Abstract: Provided herein are methods for treating diabetes, obesity, and other metabolic diseases, disorders or conditions comprising chemosensory receptor ligands. Also provided herein are chemosensory receptor ligand compositions and the preparation thereof for the methods of the present invention.

Abstract: Methods and compounds for preventing or reducing the toxic side effects of cardiac glycosides by inhibiting the mitochondrial sodium-calcium exchanger (mNCE) are provided. Methods and compositions for preventing or reducing the occurrence of conditions associated with heart failure, including, but not limited to, sudden cardiac death and contractile decompensation, by inhibiting the mNCE also are provided.

Abstract: A method and medicine for treating leukemia or other cancer includes administering to a patient diagnosed with leukemia or other cancer a treatment regimen that includes periodic doses of a combination of emodin and digoxin.

Abstract: A method for determining the risk, severity or progression of cardiovascular disease, such as cardiac heart failure. A method for determining the likelihood of admission to the hospital for cardiac heart failure. The methods include determining the concentration of ET-1 and the concentration of one or more of biomarkers selected from the group consisting of cardiac troponin (e.g., cTnI, cTnT), VEGF, BNP, NT-proBNP, and IL-6 in a blood, serum or plasma sample from the patient.

Abstract: Disclosed is the use of a cardiac glycoside to decrease or inhibit the secretion of proinflammatory mediators in the treatment of disease conditions characterized by elevated levels of the proinflammatory mediator. The cardiac glycoside is administered to a mammalian subject in need of such treatment, and dosage is adjusted to the mass of the recipient and the need of the recipient to reduce or inhibit the level of the proinflammatory mediator. The proinflammatory mediators suppressed by the invention include IL-8, IL-6, TNFalpha, ICAM-1, IFNgamma, IL-1-beta, MCP-1, MIP-2, and/or epithelial-mesenchymal-transition (EMT). The cardiac glycoside, digitoxin or oleandrin, can be formulated for administration by injection or as an aerosol administered to the respiratory tract or by being ingested, or as nose drops or nasal spray. According to one use, the digitoxin controls microRNA expression in castration-resistant prostate cancer. The microRNA suppresses IL-8 and IL-6 expression in these cells.

Abstract: Described herein are methods for the treatment of cancer (e.g. melanoma, lung cancer, or other cancers). The methods involve administrating to a subject in need thereof an agonist of the IL-9 receptor (e.g. IL-9), e.g. an agent that binds and activates the IL-9 receptor, or an agent that increases IL-9 expression in the subject (e.g. administration of TH9 cells that express IL-9, or administration of an inhibitor of ROR).

Abstract: A steroid compound of the Formula (1): [wherein R1 represents a group selected from the group consisting of H, CH3, C2H5, C3H7 and CH (CH3)2, R2 represents a group selected from NH2, NHAc and OCOR1, R3 represents a group selected from the group consisting of CH3, COOCH3 and CH2OCOR1.

Abstract: The present invention relates to use of an active ingredient selected from ginsenoside Rg1, its metabolites ginsenoside Rh1 and Ppt for preparing a medicament and a health care product for improving sexual function of male mammals, and for providing the effect of spermatogenesis. The present invention further relates to a pharmaceutical composition for improving sexual function of male mammals, and/or for providing the effect of spermatogenesis, which comprises at least one active ingredient selected from ginsenoside Rg1, its metabolites ginsenoside Rh1 and Ppt, and a pharmaceutically acceptable excipient.

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: The present invention relates to a method for manufacturing uniform size polymeric nanoparticles containing poorly soluble drugs, and more particularly, to a method for manufacturing uniform size polymeric nanoparticles containing poorly soluble drugs, including a first step of dissolving a biodegradable polymer in a non-volatile polar organic solvent, a second step of adding poorly soluble drugs to water and the biodegradable polymer solution to produce a dispersion, and a third step of adding the dispersion to emulsifier solutions in a batch under the condition of low mechanical energy level stirring.

Abstract: The present invention relates to methods and compositions for increasing telomerase activity in cells. Such compositions include pharmaceutical, including topical, and nutraceutical formulations. The methods and compositions are useful for treating diseases subject to treatment by an increase in telomerase activity in cells or tissue of a patient, such as, for example, HIV infection, various degenerative diseases, and acute or chronic skin ailments. They are also useful for enhancing replicative capacity of cells in culture, as in ex vivo cell therapy and proliferation of stem cells.

