Abstract: Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as prostate-specific antigen (PSA) and cathepsin B are provided, as well as compositions comprising these conjugates. Methods of using these conjugates in the treatment of prostate diseases are also provided.

Abstract: A compound represented by the general formula (I) or a salt thereof, wherein R represents a group represented by the following formula (A), (B) or (C) wherein R1 and R2 independently represent a C1-6 alkyl group, R3 represents an amino group, a mono(C1-6 alkyl)amino group, a di(C1-6 alkyl)amino group or a C1-6 alkoxy group and X-represents an anion, and n represents an integer of 2 to 5. The compound or a salt is useful as a ligand of inositol-1,4,5-trisphosphate (IP3) receptor.

Abstract: Isoflavones are modified by esterification at one or more of the C4′, C5, C6, and C7 positions to promote bioavailability, and especially to enhance solubility over the corresponding unesterified isoflavones. Preferred modifications produce a carboxylic acid hemiester or a phosphate ester which is biologically hydrolysable. Preferred starting isoflavones are genistin and daidzin, and still more preferably comprises an aglycone form such as genistein or daidzein. Esterified isoflavones may be employed therapeutically or prophylactically for a variety of conditions, provided as a dietary supplement, or added to natural or processed food-stuffs. Further preferred uses include incorporation of contemplated compounds into topical formulations, and especially cosmetic topical formulations.

Abstract: The present invention provides novel benzopyran compounds, pharmaceutically acceptable salts thereof and stereoisomers thereof where the benzopyran compounds of the invention are compounds according to Formula I: The present invention further provides pharmaceutical compositions which possess anti-estrogenic activity and comprise at least one benzopyran compound of the invention and a method of treating breast cancer by administration of an effective amount of a benzopyran compound provided by the present invention.

Abstract: Compounds of the formula wherein X in each of formulas (1) and (2) represents a substituted or unsubstituted alkylene, alkenylene, or alkynylene linker of 2-6C; Y is of the formula  or a stereoisomer thereof, wherein R1 is substituted or unsubstituted alkyl; each R2 is independently H, hydroxy, alkoxy (1-6C) or lower alkyl (1-4C); R3 is H, hydroxy, or alkoxy (1-6C); or Y is of the formula  wherein each n is 1, Z is N, K comprises a substituted or unsubstituted aromatic carbocyclic or heterocyclic ring system which may optionally be spaced from the linkage position shown in formula (7) by a linker of 1-2C, or in formula (7), Z may be spaced from the carbon bonded to X by ═CR6— wherein R6 is H or linear, branded or cyclic alkyl (1-6C), R5 is H or linear, branched or cyclic alkyl, and R′ represents a cation, H or a substituted or unsubstituted alkyl group of 1-6C, promote bone formation and are thus useful in treating oste

Abstract: In vitro methods for qualitative screening and/or quantitative determination of the functional activity of components of the Protein C anticoagulant pathway of blood coagulation are described. The methods entail measuring the conversion rate of a substrate by an enzyme, the activity of which is related to the Protein C anticoagulant activity, in a blood sample of a human comprising coagulation factors and said substrate, after at least partial activation of coagulation through the intrinsic, extrinsic or common pathway and triggering coagulation by adding calcium ions; and comparing said conversion rate with the conversion rate of a normal human blood sample determined in the same way. The methods include the addition of additional metal ions to the sample to enhance activity, sensitivity and resolution. Kits and reagents for use in the methods are also provided.

Abstract: A polybifunctional reagent having a polymeric backbone, one or more pendent photoreactive moieties, and two or more pendent bioactive groups. The reagent can be activated to form a bulk material or can be brought into contact with the surface of a previously formed biomaterial and activated to form a coating. The pendent bioactive groups function by promoting the attachment of specific molecules or cells to the bulk material or coated surface. Bioactive groups can include proteins, peptides, carbohydrates, nucleic acids and other molecules that are capable of binding noncovalently to specific and complimentary portions of molecules or cells.

Abstract: The present invention is directed to novel water-soluble prodrugs of aliphatic or aromatic hindered hydroxyl group containing pharmaceuticals.

