KR20130119424A - Ingredients derived from sphaeranthus indicus - Google Patents

Abstract

The present invention is a natural energy enhancer for providing the expression and sustained maintenance of energy and mental arousal in mammals, which is standardized with at least one furanolide / udesmanoid sesquiterpene compound, Plant components derived from Sphaeranthus indicus) and compositions thereof are disclosed. The present invention also relates to the above plant component (s) for promoting physical activity, physical exercise, mental arousal, energy level, endurance level, circulatory health, vascular health, and better mental health in warm blooded animals. And the use of ingredients and compositions for food additive preparations, such as dietary supplements, food additives, beverages, snacks or energy drinks.

Description

INGREDIENTS DERIVED FROM SPHAERANTHUS INDICUS}

The present invention is a natural energy enhancer for providing the expression and sustained maintenance of energy and mental arousal in mammals comprising at least one furulanolide / eudesmanoid sess derived from Sphaeranthus indicus. A plant component or a composition (s) thereof selected from extracts and fractions normalized to quiterpene compound (s).

The invention also provides for the development and sustained maintenance of energy and mental arousal, such as promoting physical activity, physical exercise, mental arousal, energy level, endurance level, circulatory health, vascular health, or better physical and mental health. And food ingredient preparations such as beverages, dietary ingredient preparations, snacks, and energy drinks containing said plant ingredient or composition (s) thereof.

Physical activity, such as exercise, especially in the heat, demands the body's need for carbohydrate storage, such as muscle glycogen, liver glycogen, and plasma glucose. Loss of water, redistribution and loss of electrolytes, and depletion of endogenous carbohydrates are the primary causes of fatigue / fatigue that impair human workability. In order to maintain the physical ability of the human body, it is essential that water, electrolytes, carbohydrates, and other nutrients be provided in a timely and appropriate manner. Fluid replacement during physical activity has proven to be effective in preventing dehydration and high fever.

The basic force and condition behind all activity in human life is the existence of energy. Energy is an essential essence necessary to sustain life, which is necessary for all the sun's existence-every act of using energy-for thought, feeling, walking, eating, drinking, dreaming, breathing, etc. You will feel and experience it as energy is consumed. The energy we experience immediately after a meal (such as sweets), or the hype we get from the consumption of coffee, comes not from the accumulation of energy, but from the consumption of energy from the body's energy stores. Age, fatigue and stress make people feel energy deficient. Drag in this energy very often impairs the mental arousal of the human body. Appropriate energy demands of the human body will increase its efficiency on the job site and in personal care.

Dietary supplements are used by physically active or pharmacological people to increase their physical activity, physical fitness and improve their health, or injuries and chronic fatigue, or suppressed immune function It is used to reduce the potentially negative consequences of physical activity.

Many energy beverages, adjuvants, and food additive formulations are currently available on the market. However, they are completely filled with disaccharides, carbohydrate complexes, proteins, amino acids and vitamins, along with many other ingredients. Many of these agents generate instant energy too quickly and do not hold over long periods of time. In addition, these agents tend to increase blood glucose levels rapidly, followed by rapid depletion. This can sometimes lead to complications. Therefore, there is a great need for natural supplements that improve energetic feeling, general agility, patience and mental arousal. Research is underway in many research groups around the world to develop better products to meet these needs.

Therefore, the present invention meets the need present in the art by providing component (s) or composition (s) that provide energy and / or mental arousal. Accordingly, the present invention provides component (s) and / or composition (s) that can increase energy levels for a long time in a mammal to enhance energy levels and mental arousal, thus addressing this need.

Summary of the invention:

In a major embodiment, the present invention relates to at least one furulanolide / udesmanoid sesquiterpene compound derived from Sphaeranthus indicus for the expression and sustained maintenance of energy and mental arousal. S) herb ingredient selected from extracts and fractions normalized or compositions thereof. The Sparantus-derived ingredients and compositions thereof may be used to enhance physical activity, physical fitness, mental arousal, energy levels, endurance levels, circulatory health, vascular health, or for better physical and mental health in mammals. useful.

In another embodiment, the present invention relates to a dietary supplement, a food additive formulation such as beverages, snacks, and energy drinks containing said ingredient (s) or composition (s) thereof for the expression and sustained maintenance of energy and mental arousal. It is about manufacture. The formulations are useful for enhancing physical activity, physical exercise, mental arousal, energy levels, endurance levels, circulatory health, vascular health in mammals or for better physical and mental health.

In further embodiments, energy in warm-blooded animals; For the manifestation and sustained mental arousal and also to promote physical activity, physical exercise, mental arousal, energy levels, endurance levels, circulatory health, vascular health, or better mental health, the extract or fraction may be 7-hydrated. Roxyfurulanolide, analogs thereof or compositions thereof are standardized.

In another embodiment, the present invention provides an extract (s), fraction (s), active compound (s), plant derived from a plant (s), animal (s), or microorganisms with proven therapeutic health benefits. Chemical (s); At least one furulanoid derived from Sphaeranthus indicus, in combination with at least one component selected from pharmaceutically or dietarily acceptable ingredients, active ingredients, vitamins, amino acids and minerals / A composition as described above comprising at least one plant component selected from extracts and fractions normalized to euesmanoid sesquiterpene compound (s).

In another embodiment, one or more plant components or compositions thereof derived from Sphaeranthus indicus are selected from the group consisting of energy in warm-blooded animals; It is also useful for the manifestation and sustained mental arousal of physical activity, physical exercise, mental arousal, energy levels, endurance levels, circulatory health, vascular health, or even better mental health.

In another embodiment, the present invention provides a method of increasing natural energy to provide expression and sustained maintenance of energy and mental arousal in a mammal, wherein the method is derived from Sphaeranthus indicus. Extracts, fractions, compounds; Supplementing or treating said mammal with at least one plant component or composition thereof selected from extracts or fractions normalized to the active compound.

