Abstract: The present invention relates to a process for the isolation of a novel oligospirostanoside structurally constructed as 3-0-[&agr;-L-rhamnopyranosyl-(1→2)-&agr;-L-rhamnopyranosyl-(1→4)-0-&bgr;-D-glucopyranosyl]-25(S)-5&bgr; spirostan-3&bgr;-ol isolated from Asparagus racemosus and biologically evaluated as a potent immunomodulatory agent.

Abstract: The invention features polymeric biomaterials formed by nucleophilic addition reactions to conjugated unsaturated groups. These biomaterials may be used for medical treatments.

Abstract: Androgen glycosides provide free, circulatory androgen on oral administration as they are subject to less, first pass breakdown by the liver.

Abstract: A 19-norbufalin derivative compound of formula (I) and isomers pharmaceutically acceptable salts thereof. Compounds of formula (I) are Na+,K+-ATPase inhibitors and can be used in the treatment of cardiac and/or vascular malfunction, renal malfunction, as digoxin antagonists, for treatment of CNS disorders and for the treatment of malignant and proliferative cell diseases.

Abstract: The present invention relates to novel human secreted proteins and isolated nucleic acids containing the coding regions of the genes encoding such proteins. Also provided are vectors, host cells, antibodies, and recombinant methods for producing human secreted proteins. The invention further relates to diagnostic and therapeutic methods useful for diagnosing and treating disorders related to these novel human secreted proteins.

Abstract: This invention provides isolated nucleic acids encoding mammalian NPFF receptors, purified mammalian NPFF receptors, vectors comprising nucleic acid encoding mammalian NPFF receptors, cells comprising such vectors, antibodies directed to mammalian NPFF receptors, nucleic acid probes useful for detecting nucleic acid encoding mammalian NPFF receptors, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding mammalian NPFF receptors, transgenic, nonhuman animals which express DNA encoding normal or mutant mammalian NPFF receptors, methods of isolating mammalian NPFF receptors, methods of treating an abnormality that is linked to the activity of the mammalian NPFF receptors, as well as methods of determining binding of compounds to mammalian NPFF receptors, methods of identifying agonists and antagonists of NPFF receptors, and agonists and antagonists so identified.

Abstract: Compounds having the formula: wherein T is a polycycloalkylidene group (e.g., adamant-2-ylidene); R is a C1-20 alkyl, aralkyl or cycloalkyl group; and Y is a fluorescent chromophore (e.g., m-phenylene), produced by reacting a compound having the formula: with an R-ylating agent (e.g., R2 SO4) in the presence of an alkali metal alkoxide in a polar aprotic solvent. Also, compounds having the formula: are produced by reacting a compound having the formula: with wherein X is an electronegative leaving group (e.g., a halogen anion such as chloride ion) in the presence of a Lewis base (e.g., a trialkyl-amine) dissolved in an aprotic organic solvent (e.g., benzene or toluene). Also, compounds having the formula are produced by reacting a compound of the formula with a tetra-O-acylated-O-hexopyranoside halide, then hydrolyzing off the protective acyl groups.

Abstract: A method for purifying a polysaccharide from group B &bgr;-hemolytic Streptococcus (GBS) bacteria includes contacting a bacterial fermentation stock with a hydrophobic interaction chromatography (HIC) resin. Additional steps may include a phenol/saline extraction and an ion exchange chromatography. The method results in a product having very high purity. The product of the purification provides a composition which is highly useful in both research and therapeutic settings.

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.

Abstract: The present invention provides a lipid-modified insulin comprising an insulin molecule linked to an alkyl group by an amine linkage. Preferably, the alkyl group is a straight chain carbon comprising from about 14 to 20 carbon atoms. Preferably, the alkyl group is linked to the B1 phenylalanine or the B29 lysine. The present invention also provides a liposome comprising such lipid-modified insulin. Preferably, the liposomes are small unilamellar vesicles (SUVs) which have a particle size of less than 100 nm.The present invention also provides a method for making a lipid-modified insulin. The method comprises reacting the protein with a hydrophobic aldehyde in the presence a reducing agent to provide a lipid-modified insulin in which an amino acid of the insulin is linked to an alkyl group by an amine linkage.The present invention also relates to a method of killing hepatoma cells, particularly the hepatoma cells that are found in a hepatocellular carcinoma.