Abstract: Disclosed is a nanoparticulate complex comprising an artificial phosphate receptor of formula (I): P-[L-[-N(CH2-2-pyridyl)2]]p.pZN2+ (I) wherein P represents a nanoparticulate substrate, L represents a linking group, and p is an integer of ?1. Also disclosed are a method for silencing a gene in a cancer patient in need thereof, a method for treating or preventing cancer in a patient in need thereof, and a method for targeting a cell in cancer treatment comprising use of the nanoparticulate complex, for example, a DPA/Zn-functionalized nanoparticulate complex.

Abstract: The present invention provides molluscicidal saponins and saponin fractions from Camellia sinensis, together with compositions comprising such saponins and saponin fractions, and methods of preparing same. Methods for the control of molluscs, including terrestrial molluscs, such as slugs or snails, using the saponins and saponin fractions or compositions comprising said saponins or saponin fractions optionally together with one or more pesticidal agents including molluscicidal agents, are also provided.

Abstract: A phosphodiesterase type III (PDE III) inhibitor or Ca2+-sensitizing agent or a pharmaceutically acceptable derivative thereof is provided for the preparation of a medication for the reduction of the heart size of a patient suffering from heart failure.

Abstract: Provided are a number of compounds structurally related to OSW-1, a natural compound that binds OSBPs. Also provided are pharmaceutical compositions comprising the OSW-1 analogs, as well as methods for use of these OSW-1 analogs, or pharmaceutically acceptable salts, enantiomers, or stereoisomers thereof in the treatment of atherosclerosis. Alzheimer's disease, and cancer, including p21-deficient cancer. Conjugates of OSW-1 analogs with monoclonal antibodies, including monoclonal antibodies targeted to cancer cells, are also provided. Also provided are pharmaceutical compositions comprising the conjugates, as well as methods for use of these conjugates, in the treatment of cancer, including p21-deficient cancer.

Abstract: The present invention relates to a novel compound derived from ginsenoside Rh2, the preparation methods and the use thereof in treating cancers.

Abstract: The present invention disclosed a medical use of cucurbitane triterpenoids represented by the following formula and isolated from Momordica charantia L. of Cucurbitaceae family in the preparation of medications for prevention and treatment of diabetes and obesity. The above cucurbitane triterpenoids may be acted as a glucose uptake stimulator, an agonist for the translocation of glucose transporter 4 (GLUT4) to the cell membrane, and an activator of adenosine monophosphate-activated protein kinase (AMPK). They may have potential for the prevention and treatment of diabetes and obesity.

Abstract: The present invention provides glycoside compounds, methods of preparing such compounds, pharmaceutical compositions comprising such compounds, and a method for the treatment of hyperproliferative diseases using the same.

Abstract: Compounds from 14 Kenyan plants, including from the root of Dovyalis abyssinica and Clutia robusta have been characterized and isolated, and their uses are disclosed.

Abstract: The invention describes novel triterpenoid 2-deoxy glycosides of general formula I, wherein at least one of the substituents X1 and R2 contains a 2-deoxy glycosidic group, method of preparation thereof, their cytotoxic activity and a pharmaceutical formulation containing these compounds.

Abstract: The present invention relates to mono- and combination therapies for melanoma, and in particular, metastatic melanoma. Drugs for use in such therapies in include RO 31-8220, bafetinib, and cardiac glycosides.

Abstract: The present invention relates to methods for treating or preventing pulmonary hypertension, reducing mortality in a subject experiencing pulmonary hypertension, or inhibiting ADP-mediated vasoconstriction of pulmonary arteries in a subject, comprising administering to the subject an effective amount of a pharmaceutical composition comprising a reversible P2Y12 receptor antagonist. Also provided are related medicaments, pharmaceutical compositions, and methods for preparing the medicaments.

Abstract: Steroid compounds are disclosed that have a formula represented by the following: and wherein m, n, t, u1, u2, v1, v2, R1a, R1b, R2a, R2b, R3a, R3b, R3c, R3d, and Y are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the treatment or prevention of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.

Abstract: The present invention relates to combination therapies for melanoma, and in particular, metastatic melanoma. Drugs for use in such therapies in include BRAF inhibitors such as PLX 4720 and PLX 4734 in combination with RO 31-8220, bafetinib or cardiac glycosides.

