Abstract: The present invention provides methods of producing libraries of compounds with enhanced desirable properties and diminished side effects as well as the compounds produced by the methods. In preferred embodiments, methods of the present invention use a universal chemical glycosylation method that employs reducing sugars and requires no protection or activation. In a preferred embodiment, the invention provides a library of neoglycoside digitoxin analogs that includes compounds with significantly enhanced cytotoxic potency toward human cancer cells and tumor-specificity, but are less potent Na+/K+-ATPase inhibitors in a human cell line than digitoxin.

Abstract: Treatments for conditions involving detrimental activity of the enzyme core 2 GlcNAc-T are provided using compounds of the formula I wherein R1 is H, —OH, C1-6 alkoxy, —NR5R6, or Sac 1; R2 is H, —OH, C1-6 alkoxy or Sac 2; R3 is H, —OH, C1-6 alkoxy or Sac 3; R4 is H, C1-6 alkyl, C1-6 hydroxyalkyl or C1-6-alkoxy-C1-6-alkyl; R5 is H, C1-6 alkyl or C1-6 acyl; R6 is H, C1-6 alkyl or C1-6 acyl; Sac 1 Sac 2 and Sac 3 are independently selected saccharide moieties; and Z is a steroid moiety; or a pharmaceutically acceptable salt, ether or ester form thereof.

Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.

Abstract: The present invention provides methods and formulations for optimizing the anti-cancer and anti-HIV activities of a camptothecin drug, including camptothecin and its related analogs including 9-aminocamptothecin and 9-nitrocamptothecin. The invention involves methodologies and formulations that limit human serum albumin-mediated reduction of the anti-cancer and anti-HIV effects of the camptothecins, and the methods and formulations provide combination therapies in which binding of the camptothecin agent to human serum albumin can be modulated by the administration of a competing agent such as ibuprofen, clofibrate or clofibric acid that also binds human serum albumin. Reduced camptothecin drug binding to human serum albumin can result in elevated camptothecin free drug levels and thus improve the effectiveness of treatment regimens involving these drugs. Further agents such as methotrexate and AZT can also be used in cancer and HIV-positive patients employing camptothecin drugs.

Abstract: Systems and methods are provided herein that provide for promoting cellular health and treatment of cancer, and allied diseases such as diabetes and glaucoma.

Abstract: Disclosed herein are substituted phenethylamine alpha adrenergic receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention provides therapeutically active compounds and compositions as NMDA and MC receptor antagonists, which are useful in preventing and treating central nervous system disorders by inhibiting over-activation of NMDA and/or MC receptors. In one aspect, the present invention provides methods of treating and/or preventing neurodegenerative diseases and neuropathological disorders, methods of providing neuroprotection under stress conditions such as a stroke, methods of enhancing the brain's cognitive functions and methods of treating depression, anxiety and cachexia induced by a chronic disease in mammals and humans.

Abstract: The invention provides a multi-compartmented container suitable for the delivery of pharmaceuticals, medicines, vitamins, and the like.

Abstract: A method for inhibiting proliferation of Helicobacter pylori including a compound that can simply be mass-produced, can specifically inhibit the proliferation of H. pylori, which has high safety and never generates any resistant bacteria, as well as a diet of a food or beverage, and a pharmaceutical preparation containing the proliferation inhibitor of Helicobacter pylori. The proliferation inhibitor of Helicobacter pylori comprises an alpha-N-acetyl-glucosaminyl bond-containing monosaccharide derivative represented by the following chemical formula (1) GlcNAc1-alpha-O—Y ??(1) (in the formula (1), Y is a straight-, branched- or cyclic-aliphatic hydrocarbon group having 1 to 27 carbon atoms or a straight-, branched- or cyclic-acyl group having 1 to 27 carbon atoms). The diet of the food, the beverage or the pharmaceutical preparation comprises the proliferation inhibitor of Helicobacter pylori.

