HK1158949A - Use of alisma orientale in cosmetics and compositions thereof - Google Patents
Use of alisma orientale in cosmetics and compositions thereof Download PDFInfo
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Description
Technical Field
The present invention relates generally to cosmetic compositions and their use, and more particularly, to cosmetic compositions and their use in improving the condition and appearance of skin or hair.
Background
Active ingredients or ingredients derived from plants and plant seeds are commonly used for a wide variety of pharmaceutical, treatment and cosmetic purposes. Such active ingredients may be obtained from the whole plant or different parts of the plant, such as seeds, needles, leaves, roots, bark, cones, stems, rhizomes, callus cells, protoplasts, organs and organ systems and meristems. The active ingredient or ingredients may be incorporated into the compositions in various forms. Such forms include pure or semi-pure ingredients, solid or liquid extracts or derivatives or solid natural plant materials. The plant material may be incorporated in various sub-forms, such as whole, chopped, ground or crushed forms.
A problem often encountered with the use of active agents, components or ingredients derived from natural plant materials and/or plant seeds is their relatively low level of naturally occurring. Such low levels often require processing of relatively large amounts of natural plant material in order to obtain the desired or useful amount of active ingredient. For rare plants or plant seeds, such large quantities may be unavailable or difficult to obtain.
There is a positive interest in the cosmetics industry to develop products that can be topically applied to the skin that provide anti-acne, anti-oil, and anti-cellulite benefits. There is an increasing demand for cosmetics to enhance the appearance of skin. Consumers are concerned with alleviating or delaying the signs of excessive sebum accumulation, production or secretion and excessive accumulation or production of subcutaneous fat. In adolescence, the skin tone is mainly caused by hormonal changes, i.e. the colour and appearance of the skin look oily.
Sebum is an oily secretion containing fat, keratin and cellular material produced by the sebaceous glands belonging to the small ducts adjacent to the hair follicle. Sebum is secreted into the skin and hair. Both excess and deficiency of sebum are undesirable. Excess sebum is associated with oily skin or hair and acne. This is particularly common in adolescents, as an increase in sex hormone levels stimulates sebum production. Cosmetics that provide anti-acne, anti-oil and anti-cellulite benefits are highly desirable to both manufacturers and consumers.
Among traditional Chinese medicines, Alisma orientale (Alisma orientale) has been used as a herbal medicine for inducing diuresis and removing dampness from the body, improving renal function, promoting blood circulation, increasing metabolism, and lowering blood sugar, lipid and cholesterol levels. Alisma orientale of the alisma genus and alisma family, which is a plant latin named alismarientale (Sam.) Juzep. (a variant alisma orientale l. var. orientale Sam.) (a.k.a. "alisma orientale", "alisma orientale (Ze Xie)", "Fu alisma orientale (Fu Ze Xie)", or "Jiang Ze Xie" (chinese name) or "alisma orientale (Rhizoma alimatis)" (drug name)), is commonly found in europe, africa, east asia, such as china and north america.
Topical cosmetic compositions having an active ingredient, agent or ingredient derived from natural plant materials or extracts thereof are desirable in treating, preventing, controlling, ameliorating, inhibiting and/or reducing the signs of excessive cortical accumulation, production or secretion, including oily, shiny, or acne-prone skin, oily hair, oily scalp or unpleasant body odor and increased subcutaneous fat or cellulite.
Excessive sebum production is a particularly common problem in adolescents, which results in an oily or shiny appearance of the skin, which is one of the major factors leading to acne. Sebum is the semi-fluid secretion of sebaceous glands, which is composed mainly of fat, keratin and cellular material. The oily/shiny appearance of skin is caused by excessive sebum secretion in the sebaceous glands. In addition, odors are emitted as a result of excessive cortical accumulation, production, or secretion. The traditional approach to solving oily or shiny skin is to use powders that provide an immediate masking effect by absorbing excess sebum on the skin surface. This approach has only short term beneficial effects and has a very low degree of effect on conditions such as acne caused by excessive cortical production.
Cellulite is a subcutaneous uneven type of fat and accumulates primarily on the hips, thighs and limbs of many women. This is quite unsightly, as it gives the tissue lying beneath the skin a "orange peel" or "curd" like appearance. Pinching the skin creates a "mattress-like appearance" of the raised and depressed fat layers. One may be able to feel soft knots of fat trapped inside the hardened connective tissue. Cellulite can be caused by a number of factors, including genetic, intestinal, circulatory, lymphatic, hormonal, and lifestyle factors. Diet to reduce additional fat intake, exercise to increase fat metabolism and prevent cellulite buildup, and massage and/or hydrotherapy can help stimulate lymphatic drainage and reduce cellulite. However, all of these ways of reducing cellulite or subcutaneous fat are limited, producing little visible result over an extended period of time.
Thus, safe, effective, natural and novel composition ingredients that treat, prevent, reduce, inhibit and/or ameliorate the signs of excessive accumulation, production or excretion of sebum and subcutaneous fat would be advantageous for formulating skin or hair treatments and products. As described herein, the present invention provides new and beneficial methods and compositions for treating conditions associated with excess accumulation, production, or secretion of sebum and subcutaneous fat, and the like, and modes of action thereof, skin and hair articles, and personal care products for skin.
Disclosure of Invention
It is an object of the present invention to provide topical cosmetic compositions that can deliver effective levels of active ingredients (extracts, components or ingredients) from natural plant materials.
It is another object of the present invention to provide a topical cosmetic composition having a natural plant component or blend of natural plant components in a cosmetically, dermatologically, physiologically, or pharmaceutically acceptable excipient, carrier, or diluent.
It is another object of the present invention to provide topical compositions having lipolysis-stimulating active ingredients in a cosmetically, dermatologically, physiologically or pharmaceutically acceptable excipient, carrier or diluent.
It is another object of the present invention to provide topical compositions that deliver active ingredients derived from plants or extracts thereof in amounts sufficient to stimulate lipolysis and inhibit PPAR-gamma upregulation, stearoyl-coa desaturase upregulation, and adiponectin production.
It is another object of the present invention to provide a topical composition having an extract isolated from the Alisma orientale plant for treating, preventing, controlling, ameliorating, inhibiting and/or reducing the signs of excessive cortical accumulation, production or secretion, including oily, shiny, or acne-prone skin, oily hair, oily scalp, or an increase in body odor and subcutaneous fat or cellulite, thereby improving the aesthetic appearance of skin-related conditions, including, but not limited to, skin, hair, and unpleasant body odor.
It is another object of the present invention to provide methods of topically applying such compositions to the skin. Since hair is derived from skin, the methods and compositions of the present invention also relate to hair.
It is an object of the present invention to provide a method of delivering a consistent level of an active ingredient to the skin by topically applying a composition having one or more natural plant actives, components or ingredients.
These and other objects and advantages of the present invention, as well as equivalents thereof, are achieved by cosmetic compositions having a single natural plant component or a blend of natural plant components and the use of such compositions in topical applications.
Detailed Description
The present invention relates to topical compositions having natural plant materials (extracts, components, or ingredients) or active agents or ingredients derived therefrom. More particularly, the present invention relates to topical compositions for improving the condition and aesthetic appearance of skin, including, but not limited to, hair or odor associated with excessive sebum production from skin pores. Still more particularly, the present invention relates to methods of using the topical compositions not only for improving the aesthetic appearance of skin-related conditions, such as reducing excessive accumulation of cellulite and subcutaneous fat or producing and treating acne-, oily-or shiny-prone skin and oily conditions, but also for suppressing or reducing the unpleasant odors associated with fat release.
