound, α-mangosteen and γ-mangosteen for or separately or combine and change in the scope between 0.01%-99.99% in the derivative extract of mangosteen or cut.
According to claim 1 to 3 desired medicinal herb components or composition, wherein said composition or composition are formulated as dietary supplements, food composition, beverage, snack or energy drink.
10. according to claim 1 the standardized 7-hydroxyl of the medicinal herb components derived from Herba Sphaeranthi indici Er Yetainei is used for strengthening physical exertion, healthy, brains dexterity warm-blooded animal, strengthens energy level, endurance level, circulation is healthy, blood vessel supervises and for better mental health.
11. composition according to claim 2 is used for strengthening physical exertion, healthy, brains dexterity warm-blooded animal, strengthens energy level, endurance level, circulation is healthy, blood vessel supervises and for better mental health.
12. strengthen the method with the brains dexterity kept that natural energy provides energy under sick and stable state in needed warm-blooded animal and mammal, wherein said method comprises to main body or mammal or the warm-blooded animal medicinal herb components as derivative in desired at least a Herba Sphaeranthi indici in claim 1 to clothes treatment effective dose, is selected from least a in the standardized Er Yetai lactone of extract and cut/folium eucalypti lactone sesquiterpenoids.
13. strengthen the method with the brains dexterity kept that natural energy provides energy under sick and stable state in needed warm-blooded animal and mammal, wherein said method comprises in main body or mammal or the warm-blooded animal composition as desired in claim 2 to clothes treatment effective dose.
14. strengthen the method with the brains dexterity kept that natural energy provides energy under sick and stable state in needed warm-blooded animal and mammal, wherein said method comprises in main body or mammal or the warm-blooded animal composition as desired in claim 3 to clothes treatment effective dose.
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AU2011300376B2 (en) 2015-12-03
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Application publication date: 20130515