Abstract: Processes for the preparation of Caralluma extract which includes shade-drying of Caralluma plant material; ii) treating the dried Caralluma plant material by at least one operation selected from a group consisting of sorting, cleaning and sizing to obtain Caralluma plant material meant for extraction or any combination thereof; iii) extracting the Caralluma plant material with a first solvent for at least two initial iterations followed by at least two subsequent iterations with a second solvent at controlled temperature to obtain a diluted extract; iv) removing the solvent from the diluted extract by distillation at a temperature below about 40° C. to obtain a concentrate; v) chilling the concentrate at a temperature of about 6 to about 10° C. for a period of about 7 to about 8 hours to obtain a chilled concentrate; vi) filtering the chilled concentrate to obtain a filtrate; vii) concentrating the filtrate at a temperature below about 60° C.

Abstract: Device for treating urinary infections comprising a catheter and a container, wherein the container comprises a cholesterol-binding agent. Patients who are using a urinary catheter to empty the bladder of urine are very prone to get an infection and the risk of getting a catheter associated Urinary Tract Infections (UTI) is high. The introduction of a cholesterol-binding agent facilitates a more effective curing of the infection.

Abstract: As described herein, the present invention provides methods for preparing compounds useful for treating or lessening the severity of a neurodegenerative disorder. The present invention also provides methods of treating or lessening the severity of such disorders wherein said method comprises administering to a patient a compound of the present invention, or composition thereof. Said method is useful for treating or lessening the severity of, for example, Alzheimer's disease.

Abstract: Mammalian subjects having a neoplasm are treated with a virus, a fluoropyrimidine, for example 5-fluorouracil, and a camptothecin compound. The virus is selected from the group consisting of a Newcastle disease virus, a measles virus, a vesicular stomatitis virus, an influenza virus, a Sindbis virus, a picornavirus, and a myxoma virus.

Abstract: A method of treating preeclampsia including administering a therapeutically effective dose of resibufagenin to a patient having preeclampsia. Effecting the determination of the presence of preeclampsia may be by determining whether there has been a substantial elevation in marinobufagenin which may be blood-derived or urine-derived and if such elevation does exist, concluding that preeclampsia does exist. The method may advantageously be practiced by employing urine, blood serum or blood plasma as the body specimen containing the protein in determining whether a patient has preeclampsia. In another embodiment, bufodienolide derivatives other than resibufagenin may be employed in lieu of thereof or in combination therewith. In another embodiment, resibufagenin analogues may be employed in the treatment of preeclampsia.

Abstract: A pharmaceutical composition for preventing and treating cancer comprising furost-5-ene-3,22,26-triol glycoside, which can be used to prevent and treat cancer by promoting apoptosis.

Abstract: The present invention provides lipase inhibitory agents comprising a gallotannin or ellagitannin component(s) isolated from teas or Tellima grandiflora as well as foods and beverages and medicines containing said inhibitory agents. The present invention provides lipase inhibitory agents comprising at least one of compounds represented by formula I below: wherein R1, R2 and R3 independently represent H or a gallic acid residue, and R4 and R5 represent H or a gallic acid residue, or R4 and R5 together form an HHDP group represented by the formula below: provided that at least two of R1 to R5 represent a gallic acid residue or when all of R1, R2 and R3 are H, R4 and R5 together form the HHDP group; as well as foods and beverages and medicines containing said lipase inhibitory agents.

Abstract: The present invention relates to new isopropoxyphenylmethyl inhibitors of SGLT2, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: One aspect of the invention is concerned with cannabimimetic pyrazole analogs. Another aspect of the invention is concerned with new and improved pyrazole analogs having high affinities and/or selectivities for the CB1 cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and methods of administering therapeutically effective amounts of the inventive analogs to provide a physiological effect.

Abstract: The present application relates to novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridine-3-carboxamides, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.

Abstract: The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; Z; A; B; E; X; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: DNA viral infections of the eye are treated or prevented by the application of a composition including a diuretic and/or a cardiac glycoside dissolved in a water/ethanol solution wherein the level of the ethanol is adjusted to be acceptable to the eye.

Abstract: The present invention relates to a method for reducing the toxicity of cardiac glycosides comprising the coadministration of a therapeutically effective amount of cardiac glycoside and a therapeutically effective amount ranolazine. This invention also relates to pharmaceutical formulations that are suitable for such combined administration.