1 shows the energy endurance ability of LI2508 for swimming parameters. Bars represent rest time, slow motion time and fast motion time in seconds. Values are expressed as mean ± SEM, n = 6. * P <0.05, ** p <0.01 compared to control (ANOVA followed by Turkey's Test)
2 shows the percentage of the energy endurance capacity of LI12508. Bars represent percentages of rest, slow and fast movement times in seconds.
3 shows the energy endurance ability-average travel distance in mm. Bars represent mean shifted by control group and test group of animals supplemented with 100 mg / kg or 250 mg / kg body weight. Values are expressed as mean ± SEM, n = 6. ** p <0.01 compared to control (ANOVA followed by Turkish test)
4 shows energy endurance ability. Bars represent the mean rates seen by animals in control and test groups (100 mg / kg or 250 mg / kg body weight). Values are expressed as mean ± SEM, n = 6. * P <0.05 compared to control (ANOVA followed by Turkish test)

DETAILED DESCRIPTION OF THE INVENTION [

For the purposes of the present invention, the phrase 'herbal ingredient' or 'herbal ingredients' or 'said herbal ingredients' used in the specification and claims of the present invention Extract (s), fraction (s) derived from Sphaeranthus indicus; Extract (s) or fraction (s) or composition (s) thereof standardized with at least one furulanolide / udesmanoid sesquiterpene compound (s). The phrase 'plant component' or 'plant components' are used interchangeably throughout the specification, and the same may be appreciated by those skilled in the art.

The term 'composition' or 'compositions' or 'mixture' or 'mixtures' means extract (s), fractions (derived from Sphaeranthus indicus). Or combinations of one or more components or other biologically active ingredients selected from compound (s).

The terms 'biologically active ingredient' or 'biologically active ingredients' are used to prepare the composition and also include plant (s), animal (s), having proven therapeutic health benefits, Or extract (s), fraction (s), active compound (s), phytochemical (s) derived from a microorganism; Powder (s); It refers to other ingredients selected from pharmaceutically or dietarily acceptable active ingredients, vitamins, amino acids and minerals.

The term 'weak people' means individuals who do or do not suffer from disease, and the weakness may be physical or mental.

The term 'subject' or 'subjects' means warm blooded animals, cold blooded animals, birds, horses, humans or any sex mammal.

In the search for a new anti-obesity adjuvant, we searched a number of plant extracts for anti-lipogenic activity using in vitro assays on 3T3-L1 pre-adipocyte cells. It was found that extracts of Sphaeranthus indicus exhibit potent anti-lipogenic activity. Subsequent studies have shown that Sphaeranthus indicus can strongly improve a wide range of metabolic protein markers directly related to obesity, diabetes, cardiovascular disease and other metabolic diseases. The anti-obesity efficacy of Sphaeranthus indicus has been confirmed in vivo studies in the diet-induced obesity and diet-induced metabolic syndrome models of Sprague Dawley rats. Details of the above experiments and findings can be found in the inventors' prior Indian patent applications and corresponding PCT applications, ie, 224 / CHE / 2009 filed Feb. 2, 2009; PCT / IN2010 / 000053, filed February 1, 2010.

In the present invention, to assess their efficacy as an anti-obesity adjuvant in a double blind placebo controlled study in human volunteers of obesity, a spa standardized with 5% 7-hydroxyfurulanolide Sparanthus indie standardized with 5% 7-hydroxyfurulanolide in combination with Lantus Indicus extract (LI12508) and Garcinia mangostana extract (LI80018) standardized with 10% α-mangostin The study was performed using a composition comprising Curse extract (LI12507F). Sixty obese volunteers (27.6% male; 72.4% female; age 22-50 years old) were included in a 56-day, randomized, double-blind, placebo-controlled trial. Participants ((BMI 30-40) were randomly divided into three groups; placebo, LI12508 group and LI12507F group.Participants took 600 mg / day of LI12508 and 800 mg of LI12507F formulation in two divided doses or two. Taken in the same placebo capsule, and all of them continued calorie-controlled meals (2000 calories per day) and walked for 30 minutes for 8 weeks, including various parameters including physical, anthropomorphic, and biochemical parameters, and A questionnaire based evaluation, including the quality of the questionnaire, was studied: S. indicus extract (LI12508) and its formulation LI12507F provided significant weight loss in both treatment groups and also increased serum triglyceride levels. Indications for potential use in the regulation indicated that both LI12508 and LI12507F were in adjuvant-treated volunteers when compared to placebo treatment groups. It also showed poor improved quality and improved energy, athletic performance and endurance, which resulted in increased mobility, increased walking speed, increased walking distance, no fatigue, no fatigue, a bright and active feeling. Include.

Driven by these surprising results, we evaluated the ability of the test materials LI12508 and LI12507F to enhance ATP levels in cell models. Intracelluar ATP levels in cells treated with LI12508 and LI12507F were measured with an ATP detection assay system based on luminescence, ATPlite (PerkinElmer Inc., Waltham, Mass.). Briefly, the same number of L6 rat myocytes were placed in each well of a 96-well cell culture plate and incubated in DMEM supplemented with 10% FBS. Cells were treated with 50 pg / mL of test samples (LI12508 and LI12507F). From standard curves plotted using luminescent unit versus known concentrations of ATP, intracellular ATP levels were measured quantitatively and the results compared to those obtained from the control treated samples as summarized in Table 1. Both Sparanthus indicus extract (LI12508) and its composition (LI12507F), standardized to 5% 7-HF, significantly increased ATP levels in rat muscle cells when compared to controls.

The male and female energy endurance ability of LI12508 Swiss albino according to oral administration (Swiss albino ) mice were further evaluated. Twenty week-old Swiss albino mice were selected, examined for health, and divided into three groups of six (3 males and three females). For one week, animals in the control group were orally administered with 0.5% CMC, and the treatment group was administered once daily with test substance LI12508 at 100 mg / kg or 250 mg / kg body weight. On day 7, after 1 hour of treatment, energy endurance was tested by a forced swimming test using a SMART video tracking system (Panlab SLU). Rest time and percentage thereof, slow movement and percentage thereof, fast movement and percentage thereof, total path length and average speed of swimming were analyzed using SMART video tracking software and the data are summarized in Table 2. do.