It is understood that reference to skin also includes hair. The hair itself is dead, but it is produced by living cells. Those cells are epidermal in nature and origin, and like other appendages of the skin, hair is also actually epidermal. Hair is also prone to oil flooding due to excessive sebum accumulation, production or secretion. Thus, the compositions of the present invention are also useful for preventing, reducing and improving oil hair.
The present invention relates to a novel use of alisma plants or extracts thereof in face, hair and/or body cosmetics. More particularly, the present invention relates to the use of topical compositions having natural plant material or extracts thereof, wherein the plant component stimulates lipolysis and/or inhibits PPAR-gamma up-regulation, stearoyl-coa desaturase up-regulation and adiponectin production, for treating, preventing, ameliorating and/or reducing the signs of excessive sebum production and/or improving the aesthetic appearance of skin-related conditions. The plant components may be derived from: alismataceae, in particular Alisma orientale, Alisma orientale variety (Alismata var. orientale), or Alisma orientale, also known as Ze Xie, Alisma (Alisma), Alisma orientale (Alismatis Rhizoma), great thrat, Scutellaria baicalensis (Mad-Dog Weed), Isopistil (Mud Plantain), Tse Hsieh, or Plantago asiatica (Water Plantain).
The ingredients of these plants that reduce subcutaneous fat by lipolysis are effective when topically applied, and as no wishing to be bound by theory, lipids are broken down by the active components in the composition comprising alisma plants or extracts thereof. Topical application of the alisma plant ingredients also facilitates targeted delivery of the active ingredient without the need for injection or expertise of healthcare practitioners.
Accordingly, the present invention provides novel compositions and methods using components of alisma orientale extract which have recently been found to be effective in treating, preventing, ameliorating and/or reducing the signs of excessive sebum production or excessive accumulation or production of subcutaneous fat and/or improving the aesthetic appearance of conditions associated with skin, hair or unpleasant body odor by daily administration.
Composition comprising alisma plants
For purposes of the present invention, the alisma plants may be in any form, including, but not limited to: whole plants, dried plants, ground plants, or parts thereof, including, but not limited to, seeds, needles, leaves, roots, bark, cones, stems, rhizomes, callus cells, protoplasts, organs and organ systems and meristems; an extract, dried extract, synthetic extract or a component and/or fraction found in or isolated from a plant and/or plant part or an extract derived directly from or synthesized by a plant; or any combination thereof.
In one embodiment, the topical composition of the present invention is used to improve the aesthetic appearance of conditions associated with skin, particularly juvenile skin, by any of the following methods:
1. reducing oil production by sebaceous glands;
2. reducing lipid synthesis in subcutaneous adipose tissue;
3. reducing triglyceride synthesis in subcutaneous adipose tissue;
4. preventing and/or ameliorating conditions involving the skin associated with the involvement of induced lipolysis;
5. preventing and/or ameliorating conditions involving the skin associated with non-selective or partially selective PPAR receptor stimulators/upregulators;
6. preventing and/or ameliorating conditions involving skin associated with stearoyl-coa desaturase activity;
7. preventing and/or ameliorating conditions involving the skin associated with adiponectin production;
8. preventing, ameliorating or treating acne;
9. preventing, ameliorating or treating oily skin;
10. preventing, ameliorating or treating oil hair;
11. preventing, ameliorating or treating oily scalp;
12. preventing, ameliorating, or treating blemishes; and
13. preventing, ameliorating or treating rashes or "eruptions";
14. preventing, ameliorating or treating body odor associated with excessive sebum production;
15. preventing, ameliorating or treating cellulite in adult humans;
16. preventing, ameliorating or managing excessive accumulation or production of subcutaneous fat in an adult; and
17. improving the skin texture.
The composition may have an amount of alisma orientale extract of from about 0.0001% to about 50%, preferably from about 0.001% to about 20%, more preferably from about 0.01% to about 2%, and most preferably from about 0.05% to about 1%, based on the total weight of the composition.
In another embodiment, the alisma plant extract as used herein also includes "synthetic" extracts, i.e. various combinations of known alisma plant components and/or constituents which are combined so as to substantially mimic the composition and/or activity of a alisma plant extract of natural origin. Such synthetic extracts are included in the term "alisma plant extract". Most preferably, the synthetic extract has substantially the same amount of active ingredient as the natural extract. The correspondence in the quantitative association of active components between synthetic extracts and plants or natural extracts can also be described as "percent commonality".
Another embodiment relates to synthetic extracts having about 50% or more than 50% commonality with the chemical composition of the plant or natural extract. For example, synthetic extracts have about 50% or more of the components found in plant or natural extracts. The chemical composition of the synthetic extract may have a commonality of about 70% or more with the chemical composition of the plant or natural extract. Synthetic extracts may have a commonality of about 90% or more than 90% with the chemical composition of a plant or natural extract. The plant or natural extract used for comparison is most preferably derived from the alisma plant.
For use in the compositions of the present invention, the plant material and/or active ingredient is preferably derived directly from the alisma plant, including seeds, needles, leaves, roots, bark, cones, stems, rhizomes, callus cells, protoplasts, organs and organ systems and meristems. The component may be in pure form, semi-pure form or impure form. In one embodiment, the ingredient is in the form of an extract obtained by extracting the rhizome of alisma orientale with a 50% water/50% ethanol solution (example 1).
Briefly, organic solvent extraction methods involve washing and extracting the plant material with an organic solvent. Non-limiting examples of the organic solvent include methanol, ethanol, isopropanol, dichloromethane, chloroform, hexane, xylene, and petroleum ether. Extractors can be used for organic solvent extraction, as is well known in the art.
Organic solvent extraction involves collecting raw materials containing the desired components from the plant, such as seeds, needles, leaves, roots, bark, cones, stems, rhizomes, callus cells, protoplasts, organs and organ systems and meristems. These plant materials were ground to small particle sizes and then placed into an extractor with a measurable raw material inlet of a charging machine. The plant material is pushed into the extractor with a pusher and slowly moved forward. Organic solvent (e.g., ethanol) may be added to the extractor through a solvent inlet at the top of the waste discharge outlet. Due to the difference in gravity and equilibrium, the solvent flows forward to the feedstock inlet, saturates the feedstock and flows out from the opposite side of the solvent inlet. Since the plant material and the solvent move in opposite directions to each other, the plant material is constantly immersed in a solution containing a low concentration of the extract. As a result of the equilibration, high yields of plant components can be obtained by continuous extraction of plant material from low concentration solutions.
Extraction times of about 1 to 8 hours are suitable, and more preferably about 2 to 6 hours, and most preferably about 3 to 5 hours. The extraction temperature is from about 30 ℃ to 90 ℃, preferably from about 40 ℃ to 70 ℃, and more preferably from about 50 ℃ to 60 ℃. The collected extract is then fine filtered to remove debris and used directly or concentrated, for example by distillation of the solvent or by conventional processing, and is also provided in powder form.
