Abstract: Tetrasubstituted glucopyranosylated benzene derivatives of general formula (I) as defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.

Abstract: A compound of formula (I) or a polymorphic form thereof can be used for the preparation of a cosmetic or dermato logical composition for the treatment of skin ageing.

Abstract: Disclosed is the most optimal biomarker for the BIOLOGICAL POTENCY of Emblica Officinalis Gaertn. (Amla) fruit and products standardized for 5% and above w/w of the said biomarker. Further, the products described herein contain from about 0.00010% to about 4% of free ascorbic acid depending on the raw material used. The optimal biomarker for amla described herein above is represented by STR#1.

Abstract: The invention relates to a D-glucopyranose 1-[3,5-bis(1,1-dimethyl-ethyl)-4-hydroxybenzoate compound defined by formula (I). It applies in particular to the preparation and the use of this compound and of its derivatives for the preparation of medicaments for the treatment and/or prevention of infections with enveloped viruses, and in particular, in humans, the herpes virus, the Aids virus, the flu virus, the hepatitis B virus, the hepatitis C virus, the dengue virus and the ebola virus, and, in animals, the porcine pseudorabies virus, for example.

Abstract: Activated fatty acids, pharmaceutical compositions including activated fatty acids, methods for using activated fatty acids to treat a variety of diseases, and methods for preparing activated fatty acids are provided herein.

Abstract: A method of eliminating the reactivity of lipoarabinomannan contained in a sample to a Limulus reagent including at least the step of allowing the sample containing lipoarabinomannan to coexist together with a metal salt or a buffer; and a method of assaying an endotoxin and a method of detecting an endotoxin-associated disease by using the above-described method.

Abstract: The invention provides methods and compositions for preparing antibodies and antibody derivatives with reduced core fucosylation.

Abstract: Estrogenic compositions comprising nyasol and analogs thereof are provided. Also provided are methods of using said extracts to achieve an estrogenic effect, especially in a human, e.g. a female human. In some embodiments, the methods include treatment of climacteric symptoms. In some embodiments, the methods include treatment of estrogen receptor positive cancer, such as estrogen responsive breast cancer. In some embodiments, the methods include treatment or prevention of osteoporosis.

Abstract: The invention relates to the preparation of phenolics derivatives by enzymatic condensation of phenolics selected among pyrocatechol or its derivatives with the glucose moiety of sucrose. The production of said phenolics derivatives is achieved with a glucosyltransferase (EC 2.4.1.5). These O-?-glucosides of selected phenolics are new, have a solubility in water higher than that of their parent polyphenol and have useful applications in cosmetic and pharmaceutical compositions, such as antioxidative, antiviral, antibacterial, immune-stimulating, antiallergic, antihypertensive, antiischemic, antiarrhythmic, antithrombotic, hypocholesterolemic, antilipoperoxidant, hepatoprotective, anti-inflammatory, anticarcinogenic antimutagenic, antineoplastic, anti-thrombotic, and vasodilatory formulations, or in any other field of application.

Abstract: Compounds of the formula: are described, along with pharmaceutical compositions containing these compounds, and methods of using the compounds to prevent and to treat cancer in mammals, including humans.

Abstract: The present invention provides a novel ascorbic acid derivative as a provitamin C with improved stability in the body and prolonged life in the body compared to conventionally known 2-O-(?-D-glucopyranosyl)ascorbic acid. The composition comprising the novel compound 2-O-(?-D-glucopyranosyl)ascorbic acid has been extracted from plants such as from Ningxia Lycium barbarum L. and/or Lycium chinense Mill. The compositions comprising 2-O-(?-D-glucopyranosyl)ascorbic acid may be enzymatically synthesized using ?-D-glucosyltransferase. Pure 2-O-(?-D-glucopyranosyl)ascorbic acid may be produced from such compositions. Alternatively, 2-O-(?-D-glucopyranosyl)ascorbic acid may be produced by chemical synthesis. The 2-O-(?-D-glucopyranosyl)ascorbic acid results in higher stability and a prolonged life of vitamin C when ingested in the body compared to the corresponding ?-D-glucopyranosyl derivative, and is therefore highly suitable as a provitamin C to be used in cosmetics and foods.

Abstract: A method of eliminating the reactivity of lipoarabinomannan contained in a sample to a Limulus reagent including at least the step of allowing the sample containing lipoarabinomannan to coexist together with a metal salt or a buffer; and a method of assaying an endotoxin and a method of detecting an endotoxin-associated disease by using the above-described method.