Abstract: A packaging cell line capable of complementing recombinant adenoviruses based on serotypes from subgroup B, preferably adenovirus type 35. The cell line is preferably derived from primary, diploid human cells transformed by adenovirus E1 sequences either operatively linked on one or two DNA molecules, the sequences operatively linked to regulatory sequences enabling transcription and translation of encoded proteins. Also, a cell line derived from PER.C6 that expresses functional Ad35 E1B sequences. The Ad35-E1B sequences are driven by the E1B promoter and terminated by a heterologous poly-adenylation signal. The new cell lines are useful for producing recombinant adenoviruses. The cell lines can be used to produce human recombinant therapeutic proteins such as human antibodies. In addition, the cell lines are useful for producing human viruses other than adenovirus such as influenza, herpes simplex, rotavirus, and measles.

Abstract: The present invention relates to a highly potent herbal composition for improving overall mental performance in children, adults and mentally deficient people characterized by using extracted active plant materials from Brahmi herb and at least one of the herbs from Acorus calamus and Celestrus paniculatus oil.

Abstract: The invention relates to the use of a composition containing, preferably in a physiologically acceptable medium comprising an aqueous phase, at least one oxidation-sensitive hydrophilic active principle selected from the group consisting of ascorbic acid and its derivatives and at least one non-crosslinked N-vinylimidazole polymer or copolymer, the active principle and the polymer or copolymer both being present in the aqueous phase, for promoting the synthesis of epidermal ceramides and/or for improving the barrier function of the skin, among other uses.

Abstract: The present invention provides methods and compositions for the oral administration of Lactobacillus and/or other probiotic organisms, such as Bifidobacterium, for establishment and maintenance of a healthy urogenital flora. The invention also provides methods and compositions to reduce the risk of disease, including onset of preterm labor due to vaginal and cervical infection. The invention also provides ex vivo methods of restoring healthy gastrointestinal and vaginal flora.

Abstract: Disclosed herein are the methods of using the H4-1BB protein, ligands to this protein, and various mAbs either directed against H4-1BB or other molecules that can be used therapeutically. The nature and importance of the H4-1BB molecule provides the ligands and related co-stimulatory molecules the ability to enhance or suppress T-cell activation and proliferation. By treating T-cells that have expressed receptor protein H4-1BB with one of the four anti-H4-1BB monoclonal antibodies disclosed herein activation or inhibition of the immune response is seen. Also disclosed herein is cDNA for the human receptor H4-1BB. The cDNA of the human receptor H4-1BB is about 65% homologous to the mouse cDNA 4-1BB and was isolated by using probes derived from murine cDNA 4-1BB. A fusion protein for detecting cell membrane ligands to human receptor protein H4-1BB was developed.

Abstract: In various aspects, the invention provides compounds that bind to one or more RANTES receptors for the treatment of chemokine mediated disease states, such as compounds of formula (I): 1

Abstract: Disclosed herein is a stabilization method of nano-sized emulsion by using lecithin and tocopheryl derivatives represented by the following formula (I) and 1

Abstract: A conjugate of somatostatin-spacer-drug and a method of making the same. The conjugate can be used to enhance an anti-cancer drug's specificity on the targeted tumor cells, thus increasing its therapeutic efficacy while reducing side-effects.

Abstract: The invention relates to a method for producing L(−)-carnitine. The aim of the invention is to depict a method which permits the synthesis of L(−)carnitine from crotonobetaine. crotonobetaine salts or derivatives in an ecologically advantageous manner by immobilizing cells of Escherichia coli 044 K74 in a continuously operating cell recycle reactor. Growing or resting cells of E. coli are retained in a continuously operating cell recycle reactor by micro or ultrafiltration membranes which are arranged as a flat membrane module or hollow chamfer module.

Abstract: 3-Deoxyflavonoid compounds and methods for inhibiting T-cell activity and treating diseases and disorders (e.g., autoimmune disorders, inflammatory disorders, diabetes, ALS, MS, rheumatoid arthritis, etc.). In some cases the efficacy and/or duration of action of luteolin and/or other 3-dioxyflavinoid compounds may be increased by administering such compounds along with Rutin, a Rutin congener and/or a Rutin derivative. Also, in some cases, first pass metabolism of luteolin or other 3-deoxyflavinoids may be avoided by administering such compounds by parenteral routes (e.g., sublingual, buccal, intranasal, injection, etc.).

Abstract: The present disclosure describes the use of genetic variance information for folate transport or metabolism genes or pyrimidine transport or metabolism genes in the selection of effective methods of treatment of a disease or condition. The variance imformation is indicative of the expected response of a patient to a method of treatment. Methods of determining relevant variance information and additional methods of using such variance information are also described.