Similarly, aqueous-organic solvent extraction involves initially collecting raw materials containing the desired alkaloid from the plant, such as seeds, needles, leaves, roots, bark, cones, stems, rhizomes, callus cells, protoplasts, organs and organ systems and meristems of the plant, which are ground to small particle size. Depending on the solubility and stability of the desired extract under acidic or basic or alkaline conditions, the ground plant material is immersed in an aqueous acidic or basic solution. For extraction under acidic conditions, an acid such as hydrochloric acid or sulfuric acid is added to the water, for example, at a concentration of about 3% (w/v). For extraction under alkaline conditions, a base such as sodium hydroxide or sodium carbonate is added to the water. The extraction time and extraction temperature are generally similar to those used in the organic solvent extraction process described above.
The extract was then collected and fine filtered to remove debris. An alkaline agent (e.g., ammonia) or an acidifying agent (e.g., sulfuric acid) may be added to the extract to neutralize the solution by adjusting the pH, depending on the acidity or basicity of the collected extract. The aqueous extract can be used directly, concentrated or dried. Alternatively, an organic solvent may then be added to the neutralized solution to transfer the active ingredients of the extract from the aqueous phase to the organic phase. Examples of such organic solvents include, but are not limited to, ethanol, isopropanol, butanol, pentanol, hexanol, and xylene. The extract containing the transferred active ingredients of the extract dissolved in an organic solvent can be used as such, as a concentrate or dried.
Different plants containing different ingredients can be mixed with each other and extracted. This method of mixed extraction can be preferably used for extracting those plants containing components having similar solubility in the solvent used for extraction, such as ethanol. The mixture of extracts may be concentrated and stored in a suitable solvent.
Preparation
Compositions of the present invention comprising components from alisma plants include, but are not limited to: formulations for topical application; an antioxidant; an anti-inflammatory agent; a sunscreen agent; cosmetic agents, including cosmetics; agents for reducing excess subcutaneous fat, such as anti-cellulite creams, or agents for treating excess sebum production of oily skin or hair, blemishes, or acne; personal care products such as antiperspirants or deodorants; topical formulations; skin permeation enhancers, and the like. In addition, a variety of product forms can be formulated according to the present invention that contain such constituents of the Alisma orientale plant component and additional ingredients. The compositions may be prepared in the form of targeted delivery systems, such as creams, lotions, gels, toners, serums, transdermal patches, and the like, particularly for topical application. Targeted delivery and/or penetration enhancement may also be performed by iontophoresis.
The present invention further provides compositions comprising alisma plant components, preferably for topical application or targeted delivery. The compositions of the present invention are suitable for all skin types, such as sensitive, normal or oily. In particular embodiments, the compositions may be preferably used for oily skin or hair types. These compositions are applied to the skin or hair for a period of time sufficient to improve the aesthetic appearance associated with the skin, including signs of excessive sebum production, such as oily skin or hair, acne, body odor, and/or subcutaneous fat, such as cellulite. The composition may be applied topically 1, 2 or more times per day, preferably 1 time per day. Daily administration may be performed for a period of 1 week, 2 weeks, 4 weeks, or more than 4 weeks.
The compositions may be formulated as liposomes which may contain other additives or substances and/or may be modified so as to more specifically reach or remain on the site following administration. The compositions of the present invention provide improvements in aesthetic appearance associated with skin by treating one of the following conditions: excess sebum production, such as oily skin or hair, conditions associated with acne, conditions associated with body odor, and cellulite or excess subcutaneous fat.
Another embodiment of the present invention includes compositions comprising a cosmetically or dermatologically acceptable formulation suitable for contacting living animal tissue, including human tissue, with virtually no adverse physiological effects on the user. The compositions encompassed by the present invention may be prepared in any cosmetically and/or dermatologically suitable form, preferably as a lotion or cream, but also in the form of an anhydrous or aqueous base, as well as in the form of a sprayable liquid. Other suitable cosmetic forms for use in the compositions of the present invention include: such as a lotion, cream, balm, gloss, lotion, mask, serum, toner, ointment, spray, wax-based stick, or towelette. In addition, the compositions contemplated by the present invention may include: one or more cosmetically acceptable adjuvants commonly and well known to those skilled in the art, such as colorants, fragrances, emollients, moisturizers, preservatives, vitamins, chelating agents, thickeners, perilla oil (perilla oil) or perilla oil (perilla seed oil) (WO 01/66067- "method of treating skin disorders", incorporated herein), and the like; and other botanical preparations such as aloe, chamomile, and the like, and are described further below.
In addition, the present invention encompasses transdermal delivery means, such as patches and the like, with or without a suitable permeation enhancer. The methods and compositions encompassed by the present invention provide a means by which the Alisma components can be effectively administered in a transdermal system. Thus, the transdermal means of delivering the composition or formulation (typically containing a permeation enhancing composition) to the skin is that of a transdermal patch or similar device known and described in the art. Examples of such devices are disclosed in US5,146,846; US5,223,262; US4,820,724; US4,379,454; and US4,956,171, all of which are incorporated herein by reference, but such descriptions are not meant to be limiting. Storing and delivering the composition on the skin, including hair, and forming a transdermal form of the active composition is convenient and well suited for the purposes of the present embodiments. In a preferred method, administration is via a sustained release carrier, vehicle or diluent, such as a topically applied sustained release patch. Preferably, when a topical patch is used, the patch is applied to the desired area for an extended period of time. Preferably the extended period of time is longer than 1 hour, most preferably the extended period of time is overnight, i.e. when the user is sleeping.
The alisma plant component of the present invention is preferably comprised in a cosmetically or dermatologically acceptable vehicle, diluent or carrier for treating, reducing, ameliorating or preventing conditions associated with excess accumulation, production or secretion of sebum and excess accumulation or production of subcutaneous fat.
In embodiments including topical applications, the compositions of the present invention comprise a medium (excipient, diluent, or carrier) that is compatible with human skin, including hair. The composition may be formulated as an aqueous phase, an oily phase, an alcohol-based or water/alcohol-based solution, an ointment, a lotion, a gel, an oil-in-water emulsion or a water-in-oil emulsion, a three-phase water-oil-water emulsion having the appearance of a cream or gel, a microemulsion or an aerosol.
The aqueous phase is a mixture of one or more water-soluble or water-dispersible components, which may be liquid, semi-solid, or solid at room temperature (25 ℃). The vehicle comprises, or may be in the form of, a suspension, dispersion or solution in an aqueous or hydro-alcoholic carrier which may contain a thickening or gelling agent. One skilled in the art can select the appropriate cosmetic form, the components contained therein, and the method of preparation thereof based on the knowledge of one skilled in the art.
In one embodiment, the composition may comprise an aqueous phase which may contain water or a mixture of water and at least one hydrophilic organic solvent, in particular an alcohol, especially a linear or branched lower monohydric alcohol containing from 2 to 5 carbon atoms, such as ethanol or propanol; polyols, such as propylene glycol, sorbitol, glycerol, diglycerol, panthenol or polyethylene glycol and mixtures thereof. The aqueous phase may comprise from about 0.5 wt% to about 99.99 wt% of the total weight of the composition.
In another embodiment, when the composition of the present invention is in the form of an emulsion, the composition may also optionally comprise a surfactant, preferably in an amount of from about 0.1% to about 30% by weight, and particularly from about 1% to about 20% by weight, based on the total weight of the composition.
In another embodiment of the invention, the composition may further comprise a thickening polymer, such as an amphiphilic polyurethane; polyacrylic acid homopolymers or copolymers; polyesters and/or hydrocarbon-based resins.
One embodiment of the present invention relates to compositions of the present invention which may further comprise an oil phase comprising an oil-soluble or oil-dispersible component which is liquid at room temperature (25 ℃) and/or an oily or waxy substance which is solid at room temperature, such as waxes, semisolids, gums and mixtures thereof. The oil phase may also contain an organic solvent.