Abstract: A Fraxinus excelsior seed extract that can be administered for therapeutic treatment of a subject, including a human, by blocking fat synthesis, activating PPAR-alpha, increasing hypoglycemic activity, reducing bodyweight, controlling fasting plasma insulin levels against hyperinsulinemia, and promoting insulin sensitivity and causing a beneficial acute insulinotropic effect. The Fraxinus excelsior seed extract includes, inter alia, an isolated compound (2S,3E,4S) 2H-Pyran-4-acetic acid-3-ethylidene-2-[(6-O-?-D-glucopyranosyl-?-D-glucopyranosyl) oxy]-3,4-dihydro-5-(methoxycarbonyl)methyl ester, commonly called excelside A, an isolated compound (2S,3E,4S) 2H-Pyran-4-acetic acid-3-ethylidene-2-[(6-O-?-D-glucopyranosyl-?-D-glucopyranosyl)oxy]-3,4-dihydro-5-(methoxycarbonyl) 2-(4-hydroxyphenyl)ethyl ester, commonly called excelside B, and the compounds G15, G13, nuzhenide, and oleoside dimethyl ester.

Abstract: This invention provides compositions, methods and process of producing extracts from Xanthoceras sorbifolia. The extract comprises alkaloids, coumarins, saccharides, proteins, polysaccharides, glycosides, saponins, tannins, acid, flavonoids and others. The composition can be used for treating breast, leukocyte, liver, ovarian, bladder, prostate, bone or brain cancer. This invention provides compounds comprising at least one sugar, a triterpene, such as Sapogenin, and at least one side chains at Carbon 21 and 22, such as Angeloyl groups. The compounds of the present have various pharmaceutical and therapeutic applications, including treating breast, leukocyte, liver, ovarian, bladder, prostate, bone or brain cancer.

Abstract: Novel compounds such as compounds designated herein as Y or Y3, Y1, Y2, Y8, Y9 and Y10 are disclosed. These compounds have anticancer activity. The compounds of the present invention are obtainable from plants in the sapindaceae family, such as Xanthoceras sorbifolia, or other natural sources or products. The compounds of the present invention may also be synthesized chemically.

Abstract: The present invention provides a method of identifying a drug candidate capable of removing peptide, oligopeptide, polypeptide or protein from fibril or aggregate, which includes measuring, in the presence of a test compound, the concentration of a soluble peptide, a soluble oligopeptide, a soluble polypeptide or a soluble protein in an equilibrium state in a solvent. Moreover, the present invention provides a dissolution promoter to remove peptide, oligopeptide, polypeptide or protein from fibril or aggregate, which contains the compound obtained by the identification method as an active ingredient.

Abstract: The present invention relates to an oral care composition, which contains a compound represented by the formula (A): (wherein, R represents a substituted or unsubstituted, linear or branched alkyl group having from 6 to 18 carbon atoms, G represents a galactose residue, m stands for an integer of from 0 to 200, and n stands for an integer of from 1 to 30); and a coaggregation inhibitor of bacteria of the genus Fusobacterium and cariogenic bacteria, which contains the compound as an effective ingredient. The composition for oral cavity according to the present invention inhibits coaggregation of bacteria of the genus Fusobacterium with cariogenic bacteria so that it has an excellent caries preventive effect.

Abstract: Two hitherto unreported novel hemiterpene glycosides were isolated in substantially pure form from the root of Ilex pubescens. The chemical structures and some properties of these hemiterpenes have been elucidated. These hemiterpene glycosides possess anti-platelet aggregation activity more potent than those of salvianolic acid B and aspirin and may be used in pharmaceutical compositions in humans and mammals in need of such treatment.

Abstract: The present invention relates to a process for preparing thiophene-glycoside derivatives of the general formula (I)

Abstract: A monosaccharide compound of formula I as shown in the specification. Processes for the preparation of the compound of formula I and methods of screening for antibacterial or antibiotic compounds involving the compound of formula I.

Abstract: The hexuronic acid derivative represented by the following formula 1 or a salt thereof is used as an active ingredient of a heparin/heparan sulfate sulfotransferase inhibitor. In the formula, each of R1, R2, and R3 independently represent(s) SO3? or H which may have a substituent, provided that at least one thereof represents SO3?; X represents OR4, SR4, N(R4)2, or C(R4)3, R4 independently represents H, alkyl, alkenyl, alkynyl, acyl, aryl, or aralkyl group; one of R5 and R6 represents COOH while the other represents H; and the wavy line represents ?-glycosidic bond or ?-glycosidic bond.