Abstract: Immune enhancement compositions for vaccines for virus, bacteria and/or infectious pathogens which contain stable activity-type antioxidant provitamins; a method of enhancing the immunity of vaccines for virus, bacteria and/or infectious pathogens with use of these compositions; and use of the above composition. As the stable activity-type antioxident provitamins, at least one compound selected from among L-ascorbic acid derivatives and &agr;-tocopherly phophates is used.

Abstract: The present invention provides synthetic methods and compositions for treatment of autoimmune and anti-inflammatory disorders comprising administering an effective amount of a derivative of triptolide alone or in combination or alternation with other anti-autoimmune or anti-inflammatory compounds.

Abstract: Orthomolecular Vitamin E derivative compounds, compositions, and their uses for effecting aging and longevity, nerve activity, hematopoiesis and maintenance of blood cells, hepatic activity, nephritic activity, heart and cardiovascular function, pulmonary function, muscular function, cartilage, bone, and joint health, gastrointestinal function, reproductive system function, vision, immune function, cell membrane integrity, and pain and inflammation; preventing or treating diseases or conditions; treating cancers or obesity; and reducing the risk of Sudden Infant Death Syndrome in an animal.

Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes.

Abstract: Sperm, oocyte, and embryo survival and function is improved in vivo or in vitro by the use of a polysaccharide containing arabinose, galactose and/or hexuronic acid. In particular, a nonspermicidal lubricant containing such a polysaccharide (e.g., gum arabic, pectin, or galacturonic acid) increases the fertilization potential of the sperm during coitus, artificial insemination or sperm collection. Similarly, a freezing medium containing a polysaccharide containing arabinose, galactose and/or hexuronic acid enhances sperm, oocyte, or embryo viability.

Abstract: A method for measurement of the hepatitis C virus (HCV) characterized by measuring HCV core antigen and HCV core antibody by their binding with probes in the presence of an anionic surfactant or a non-ionic surfactant, or both.

Abstract: The present invention relates to the storage agent for preservation of an animal cell or organ and preserved process. Ordinary method of cell storage is employed preserving method by freezing at extra low temperature of −196° C. and the survival ratios of cells after thawing and fusion is low, about 10 to 30%. The period of validity is a very short time of 12 to 72 hours. The storage agent can make protein stabilize to protein type storage agent, and prevent, treat and improve organ injury caused on an organ transplant operation by adding the polyphenol.

Abstract: The present invention provides an antiproliferative compound having the structural formula 1

Abstract: A composition and method for minimizing the absorption of triglycerides and fats in the gastrointestinal tract is described. The composition comprises psyllium and chitosan in a ratio range of 2:1 to 11:1 by weight, preferably 2:1 to 9:1, and most preferably 2:1 to 4:1 to provide a synergistic fat-binding effect.

Abstract: The inventors propose a combination of an HMG-CoA reductase inhibitor (also referred to as “HMG-CoA inhibitor(s)”), and COX-2 inhibitor for the treatment of cancer especially prostate cancer and a method of treatment of cancer by that combination, especially prostate cancer. The inventors propose a combination of an HMG-CoA reductase inhibitor, COX-2 inhibitor, and glutathione pathway enhancing and detoxifying compound, particularly cystine, for the treatment of cancer especially prostate cancer and a method of treatment of cancer by that combination, especially prostate cancer. Also contemplated is the addition of lipoic acid and compounds to maintain adequate levels of Selenium, Vitamin C and Vitamin E. Based on the clinical results of retardation, but not cure of cancer, the combination has the characteristic of sufficiently interfering with replication and apparently restoring the immune system capacity to manage cancer.

Abstract: Multifunctional, polyionic copolymers with molecular architectures and properties optimized for specific applications are synthesized on/or applied to substrate surfaces for analytical and sensing purposes. The coatings are particularly useful for suppression of non-specific interaction, adsorption or attachment of molecular or ionic components present in an analyte solution. Chemical, biochemical or biological groups can be coupled to, integrated into or absorbed to the multifunctional polymer that are able to recognize, interact with and bind specifically to target molecules in the material containing the analyte to be detected. These multifunctional polymer coatings are compatible with a variety of different established methods to detect, sense and quantify the target molecule in an analyte.