Suitable oily substances which are liquid at room temperature, commonly referred to as oils, include: hydrocarbon-based oils of animal origin, such as perhydrosqualene; hydrocarbon-based vegetable oils, such as liquid triglycerides of fatty acids of 4 to 10 carbon atoms, for example heptanoic acid or caprylic acid triglycerides, or oils, such as sunflower oil, corn oil, soybean oil, grapeseed oil, castor oil, avocado oil, caprylic/capric acid triglycerides, jojoba oil; linear or branched hydrocarbons of mineral or synthetic origin, such as liquid paraffin and its derivatives, vaseline; synthetic esters and ethers, particularly esters of fatty alcohols; such as isopropyl myristate, 2-ethylhexyl palmitate, 2-octyldodecyl stearate, isostearyl isostearate; hydroxylated esters such as isostearyl lactate, octyl hydroxystearate, octyl dodecyl hydroxystearate, heptanoates, octanoates and decanoates of fatty alcohols; polyol esters such as propylene glycol dicaprylate, octylene glycol diheptanoate, diethylene glycol diisononanoate, and pentaerythritol esters; fatty alcohols having 12 to 26 carbon atoms, such as octyldodecanol, 2-butyloctanol, 2-hexyldecanol, 2-undecylpentadecanol, oleyl alcohol; fluorine oil and/or fluorosilicone oil based on partial hydrocarbon; silicone oils such as volatile or non-volatile linear or cyclic Polymethylsiloxanes (PDMS) that are liquid or semi-solid at room temperature, such as cyclic polydimethylsiloxanes and polydimethylsiloxanes, optionally containing phenyl groups, e.g. phenyltrimethicones, siloxanes and mixtures thereof. These oils are generally present in an amount of about 0 wt.% to about 90 wt.%, preferably about 1 wt.% to about 80 wt.%, based on the weight of the oil phase.
The oil phase of the compositions of the present invention may also comprise one or more cosmetically acceptable organic solvents. These solvents are present in an amount of about 0 wt% to about 60 wt%, preferably about 1 wt% to about 30 wt%, based on the total weight of the composition, and may be selected from the group consisting of lipophilic organic solvents, amphiphilic organic solvents, and mixtures thereof. Suitable solvents that may be used in the compositions of the present invention include: acetates such as methyl acetate, ethyl acetate, butyl acetate, amyl acetate or 2-methoxyethyl acetate; isopropyl acetate; hydrocarbons such as toluene, xylene, p-xylene, hexane or heptane; ethers containing at least 3 carbon atoms and mixtures thereof.
The composition of the present invention may further comprise any component commonly used in the cosmetic field. These components include preservatives, aqueous phase thickeners (polysaccharide biopolymers, synthetic polymers) and fatty phase thickeners, fragrances, hydrophilic and lipophilic active agents and mixtures thereof. The amounts of these various components are those conventionally used in the cosmetic arts to achieve their intended purpose and generally range from about 0.01% to about 20% by weight of the total weight of the composition. The nature of these components and the amounts thereof must be compatible with the process for producing the compositions of the invention.
The compositions of the present invention may also comprise an additional particulate phase, which is generally present in an amount of from about 0% to about 30% by weight, preferably from about 0.05% to about 20% by weight, based on the total weight of the composition, and may contain pigments and/or pearlescent agents and/or fillers used in cosmetic compositions.
Suitable inorganic pigments include, but are not limited to, titanium oxide, zirconium oxide, and cerium oxide, as well as zinc oxide, iron oxide, chromium oxide, and ferric blue. Suitable organic pigments include barium, strontium, calcium and aluminum lakes and carbon black. Suitable pearlescent agents include mica coated with titanium oxide, iron oxide or natural pigments. The filler is generally present in an amount of about 0 wt% to about 20 wt%, preferably about 0.1 wt% to about 10 wt%, based on the total weight of the composition. Suitable fillers include talc, silica, zinc stearate, mica, kaolin, nylon (especially orgasol) powder, polyethylene powder, teflon, starch, boron nitride, copolymer microspheres such as expancel (nobel industrie), polytrap (dow corning) and silicone resin microbeads (tosearl from Toshiba).
The oil phase of the compositions of the present invention may comprise one or more waxes, gums or mixtures thereof. Waxes include hydrocarbon-based waxes, fluoro waxes, and/or silicone waxes, and may be derived from vegetable, mineral, animal, and/or synthetic sources. The compositions of the present invention may contain from about 0% to about 20% by weight of wax, based on the total weight of the composition. Gums are typically high molecular weight PDMS, sodium carboxymethylcellulose or polysaccharides, and semi-solid materials are typically hydrocarbon-based compounds such as, but not limited to, lanolin and its derivatives, or may be PDMS.
Furthermore, as noted above, the composition may be in the form of a vesicular dispersion containing ionic and/or nonionic lipids. Dosage units suitable for such compositions may be formulated according to techniques well known and used in the art.
More specifically, the composition for topical application may be a protective composition for the skin, preferably the face, neck, hands, feet or other body areas. Non-limiting examples include day creams or lotions, night creams or lotions, ointments, sun creams, lotions, oils, ointments, gels, masks, body lotions, cosmetics (foundations), artificial tanning compositions, depilatories, emulsifiers, patches or solids, for example cast or cast in sticks or discs.
Another specific embodiment of the present invention relates to the delivery of such compositions by using targeted delivery systems, such as liposomes, microspheres (see, e.g., U.S. patent No. 5,770,222 to Unger et al, incorporated herein by reference), and the like, such that the alisma composition and/or active ingredient can more readily reach and affect the muscle layer of the area of application, such as the face or neck or other areas of the skin.
In another embodiment, the topical compositions of the present invention may further comprise one or more of the following ingredients: skin penetration enhancers, emollients, skin plumpers, optical diffusers, sunscreens, exfoliation promoters, and antioxidants. Detailed descriptions of these and other suitable cosmetic ingredients can be found in the following publications: international Cosmetic Ingredient Dictionary and Handbook, 10th edition (2004), published by Cosmetic, Toiletry and fragrance Association (CTFA), pp 2177-2299, which publication is incorporated herein by reference in its entirety.
Emollients provide the functional benefit of enhancing skin smoothness and reducing the appearance of fine lines and coarse wrinkles. Examples include isopropyl myristate, petrolatum, isopropyl lanolate, silicones (e.g., polymethylsiloxane, polydimethylsiloxane), oils, mineral oils, fatty acid esters, or any mixture thereof. The emollient preferably comprises about 0.1 wt% to about 50 wt% of the total weight of the composition.
The skin plumping agent is used as collagen protein enhancer for skin. An example of a suitable and preferred skin plumper is palmitoyl oligopeptide. Other skin plumping agents are collagen and/or glycosaminoglycan (GAG) fortifiers. The skin plumper preferably comprises about 0.1 wt% to about 20 wt% of the total weight of the composition.
Optical diffusers are particles that alter the visual acuity at the skin surface, resulting in blurred vision and reduction of, for example, lines and wrinkles. Examples of the optical diffuser that can be used in the present invention include, but are not limited to, boron nitride, mica, nylon, polymethyl methacrylate (PMMA), polyurethane powder, sericite, silica, silicone powder, talc, teflon, titanium dioxide, zinc oxide, or any mixture thereof. The optical diffuser preferably comprises about 0.01 wt% to about 20 wt% of the total weight of the composition.