Based on the results obtained, for animals supplemented with test substance LI12508 100 or 250 mg / kg, there was a dose dependent decrease in mean resting time. This mean reduction in resting time observed in the treatment group is statistically significant when compared to the control. In addition, as shown in Figs. 1 to 3, the average increase in slow swimming time, fast swimming time and mean distance in all treatment groups supplemented with LI12508 (100 mg / kg and 250 mg / kg) was also compared with the control group. Significant in comparison. As shown in FIG. 4, a significant increase in mean rate was observed in animals treated at 250 mg / kg p.o compared to the control group. The increase in mean slow swimming time and mean fast swimming time was longer for animals treated with LI12508 (100 mg / kg and 250 mg / kg) to swim for longer periods of time, instead of the rest observed in control animals treated with vehicle. Demonstrates preference for The increase in mean swimming speed observed in animals treated with 250 mg / kg LI12508 further supports the increase in mean distance covered by the animals within a shorter time compared to the other two groups. This indicates that animals treated with LI12508 were very active and energetic for 15 minutes of forced swim time, and also tended to swim slowly or quickly for most of the time rather than resting compared to the control group treated with 0.5% CMC. Indicates. Longer distances covered and shorter resting times at higher speeds observed in animals treated with LI12508 indicate that LI12508 improves energy and endurance. Thus, it is clear that Sparanthus indicus extract can increase energy levels and endurance.

The results indicate that the composition of the Slantus indicus extract (LI12508) standardized with 5% 7-hydroxyfurulanolide (LI12508) and its composition (LI12507F) in combination with the Garcinia mangostana extract standardized with 10% α-mangosteen It demonstrates that it can be a powerful natural supplement that provides the expression, sustained maintenance of energy, physical endurance and mental arousal in animals.

Thus, in a major embodiment, the present invention provides at least one furulanolide / udesmanoid sesquiterpene compound derived from Sphaeranthus indicus for the expression and sustained maintenance of energy and mental arousal Disclosed is a plant component or composition (s) thereof selected from extracts and fractions normalized to (s). Ingredients derived from the sparantus and compositions thereof are useful for enhancing physical activity, physical exercise, mental arousal, energy levels, endurance levels, circulatory health, vascular health in mammals, or for better physical and mental health. .

In another embodiment, the present invention is a natural energy enhancer for providing expression and sustained maintenance of energy and mental arousal in warm-blooded animals or mammals, Garcinia mangostana fruit peel extract, Osmium basilisum basilicum, Zingiber officinalis, Tribulus terrestris, vitamins, amino acids, taurine, Ginkgo biloba extract, Rhodiola and guarana extract Disclosed are compositions comprising plant components derived from Sphaeranthus indicus in combination with at least one biologically active ingredient selected from, and optionally comprising additives, diluents or carriers.

In another embodiment, the present invention provides a natural energy enhancer for providing enhanced physical and mental activity, expression of energy and mental arousal and sustained maintenance in mammals, wherein the extract is standardized with 7-hydroxyfurulanolide or an analog thereof. And plant components derived from at least one Sphaeranthus indicus selected from fractions, or mixtures thereof.

In another embodiment, the present invention enhances the expression and sustained maintenance of energy to promote physical or mental activity, physical activity, physical exercise, mental arousal, energy level, endurance level, circulatory health, vascular health in a mammal or Or from Sparantanthus indicus in combination with at least one component selected from extracts, fractions or compounds derived from Garcinia mangostana as a natural energy enhancer for better physical and mental health. At least one plant component selected from extracts or fractions standardized with at least one furulanolide / eudesmanoid sesquiterpene compound (s) derived, and optionally from additives, diluents, vitamins or amino acids. A composition comprising at least one component selected.

In another embodiment, the present invention provides a natural energy enhancer for promoting physical or mental activity, expression and sustained maintenance of energy and mental arousal in a mammal, comprising extracts, fractions or derived from Garcinia mangostana. At least one plant component selected from extracts, fractions or compounds derived from Sphaeranthus indicus in combination with at least one component selected from the compounds, optionally from additives, diluents, vitamins or amino acids Provided are compositions comprising at least one component selected.

In another embodiment, the present invention provides for physical or mental activity, energy that enhances physical activity, physical exercise, energy levels, endurance levels, circulatory health, vascular health in mammals or for better physical and mental health. , At least one furulanolide, such as 7-hydroxyfurulanolide (1) derived from Sphaeranthus indicus, as a natural energy enhancer to provide the manifestation and sustained maintenance of mental arousal Garcinia mangostana standardized with at least one plant component selected from extracts or fractions standardized with the eudesmanoid sesquiterpene compound, and α-mangosteen (2) or γ-mangosteen (3). ) Extract and optionally a suitable additive.

In another embodiment, the present invention provides a natural energy enhancer for providing expression and sustained maintenance of enhanced physical or mental activity, energy and mental arousal in a mammal, and is derived from Sphaeranthus indicus. Provided is a composition comprising at least one plant component selected from extracts or fractions standardized with% 7-hydroxyfurulanolide and Garcinia mangostana extract standardized with 10% α-mangosteen and suitable additives. do.

In another important embodiment, examples of enhanced physical activity include increased endurance and improved speed, stamina, strength, patience, flexibility, agility, balance, focus coordination, reaction time, fatigue recovery, Includes an increase in sexual energy. Examples of enhanced mental activity include improved sharpness, attention span, mental arousal, cognitive function, mood elevation, and recovery of mental fatigue (eg, due to high-intensity physical exercise) or Includes reduction.

In another embodiment, the present invention provides the above component (s) for improving physical activity, physical fitness, mental arousal, energy level, endurance level, circulatory health, vascular health, or even better mental health in warm blooded animals. ) Or the preparation of dietary supplements such as beverages, snacks and energy drinks, food additive formulations comprising the composition (s) thereof.