Abstract: Described are ortho carboxy phenol derived acetals and compositions containing ortho carboxy phenol derived acetals which are useful for delivering biologically active compounds to cells. The acetals can be used to reversibly link up to three different molecules and have rapid hydrolysis kinetics in conditions which are present in a cell as well as in vivo. Cleavage of the acetal enhances delivery of the biologically active compound.

Abstract: Compounds represented by the general formula (1) or pharmaceutically acceptable salts thereof, effective in the prevention and/or treatment of infections with microbes: (1) (a) wherein R1 is hydrogen or straight-chain C1-6 alkylcarbonyl; R2 is hydrogen or C1-6 alkylcarbonyl; R3 is hydrogen, C1-6 alkyl, C1-6 alkylcarbonyl, C1-6 alkenyl, C2-6 alkenylcarbonyl, C2-6 alkynyl, or an Ar—B— group (wherein Ar is aryl or a heterocyclic group; and B is C1-6 alkyl, C1-6 alkylcarbonyl, C2-6 alkenyl, C2-6 alkenylcarbonyl, or C2-6 alkynyl); R5, R6, R7 and R8 are each hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, or an Ar—B?— group (wherein B? is C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl); X is oxygen or —NR4— (wherein R4 is hydrogen, C1-6 alkyl or C1-6 alkyl which may be substituted with Ar); and R4? is hydrogen or a group represented by the general formula (a) (wherein R3? and R4? are each hydrogen or straight-chain or branched C1-6 alkylcarbonyl)

Abstract: A means and method for increasing or inhibiting the secretion of cytokines using gallotannins and ellagitannins is described. The preferred cytokine release inhibiting compounds are dimeric gallotannins having a linker molecule that misaligns the carbohydrate cores of the compounds. The preferred cytokine release promoting gallotannins and ellagitannins include a diaryl ether linker unit. In comparison to the more structurally complex ellagitannins, the compounds of this invention are structurally simpler, easier to synthesize, and more potent.

Abstract: Novel compounds such as compounds designated herein as Xanifolia-Y or -Y3, -Y1, -Y2, -Y8, -Y9 and -Y10 are disclosed. These compounds have anticancer activity. The compounds of the present invention are obtainable from plants in the sapindaceae family, such as Xanthoceras sorbifolia, or other natural sources or products.

Abstract: The compound of the present invention is a component originated from a natural material, camu camu (Myrciaria dubia), has strong antioxidative activity and stable whitening effect, and is represented by the formula (1).

Abstract: A dry hydrocolloid powder with cold-gel capabilities is produced by: dissolving a hydrocolloid comprising polysaccharide chains in an aqueous solution; heating the dissolved hydrocolloid solution to a temperature and for a time sufficient to induce a substantial alteration in the tertiary structure of the polysaccharide chains of the hydrocolloid; cooling the dissolved hydrocolloid solution to a temperature and for a time sufficient to substantially return the polysaccharide chains of the hydrocolloid to their original tertiary structure, wherein the polysaccharide chains form a gelling network; and drying the cooled hydrocolloid solution to form a dry powder. In some embodiments, the dry powder has a viscosity of between about 10 and 40 mPa-s when reconstituted in a 2% weight/weight solution at 25 degrees C. In other embodiments, the dry powder has a water absorption of greater than 20 g H2O/g powder.

Abstract: A process for producing hydrazinomonosaccharide derivatives and use of hydrazines in determining the structures of aldose and ketose monosaccharides located at the reducing ends of saccharides.

Abstract: Anthraquinones are described which have anticancer or antitumor activity and which are useful for inhibiting cancer cells and cells comprising tumors in vitro or in vivo. Preferably, the anthraquinones have the chemical formula: wherein R1 is selected from the group consisting of hydrogen, alkyl, and substituted alkyl; R2 is a group containing 1-12 carbons selected from the group consisting of alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate and combinations thereof; and R3 is a group containing 1 to 12 carbons selected from the group consisting of methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, and combinations thereof.

Abstract: The present invention provides an amine salt of a lignan compound, i.e., [1-O-[4-(3,4-dimethoxyphenyl)-2-(3-ethylpentanoyl)-5,6,7-trimethoxy-3-(methoxycarbonyl)naphthalen-1-yl]-beta-D-glucopyranoside]uronic acid, which is useful as a medicament. The present invention also provides a method for purifying said lignan compound.

Abstract: A drug complex characterized in that a residue of a drug compound such as antineoplastic agents and a carboxy(C1-4)alkyldextran polyalcohol obtained by treating a dextran under conditions that enable substantially complete polyalcoholization are bound to each other by means of a spacer comprising an amino acid or a spacer comprising peptide-bonded 2 to 8 amino acids. Said complex is characterized in that it has excellent selectivity to tumorous sites so as to exhibit high antineoplastic activity and also achieves reduced appearance of toxicity.