Sunscreens protect the skin from ultraviolet light. In an illustrative embodiment of the present invention, the sunscreen may provide both UVA and UVB protection by using a single sunscreen or a combination of sunscreens. Among the sunscreens which may be used in the present invention are avobenzone, cinnamic acid derivatives (such as octylmethoxy cinnamate), octyl salicylate, oxybenzone, titanium dioxide, zinc oxide or any mixture thereof. The sunscreen agent may comprise from about 1 wt% to about 30 wt% of the total weight of the composition. The addition of sunscreen agents protects the skin from UV radiation.
The compositions of the present invention with sunscreen agents provide additional improvements in the aesthetic appearance of skin, including at least one of the following: minimizing sunburn, minimizing tanning, and reducing redness.
In one embodiment of the present invention, the composition may further comprise one or more exfoliation promoters. Suitable examples of the exfoliation promoters that can be used in the present invention include: alpha Hydroxy Acids (AHAs); benzoyl peroxide; a beta hydroxy acid; keto acids such as pyruvic acid, 2-oxopropanoic acid, 2-oxobutanoic acid, and 2-oxopentanoic acid; oxoacids disclosed in U.S. Pat. Nos. 5,847,003 and 5,834,513 (the disclosures of which are incorporated herein by reference); salicylic acid; urea; or any mixture thereof. Preferred exfoliation promoters are 3, 6, 9-trioxaundecanedioic acid, glycolic acid, lactic acid or any mixture thereof. (see also Dictionary at page 2205).
When embodiments of the present invention include an exfoliation promoter, the composition contains about 0.1 wt% to 30 wt%, preferably about 1 wt% to about 15 wt%, and more preferably about 1 wt% to about 10 wt%, of the exfoliation promoter, based on the total weight of the composition.
In addition to the above, antioxidants function to scavenge free radicals from the skin in order to protect the skin from environmental aggressors. Examples of antioxidants that may be used in the compositions of the present invention include: compounds with phenolic hydroxyl functionality, such as ascorbic acid and its derivatives/esters; beta-carotene; a catechin; curcumin; ferulic acid derivatives (e.g. ethyl ferulate, sodium ferulate); gallic acid derivatives (e.g. propyl gallate); lycopene; reducing the acid; rosmarinic acid; tannic acid; tetrahydrocurcumin; tocopherol and derivatives thereof; uric acid; or any mixture thereof. Other suitable antioxidants are those compounds which carry one or more mercapto functions (-SH) in reduced or non-reduced form, such as glutathione, lipoic acid, thioglycolic acid and other sulfhydryl compounds. The antioxidant can be inorganic, such as bisulfite, metabisulfite, sulfite, or other inorganic salts and sulfur-containing acids. The compositions of the present invention may contain an antioxidant in an amount preferably from about 0.001 wt% to about 10 wt%, and more preferably from about 0.01 wt% to about 5 wt%, based on the total weight of the composition. See also Dictionary, page 2184.
In one embodiment of the invention, the composition may also have one or more of the following cosmetic and pharmaceutical active agents, excipients, components or adjuvants: an anesthetic; antibiotics, such as erythromycin and tetracycline, salicylic acid, antiallergic agents, antifungal agents, antibacterial agents, anti-irritant agents, anti-inflammatory agents, antimicrobial agents, analgesic agents, nitric oxide synthase inhibitors, insect repellents, self tanning agents, skin permeation enhancers, skin coolants, chelating agents, colorants, including dyes, lakes, and pigments that may be untreated or chemically surface treated to improve wettability or some other property; emollients, emulsifiers, fragrances, moisturizers, lubricants, skin protectants, moisturizers, pH adjusters, preservatives, stabilizers, surfactants, thickeners, film formers, plasticizers, viscosity modifiers, vitamins, or any mixture thereof. The amounts of these various substances are those conventionally used in the cosmetic or pharmaceutical field to achieve their intended purpose, and they may for example represent from about 0.01% to 20% by weight of the total composition.
Non-limiting examples of active agents useful in formulating the compositions of the present invention include, in addition to the active ingredient of Alisma orientale, those agents that have an effect on the treatment of wrinkles and/or fine lines, such as keratolytic agents, i.e., agents that have desquamation, exfoliation or scrubbing properties or agents that soften the stratum corneum of the skin. Other examples of anti-wrinkle or anti-fine line actives include hydroxy acids and retinoids. For example, these active agents may be formulated at about 0.0001% to 5% by weight of the total composition.
Suitable hydroxy acids include: for example glycolic acid, lactic acid, malic acid, tartaric acid, citric acid, 2-hydroxyalkanoic acids, mandelic acid, salicylic acid and alkyl derivatives thereof, including 5-n-octanoylsalicylic acid, 5-n-dodecanoylsalicylic acid, 5-n-decanoylsalicylic acid, 5-n-octylsalicylic acid, 5-n-heptyloxysalicylic acid, 4-n-heptyloxysalicylic acid and 2-hydroxy-3-methylbenzoic acid or alkoxy derivatives thereof, such as 2-hydroxy-3-methoxybenzoic acid.
The emulsifier is generally present in the composition in an amount of about 0.01% to about 30% by weight, and preferably about 0.5% to about 30% by weight, based on the total weight of the composition. However, not all compositions necessarily include an emulsifier (see, e.g., Dictionary, pages 2276-2285).
Non-limiting examples of suitable thickeners include xanthan gum, hydroxypropyl cellulose, hydroxyethyl cellulose, carbomer, gum arabic, Sepigel 305 (available from Seppic co., france) and clays such as magnesium aluminum silicate (see, e.g., Dictionary, page 2293-2299).
The topical compositions of the present invention may include one or more moisturizers, and their effectiveness may be enhanced by such moisturizers as ureas, pyrrolidone carboxylic acid, amino acids, sodium hyaluronate, certain polyols, and other compounds that are hygroscopic (see Dictionary, page 2244).
The general activity and mildness of the topical compositions of the present invention on the skin may also be enhanced by neutralization to a pH of from about 3.5 to about 7.0, most preferably to a pH of from about 3.7 to about 5.6. Such neutralization preferably uses one or more of aluminum hydroxide, potassium hydroxide, sodium hydroxide, arginine or other amino acids and/or triethanolamine.
Typical retinoids include, but are not limited to, retinoic acid (e.g., all-trans or 13-cis) and its derivatives, retinol (vitamin a) and its esters, such as retinyl palmitate, retinyl acetate and retinyl propionate and their salts.
The topical compositions of the present invention can be further formulated according to procedures known in the art to make cosmetic compositions such as lotions, gels, creams, lotions, conditioners, shampoos, deodorants, antiperspirants, ointments, creams, sticks, compact, color pens, essences and serum as well as other topical cosmetic vehicles. It is also contemplated that the topical compositions of the present invention may be incorporated into delivery systems such as liposomes and topical patches, tapes and sprays.
Use method of alisma plants
In another embodiment, the present invention encompasses methods of improving the aesthetic appearance associated with skin, including hair and body odor, comprising applying to the skin and hair a composition comprising at least one ingredient of an Alisma plant. In a particular embodiment, the ingredient is an extract of alisma orientale in a pharmaceutically, physiologically, cosmetically and dermatologically acceptable medium and in an amount effective to treat, reduce, prevent and/or ameliorate the signs of excessive sebum production, oily or shiny skin, acne prone skin, oily hair and body odor associated with excessive sebum production, excessive subcutaneous fat and cellulite. Compositions containing alisma extract in a medium preferably stimulate lipolysis, inhibit PPAR-gamma, stearoyl-coa desaturase or adiponectin so as to treat, reduce, prevent and/or ameliorate these skin-related conditions. Topical application of a composition containing alisma orientale ingredients is preferred.