In another embodiment, the invention relates to extract (s), fraction (s), compound (s), activity derived from Sphaeranthus indicus as a natural enhancer of immediate energy, physical activity in warm blooded animals. Provided are at least one plant component and composition selected from extracts or fractions normalized to Compound (s) / 7-hydroxyfurulanolide or analogs thereof.

In other embodiments, extracts and / or fractions or compositions thereof standardized with 7-hydroxyfurulanolide, analogs thereof, may be used to enhance physical activity or energy levels in warm blooded animals.

In another embodiment, the invention provides extract (s), fraction (s), active compound (s), phytochemistry derived from plant (s), animal (s), or microorganisms with proven therapeutic health benefits. Substance (s); Powder (s); A composition is provided comprising a biologically active ingredient in combination with one or more ingredients selected from pharmaceutically or dietarily acceptable ingredients, active ingredients, vitamins, amino acids and minerals.

In another embodiment, the invention provides Garcinia mangostana extract, Osmium basilicum, Zingiber officinalis, Tribulus terrestris, Vitamin B 7-hydroxypuranolide, in combination with at least one biologically active ingredient selected from vitamin C, vitamin E, taurine, Ginkgo biloba extract, Rhodiola and guarana extract Or a composition comprising a Sparantus indicus extract or fraction standardized to an analog thereof.

In another embodiment, the present invention provides a natural energy enhancer for providing expression and sustained maintenance of energy and mental arousal in warm blooded animals or mammals, Garcinia mangostana fruit peel extract, Osmium basilisum basilicum, Zingiber officinalis, Tribulus terrestris, vitamins, amino acids, taurine, Ginkgo biloba extract, Rhodiola and guarana extract Disclosed are compositions consisting of plant components from Sphaeranthus indicus, optionally in combination with at least one biologically active ingredient selected from, and optionally in combination with additives, diluents or carriers.

In another embodiment, the present invention provides a natural energy enhancer for providing expression and sustained maintenance of energy and mental arousal in warm-blooded animals or mammals, wherein Garcinia mangostana fruit peel extract is α-mangosteen or γ. Discloses compositions standardized to mangosteen or both and optionally optionally combined with at least one additive / diluent.

In a further exemplary embodiment, the biologically active ingredient of the present invention for preparing the composition is B vitamins, including thiamin, riboflavin, niacin, pantothenic acid, pyridoxine, biotin, sinanocobalamin, folinic acid, calcium poly Non-limiting ingredients such as vitamins selected from choline and / or folic acid, including reduced forms of folic acid such as, but not limited to, calcium folinate and methyltetrahydrofolate; It may further comprise a species or more. B-complex vitamins are also water-soluble to help break down carbohydrates into glucose to provide energy to the body, break down fats and proteins to help normal function of the nervous system, and muscle tone in the stomach and intestines. It is a vitamin. Specific forms of the B vitamins in the composition include d-calcium pantothenate, niacinamide, pyridoxine hydrochloride, and thymine mononitrate; Or amino acids.

In another embodiment, plant components or mixtures thereof and / or composition (s) derived from Sphaeranthus indicus selected from extracts or fractions standardized with 7-hydroxyfurulanolide or analogs thereof Increases circulation, metabolic efficiency, regulates neurotransmitters, and raises oxygen levels in the brain. Benefits of enhanced circulation in the brain include improved short and long term memory, increased response time and increased mental clarity.

In another embodiment, the plant component or composition (s) thereof is not only useful for enhancing energy levels, mental alertness, endurance levels, circulatory health and vascular health, but also for providing nutritional support. It can also be used as an energy booster for patients, for example cancer patients or AIDS patients. It is also useful for enhancing motor activity in humans and animals, such as horses.

In another embodiment, the plant component and / or composition (s) thereof are prepared in a natural manner by, for example, athletes, endurance and people engaged in multi-discipline sports, the elderly and patients. As well as to increase mental and physical efficiency and to inhibit susceptibility to diseases such as colds, bacterial and viral infections. The components and compositions of the present invention may be formulated as "fitness drinks" which may be taken with breakfast, or may be formulated in the form of concentrates, in which such drinks may be used regularly.

In other embodiments, naturally obtained, synthesized, or semi-synthesized 7-hydroxyfurulanolide or an analog thereof is useful for physical or mental activity.

In another embodiment, the one or more analogues of 7-hydroxyfurulanolide that can be used to prepare the composition include frullanolides; 11α, 13-dihydro-3α, 7α-dihydroxy-4,5-epoxy-6β, 7-udedesmanolide (11α, 13-dihydro-3α, 7α-dihydroxy-4,5-epoxy-6β, 7-eudesmanolide); 11α, 13-dihydro-7α-acetoxy-3β-hydroxy-6β, 7-udesme-4-enolide (11α, 13-dihydro-7α-acetoxy-3β-hydroxy-6β, 7-eudesm- 4-enolide); 3-keto-β-eudesmol; 11α, 13-dihydro-3α, 7α-dihydroxyudesme-4-ene-6α, 12-oxide (11α, 13-dihydro-3α, 7α-dihydroxyeudesm-4-en-6α, 12-olide ); 11α, 13-dihydro-3α, 7α-dihydroxyfurulanolide (11α, 13-dihydro-3α, 7α-dihydroxyfrullanolide); 11α, 13-dihydro-7α, 13-dihydroxyfurulanolide (11α, 13-dihydro-7α, 13-dihydroxyfrullanolide); 11α, 13-dihydro-7α-hydroxy-13-metaoxyfurulanolide (11α, 13-dihydro-7α-hydroxy-13-methaoxyfrullanolide); 2α, 7α-dihydroxy-4-ene-11,13-dihydroudesume-6,12-oxide (2α, 7α-dihydroxy-4-en-11,13-dihydroeudesm-6,12-olide ); 2α-hydroxycostic acid; 3-keto-7α-hydroxyeudesm-4-en-6,12-olide (cryptomeridiol); 4-epicryptomeridiol; Sparanthanolide; 2α-hydroxysphaerantholide; 2α-acetoxysphaerantholide; 2α, 7α-dihydroxysphaerantholide; 2α-acetoxy-7α-hydroxysphaerantholide and 2α-acetoxy-5α-hydroxyisosphatorantholide.