Abstract: A method for purifying a polysaccharide from group B .beta.-hemolytic Streptococcus (GBS) bacteria includes contacting a bacterial fermentation stock with a hydrophobic interaction chromatography (HIC) resin. Additional steps may include a phenol/saline extraction and an ion exchange chromatography. The method results in a product having very high purity. The product of the purification provides a composition which is useful in both research and therapeutic settings.

Abstract: New glucose-based surfactants and methods of their synthesis are described. The surfactants are synthesized through the preparation of an intermediate glucose 4,6-cyclic sulfate. The surfactants are economical to prepare and have excellent surface-active properties.

Abstract: Sucrose ester and ether products, useful as food or beverage bulking agents, reduced calorie sweeteners, fat replacement agents, stabilizing agents, thickening agents and emulsifying agents; adhesives; biodegradable plastics and films; sizing agents for paper and textiles; ethical pharmaceuticals and new fibers are prepared by using a two-phase reaction system in which sucrose is dissolved in an alkaline, aqueous solution and an acidic reagent such as a bifunctional acid dichloride or epoxide is added to the sucrose in a water-immiscible organic solvent. Several types of products are produced: water-insoluble sucrose ester (ether) copolymers; water-soluble sucrose ester (ether) copolymers; sucrose ester (ether) dimers; and intramolecular, cyclic sucrose esters (ethers). These products can be further varied by using different kinds of acid dichlorides or epoxides that contain different kinds of functional groups.

Abstract: A method for purifying a polysaccharide from group B .beta.-hemolytic Streptococcus (GBS) bacteria includes contacting a bacterial fermentation stock with a hydrophobic interaction chromatography (HIC) resin. Additional steps may include a phenol/saline extraction and an ion exchange chromatography. The method results in a product having very high purity. The product of the purification provides a composition which is highly useful in both research and therapeutic settings.

Abstract: This invention relates to ginsenoside Mc with formula (I), ##STR1## an intestinal flora metabolite of ginseng saponin and anticancer agent containing it as an active ingredient. In addition to a novel compound, the anticancer agent of this invention consists of one active ingredient elected from compound K, compound Y or 20(S)-protopanaxatriol, intestinal flora metabolites of ginseng saponin, together with one or more pharmaceutically acceptable carriers. Said agent is a novel type of potential anticancer agent since it has immunopotentiating actions including inhibitory actions on the vascularization of tumors and extravasation of cancer cells.

Abstract: Substances comprising disaccharides and substances comprising carboxylated and/or sulfated oligosaccharides in substantially purified form, and methods of using same, are disclosed for the regulation of cytokine activity in a host. For instance, the secretion of active Tumor Necrosis Factor Alpha (TNF-.alpha.) can be either inhibited or augmented selectively by administration to the host of an effective amount of a substance of the invention. Thus, the present invention also relates to pharmaceutical compositions and their use for the prevention and/or treatment of pathological processes involving the induction of active cytokine secretion, such as TNF-.alpha.. The invention also relates to the initiation of a desirable immune system-related response by the host to the presence of activators, including pathogens. The substances and pharmaceutical compositions of the present invention may be administered daily, at very low effective doses, typically below 0.

Abstract: The invention relates to a polysaccharide toxin from group B .beta.-hemolytic Streptococcus (GBS) having improved purity. The improved purity of the toxin, 95%, is achieved by the method of purification wherein a bacterial fermentation stock is subjected to chromatography with hydrophobic interaction chromatography (HIC) resin, extraction with a phenol/saline solution followed by ion exchange chromatography. The purified GBS toxin has a molecular weight of about 300 kD and a relative carbohydrate ratio of rhamnose:mannose:galactose:glucose:N-acetyl glucosamine:N-acetyl galactosamine of about 0:1:3:1:1:1, respectively. The GBS toxin is useful for treatment of tumors and other medical conditions.

Abstract: A crystalline monohydrate of (3.beta.,5.alpha.,25R)-3-?(.beta.-D-cellobiosyl)oxy!spirostan-11-one that is useful as a hypocholesterolemic or antiatherosclerosis agent.