One embodiment of the present invention relates to a method of applying an effective amount of a plant or plant extract derived therefrom to induce lipolysis in an affected area of skin or hair. Lipolysis is the process by which triglycerides are hydrolyzed into glycerol and free fatty acids. Lipolysis releases Free Fatty Acids (FFA) into the bloodstream where they can be re-esterified by adipocytes or transported to other tissues and play other roles throughout the body. Breakdown of triglycerides in adipocytes leads to release of free fatty acids and glycerol into the medium. The plant is preferably Alismatis rhizoma, and more preferably Alismatis rhizoma extract. Alisma orientale plant or extract thereof may be used as a lipolysis inducer and thereby treat or reduce conditions associated with excessive sebum accumulation, production or secretion and subcutaneous fat, including cellulite.
In one embodiment of the above method, an effective amount of an inhibitor of PPAR upregulation in a topical composition is administered to the affected area. Preferably, the PPAR upregulation inhibitor is an Alisma orientale plant or extract thereof, more preferably the extract is from the rhizome of an Alisma orientale plant. The peroxisome proliferator-activated receptor gamma (PPAR- γ) structurally belongs to the nuclear transcription factor superfamily and has physiological and pathological significance for the activation of this receptor, especially in the control of lipid metabolism and inflammatory responses. Nuclear hormone receptors are ligand-dependent intracellular proteins that, upon activation by a suitable ligand, stimulate the transcription of specific genes by binding to specific DNA sequences. PPAR-gamma activity is modulated by the binding of small lipophilic ligands, primarily fatty acids derived from nutritional or metabolic pathways normally controlled by PPAR-gamma. PPAR- γ is said to be the central cup of the feed forward pathway that favors adipocyte differentiation and energy storage. Alisma orientale plant or extract thereof can be used as PPAR up-regulation inhibitor, thereby providing positive effects on acne and cellulite.
One embodiment of the present invention relates to a method of applying to an affected area an effective amount of a plant or plant extract derived therefrom for inhibiting stearoyl-coa desaturase. The plant is preferably Alismatis rhizoma, and more preferably Alismatis rhizoma extract. The lipid composition of the cell membrane is regulated in order to maintain membrane fluidity. The key enzyme involved in this process is membrane-bound stearoyl-coa desaturase (SCD), the rate-limiting enzyme in the synthesis of monounsaturated fatty acids from saturated fatty acid cells. The proper ratio of saturated to monounsaturated fatty acids contributes to the film fluidity. Oleic acid and palmitoleic acid are the major monounsaturated fatty acids in fat stores and membrane phospholipids. These fatty acids are synthesized by hard fatty acyl-coa desaturase. Modulation of stearoyl-coa desaturase is therefore of considerable physiological importance and its activity is sensitive to dietary changes, hormonal imbalances, temperature changes, metals, alcohols, peroxisome proliferators and phenolic compounds. Alisma orientale plant or an extract thereof is useful as an inhibitor of SCD activity, thereby treating or reducing conditions associated with excessive sebum accumulation, production or secretion, as well as subcutaneous fat, including cellulite.
Another embodiment of the invention relates to a method of applying to an affected area of skin or hair an effective adiponectin-inhibiting amount of a plant or plant extract derived therefrom. The plant is preferably Alismatis rhizoma, and more preferably Alismatis rhizoma extract. Adipocytes express a variety of proteins that play a role in the homeostatic control of glucose and lipid metabolism, including the 30-kDa protein (Acrp30), known as the adipocyte complement-associated protein, or adiponectin, an adipocyte factor. The secretion of adiponectin by adipocytes is enhanced by insulin stimulation, while the reduced expression is associated with insulin resistance, thus providing support for the association between type II diabetes and obesity (Nedvidkova J et al, "adiponectin, an adipocyte-derived protein" -Physiol Res., Nov.15, 2004; Meier U and Gressner AM. "endocrine regulation of energy metabolism-a review of the pathological biochemical and clinical chemistry aspects of leptin, ghrelin, adiponectin, and resistance proteins" -Clin Chem.50 (9): 1511-25, 2004; Gil-Campos M et al, "adiponectin, a loop deficient in insulin resistance and obesity" -in Clin Nutr.23 (5): 963-74, 2004; all of these documents are incorporated herein by reference). It has been shown that the occurrence of non-insulin dependent (type 2) diabetes mellitus is associated with dysregulation of adiponectin secretion (Putz DM et al, "obesity, type 2 diabetes mellitus and adiponectin and C-reactive protein in monotherapy" -Metabolism 53 (11): 1454-61, 2004; Gil-Campos, supra; both of which are incorporated herein by reference). In supporting the correlation between obesity and type 2 Diabetes, it has been demonstrated that a reduction in circulating adiponectin levels is associated with insulin resistance and that adiponectin appears to be a potent insulin potentiator with adipose tissue associated with overall glucose metabolism (Shetty GK et al, "circulating adiponectin and resistance protein levels associated with metabolic factors, inflammatory markers, and vascular reactivity in diabetic patients and subjects at risk for Diabetes" -Diabetes Care.27 (10): 2450-7, 2004; Schulze MB et al, "relationship between adiponectin and glycemic control, lipid, and inflammatory markers in men with type 2 Diabetes" -Diabetes Care.27 (7): 1680-7, 2004; both of which are incorporated herein by reference). Alisma orientale plant or extract thereof is useful as an adiponectin production inhibitor, whereby conditions associated with excessive sebum accumulation, production or secretion, as well as subcutaneous fat, including cellulite, can be treated or reduced.
Another embodiment of the present invention is directed to a method of improving the aesthetic appearance of a condition associated with skin and comprising applying to the skin or introducing by targeted delivery a composition comprising one or more alisma orientale ingredients in an amount effective to improve the aesthetic appearance of a condition associated with skin and associated with excessive sebum production and excessive accumulation or production of subcutaneous fat.
It will be appreciated by those skilled in the art that cosmetic treatments may be performed, for example, by topically applying a cosmetic composition as described herein, including the use of the plant extract, component and/or constituent containing compositions of the present invention, in accordance with conventional techniques for administering such compositions. Conventional and commonly practiced techniques include applying creams, lotions, gels, masks, serum, ointments, patches, cosmetics, make-up remover, deodorants, antiperspirants or sunscreen compositions to the skin; sprays are also envisaged as forms of application.
Detailed Description
The following examples describe specific aspects of the invention in order to explain the invention and to provide those skilled in the art with a description of the methods of the invention. These examples should not be used to limit the invention, as they merely provide specific ways to understand and practice the invention and its various aspects.
Example 1
The plant extracts of the present invention can be extracted from natural sources by using water-organic solvent extraction methods well known in the art. One such extraction method is described below.
Preparation of the extract
Suitable methods for preparing the extracts for use in preparing the compositions of the present invention are described below.
The process for preparing the extract from fresh rhizome of alisma orientale is carried out by first washing and drying the plant material. The dried plant material is then crushed and ground into a powder by hand. The ground weight of plant material was extracted once at 70 ℃ and in the same weight of 50% ethanol/water solution for about 30 minutes. The material is retained as a liquid extract without drying the extracted material. This liquid material can then be added to the aqueous phase during the cosmetic formulation process.