In the present invention, the concentrations of 7-hydroxyfurulanolide or furulanolide / udesmanoid sesquiterpene compounds derived from Sphaeranthus indicus range from 0.01% to 99.99%, respectively or together. .

In the composition, the concentrations of Garcinia mangostana fruit peel extract, α-mangosteen and γ-mangosteen, respectively or together, range from 0.01% to 99.99%.

In another embodiment, the plant component (s) or composition (s) of the present invention comprise: ATP levels / generation; Aerobic activity by affecting lactic acid metabolism and reducing fatigue, as well as for reducing one or more biological energy markers, including but not limited to nitric oxide levels, NADH balance, leptin levels, adipocyte derived peptides And to improve the ability.

In another embodiment, the plant component (s) are anti-diabetic activity, anti-hyperlipidemic activity, anti-obesity activity, anti-hypertensive activity, anti-platelet aggregation activity, anti-infective activity, anti-atherogenic activity, It may further be combined with one or more active ingredients, including anti-inflammatory activity, anti-oxidative activity and bio-enhancing activity.

In further exemplary embodiments, the composition may comprise a blowing agent. As will be appreciated, the blowing agent is a material which, individually or together, comprises one or more compounds which release gas upon contact with water. The released gas is generally oxygen or most commonly carbon dioxide. Preferred blowing agents include acid and base components which react in the presence of water to produce carbon dioxide gas. The acid component may comprise one or more acids, and the base component may comprise one or more bases. Preferably, the base component comprises an alkali metal or alkaline earth metal carbonate or bicarbonate and the acid component comprises an aliphatic carboxylic acid. Non-limiting examples of suitable bases used as base components include carbonates (eg calcium carbonate), bicarbonates (eg sodium bicarbonate), sesquicarbonates, and mixtures thereof. Sodium bicarbonate is a preferred base.

Non-limiting examples of suitable acids used as acid components include citric acid, lactic acid, glutaric acid, phosphoric acid, acetic acid, tartaric acid, malic acid, fumaric acid, adipic acid, succinic acid, oxaloacetate, acid anhydrides of the acid. ), Acid salts of the acids, and combinations thereof. Citric acid is the preferred acid.

In further exemplary embodiments, the composition may comprise a sweetening agent. Preferred sweeteners for use in the present invention include sucrose, fructose, dextrose, maltose, lactose, high fructose corn syrup solids, invert sugar, sorbitol Sugars and sugar alcohols such as sugar alcohols, as well as mixtures of these sugars and sugar alcohols. In order to deliver lower levels of solids per dosage, it may be desirable to use high intensity sweeteners with sugars or sugar alcohols. Such high intensity sweeteners include saccharin, cyclamates, acesulfame K, L-aspartyl-L-phenylalanine lower alkyl ester sweeteners (eg aspartame); L-aspartyl-D-alanine amide; L-aspartyl-D-serine amide; L-aspartyl-L-1-hydroxymethylalkanamide sweetener; L-aspartyl-1-hydroxyethylalkanamide sweetener; And L-aspartyl-D-phenylglycine esters and amide sweeteners. Additional sweeteners contemplated for use with the compositions disclosed herein are sweeteners derived from stevia, sweeteners derived from momordica grosvenorii, and mogrosides. Contains sweeteners. A particularly preferred sweetener system is the combination of sucralose with acesulfame K and corn syrup solids.

In other exemplary embodiments, the composition may be dissolved in water or in another suitable liquid suitable for human consumption.

In other embodiments of the present invention, various suitable solvents that may be used to prepare extracts and fractions or to extract or fractionate plants such as Spareranthus indicus, Garcinia mangostana are ethanol C ₁ -C ₅ alcohols such as methanol; Water and mixtures thereof; C ₁ -C ₇ hydrocarbons such as hexane; Esters such as ethyl acetate, and the like and mixtures thereof.

In other embodiments, the components and compositions of the present invention may be formulated in dry form, liquid form, food, dietary supplement or other suitable form such as tablets, capsules or soft chew.

In another embodiment, the plant component (s) or composition (s) are controlled release tablets using a controlled release polymer-based coating by techniques including nanotechnology, microencapsulation, colloidal carrier systems, and other drug delivery systems. It can be delivered in the form of.

In another embodiment of the invention, the plant ingredient (s) or compositions thereof, nutritional / dietary supplements, solid foods such as chocolate or nutritional bars, semi-solid foods such as creams or jams or gels and refreshing beverage, lactic acid bacteria beverage, drop, candy, chewing gum, sticky candy, yogurt, ice cream, pudding, soft red beans jelly, jelly, cookie, tea, soft drink, juice, milk, coffee, cereal Healthy foods, such as beverages such as snack bars, or the like, or as dosage forms of foods for particular health use.

Flavorant (s) that can be used in the composition are not related to the inventive concept disclosed herein, and those skilled in the art are familiar with the wide range of flavors available. Therefore, any suitable perfume or combination of spices, natural and / or artificial, is within the scope of the present disclosure.

In another exemplary embodiment, the composition may further comprise a food colorant to improve the visual appearance of the drink made from the composition.

Flavoring agents or flavoring agents can provide fruity, cola, vanilla, or chocolate flavors, which are illustrative and not restrictive. Natural or synthetic sweeteners such as sucrose, sucralose, aspartame, and / or acesulfame potassium, neotam, polydextrose, glycerin, sorbitol, and xylitol can be used, These are exemplary and not limiting. Colorants can be added. Materials such as citric acid, fumaric acid, adipic acid, tartaric acid and in some cases lactic acid may be added to control the tartness.

Additional ingredients in the form of analgesics (eg aspirin), mild stimulants (eg green tea) other than caffeine as mentioned above, or emollients (eg melatonin) may be added to the particular product. .