Abstract: The invention provides therapeutic and biological uses of chemokine-receptor-binding compounds (including chemokine receptor ligands such as chemokine receptor agonists or antagonists), such as benzopyrone derivatives, including uses in the treatment of disease states mediated by chemokines. The relevant chemokine may for example be interleukin-8 (IL-8), and the relevant chemokine receptors may for example be corresponding chemokine receptors (CXCR-1 and/or CXCR-2). In other aspects, the invention provides corresponding pharamaceutical compositions and therapeutic methods. In one aspect, for example, the invention provides for the use of [7-[benzopyrone-5′(3′-amino)-thiazole]-phenylalanine-benyl ester in the treatment of disease.

Abstract: In a new pharmaceutical combination, the herb, Vitex agnus-castus (chasteberry), enhances hormone balance by increasing progesterone release and, therefore, ovulation frequency. The antioxidants, green tea, vitamin E, and selenium, improve overall reproductive health. L-arginine, an amino acid, stimulates the reproductive organs by improving circulation. Folic acid, vitamins B6 and B12, iron, zinc and magnesium help promote womens' fertility. Sperms are highly susceptible to free radical or oxidative damage from environmental toxicants and natural aging. Vitamins C and E, coenzyme Q10 and selenium are all potent antioxidants that help improve sperm counts and quality. Ferulic acid, an antioxidant found in Dong quai, also improves sperm quality. Zinc and B vitamins (B6, B12 and folate) are critical nutrients in male reproductive systems for hormone metabolism, sperm formation and motility. The amino acid, L-carnitine, promotes formation of healthy sperm.

Abstract: Disclosed is a method for fabricating biosensors, using hydrophilic polyurethane. Bio-active reagents, including enzymes, antibodies, antigens, cells and receptors, are mixed with hydrophilic polyurethane and the mixture is directly coated over a signal transducer to form a sensing film which serves as a signal detector. The method using hydrophilic polyurethane allows the simplification of the fabrication of biosensors without conducting complicated chemical reactions and washing steps, such as crosslinking. The bio-active reagent entrapped within the hydrophilic polyurethane film can retains its high activity for an extended period of time and the intrinsic potentiometric response of the underlying ion-selective polymeric membrane is not affected by the bio-active reagent immobilized polyurethane film coated on its sensing surface. Therefore, the biosensors are superior in specificity, selectivity, and stability.

Abstract: The present invention relates to rapid, reliable and effective assays for screening and identifying pharmaceutically effective compounds that specifically inhibit the biological activity of fungal GTPase proteins, particularly GTPases involved in cell wall integrity, hyphael formation, and/or other cellular functions critical to pathogenesis.

Abstract: The present invention provides an antiproliferative compound having a structural formula 1

Abstract: The present invention relates to complexes of proanthocyanidin A2 and one or more phospholipids, pharmaceutical compositions containing the complex of proanthocyanidin A2 and one or more phospholipids, and methods of treating or preventing atherosclerosis and myocardial and cerebral infarction in a patient by administering the complex of proanthocyanidin A2 and one or more phospholipids, as well as methods of forming such complexes

Abstract: In accordance with the present invention there are provided novel Spray-Dried Lipid Microparticles (SDLM) that are comprised of lipid, a ligand and agent. The ligand is specific for a cell surface receptor, thereby enabling targeting of the agent to cells bearing receptors specific for the targeting ligand. In invention embodiments wherein the receptor internalizes upon ligand binding, there are provided compositions and methods for the introduction of agent into specifically targeted cells. In a particular embodiment, the ligand is specific for antigen presenting cells (APC) and the agent is a defined antigen. In this manner, immune responses can be induced against specific antigens, including those which are normally not very antigenic due to the fact that they are inefficiently internalized by APC.

Abstract: Water soluble triptolide prodrugs are used as anticancer agents, and are found to be more effective in vivo, at lower doses, in reducing tumor size than the widely used chemotherapeutic agents 5-fluorouracil and irinotecan.

Abstract: The invention provides isolated nucleic acids molecules, designated 26583 nucleic acid molecules, which encode novel serine/threonine phosphatase family members. The invention also provides antisense nucleic acid molecules, recombinant expression vectors containing 26583 nucleic acid molecules, host cells into which the expression vectors have been introduced, and nonhuman transgenic animals in which a 26583 gene has been introduced or disrupted. The invention still further provides isolated 26583 proteins, fusion proteins, antigenic peptides and anti-26583 antibodies. Diagnostic methods utilizing compositions of the invention are also provided.