Abstract: In accordance with this invention novel compounds are provided that are selected from saturated and unsaturated pyrans and furans substituted with at least a phosphonate group and a heterocyclic base. These compounds are useful as antiinfectives, flame retardants, diagnostic oligonucleotides and immunogens.

Abstract: This invention relates to certain steroidal glycosides of Formula I ##STR1## wherein the values for the variables are described herein, which are useful as hypocholesterolemic agents and antiatherosclerosis agents and certain protected intermediates useful in the preparation of said steroidal glycosides.

Abstract: Compositions of sterodial glycosides are described wherein the glycoside is linked directly, or indirectly to a desired steroidal compound via a carbon, or similar stable linkage, and methods of using the compositions to treat patients by binding to and/or blocking cellular receptors for a variety of diseases including cancer, inflammation, and autoimmune diseases.

Abstract: Monomeric bile acid derivatives, processes for their preparation and the use of these compounds as medicamentsMonomeric bile acid derivatives of the formula IZ--X--GS I,in which GS, X and Z have the meanings given, and processes for their preparation are described. The compounds have useful pharmacological properties and can therefore be used as medicaments.

Abstract: Processes for the synthesis of tigogenin beta-O-cellobioside heptaalkanoate which is an intermediate for the known hypo-cholesterolemic agent tigogenin beta-cellobioside. The process comprises reacting .alpha.-cellobiosyl bromide heptaalkanoate and .beta.-tigogenin in the presence of zinc fluoride or zinc cyanide under conditions capable of forming said tigogenyl .beta.-O-cellobioside heptaalkanoate. The analogous preparations of hecogenin .beta.-O-cellobioside heptaalkanoate 11-ketotigogenin .beta.-O-cellobioside heptaalkanoate, and diosgenin .beta.-O-cellobioside heptaalkanoate are also disclosed. The process provides both high .beta.-anomeric selectivity and high yields.

Abstract: Saponin/antigen conjugates and the use thereof for enhancing immune responses in individuals are disclosed. The saponins may be substantially pure or mixtures of saponins.

Abstract: The present invention provides cleavable conjugates whose linkers contain a labile bond that is cleavable under a variety of mild conditions, including weakly acidic. Since the agent may be bonded directly to the linker, cleavage can result in release of native agent. The invention also provides methods for producing cleavable conjugates. Preferred agents include drugs, toxins, biological response modifiers, radiodiagnostic compounds, radiotherapeutic compounds, and derivatives thereof. The targeting molecule employed in the invention may be an intact molecule, a fragment thereof, or a functional equivalent thereof. In a particularly preferred embodiment, the targeting molecule is a monoclonal antibody directed towards a tumor-associated antigen in man. The invention further provides methods for delivering to the cytoplasm of a target cell an agent free of its targeting molecule carrier.

Abstract: The present invention provides N- and O-substituted aminophenol derivatives of the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, G and L are as hereinbefore defined. The present invention also provides intermediates for the preparation of these aminophenol derivatives of general formula (I), as well as the use of the aminophenol derivatives of general formula (I) for the determination of hydrolases, as well as for the preparation of agents for carrying out determinations of hydrolysis.

Abstract: Glycosides having neotigogenin aglycone moieties, administered orally to mammals are shown to inhibit the absorption of cholesterol. These compounds are useful in the treatment of hypercholesterolemia. Particular compounds are derived from tomato seeds and include neotigogenin trisaccharide.

Abstract: Hair treatment compositions containing (a) an alkyl polyglycoside of the formula IR.sup.1 O--[G].sub.p (I)wherein R.sup.1 is an alkyl or alkenyl radical having from 6 to 22 carbon atoms, G is a sugar unit having 5 or 6 carbon atoms and p is a number from 1 to 10; (b) a protein hydrolyzate having an average molecular weight in the range from 500 to 10,000 and, (c) a monomeric cationic surfactant provide hair with hold, body, stylability, strength and bounce.

Abstract: Cardioactive steroidal compounds of the formula I ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 have the meanings shown in the description, and pharmaceutical compositions containing them.

