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Butanol extract of bidens pilosaRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Plant Material Or Plant Extract Of Undetermined Constitution As Active Ingredient (e.g., Herbal Remedy, Herbal Extract, Powder, Oil, Etc.)Butanol extract of bidens pilosa description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070053998, Butanol extract of bidens pilosa. Brief Patent Description - Full Patent Description - Patent Application Claims
BACKGROUND [0001] T cells, a class of lymphocytes developed in the thymus, are responsible for cell- and antibody-mediated immunity. Two major classes of T cells perform very different functions. CD8.sup.+ cytotoxic T cells kill infected cells or eliminated microorganisms, and CD4.sup.+ helper T cells help activate responses of other white cells, mainly by secreting a variety of local mediators lymphokines, interleukins, or cytokines. [0002] There are two subsets of helper T cells, i.e., Th1 and Th2 cells, which function differently. Th1 cells mediate cellular immunity. They are related to rheumatoid arthritis, non-obese diabetes, and colitis. Th2 cells mediate humoral immunity. They are related to humoral immune response, asthma, inflammation, and allergy. Both Th1 and Th2 cells are derived from naive helper T cells (Th0). SUMMARY [0003] This invention is based on a surprising finding that a butanol extract from Bidens pilosa and three compounds isolated from this plant effectively inhibit Th1 cell differentiation and promote Th2 cell differentiation. [0004] Thus, one aspect of this invention is a Bidens pilosa extract prepared by a method including (1) stirring a pulverized Bidens pilosa plant in water (e.g., boiling water) to form a suspension, (2) collecting an aqueous solution from the suspension, and (3) extracting the aqueous solution with butanol to provide the extract. [0005] Also within the scope of this invention are compounds of formula I shown below: wherein R.sub.1 is H, alkyl, aryl, or cyclyl; R.sub.2 is pyranose; R.sub.3 is H or alkyl; m is 2, 3, or 4; n is 0; o is 0, 1, 2, 3, 4; and p is 1, 2, 3, or 4. These compounds are either present in the above-described extract or analogues thereof. [0006] Referring to formula I, R.sub.1 can be methyl, R.sub.2 can be .beta.-glucopyranose, R.sub.3 can be H, m can be 4, o can be 2, and p can be 1. [0007] Yet another aspect of this invention is a method of inhibiting Th1 cell differentiation or promoting Th2 cell differentiation. The method includes administering to a subject an effective amount of the above-described Bidens pilosa extract or a compound of formula II: wherein R.sub.1 is H, alkyl, aryl, or cyclyl; R.sub.2 is pyranose; R.sub.3 is H or alkyl; m is 2, 3, 4, 5, or 6; n is 0, 1, 2,or 3; o is 0, 1, 2, 3, 4; and p is 1, 2, 3, or 4. [0008] Referring to formula II, R.sub.1 can be methyl, R.sub.2 can be .beta.-glucopyranose, and R.sub.3 can be H. [0009] Set forth below are three exemplary unsaturated compounds that can be used to practice this method: [0010] Also within the scope of this invention is a composition containing the above-described Bidens pilosa extract or a compound of formula II and a pharmaceutically acceptable carrier, as well as use of the composition for the manufacture of a medicament for inhibiting Th1 cell differentiation, promoting Th2 cell differentiation, or treating Th1 or Th2-mediated disorders. [0011] The details of one or more embodiments of the invention are set forth in the description below. Other features, objects, and advantages of the invention will be apparent from the description, and from the claims. DETAILED DESCRIPTION [0012] This invention relates to a Bidens pilosa extract and its use in inhibiting Th1 differentiation from Th0 and promoting Th2 differentiation from Th0. [0013] The extract can be prepared from Biodens pilosa plant by first extracting the plant with water and then extract the water solution with butanol. A detailed procedure of preparing such an extract is provided in an example below. The Bidens pilosa plant is a tropical weed used widely in herbal medicine. Its cultivation, growth, taxonomy, and agriculture practice are well known in the art. See, e.g., Duke. J. A. et al. Medicinal Plants of China, Reference Publications, Inc. 1985. [0014] This invention also relates to the compounds of formula I or formula II described above. These compounds can be either isolated from the above-described extract or synthesized by conventional methods. The isolation can be conducted by extraction, thin layer chromatography, high pressure liquid chromatography, and/or other suitable techniques. The synthesis includes total synthesis from smaller molecules and modification of functional groups on analogous compounds. [0015] The chemicals used in the synthesis may include, for example, solvents, reagents, catalysts, protecting group and deprotecting group reagents. In addition, various synthetic steps may be performed in an alternate sequence to give the desired compounds. Synthetic chemistry transformations and protecting group methodologies (protection and deprotection) useful in synthesizing applicable fused pyrazolyl compounds are known in the art and include, for example, those described in R. Larock, Comprehensive Organic Transformations, VCH Publishers (1989); T. W. Greene and P. G. M. Wuts, Protective Groups in Organic Synthesis, 2d. Ed., John Wiley and Sons (1991); L. Fieser and M. Fieser, Fieser and Fieser's Reagents for Organic Synthesis, John Wiley and Sons (1994); and L. Paquette, ed., Encyclopedia of Reagents for Organic Synthesis, John Wiley and Sons (1995) and subsequent editions thereof. [0016] The above-described extract and compounds inhibit Th1 cell differentiation and promote Th2 differentiation. Thus, this