Abstract: The present invention relates to a ternary glucosyl complex which is a bioprecursor of at least one retinoic active ingredient for percutaneous application, having formula (I), wherein E represents a linear hydrocarbon spacer group that is branched or cyclized and has an aliphatic or aromatic content capable of containing one or several heteroatoms of oxygen and carrying one or several carbonyl groups; A represents a radical of a molecule of said retinoic active ingredient linked to the spacer group by a carboxylate function and n=1 or 2.

Abstract: The present invention relates to a novel nitrile glycoside of Formula I named NIAZIRIDIN and to analogues and derivatives thereof. The present invention also relates to a process for the isolation of a novel nitrile glycoside of Formula I below named NIAZIRIDIN and its derivatives and analogues by bioactivity-guided fractionation from the pods of Moringa oleifera. The present invention particularly relates to the bioenhancing activity of the novel nitrile glycoside of Formula I below named NIAZIRIDIN and its derivatives and analogues in enhancing bioactivity of commonly used antibiotics such as rifampicin, tetracycline and ampicillin against Gram (+) and (−) bacteria. The biomolecule also enhances the absorption of drugs, vitamins and nutrients through the gastro-intestinal membrane increasing their bio-availability. Therefore niaziridin can be used in combination therapy with drugs and nutrients resulting in reduced drug associated toxicity, reduced cost and duration of chemotherapy.

Abstract: The present invention provides a method for efficiently producing &bgr;-D-ribofuranose derivatives or optical isomers thereof, useful as synthetic intermediates of pharmaceutical nucleic acid-series products. The method comprises a step of producing 1-O-benzyl-&bgr;-D-ribofuranose-2,3,5-triacetate or an optical isomer thereof by allowing &bgr;-D-ribofuranose-1,2,3,5-tetraacetate or an optical isomer thereof to react with a benzyl alcohol in the presence of acid catalysts and a step of hydrolyzing the resulting 1-O-benzyl-&bgr;-D-ribofuranose-2,3,5-triacetate in the presence of a base to produce 1-O-benzyl-&bgr;-D-ribofuranose or an optical isomer thereof.

Abstract: Compound JK represented by the general formula (1): wherein R is H or —CH3; or a pharmaceutically acceptable salt thereof. Compound JK has an excellent antimicrobial activity even against resistant strains including MRSA and is useful as an anti-microbial agent.

Abstract: A medicament for treatment of a viral infection which comprises as an active ingredient a compound represented by the following formula (I) or its Pharmaceutically acceptable salt, or a hydrate thereof or a solvate thereof.

Abstract: This invention relates to novel aldehyde containing compounds and their uses as adjuvants and immunoeffectors.

Abstract: Compounds according to formula I: T1—L—T2   (I), wherein T1 is a taxoid group, preferably of Formula II: wherein R1 is C6H5; R2 is O; L is a linking group; and T2 is a substituent selected from the group consisting of epipodophyllotoxin, amsacrine, ellipticine, anthracycline antibiotic, mitoxantrone, and colchicine groups, and pharmaceutically acceptable salts thereof, are provided herein. The compounds are useful in, among other things, treating tumors or cancer in subjects in need thereof, inducing cellular differentiation, and inhibiting cellular mitosis.

Abstract: Derivatives of sphingolipids of the formula: are provided wherein the substituents are as defined in the specification and wherein there is at least one R2 substituent in the sphingolipid derivative. The compounds are useful in the treatment of of abnormal cell proliferation, including benign and malignant tumors, the promotion of cell differentiation, the induction of apoptosis, the inhibition of protein kinase C, and the treatment of inflammatory conditions, psoriasis, inflammatory bowel disease as well as proliferation of smooth muscle cells in the course of development of plaques in vascular tissue. The invention also includes a method for triggering the release of cytochrome c from mitochondria that includes administering an effective amount of a sphingolipid or its derivative or prodrug to a host in need thereof.

Abstract: The present invention provides an amine salt of a lignan compound, i.e., [1-O-[4-(3,4-dimethoxyphenyl)-2-(3- ethylpentanoyl)-5,6,7-trimethoxy-3- (methoxycarbonyl)naphthalen-1-yl]-beta-D- glucopyranoside]uronic acid, which is useful as a medicament. The present invention also provides a method for purifying said lignan compound.