Abstract: A series cardenolide derivatives including structure of formula I from the root of Reevesia formosana have provided. In formula (1) and (2), where R3, R5, R10 and R16 are as defined in the specification. The derivatives compounds showed potent cytotoxicity against MCF-7, NCI-H460, and HepG2 cancer cell lines.

Abstract: Using a Pharmaceutically Suitable Preparation containing one more Cardio Glycosides such as THEVETIN B, THEVETIN A, PERUVOSIDE, THEVOFOLIN, OLEANDRIN, NERIIFOLIN, THEVETOXIN Derived or Extracted from the Yellow Oleandrin Plant (Oleandrin Peruviana), White Oleandrin Plant (Nerium Oleander) and or other Plants in the Apocynaceae Genus, in the Dogbane Plant Family and or extracted from plants or animals including plants and animals such as Foxglove or synthetic man-made, and or a combination of synthetic and natural thereof in Pharmaceutically Suitable Preparation in a Pharmaceutically Suitable Dose, example orally or intravenously, of which the Prescriber of the said Preparation, or Doctor, based on the overall health of the Patient will prescribe the best Dosage, The Best Mode of Dosage example orally or intravenously, which is best suited to have the Most Desirable Therapeutic Effect

Abstract: The present invention concerns a molecular signature of cutaneous pigmentary spots, comprising the genes MXRA5, LYZ, CTSL2, PLAU, TIMP1, EFEMP1, ECM1, ASPN, HS3ST6, PAPLN, CHSY1 and FLRT2, and various applications of this signature. In particular, the invention concerns a method for characterizing a known or suspected pigmentary spot in a human being, comprising comparing the levels of expression in skin samples obtained from said spot and from adjacent undamaged skin, of at least one dermal gene linked to matrix remodelling or to its extracellular proteoglycan and glycoprotein components, selected from the list constituted by the genes MXRA5, LYZ, CTSL2, PLAU, TIMP1, EFEMP1, ECM1, ASPN, HS3ST6, PAPLN, CHSY1 and FLRT2. The invention also concerns methods for evaluating the efficacy of a pigmentary spot treatment, cosmetic and therapeutic methods for the treatment of pigmentary spots, and various modulators for said genes, and their use.

Abstract: Known or suspected traumatic brain injuries may be treated therapeutically by administering a therapeutically effective dose of resibufogenin. A preferred method for determining if a patient has a traumatic brain injury includes obtaining a body specimen from the patient, determining the concentration of marinobufagenin in the body specimen, comparing the concentration of marinobufagenin to the concentration in such body specimens in normal patients, and if the marinobufagenin concentration is substantially above the concentration of a normal patient, concluding traumatic brain injury exists. In a preferred embodiment, a substantial elevation is deemed to be an increase of about 30 percent above the marinobufagenin concentration of a normal patient. The body specimen may be blood, urine, or cerebrospinal fluid.

Abstract: The present invention provides therapeutically active compounds and compositions as NMDA and MC receptor antagonists, which are useful in treating central nervous system disorders by over-activation of NMDA and/or MC receptors. In one aspect, the present invention provides methods of enhancing brain's cognitive function and reducing neuronal cell death in mammals and humans.

Abstract: The present invention provides therapeutically active compounds and compositions as NMDA and MC receptor antagonists, which are useful in treating central nervous system disorders by over-activation of NMDA and/or MC receptors. In one aspect, the present invention provides methods of enhancing brain's cognitive function and reducing neuronal cell death in mammals and humans.

Abstract: The invention provides methods for treating inflammatory and autoimmune diseases by administering to the subject an effective amount of a cardiac glycoside, where the dose is effective to suppress or prevent initiation, progression, or relapses of the disease, including the progression of established disease. In some embodiments, the methods of the invention comprise administering to a subject determined to have rheumatoid arthritis or systemic lupus, or a pre-clinical disease state thereof, an effective amount of a cardiac glycoside, to suppress or prevent activity of the disease. In other embodiments, the methods of the invention comprise administering to a subject determined to have insufficient endogenous cardiac glycosides, an effective amount as a supplement to counteract the effects of cardiac glycoside deficiency.

Abstract: The invention provides compounds of formula I, II, III, or IV: wherein R1 to R11, X, and Y have any of the values defined in the specification. The compounds inhibit Na, K-ATPase ?4 and are useful as contraceptive agents.