invention relates to methods of inhibiting Th1 cell differentiation, promoting Th2 differentiation, or treating a Th1-mediated disorder or a Th2-mediated disorder by administering to a subject in need thereof an effective amount of the active extract or one or more of the active compounds. The term "an effective amount" refers to the amount of the active substance which is required to confer one of the above-described effects in the subject. Effective amounts may vary, as recognized by those skilled in the art, depending on route of administration, excipient usage, and the possibility of co-usage with other agents. The term "treating" refers to administering such an active substance to a subject that has a Th1-mediated disorder or a Th2-mediated disorder, or has a symptom of the disorder, or has a predisposition toward the disorder, with the purpose to cure, heal, alleviate, relieve, alter, remedy, ameliorate, improve, or affect the disorder, the symptoms of the disorder, or the predisposition toward the disorder. The terms "Th1-mediated disorder" and "Th2-mediated disorder" refers to disorders which can be treated by mediating Th1 cell differentiation and Th2 differentiation, respectively. Examples of Th1-mediated disorders include, but are not limited to, non-obese diabetes, Crohn's colitis, autoimmune hemolytic anemia, rheumatoid arthritis, autoimmune encephalitis, multiple sclerosis, or autoimmune myocarditis. [0017] To practice one of the above-described methods, one administers to a subject in need thereof orally, rectally, parenterally, by inhalation spray, or via an implanted reservoir a composition that contains either the extract or one or more of the compounds. The composition may also contain a pharmaceutically acceptable carrier. The term "parenteral" as used herein includes subcutaneous, intracutaneous, intravenous, intramuscular, intraarticular, intraarterial, intrasynovial, intrastemal, intrathecal, intralesional and intracranial injection or infusion techniques. [0018] An oral composition can be any orally acceptable dosage form including, but not limited to, tablets, capsules, emulsions and aqueous suspensions, dispersions and solutions. Commonly used carriers for tablets include lactose and corn starch. Lubricating agents, such as magnesium stearate, are also typically added to tablets. For oral administration in a capsule form, useful diluents include lactose and dried corn starch. When aqueous suspensions or emulsions are administered orally, the active ingredient can be suspended or dissolved in an oily phase combined with emulsifying or suspending agents. If desired, certain sweetening, flavoring, or coloring agents can be added. [0019] A sterile injectable composition (e.g., aqueous or oleaginous suspension) can be formulated according to techniques known in the art using suitable dispersing or wetting agents (such as, for example, Tween 80) and suspending agents. The sterile injectable preparation can also be a sterile injectable solution or suspension in a non-toxic parenterally acceptable diluent or solvent, for example, as a solution in 1,3-butanediol. Among the acceptable vehicles and solvents that can be employed are mannitol, water, Ringer's solution and isotonic sodium chloride solution. In addition, sterile, fixed oils are conventionally employed as a solvent or suspending medium (e.g., synthetic mono- or di-glycerides). Fatty acids, such as oleic acid and its glyceride derivatives, are useful in the preparation of injectables, as are natural pharmaceutically-acceptable oils, such as olive oil or castor oil, especially in their polyoxyethylated versions. These oil solutions or suspensions can also contain a long-chain alcohol diluent or dispersant, or carboxymethyl cellulose or similar dispersing agents. [0020] An inhalation composition can be prepared according to techniques well known in the art of pharmaceutical formulation and can be prepared as solutions in saline, employing benzyl alcohol or other suitable preservatives, absorption promoters to enhance bioavailability, fluorocarbons, and/or other solubilizing or dispersing agents known in the art. [0021] A topical composition can be formulated in form of oil, cream, lotion, ointment and the like. Suitable carriers for the composition include vegetable or mineral oils, white petrolatum (white soft paraffin), branched chain fats or oils, animal fats and high molecular weight alcohols (greater than C12). The preferred carriers are those in which the active ingredient is soluble. Emulsifiers, stabilizers, humectants and antioxidants may also be included as well as agents imparting color or fragrance, if desired. Additionally, transderrnal penetration enhancers may be employed in these topical formulations. Examples of such enhancers can be found in U.S. Pat. Nos. 3,989,816 and 4,444,762. Creams are preferably formulated from a mixture of mineral oil, self-emulsifying beeswax and water in which mixture the active ingredient, dissolved in a small amount of an oil, such as almond oil, is admixed. An example of such a cream is one which includes about 40 parts water, about 20 parts beeswax, about 40 parts mineral oil and about 1 part almond oil. Ointments may be formulated by mixing a solution of the active ingredient in a vegetable oil, such as almond oil, with warm soft paraffin and allowing the mixture to cool. An example of such an ointment is one which includes about 30% almond and about 70% white soft paraffin by weight. Continue reading about Butanol extract of bidens pilosa... Full patent description for Butanol extract of bidens pilosa Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Butanol extract of bidens pilosa patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. 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