Abstract: The present invention relates to aminomethylcarboxylic acid derivatives general formula (I), wherein Z is (CH2)n, O, S, SO, SO2 or N—R5; n is 0, 1 or 2; X represents 1-3 substituents independently selected from hydrogen, halogen, (C1-6)alkyloxy, (C3-6)cycloalkyloxy, (C6-12)aryloxy, (C6-12)aryl, thienyl, SR6, SOR6, SO2R6, NR6R6, NHR6, NH2, NHCOR6, NSO2R6, CN, COOR6 and (C1-4)alkyl, optionally substituted with halogen, (C6-12)aryl, (C1-6)alkyloxy or (C6-12)aryloxy; or 2 substituents at adjacent positions together represent a fused (C5-6)aryl group, a fused (C5-6)cycloalkyl ring or O—(CH2)m—O; m is 1 or 2; Y represents 1-3 substituents independently selected from hydrogen, halogen, (C1-4)alkyloxy, SR6, NR6R6 and (C1-4)alkyl, optionally substituted with halogen; R1 is COOR7 or CONR8R9; R2 and R6 are (C1-4)alkyl; R3, R4 and R5 are independently hydrogen or (C1-4)alkyl; R7, R8 and R9 are independently hydrogen, (C1-4)alkyl, (C6-12)aryl or arylalkyl; or a pharmaceutically acceptable salt thereof.

Abstract: A food or food supplement which comprises a compound that enhances bone growth in vertebrates is described wherein the food or foodstuff is formulated so as to provide the desired bone growth enhancing effect.

Abstract: Ether-capped poly(oxyalkylated) alcohol surfactants having superior grease cleaning abilities and improved spotting/filming benefits are provided.

Abstract: Disclosed is a quaternary ammonium phosphate compound having formula (1) and which has an anticorrosive and a biocidal effect to have a capability of preventing corrosion of various metals including corrosive metal substances, e.g. carbon steels, iron casts, stain steels, coppers, tinning steel plates or alumina and an efficient method of preparing the same. In formula (1), R1 is a straight or a branched alkyl or aryl radical with 1 to 27 carbon atom(s) free of —OH group and may contain hetero-atoms, and both R2 and R3 are methyl groups or R2 and R3 are combined to form a heterocyclic compound with 4 to 6 of carbon atoms containing oxygen and nitrogen.

Abstract: The present invention is, directed to methods for detecting the presence of genetic polymorphisms that correlate with altered gene expression. More specifically, the present invention is directed to methods for detecting the genetic polymorphisms located in the UGT1A1 promoter. The invention also provides methods for optimizing drug dosages based upon the presence of the polymorphisms. The invention further provides methods of predicting sensitivity to xenobiotics and diagnostic kits for detecting genetic polymorphisms.

Abstract: A monoclonal antibody is provided which is directed against the human interferon type I receptor (IFN-R), which recognizes the extracellular domain of the human IFN-R and which has neutralizing capacity against the biological properties of human type I-IFN. Diagnostic and therapeutic applications for the monoclonal antibody also are provided.

Abstract: The invention provides mitochondrially targeted antioxidant compounds. A compound of the invention comprises a lipophilic cation covalently coupled to an antioxidant moiety. In preferred embodiments, the lipophilic cation is the triphenyl phosphonium cation, and the compound is of the formula P(Ph3)+XR.Z− where X is a linking group, Z is an anion and R is an antioxidant moiety. Also provided are pharmaceutical compositions containing the mitochondrially targeted antioxidant compounds, and methods of therapy or prophylaxis of patients who would benefit from reduced oxidative stress, which comprise the step of administering the compounds of the invention.

Abstract: The present invention relates to mixtures which can be isolated from grains of Eugenis Jambolana Lamarck, the preparation of such mixtures, the medicaments containing said mixtures or constituents of said mixtures, and the use of these mixtures and constituents for the preparation of a medicament.

Abstract: The present invention is directed to a method for enhancing the delivery of delta-9-tetrahydrocannabinol (“THC”) to the brain of a mammal in need of treatment with this drug, by administering water-soluble prodrugs of THC intranasally.

Abstract: Cosmetic compositions and methods are provided for revitalizing the skin especially where it is placed in an environment that can cause injury to the skin. The compositions contain an effective amount of cromolyn compounds to provide a prophylactic or repairing effect.

Abstract: Various embodiments of statin compounds are shown to enhance the formation of bone and are thus useful in treating osteoporosis, bone fracture or deficiency, primary or secondary hyperparathyroidism, periodontal disease or defect, metastatic bone disease, osteolytic bone disease, post-plastic surgery, post-prosthetic joint surgery, and post-dental implantation.