Abstract: Provided is a novel improved process for the preparation of .alpha.-D-cellobiose octaacetate via the acetylative degradation of cellulose or cellulose acetate. The title compound is provided in high yield and quality in a facile one-pot process, amenable to large-scale synthesis.

Abstract: The invention relates to alkylglycoside sulfosuccinates of the general formula (1) defined herein, useful in cosmetic preparations.

Abstract: The present invention relates to novel sweet compounds derived from the leaves of the subtropical weed Abrus precatorius, and their use as sweeteners. In particular, the present invention contemplates four novel sweet compounds isolated from A. precatorius or A. fruticulosus, and particularly, Abrusosides A, B, C and D and related compounds. The present invention also contemplates the use of these abrusosides and related compounds as sugar substitutes. The present invention contemplates the use of Abrusosides A-D as individual components or in mixtures, in a method for sweetening comestibles, foodstuffs, beverages and medicinal agents.

Abstract: The present invention provides L-isomeric nine-carbon sugars having a formed stereogenic center of R configuration, as well as methods of synthesizing the same.

Abstract: In one embodiment, this invention provides a smoking composition which contains a flavorant additive which releases menthol under normal cigarette smoking conditions.The menthol-release additive is a mixture of menthyloxycarbonylglucose compounds which include more than 35 mole percent of 1-O-menthyloxycarbonyl-.beta.-D-glucopyranose and more than about 20 mole percent of 1,6-di-O-menthyloxycarbonyl-.beta.-D-glucopyranose.

Abstract: A method of assaying, detecting, monitoring, and influencing in vitro and in vivo activity of glycosyltransferase and sugar nucleotides which are analogs of the naturally-occurring sugar nucleotides for which the glycosyltransferases are specific. These sugar nucleotide analogs include those labeled with a fluorogenic moiety at the 2' or 3' position of the ribose or at another location (e.g., on a constituent phosphate or in the nucleotide backbone), such as the UDP-galactose analog, 2'(or 3')-O-(2,4,6-trinitrophenyl)-5'-uridine diphosphate galactose (TUG). A highly specific assay for soluble glycosyltransferase has been developed which utilizes the fluorogenic sugar-nucleotide analogs. These assays rely on changes in spectral properties resulting from specific binding events of the sugar nucleotide analog and the glycosyltransferase. Assays of this invention do not rely on the use of radio-isotopes and can be used to assess glycosyltransferase activity in living cells.

Abstract: A composition of matter is provided comprising a crystalline saponin-containing complex, wherein said crystalline complex is derived from a steroidal-saponin-containing plant material. Said crystalline complex is derived from a saponin-containing plant material by forming a mixture comprising saponin-containing aqueous plant extract solids and a mixture comprising methanol, acetone and water in a volume ratio of about 0.1-20:0.1-20:1.0, and allowing the solution to stand at ambient temperature and pressure for a period of time sufficient to form the crystalline saponin-containing complex while plant fats and non-saponin carbohydrates remain substantially in solution.

Abstract: Improved processes for the synthesis of tigogenin beta-cellobioside, a known hypocholesterolemic agent, using cellobiose heptaacetate and tigogenin as starting materials.

Abstract: Preparations of drugs in admixture with certain ligands are described which, when administered to animals or humans, are less toxic than conventional drug preparations. Although the toxicity of the drug-ligand preparations described is greatly reduced, the drug retains pharmacological activity.

Abstract: Methods for the production of steroids (sapogenins) and steroidal glycosides (saponins) from cell, root-cell and shoot tissue cultures of the Yucca plant. The cultures were established and maintained in a suitable nutrient plant cell medium supplemented with growth regulators. The desired products are extracted from the cultures using conventional extraction techniques. Greater total production of steroidal glycosides occurred in root-cell, cell, and shoot tissue cultures in that order. Although the cultures may be grown under conditions ranging from total darkness to total light, steroidal glycoside production was highest in root-cell cultures grown continuously in the light as compared to those grown in the dark. Root-cell culture senescence also enhanced the yield of total steroidal glycosides. Steroids are obtained from the steroidal glycosides by acid hydrolysis to remove the sugar moieties. The production of radio-labeled steroids and steroidal glycosides is disclosed.