Abstract: This invention provides &bgr;-D-Glucuronidase substrates of the formula: wherein R1, R2, and R7-R12 are independently selected from the group consisting of: hydrogen, fluorine, chlorine, bromine, iodine, alkyl, hydroxyl, alkoxy, carboxyl and nitro groups; R3-R6 are independently selected from the group consisting of hydrogen, fluorine, chlorine, bromine, iodine, nitro and amino; and M+ is selected from the group consisting of: proton, lithium, sodium, potassium, magnesium, calcium, barium, and ammonium ion.

Abstract: The present invention relates to the novel compound 2-O-(9z,12z-octadecadienoyl)-3-O-[&agr;-D-galactopyranosyl-(1″-6′)-O-&agr;-D-galactopyranosyl]glycerol (Generic name: shinbarometin) having the chemical structure represented by the following formula: or its acetate having an excellent effect on arthritis, osteoporosis and ruptured disc, and to a pharmaceutical composition containing said compound as an effective component, in combination with a pharmaceutically acceptable auxiliary, diluent, isotonic agent, preservative, lubricant and solubilizing aid, which is formulated in the form of a pharmaceutically acceptable preparation and has a potent effect for osteoporosis, arthritis and ruptured disc.

Abstract: A method for the oxidation of substrates comprising treating an aqueous, basic solution of a substrate having an oxidizable functionality using an elemental halogen as terminal oxidant in the presence of an oxoammonium catalyst/halide co-catalyst system. Use of elemental halogen, preferably chlorine gas or elemental bromine, unexpectedly allows oxidation without significant degradation of the substrate. The substrate is preferably a monosaccharide, oligosaccharide, or polysaccharide, and the oxidizable functionality is preferably an aldehyde, hemiacetal, or a primary alcohol. An effective source of the oxoammonium catalyst is 2,2,6,6-tetramethylpiperidinyl-1-oxy (TEMPO) and a particularly economical and effective catalyst is 4-acetylamino-2,2,6,6-tetramethylpiperidinyl-1-oxy.

Abstract: Biodegradable hydrogels are formed by photocrosslinking dextran-maleic acid monoesters in which the average degree of substitution of each glucose unit of each &agr;-D-glucopyranosyl of dextran by maleic acid ranges from 0.60 to 1.6 and which have a weight average molecular weight ranging from 40,000 to 80,000 on a dextran basis. The hydrogels at pH 7 have maximum swelling ratios ranging from 500 to 1,500 percent. The hydrogels are characterized by increase in swelling ratio as average degree of substitution increases. The hydrogels are useful, for example, for drug delivery and solubility enhancers of drugs, as protective encapsulators of viruses used in gene therapy, and for conventional uses of hydrogels.

Abstract: Emulsifiers based on the reaction product of hydrocolloid and dicarboxylic anhydrides, especially useful in the preparation of oil-in-water emulsions.

Abstract: A drug complex characterized in that a residue of a drug compound such as antineoplastic agents and a carboxy(C1-4)alkyldextran polyalcohol obtained by treating a dextran under conditions that enable substantially complete polyalcoholization are bound to each other by means of a spacer comprising an amino acid or a spacer comprising peptide-bonded 2 to 8 amino acids. Said complex is characterized-in that it has excellent selectivity to tumorous sites so as to exhibit high antineoplastic activity and also achieves reduced appearance of toxicity.

Abstract: A synthetic method for the preparation of the anti-tumor drug Etoposide. In one embodiment, the method includes the direct condensation of 4′-demethyl-epipodophylloxin with 2,3-di-O-dichloroacetyl-(4,6-O-ethylidene)-&bgr;-D-glucopyranose in the presence of trimethylsilyl trifluoromethane sulfonate (TMSOTf) to yield 4′-demethylepipodophyllotoxin-4-(2,3-di-O-dichloroacetyl-4,6-O-ethylidene)-&bgr;-D-glucopyranoside, followed by conversion of the same to etoposide. Other methods include use of different Lewis acids as catalyst, as well as different substituted glucopyranosides. This method provides enhanced yields over existing synthetic techniques, reduced reaction times and permits more favorable isolation reaction procedures.

Abstract: This invention relates to novel aldehyde containing compounds and their uses as adjuvants and immunoeffectors.

Abstract: The present invention is directed to novel ketomethylene group-containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.

Abstract: A metal ion complexing compound comprising a complexing agent formed of a condensation product of an aldose and a substituted benzene. The substituted benzene includes one or more groups comprising -OH, -NH2, -COOH, or -SO3H. The compound can be complexed with at least one metal ion and used for the administration of metal ions to plants and animals.