Abstract: A preparation of a kind of 20(R)-ginsenoside Rg3 medicinal composition aqueous solution containing ginsenoside Rg3 0.5˜10 mg/ml: add 0.1-5% of ginsenoside solution to 0.1˜30% of adjuvant A, B{circle around (1)}{circle around (2)}{circle around (5)} at the temperature of 40˜100° C., the ratio of these two is 1:1˜300, add water after the solvent is recycled under reduced pressure; another kind of 20(R)-ginsenoside Rg3 medicinal composition aqueous solution contains 0.1˜2 mg/ml of 20 (R) of the ginsenoside Rg3, the preparation: add 0.1˜5% of ginsenoside solution to 20˜65% of adjuvant B{circle around (3)}{circle around (4)} at the temperature of 60˜100° C., main material to adjuvant B=1:100˜400, add water after the solvent is recycled under reduced pressure.

Abstract: The present invention relates to a pharmaceutical composition for preventing and treating inflammation and cutaneous photodamage, which contains a water-soluble extract from a plant of Solanum genus. The composition also has a photoprotective effect, and can be used as a cosmetic composition.

Abstract: A prognostic assay and kit and method of use thereof are provided. The kit and assay are used to determine the likelihood of a diseased cell or tissue having a therapeutic response to treatment with a cardiac glycoside in a disease having an etiology associated with excessive cell proliferation. The kit and assay are used to determine the ratio of isoforms of the ? subunit of Na, K-ATPase obtained from the diseased cell or tissue. The kit can be used to predict the therapeutic responsiveness of cancer or tumor in a subject to treatment with a cardiac glycoside. The kit and assay can be incorporated in a method of treating a disease or disorder having an etiology associated with excessive cell proliferation with a composition comprising a cardiac glycoside.

Abstract: The present invention relates to a novel method for processing a cultured root of purple wild ginseng for increasing saponin content and to the cultured root of the purple wild ginseng which is processed thereby. The present invention can provide the cultured root of wild ginseng having significantly higher content of a specific ginsenoside, and can increase the productivity and economic efficiency by simplifying the production process.

Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R7, R8, Z, X, b, and c are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are nitric oxide donors and have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

Abstract: The invention provides compositions with low toxicity and high bioavailability for treating cancer or for inhibiting the development of cancer

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

Abstract: The present invention pertains to methods of extracting cardiac glycosides from cardiac glycoside containing plant material, such as Nerium oleander, through use of aloe. It further provides for compositions resulting from such extractions, pharmaceutical compositions, cosmetic compositions, and methods of treating skin conditions.

Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.

Abstract: Provided are methods of reducing body fat in a subject, comprising locally (e.g., topically) administering one or more compounds of the Formula (I) and/or (V): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein X is —OR1, —SR2, or —NR3R4, and R1, R2, R3, R4, R5, R6, R7, R7?, Z, Y, n, y, and x, are as defined herein.

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: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.

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: A method of treating neurological condition in a subject by administration of a cardiac glycoside is provided. Alzheimer's disease, Huntington's disease or stroke are treated by administering a therapeutically effective amount of cardiac glycoside to a subject. The cardiac glycoside can be present in a dosage form.

Abstract: The present invention provides novel methods for the localized delivery of inotropic agents to the heart, including specific regions of the heart, such as the ventricles, for example in a subject undergoing cardiothoracic surgery, with the aim of supporting the myocardial contractile function of the heart.

Abstract: This invention relates to novel saponin compounds of formula II wherein MBz denotes p-methoxybenzoyl, and R is selected from the group comprising C6-10 aryl, C6-10 aryl-C1-4 alkyl-, C1-18 alkanoyl, C3-18 alkenyl, C6-10 aryl-C(O)—, C6-10 aryl-C1-4 alkyl-C(O)—, wherein each of the groups can optionally be substituted. These compounds possess a selective cytostatic activity, useful, e.g., in the treatment of proliferative diseases. The invention further relates to methods of preparation of the novel compounds and to a pharmaceutical composition containing these compounds.

Abstract: The invention provides crystalline forms of (R)-3-[N-(3?-chlorobiphenyl-4-ylmethyl)-N?—(3-hydroxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionic acid isopropyl ester. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases.

Abstract: A method and medicine for treating leukemia or other cancer includes administering to a patient diagnosed with leukemia or other cancer a treatment regimen that includes periodic doses of a combination of emodin and digoxin.