Abstract: Inclusion complexes of cyclodextrins, particularly .beta.-cyclodextrin, and cardiac glycosides, particularly digoxin, are disclosed. The complexes have high aqueous solubility and are useful in the preparation of pharmaceutical formulations containing cardiac glycosides for use in therapy.

Abstract: Digitonin and digitonin-related saponins are derivatized by alkoxylation. The adducts have lower toxicity, higher solubility, and reduced ability to form insoluble complexes with cholesterol, as compared to the starting material. The adducts are particularly useful as solubilizing agents for lipophilic drugs and as mycoplasma suppressors in cell cultures.

Abstract: Mixed anhydrides products are described. These mixed anhydrides are produced by reaction of a carboxylic acid-containing steroid with a material having the formula: ##STR1## wherein: X is a halogenZ is an oxygen or sulfurR is a hydrocarbonin an inert organic solvent containing a Lewis base. These mixed anhydrides may in turn be reacted with, for example, an alcohol ammonia or amine to produce the corresponding ester or amide steroid.

Abstract: There is described a new process for the preparation of optically active 2-(2',2'-dihalogenovinyl)-cyclopropane-1-carboxylic acids substituted in the 3 position, and derivatives thereof. A racemate of certain cyclobutanones is reacted with a sulfurous acid salt of an optically active base to obtain a mixture of diastereomeric 4-2-(2',2',2'-trihalogenoethyl)-cyclobutane-1-sulfonic acid salts; this mixture is then separated into the pure diastereomeric sulfonic acid salts. Either the pure diastereomeric sulfonic acid salts are converted directly to the desired optically active products, or the optically active cyclobutanones obtained from the pure diastereomeric sulfonic acids salts by decomposition is converted, in the presence of a base to the desired product. Optionally, the product, optically active 2-(2',2'-dihalogenovinyl)-cyclopropane-1-carboxylic acids can be converted to their 1',2'-dibromo derivatives.

Abstract: Nucleotides of nucleosides or bases having known cytotoxic activity are reacted with steroids, preferably corticosteroids, to form corresponding cytotoxic nucleoside-corticosteroid phosphodiester analogues of the formula: ##STR1## wherein: steroid is the residue formed by removal of a hydroxyl hydrogen atom from a natural or synthetic adrenal corticosteroid containing the characteristic cyclopentanophenanthrene nucleus which is esterified to the phosphate moiety at the 21-position;sugar is a naturally occurring pentose or deoxypentose in the furanose form, preferably ribose, deoxyribose, lyxose, xylose or arabinose and especially ribose, deoxyribose or arabinose, which is esterified to the phosphate moiety at the 5'-position and covalently bonded to the heterocycle moiety at the 1'-position to form a nucleoside; andheterocycle is a purine, pyrimidine, hydrogenated pyrimidine, triazolopurine or similar nucleoside base.

Abstract: 4,5-methano-bufadienolide-rhamnosides of the formula I ##STR1## where R.sup.1 is hydrogen or alkyl or acyl of 1 to 4 carbon atoms, R.sup.2 and R.sup.3 are identical or different and each is hydrogen or alkyl or acyl of 1 to 4 carbon atoms, or both together are ##STR2## where R.sup.4 and R.sup.5 are identical or different and each is hydrogen or alkyl or alkoxy of 1 or 2 carbon atoms.The novel compounds may be used for counteracting cardiac insufficiency.

Abstract: A readily enterally absorbable pharmaceutical composition of cardiac glycosides is disclosed which comprises a therapeutically-effective amount of at least one cardiac glycoside distributed in a vehicle comprising an absorption-enhancing amount of at least one partial glyceride of a fatty acid of medium chain length. The preparation is suited for formulating cardiac glycosides which per se are poorly enterally absorbable, in particular, k-strophanthin, g-strophanthin, and proscillaridin.

Abstract: Sterol glycosides are isolated from sterol glycoside-containing plant material by heating the material in alkaline lower alkanol at elevated temperatures in the presence of an alkali metal carbonate, bicarbonate or nitrate to effect formation and precipitation of a complex which is then isolated.

Abstract: Sterol glycosides are rendered easily absorbable through the digestive tract by dissolving or dispersing the steroid glycoside with heating into a water solution of a polymer or polymers and then removing the solvent.