In other embodiments, the plant components and compositions of the present invention are useful for mitochondrial deficiencies in both humans and animals. The plant components and compositions of the present invention may also be used to enhance or maintain physical or mental activity or to reduce infection in athletes or non-athletes who are physically stressed from strong physical exercise. In addition, the plant components and compositions of the present invention may be an activator of Sirtuin.

In another exemplary embodiment, the biologically acceptable component or composition comprises glucose, fructose, sucrose, maltose, yellow dextrin, white dextrin, aerosil, microcrystalline cellulose, calcium stearate, magnesium stearate, Sorbitol, stevioside, corn syrup, lactose, citric acid, tartaric acid, malic acid, succinic acid, lactic acid, L-ascorbic acid, dl-alpha-tocopherol, glycerin, propylene glycol, glycerin fatty esters, polyglycerol fatty esters, sucrose fat Esters, sorbitan fatty esters, propylene glycol fatty esters, acacia, carrageenan, casein, gelatin, pectin, agar, vitamin B group, nicotinamide, calcium pantothenate, amino acids, calcium salts, pigments, flavorings, preservatives , Distilled water, saline, aqueous glucose solution, alcohol, propylene glycol and And may be further combined with one or more pharmaceutically or pharmaceutically acceptable additives, carriers, and diluents, including polyethylene glycols, various animal and vegetable oils, white soft paraffin, paraffin, and waxes.

In another embodiment, the invention features a method for enhancing physical or mental activity in humans and animals and for the sustained maintenance of energy, physical endurance, and mental arousal, the method comprising: Sphaeranthus indicus Effective amount of at least one plant component and composition selected from extract (s), fraction (s), compound (s), extract or fraction standardized with active compound (s) / 7-hydroxyfurulanolide To humans and animals. Examples of improved physical activity include increased endurance and improved speed, stamina, strength, patience, flexibility, agility, balance, centering, reaction time, fatigue recovery, and also include an increase in sexual energy. Examples of improved mental activity include improved sharpness, attention time, mental arousal, cognitive function, mood elevation, and recovery or reduction of mental fatigue (eg, following high-intensity physical exercise). By appropriate administration of these ingredients or compositions, the physical or mental activity of humans and animals can be significantly enhanced without deleterious side effects.

In another embodiment, the present invention promotes physical activity, physical fitness, mental arousal in warm-blooded animals or humans or animals, enhances energy levels, endurance levels, circulatory health, vascular health, and also better mental Extracts or fractions, standardized to extract (s), fraction (s), compound (s), active compound (s) / 7-hydroxyfuranolide, derived from Sparantanthus indicus, for health It is characterized by the use of at least one plant component selected from and compositions thereof.

In another embodiment, the present invention is derived from Sphaeranthus indicus for the preparation of a medicament useful for enhancing physical or mental activity in humans or animals and for sustaining energy, physical endurance and mental arousal. The use of at least one plant component selected from extract (s), fraction (s), compound (s), extracts or fractions normalized to active compound (s) / 7-hydroxyfurulanolide, and compositions thereof to provide.

Those skilled in the art will recognize that changes may be made to the embodiments described herein without departing from the spirit of the invention. Accordingly, it is to be understood that the invention is not limited to the specific embodiments or examples described, but is intended to cover modifications within the spirit and scope of the invention as defined herein.

Example 1

Sparantus Independent coarse methanol extract (LI12500): SPA is Tuscan indicator coarse flower head (1 kg) to take the round-bottom flask, methanol (8 L) 60 - was extracted for 2 hours at 65 ℃ temperature. The extract was filtered and the raw material used was re-extracted twice with methanol under similar conditions (2 × 6 L). The extracts were combined and fine filtered and concentrated on a climbing film evaporator to give a residue (110 g). The methanol extract (LI12500) showed 11% of 7-hydroxyfurulanolide by HPLC analysis.

Sparantus Indicus Methanol Extract Standardized to 5% 7-hydroxyfurulanolide

Sparantus indicus methanol extract containing 7-hydroxyfurulanolide obtained above was diluted with microcrystalline cellulose and magnesium stearate, with 2% by weight of aerosil, to 5% 7-hydroxypuranolide A methanol extract (LI12508) on standardized Sparanthus indicus powder was obtained.

Example 2

Sparantus Indicus ethanol extract: Sparanthus indicus flower head (1 kg) was taken in a round bottom flask and extracted with ethanol (8 L) at 60-65 ° C. for 2 hours. The extract was filtered and the raw material used was re-extracted twice with ethanol under similar conditions (2 × 6 L). The extracts were combined, fine filtered and concentrated on an upward membrane evaporator to give a residue (98 g). The ethanol extract showed 12% of 7-hydroxyfurulanolide by HPLC analysis.

Example 3

Garcinia Mangostana Bark Methanol Extract ( LI80013 ): Fruit skin (1 Kg) dried in the shade of Garcinia Mangostana is powdered into a coarse powder and extracted with 90% methanol (5 L) at 60-65 ° C. for 2 hours. . The solvent was separated from the raw material by filtration. The extraction process was repeated three times with 90% methanol (2 × 3 L and 1 × 2 L). The extracts were combined, fine filtered, concentrated under reduced pressure and precipitated at ambient temperature. The precipitated solid was filtered to give a dry powder (150 g, α-mangosteen: 21% and γ-mangosteen: 2.5%).

Example 4

Garcinia mangostana methanol extract standardized to 10% α-mangosteen:

Garcinia mangostana or methanol extract containing α-mangosteen obtained in (Example 3) was diluted with microcrystalline cellulose and magnesium stearate, with 2% by weight of aerosil, and standardized to 10% α-mangosteen. Mangostana or methanol extract (LI80018) was obtained.

Example 5

Garcinia Mangostana Bark Ethanol Extract: The fruit skin (1 Kg) dried in the shade of Garcinia mangostana was powdered into a coarse powder and extracted with 90% ethanol (5 L) at 60-65 ° C. for 2 hours. The solvent was separated from the raw material by filtration. The extraction process was repeated three times with 90% ethanol (2 × 3 L and 1 × 2 L). The extracts were combined, fine filtered, concentrated under reduced pressure and precipitated at ambient temperature. The precipitated solid was filtered to give ethanol extract as dry powder (136 g, α-mangosteen: 22%).