Abstract: Azole nucleosides represented by the formulae (I) and (II); wherein A=C or N B?C or N X?H; C1-C6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo, halogen such as F, Cl, Br and I; OH, NH2, NH—(C1-C6 alkyl, cycloalkyl, aryl or heterocyclo); Z?H; C1-C6 alkyl, cycloalkyl, alkynyl, aryl, heterocyclo, halogen such as F, Cl, Br, I; OH NH2, NH—(C1-C6 alkyl, cycloalkyl, aryl or heterocyclo; E=(CH2)HONHR; n is an interger from 0-6 and more typically 0-3; R1= aryl or heterocyclo; each of W, Y, R is individually selected from the group consisting of H; C1-C6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo, halogen such as F, Cl, Br, and I; O, OH, Oalkyl, Oaryl, NH2, NH(C1-C6 alkyl, cycloalkyl, aryl or heterocyclo); provided that at least one of W, Y, and R is other than H and wherein both W and Y together can be ?O; and each D individually is OH, Oalkyl, Oaryl, FL and H; pharmaceutically acceptable salts thereof, prodrugs thereof and mixtures thereof are provided.

Abstract: The present invention relates to new phenylalanine amide inhibitors of ATP-sensitive potassium channels, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Gynostemma extract compositions containing gynostemma extract and at least a carrier liquid are used as cleaning agents, emulsifiers, skin care products, and foaming agents. The gynostemma extract alone or together with other herbal extracts is mixed with water, glycerin, or a mixture of water and glycerin to produce the surfactant composition. The extracts have distinctive surface tension altering functions, reducing the surface tension of aqueous solutions and allowing foam formation, micelle formation, and emulsification with oil, dirt and water insoluble substances, and may also be used as an emulsification agent with other ingredients in cosmetic or personal care products.

Abstract: A method of inhibiting the secretion of IL-8 and other pro-inflammatory cytokines from cells secreting elevated levels of these compounds is provided. The method includes contacting the cell with a composition comprising a cardiac glycoside such as oleandrin. The cardiac glycoside can be used to treat cystic fibrosis and other IL-8 dependent disorders by lowering levels of spontaneously secreted IL-8 and other pro-inflammatory cytokines. Oleandrin was found to suppress the secretion of IL-8 from cultured CF lung epithelial cells in the nanomolar concentration range. Structure-activity relationships (SARs) for cardiac glycosides are also elucidated.

Abstract: The present invention relates to the use of lipid containing particles, such as liposomes, iscom and/or iscom matrix and posintros, comprising at least one lipid and at least one saponin for the preparation of a pharmaceutical for the treatment of cancer. The saponins are preferably from Quillaja Saponaria Molin. Further, the particles are also delivery systems for one or several compounds for cancer treatment with complementary mechanisms. More, the invention discloses kit of parts comprising at least two parts, wherein one part comprising at least one saponin fraction which is hydrophobic having a killing effect on cancer cell; and the other part comprising at least one saponin fraction which is comparatively hydrophilic, stimulating and modulating the immune response.

Abstract: Unique compounds that can be used for inducing an immune response to Borrelia burgdorferi in a subject by administering a therapeutically effective amount of the glycolipid to the subject. Such administration is particularly useful for preventing or treating Lyme disease in a subject. The compounds(s), and therapeutically acceptable salts thereof, may be formulated into pharmaceutical or immunogenic compositions.

Abstract: The invention provides a cancer chemotherapeutic agent which has fewer side effects and excellent efficacy. The cancer chemotherapeutic agent of the invention includes a cholestanol derivative represented by formula (1): (wherein G represents GlcNAc-Gal-, GlcNAc-Gal-Glc-, Fuc-Gal-, Gal-Glc-, Gal-, or GlcNAc-) or a cyclodextrin inclusion compound thereof, and an anti-cancer agent.