Example 2
Cell culture
Removing a vial of frozen preserved egg from liquid nitrogenNormal human epidermal keratinocytes (adult or neonatal) and placed in a water bath at 37 ℃ for about 1-2 minutes or until completely thawed. The vial was then removed from the water bath and the excess water was wiped off. The vial was placed in a cell culture hood to be in a sterile state. The vial was wiped with 70% ethanol to air dry for 30 seconds. While in the cell culture hood, cells were removed from the vial and placed into a 50ml tube. Appropriate growth medium (5ml) was added dropwise while agitating the tube to allow a uniform mixture of cells and medium while limiting cell death due to osmotic changes caused by freezing the medium. The medium (25ml) was added to a 50ml tube to bring the volume to 30 ml. The medium/cell solution (15ml) was added to two 75cm cells2In flasks, or the medium/cell solution (5ml) was added to 6 tubes of 25cm2In a flask. The flask was reclosed and placed horizontally at 37 ℃ with 5% CO2For 24 hours in a humidified incubator. After 24 hours, old medium was aspirated and fresh growth medium (15ml) at room temperature was added to the cells. The growth medium was allowed to reach room temperature using a room temperature water bath without a lid before adding fresh growth medium. The flask containing the cells and fresh medium was returned to the 37 ℃ incubator. The old medium in the flask was repeatedly replaced with fresh medium until the desired degree of confluence (75%) was reached.
Decking and treatment
When normal human epidermal keratinocytes reached the desired confluency, they were removed from the incubator and the medium was aspirated off using a vacuum trap. Hank's buffered saline solution (HBSS; 10ml of 1X; Mediatech, Inc.; Herndon, Va.) was placed in the flask and the entire surface was rinsed. HBSS was then aspirated. Trypsin (0.25% solution; Mediatech, Inc.) was added in a volume of 5 ml. The flask was returned to the incubator for 8 minutes. The flasks were then removed from the incubator and 15ml of trypsin neutralizing solution (1X; Cascade biologics, Inc.; Portland, OR) was added to each flask to neutralize the trypsin. The medium/cell solution was removed from the flask and placed into a 50ml polypropylene tube. Cells 6 were spun at 1100rpm at room temperature using a bench top centrifugeAnd (3) minutes. After rotating the cells, they were resuspended in growth medium (basal medium: epitife containing calcium chloride) supplemented with 1% human keratinocyte growth factor (Cascade Biologics, Inc.), 1% penicillin/streptomycin (Mediatech, Inc.)In culture medium (Cascade Biologics, Inc.). Resuspend cells by pipetting up and down. The cell culture was then placed in a medium containing 5% CO2Was incubated in a volume of 10ml of 100mm tissue culture treated plates in a humidified incubator until 75% confluence was reached. When confluence was reached, the medium was removed and replaced with fresh growth medium containing the test active ingredient at the specified concentration. Each test active was diluted in growth medium in a vial of 10% stock solution containing excipients (i.e., water, ethanol, DMSO) and the test active. Each vehicle was tested as a control along with the active ingredients tested. The 100mm tissue culture treated plates were returned to 5% CO2The 37 c humidified incubator of (a) was kept for various times in order to establish the time course for testing the active ingredient. Tissue culture plates were collected at 1 hour, 4 hours, 8 hours, 24 hours, and 32 hours. At each time point, the growth medium was aspirated and the cells were washed with 1X phosphate buffered saline. The 1X PBS was removed and 100mm tissue culture plates were wrapped in parafilm and stored at-80 ℃ until needed.
Example 3
Lipolysis assay
Human subcutaneous preadipocytes (batch No. SL 0024; age 39.8 and BMI 28.69) were cultured in 96-well plates and allowed to differentiate in the absence of test compound for about 2 weeks to confluence, i.e., to reach a confluent monolayer of cells that was not observed with plastic plates. The lipolysis assay measures the effect of a compound on lipolysis by measuring the amount of glycerol released into the medium. For lipolysis assays, the medium was removed and the cells were gently washed 3 times with 1 Xconcentration of Krebs-Ringer bicarbonate buffer, a balanced salt solution used to maintain pH and osmotic balance (KRB; Zen Bio, Inc.; Research Triangle Park, NC). KRB in each well was removed and a fresh aliquot of 200. mu.l/well of KRB was added. One row of wells (1 time) was washed at a time to ensure that the cells remained wet and attached to the plate. All KRBs were removed and the cells were treated with 150. mu.l/well of control or 150. mu.l/well of 0.1% each of test compound (resuspended in KRB containing 1% BSA). The assays were performed in triplicate. The plates were incubated at 37 ℃ for 5 hours. At the end of the treatment, 100. mu.l/well of conditioned medium was removed from the assay plate and added to the corresponding well of a new 96-well plate. Glycerol assay reagent (100. mu.l/well) was added to the new plate. The glycerol concentration was determined by the GPO Trinder assay (Zen-Bio, Inc; Research Triangle Park, NC). The new plate was then incubated at 25 ℃ for 15 minutes. The optical density of each well of the new plate was measured at 540 nm.
Treatment of human subcutaneous preadipocytes with alisma resulted in induction of lipolysis of up to about 890% when compared to standard controls (see table 1).
TABLE 1
Example 4
Adiponectin inhibition assay
The effect of the test compound on adiponectin is determined. Human subcutaneous adipocytes induced to produce lipids using peroxisome proliferator-activated receptor (PPAR) gamma inducers were used for treatment (batch number SL 0024; age 39.8 and BMI 28.69). Two concentrations of test compound (0.1% and 1%) were added to the cells. Adiponectin secretion was measured 3 days after treatment with human adiponectin ELISA. Specific antibody pairs against human adiponectin (made by Zen Bio, inc.) one was immobilized on the wells to capture adiponectin on the test sample, and the other bound to the captured adiponectin for detection. Adiponectin present in the test sample is sandwiched between the immobilized antibody and the second antibody and detected by the following steps: anti-IgG antibody conjugated to horseradish peroxidase (HRP) was added first and then a substrate that caused an enzymatic reaction of HRP labeled by a color change was added. The concentration of adiponectin is directly proportional to the color intensity measured at 450 nm. The concentration of the test sample was calculated using the absorbance values of the adiponectin standard solutions determined at the same time.
Alisma orientale caused significant adiponectin inhibition when compared to the standard control. Adiponectin was inhibited by 729% in the presence of alisma (see, table 1).
Example 5
PPAR-gamma inhibition assay
Azgen, LLC (Saunderstown, RI) measured the effect of herbal formulations on peroxisome proliferator-activated gamma receptor (PPAR-gamma) regulated gene activation. Jensen et al performed transient co-transfection experiments in CV-1 cells derived from male adult African green monkey kidney at 3 months 1964 using a PPAR- γ expression construct and a firefly luciferase reporter gene containing a PPAR- γ response element (PPARE). Luciferase activity was measured using a dual luciferase reporter assay system. Firefly luminescence signal was normalized based on background control luminescence signal and the ratio of extract-treated wells to wells from the control. The transfected cells were then treated with a known PPAR-gamma inducer citiglitazone (10. mu.M) with or without the addition of extract. A positive response indicates the ability of the active substance to inhibit PPAR-gamma induction and thus influence the control of lipid production. A 50% solvent control was used in the comparison.