Example 6

Composition LI12506F: Composition LI12506F was prepared by mixing the methanol extract (LI12500) of Sparanthus indicus prepared above and 90% methanol extract (LI80013) of Garcinia mangostana in a ratio of 3: 1.

Example 7

Formulation LI12507F (camera sustaining ^® (Merastin ^®)): the minimum prepared in 5% of 7-hydroxy-Fu Lula fun draw standardized Spa is Tuscan indicator coarse powder extract (LI12508) and 10% α- mango standardized by sustaining Garcinia Mangostar or methanol extract (LI80018) were mixed in a ratio of 3: 1 and blended properly to obtain LI12507F.

Example 8

Composition LI12517F:

Composition LI12517F was prepared by mixing the unit doses of the following ingredients: 1 part Sparantus indicus ethanol extract (1 g) and 3 parts garcinia mangostana 90% ethanol extract (3 g).

Example 9

Normalized with Sparanthus indicus extract standardized with 5% 7-hydroxyfurulanolide (LI12508) and Sparanthus indicus extract standardized with 5% 7-hydroxyfurulanolide and 10% α-mangosteen Using a composition containing Garcinia mangostana extract (LI12507F), a test to evaluate their efficacy as an anti-obesity adjuvant in a double blind placebo controlled study in human volunteers in obesity It was. Sixty obese volunteers (27.6% male; 72.4% female; age 22-50 years old) were included in a randomized, double-blind placebo-controlled trial of 56 days. Participants (BMI 30-40) were randomly divided into three groups; Placebo, LI12508 group and LI12507F group. Participants took 600 mg / day LI12508 and 800 mg LI12507F formulations in two divided doses or two identical placebo capsules, all of which were calorie-controlled meals (2000 calories / day) for 8 weeks. ) And 30 minutes of walking. A variety of parameters, including physical, anthropomorphic and biochemical parameters, and questionnaire based evaluation, including the quality of the questionnaire, were studied. S. indicus extract (LI12508) and its formulation LI12507F provided significant weight loss in both treatment groups and also indicated signs for potential use in regulating serum triglyceride levels.

Impact of Weight on Quality on quality of life, including subject feedback being administered for all volunteers at each assessment time point, including 0, 14, 28 and 56 days of Life Questionnaire-Lite Version, IWQOL-Lite). Volunteers have shown improvements in various parameters including increased mobility, increased walking speed, increased walking distance and time, untired feeling, bright active feeling. The number of volunteers showing improvement in physical capacity and endurance was greater in the supplement group than in the placebo group.

Both LI12508 and LI12507F also exhibited unexpectedly improved quality and improved energy, athletic performance and endurance in adjuvant treated volunteers when compared to placebo treated groups. This includes increased mobility, increased walking speed, increased walking distance, not tired, not tired, bright and active.

Example 10

Intracelluar ATP levels in cells treated with LI12508 and LI12507F were measured with an ATP detection assay system based on luminescence, ATPlite (PerkinElmer Inc., Waltham, Mass.). Briefly, the same number of L6 rat myocytes were placed in each well of a 96-well cell culture plate and incubated in DMEM supplemented with 10% FBS. Cells were treated for 4 hours with different concentrations of test samples (LI12508 and LI12507F), and 50 ul of cell lysis buffer was added to each well. Vehicle control cultures were treated with 0.2% DMSO (v / v). Finally 50 ul of substrate solution was added to each well and incubated on a plate stirrer for 5 minutes at room temperature. After 10 minutes of dark adaptation, luminescence was read with a luminescence analyzer (Modulus Multimode Reader, Turner Biosystems Inc., Sunnyvale, Calif.). Serial dilutions of ATP standard solutions ranging from lxlO ^-5 M to blanks were applied to the assay plates. Intracellular ATP levels were quantitatively determined from standard curves plotted using luminescent units versus known concentrations of ATP.

S. No Test substance code Capacity pg / mL ATP concentration One Control - 2.808 2 S. Indicus 5% Extract LI12508 50 3.313 3 S. Indicus Composition LI12507F 50 6.119

Example 11:

Swiss Albino (Swiss albino ) Assessment of Energy Persistence of Plant Extracts in Mice:

18 Swiss albino mice, 20 weeks of age, were selected for health examination and adapted for 1 week prior to the start of the trial. The animals were divided into three groups of six randomly (three males and three females) at random, corresponding to two doses of test substance LI12508 (100 and 250 mg / kg body weight) and vehicle control. The animals were administered orally daily for 1 week with the assigned test substance or vehicle. Swim exercise (15 minutes) was opened after 1 hour of treatment and continued daily for 7 days. In an acrylic tank filled with water, mice were swimming while supporting a constant load (lead fish sinkers, attached to the tail) corresponding to 10% of their weight. On day 7, the 15 minute swim exercise was tracked using the SMART video tracking system (Panlab S.L.U). Swimming time or rest time, distance traveled and swimming speed were measured using tracking software. Rest time and percentage thereof, slow movement and percentage thereof, fast movement and percentage thereof, total path length and average speed of swimming were analyzed using SMART video tracking software and the data are summarized in Table 2. do. As summarized in FIGS. 1-2, there was a significant decrease in mean resting time in both 100 mg / kg and 250 mg / kg LI12508 treated groups, as compared to the control treated animals group, and mean slower male time. , Mean fast tree time, and mean travel distance. In addition, as shown in FIG. 4, animals treated at 250 mg / kg p.o showed a significant increase in mean rate compared to the control group.