Abstract: A method of treating a subject in need of therapy for a condition involving detrimental activity of the enzyme core 2 GlcNAc-T is provided, comprising administration of a therapeutically effective amount of an inhibitor of core 2 GlcNAc-T of the formula I to a patient in need thereof wherein R1 is H, —OH, C1-6 alkoxy, —NR5R6, or Sac 1; R2 is H, —OH, C1-6 alkoxy or Sac 2; R3 is H, —OH, C1-6 alkoxy or Sac 3; R4 is H, C1-6 alkyl, C1-6 hydroxyalkyl or C1-6-alkoxy-C1-6-alkyl; R5 is H, C1-6 alkyl or C1-6 acyl; R6 is H, C1-6 alkyl or C1-6 acyl; Sac 1 Sac 2 and Sac 3 are independently selected saccharide moieties; and Z is a steroid moiety; or a pharmaceutically acceptable salt, ether or ester form thereof

Abstract: New and useful compounds C. roseus cultured hairy roots are provided, by Isolating flavone glycosides together with a pharmaceutically acceptable carrier This is accomplished by immersing powdered the hairy roots in methanol to produce an extract, concentrating the extract, resuspending the extract in water, extracting the compound with organic solvent, and isolating the compound from the organic solvent.

Abstract: A method of treating a subject in need of therapy for a condition involving detrimental activity of the enzyme core 2 GlcNAc-T is provided, comprising administration of a therapeutically effective amount of an inhibitor of core 2 GlcNAc-T of formula I to a patient in need thereof wherein: R1 is H, C1-6 alkyl, C1-6 hydroxyalkyl, C1-6 alkoxy or C1-6-alkoxy-C1-6-alkyl; R2 is H, —OH or C1-6 alkoxy; S1 and S2 are independently selected saccharide moieties; and Z is a steroid moiety; or a pharmaceutically acceptable salt, ether or ester thereof.

Abstract: Unique compounds that can be used for inducing an immune response to Borrelia burgdorferi in a subject by administering a therapeutically effective amount of the glycolipid to the subject. Such administration is particularly useful for preventing or treating Lyme disease in a subject. The compounds(s), and therapeutically acceptable salts thereof, may be formulated into pharmaceutical or immunogenic compositions.

Abstract: This invention concerns novel methods of enhancing the solubility of a compound. Compositions prepared using such methods are also disclosed. Compositions prepared using the methods have various advantages over conventionally known compositions.

Abstract: Disclosed herein is the method for separation of enantiomers or isomers of digoxin. These isomers are to be used-in the treatment of heart failure without adverse or unneeded cardiac actions in humans. Additionally what is claimed is an isolate with less or no cardiac contractile effect but with AV node slowing such that the composition would be an effective therapy for the control of the ventricular response in atrial fibrillation. Also disclosed are methods for assaying these isomeric compounds present in biological fluids to enable the separation of pharmacologic actions.

Abstract: The present invention relates to compositions containing an extract of processed Panax genus plant and ginsenosides isolated therefrom for treat thrombotic diseases in human or mammal, the method for treating said diseases using thereby and the use thereof.

Abstract: Selective apoptotic extracts of Anemarrhena asphodeloides Bunge are provided. Also provided are methods of using said extracts to induce apoptosis in specific cells, especially in a human. Provided as well are uses of the extracts of Anemarrhena asphodeloides Bunge for the preparation of a medicament for the selective induction of apoptosis in a living being.

Abstract: Disclosed herein is rocuronium bromide having a potentiometrical assay of from 99% to 101% in acetic acid and perchloric acid, having less than about 0.2% area by HPLC of 2?-(4-morpholinyl)-16?-(1-pyrrolidinyl)-5?-androstan-3?-ol-17?-acetate, and having at least one of the solvents ethyl ether and dichioromethane in an amount equal to or less than about 850 ppm, and 600 ppm, respectively.

Abstract: The present invention relates to compositions containing an extract of processed Panax genus plant and saponin compounds isolated therefrom for treat the diseases caused by vascular injury in human or mammal, the method for treating said diseases using thereby and the use thereof. The extract of processed Panax genus plant and saponin compounds isolated therefrom shows suppressive effect on endothelial dysfunction and damage of blood-retinal on HUVEC and retinal vascular endothelial cell. Therefore, it can be used as the therapeutics or functional health food for treating and preventing the diseases caused by vascular injury.