No statistical significance was found for PPAR-gamma inhibition using Alisma orientale. PPAR- γ is inhibited by about 15-30% in the presence of Alismatis rhizoma (see, Table 1).
Example 6
stearoyl-CoA desaturase (SCD) assay
Azgen, LLC determined the effect of herbal formulations on the inhibition of genes regulated by stearoyl-coa desaturase (SCD). Transient co-transfection experiments were performed using the SCD expression construct and a firefly luciferase reporter gene containing an SCD response element. Luciferase activity was measured using a dual luciferase reporter assay system. Firefly luminescence signal was normalized based on background control luminescence signal and the ratio of herbal treated wells to wells from the control. No statistical significance was found for stearoyl-CoA desaturase inhibition using Alisma orientale. Alisma orientale inhibits stearoyl-coa desaturase by about 15-30% (see, table 1).
All patents, patent applications, published PCT applications and treatises, books, references, reference manuals, and abstracts cited herein are hereby incorporated by reference in their entirety to more fully describe the state of the art to which the invention pertains.
Since various changes may be made in the above subject matter without departing from the scope and spirit of the invention, it is intended that all subject matter contained in the above description or defined in the appended claims be interpreted as illustrative and descriptive of the invention. Many modifications and variations of the present invention are possible in light of the above teachings.
Claims (39)
1. A topical composition comprising:
(a) a cosmetically, dermatologically, pharmaceutically, or physiologically effective amount of at least one plant extract sufficient to reduce a condition selected from the group consisting of: excess sebum production; excess subcutaneous fat; PPAR receptor up-regulation; stearoyl-coa desaturase upregulation; and adiponectin production up-regulation; and/or any combination thereof; and
(b) a cosmetically, dermatologically, pharmaceutically, or physiologically acceptable vehicle.
2. The composition of claim 1, wherein said at least one plant extract is alisma orientale.
3. The composition of claim 2, wherein said extract is from the rhizome of the plant Alisma orientale.
4. The composition of claim 1, wherein said at least one plant extract is present in an amount effective to improve the condition and/or aesthetic appearance of skin.
5. The composition of claim 1, wherein the composition is applied for a period of time sufficient to improve the condition and/or aesthetic appearance of skin.
6. The composition of claim 1, wherein said composition is applied at least once daily for a period of time sufficient to improve the condition and/or aesthetic appearance of skin.
7. The composition of claim 1, wherein said at least one plant extract is present in an amount about 0.0001 weight% to about 50 weight% based on the total weight of the composition.
8. The composition of claim 1, wherein the extract is present in an amount of about 0.001 wt% to about 20 wt% based on the total weight of the composition.
9. The composition of claim 1, wherein said at least one plant extract is in an amount sufficient to improve the condition and aesthetic appearance of skin or hair, and wherein said condition is selected from the group consisting of: one or more blemishes, rashes, cellulite, oily skin, oily hair, oily scalp, unpleasant body odor, and/or any combination thereof.
10. A topical composition comprising:
(a) a cosmetically, dermatologically, pharmaceutically, or physiologically effective amount of an extract of alisma orientale sufficient to reduce subcutaneous fat production; and
(b) a cosmetically, dermatologically, pharmaceutically, or physiologically acceptable vehicle.
11. The composition of claim 10, wherein the plant extract reduces a condition selected from the group consisting of: excess sebum production; excess subcutaneous fat; PPAR receptor up-regulation; stearoyl-coa desaturase upregulation; and adiponectin production up-regulation; and/or any combination thereof.
12. The composition of claim 10, wherein said plant extract is from the rhizome of an alisma plant.
13. The composition of claim 10, wherein the plant extract is present in an amount effective to improve the condition and/or aesthetic appearance of skin.
14. The composition of claim 10, wherein the composition is applied for a period of time sufficient to improve the condition and/or aesthetic appearance of skin.
15. The composition of claim 10, wherein said composition is applied at least once daily for a period of time sufficient to improve the condition and/or aesthetic appearance of skin.
16. The composition of claim 10, wherein the plant extract is present in an amount of about 0.0001 wt% to about 50 wt%, based on the total weight of the composition.
17. The composition of claim 10, wherein the plant extract is present in an amount of about 0.001 wt% to about 20 wt% based on the total weight of the composition.
18. The composition of claim 13, wherein said plant extract is present in an amount sufficient to improve the condition and aesthetic appearance of skin or hair, and wherein said condition is selected from the group consisting of: one or more blemishes, rashes, cellulite, oily skin, oily hair, oily scalp, unpleasant body odor, and/or any combination thereof.
19. A method of preventing, ameliorating, reducing, or managing excess subcutaneous fat production comprising administering to a subject in need thereof the composition of claim 1 in an amount effective to prevent, ameliorate, reduce, or manage excess subcutaneous fat production.
20. The method of claim 19, wherein the composition comprises at least one plant extract, wherein said extract is alisma orientale.
21. The method of claim 20, wherein said extract is derived from the rhizome of the Alisma plant.
22. The method of claim 19, wherein the composition is administered for a period of time effective to prevent, ameliorate, reduce and/or treat excess subcutaneous fat production.
23. The method of claim 19, wherein the composition is administered by daily topical application for at least one week.
24. The method of claim 19, wherein the composition is present in an amount sufficient to improve the condition and/or aesthetic appearance of skin.
25. The method of claim 19, wherein the plant extract is present in an amount of about 0.0001 wt% to about 50 wt%, based on the total weight of the composition.
26. The method of claim 19, wherein the plant extract is present in an amount of about 0.001 wt% to about 20 wt% based on the total weight of the composition.
27. The method of claim 24, wherein said composition is applied to an area of skin or hair in need thereof in an amount sufficient to improve the condition and/or aesthetic appearance of skin or hair, and wherein said condition is selected from the group consisting of: one or more blemishes, rashes, cellulite, oily skin, oily hair, oily scalp, unpleasant body odor, and/or any combination thereof.
28. A method of improving the condition or aesthetic appearance of an affected area of skin or hair comprising topically applying an amount of the composition of claim 1 effective to improve the condition or aesthetic appearance of the affected area.
29. The method of claim 28, wherein the composition comprises an extract of alisma orientale.
30. The method of claim 29, wherein the extract is from the rhizome of the Alisma plant.
31. The method of claim 28, wherein the composition is applied for a period of time effective to improve the condition and/or aesthetic appearance of the affected area.
32. The method of claim 28, wherein the composition is administered by daily topical application for at least one week.
33. The method of claim 28, wherein the plant extract is present in an amount of about 0.0001 wt% to about 50 wt%, based on the total weight of the composition.
34. The method of claim 28, wherein the plant extract is present in an amount of about 0.001 wt% to about 20 wt% based on the total weight of the composition.
35. The method of claim 28, wherein the affected area of skin or hair is in a non-diseased state and exhibits characteristics associated with a condition selected from the group consisting of: one or more blemishes, rashes, cellulite, oily skin, oily hair, oily scalp, unpleasant body odor, and any combination thereof.
36. The method of claim 28, wherein the condition is cellulite.
37. The method of claim 28, wherein the condition is acne.
38. The method of claim 28, wherein the condition is oily skin.
39. The method of claim 28 wherein the condition is oily hair or scalp.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11/021,023 | 2004-12-22 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HK1158949A true HK1158949A (en) | 2012-07-27 |
| HK1158949B HK1158949B (en) | 2018-04-27 |
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