LI12508 energy endurance potential for forced swimming test parameters parameter
Test Items Street
(cm)
rest time
(second) rest time
(%) slow
movement
Time in seconds slow
movement
time (%) fast
movement
Time in seconds fast
movement
(%) Average
speed CMC
(Control) 39588.39
±
5247.84 662.63
±
36.94 73.57
±
4.10 192.74
±
25.99 21.40
±
2.89 45.29
±
12.96 5.03
±
1.44 111.40
±
6.72 LI12508
100 mg / kg 48345.11 **
±
2549.01 574.63 *
±
31.56 64.83
±
2.90 245.57 *
±
19.48 27.87
±
2.33 64.09 *
±
5.36 7.30
±
0.71 116.27
±
2.71 LI12508
250 mg / kg 57160.52 **
±
4810.60 565.71 **
±
24.78 62.80
±
2.75 252.40 **
±
14.82 28.02
±
1.65 82.71 **
±
12.83 9.18
±
1.42 125.96 *
±
6.39

Values are expressed as mean ± S.E.M, where n = 6.

* P <0.05, ** p <0.01 compared to CMC control (ANOVA followed by Turkey test)

Claims (14)

SPA selected from extracts and fractions standardized with at least one furulanolide / udesmanoid sesquiterpene compound as a natural energy enhancer for providing expression and sustained maintenance of energy and mental arousal in warm-blooded animals or mammals Plant component derived from Sphaeranthus indicus. At least one selected from extracts and fractions standardized with at least one prulanolide / udesmanoid sesquiterpene compound as a natural energy enhancer for providing expression and sustained maintenance of energy and mental arousal in warm-blooded animals or mammals Plant ingredient derived from one Sphaeranthus indicus, and Garcinia mangostana fruit peel extract, Osmium basilicum, Zingiber officinalis At least one biologically active ingredient selected from Tribulus terrestris, vitamins, amino acids, taurine, Ginkgo biloba extract, Rhodiola and guarana extract, Optionally comprising an additive, diluent or carrier. At least one selected from extracts and fractions standardized with at least one furulanolide / udesmanoid sesquiterpene compound, as a natural energy enhancer for providing the expression and sustained maintenance of energy and mental arousal in warm-blooded animals or mammals Plant components derived from one Sphaeranthus indicus, and Garcinia mangostana fruit bark extract standardized with α-mangosteen or γ-mangosteen or both, and at least one A composition comprising an additive / diluent of. The compound of claim 1, wherein the compound for standardization is 7-hydroxyfurulanolide; 11α, 13-dihydro-3α, 7α-dihydroxy-4,5-epoxy-6β, 7-udedesmanolide; 11α, 13-dihydro-7α-acetoxy-3β-hydroxy-6β, 7-udesme-4-enolide; 3-keto-β-eudesmol; 11α, 13-dihydro-3α, 7α-dihydroxyudesme-4-ene-6α, 12-oxide; 11α, 13-dihydro-3α, 7α-dihydroxyfurulanolide; 11α, 13-dihydro-7α, 13-dihydroxyfurulanolide; 11α, 13-dihydro-7α-hydroxy-13-metaoxyfurulanolide; 2α, 7α-dihydroxy-4-ene-11,13-dihydroudesume-6,12-oxide; 2α-hydroxycostic acid; 3-keto-7α-hydroxyudesme-4-ene-6,12-oxide (kryptomeridiol); 4-epicryptomemeridiol; Sparantanolides; 2α-hydroxysparantolide; 2α-acetoxysparantolide; 2α, 7α-dihydroxyspantholalide; Sphaeranthus indicus, characterized in that it is selected from the group consisting of 2α-acetoxy-7α-hydroxysparantolide and 2α-acetoxy-5α-hydroxyisospantolide or mixtures thereof. ). 3. Sphaeranthus indicus according to claim 1 or 2, obtained from or chemically synthesized from at least one plant site selected from leaves, flower heads, stems, roots, whole plants or mixtures thereof. Derived from. The method of claim 1, wherein the solvent for extraction or fractionation is C ₁ to C ₅ alcohol; C ₁ to C ₇ hydrocarbons; ester; Plant extracts and fractions, characterized in that selected from the group consisting of water and mixtures thereof. The active compound 7-hydroxyfurulanolide / other furulanolide / oil in extract (s) and fraction (s) derived from Sphaeranthus indicus. Normalized with at least one furulanolide / udesmanoid sesquiterpene compound, characterized in that the concentration of desmanoid sesquiterpen (s) is, respectively or together, in the range of 0.01% to 99.99%. Sphaeranthus indicus extract or fraction. The method of claim 2, wherein the concentrations of the active compounds α-mangosteen and γ-mangosteen in the extract (s) or fraction (s) derived from Garcinia mangostana are each or together, A composition, characterized in that the range of 0.01% to 99.99%. The plant ingredient or composition according to claim 1, wherein the ingredient or composition is formulated as a dietary supplement, a food additive, a beverage, a snack or an energy drink. The 7-hydroxy compound according to claim 1, for promoting physical activity, physical exercise, mental arousal, energy level, endurance level, circulatory health, vascular health, and better mental health in warm-blooded animals. Plant ingredient derived from Sphaeranthus indicus, standardized to furulanoid. The composition of claim 2, for promoting physical activity, physical exercise, mental arousal, for promoting energy levels, endurance levels, circulatory health, vascular health, and for better mental health in warm blooded animals. Treatment of plant components derived from at least one Sphaeranthus indicus selected from extracts and fractions standardized with at least one furulanolide / udesmanoid sesquiterpene compound according to claim 1 A method of enhancing natural energy to provide expression and sustained maintenance of energy and mental arousal in a warm blooded animal or mammal, comprising administering a scientifically effective amount to a patient or mammal or warm blooded animal. A method of enhancing natural energy to provide expression and sustained maintenance of energy and mental arousal in a warm blooded animal or mammal, comprising administering to the patient or mammal or a warm blooded animal a therapeutically effective amount of the composition according to claim 2 . A method of enhancing natural energy to provide expression and sustained maintenance of energy and mental arousal in a warm blooded animal or mammal, comprising administering to the patient or mammal or a warm blooded animal a therapeutically effective amount of the composition according to claim 3. .

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