Abstract: The present invention provides methods of diagnosing migraine attacks and determining predisposition of an individual to the development of migraine based on sodium level in the cerebrospinal fluid (CSF) and/or brain extracellular fluid. The invention also provides methods of treating migraine, wherein the individual is selected for treatment based in the individual's sodium level in the CSF and/or brain extracellular fluid. The CSF sodium level may be based on the sodium concentration in the saliva.

Abstract: To inhibit production of adipocytokines, in particular, adipocytokines that elicit insulin resistance and to prevent onset of pathosis caused by the insulin resistance, or improve the pathosis, the present invention provides an agent or a food or drink which contains 3-O-?-D-glucopyranosyl-4-methylergost-7-en-3-ol, or an organic solvent extract, a hot water extract or a squeezed liquid of a plant of the family Liliaceae or a fraction thereof which contains the compound as an active ingredient.

Abstract: The present invention relates to a method of cosmetic treatment for combating the effects of skin ageing and to novel cosmetic compositions which are particularly suitable for carrying it out. According to the invention, at least one agent for promoting the adhesion of the keratinocytes of the epidermal basal layer to the dermo-epidermal junction, especially to the collagen IV of said junction, such as, in particular, a divalent metal salt or complex, preferably magnesium aspartate or magnesium chloride, is used, optionally in association with a stimulant of collagen IV synthesis and/or a stimulant of collagen VII synthesis.

Abstract: Obtaining, producing and using metabolites having anti-botrytis cinerea properties from a natural extract of a native Chilean plant. An in vitro cultivated quillay extract (Quillaza saponaria Mol.), which allows improving the antifungal activity as the result of the enrichment of some secondary metabolites not found in the in vivo plants. Also provided are an in vivo cultivation method, an extraction method, a biocide formulation, and their applications and uses.

Abstract: A method of treating the skin and accelerating its natural anti-aging and wound-healing processes by using photorejuvenation at a specified total light flux at a specified range of wavelengths from a hand-held light source in combination with the topical ingredients including extracts. Some extracts may be panax ginseng, camellia sinensis, and/or gynostemma pentaphyllum, to effect superior transdermal penetration and intra-cellular delivery, effecting greater bioavailability and bioutilization of some other anti-aging topicals.

Abstract: Use of ginsenoside Compound-K, which structural formula is the following: in manufacturing medicaments for prevention or treatment of arthritis.

Abstract: The present invention relates to a method of inhibiting angiogenesis in a biological system. The method includes administering to the biological system an effective amount of a steroid saponin.

Abstract: A method is provided for treating, preventing or ameliorating neoplasia in a subject. This method includes administering to the subject an amount of actein or an amount of an extract of black cohosh that contains a triterpene glycoside, which amount of the actein or black cohosh is effective to treat, prevent or ameliorate the neoplasia, in combination with an amount of a statin which is effective to treat, prevent, or ameliorate the neoplasia. Related methods for treating, preventing or ameliorating breast cancer, or liver cell neoplasia are also provided. In addition, methods for modulating a cholesterol biosynthesis pathway and a stress response pathway in a subject are provided. These methods include administering to a subject a composition comprising an anti-neoplastic synergistic amount of a statin and actein. Compositions for carrying out such methods are also provided.

Abstract: The present invention relates to a method of inhibiting growth of a cancerous cell. The method includes the step of exposing the cancerous cell to an anti-cancer therapy and an effective amount of a steroid saponin.

Abstract: Extracts of Hoodia plant containing steroidal glycosides which have improved flavor, by virtue of reduced levels of discovered negative flavor compounds. Food compositions containing steroidal glycosides with reduced amounts of discovered negative flavor components are also included.

Abstract: The invention relates to plant extracts, especially based on species of the genus Agapanthus and combinations thereof with other extracts deriving from other plants. The invention further relates to the isolation, purification and identification of compounds in these extracts. The plant extracts and the isolated substances show significant antimicrobial activity, especially antifungal activity, and bio-stimulatory efficacy, when applied to other plants in vitro and in vivo, including under field conditions. The products according to this invention are suitable to be used as plant protecting agents for many crops and economic plants as an alternative for chemical pesticides.