Abstract: This invention relates to new Gymnemic acid derivatives, their preparation, pharmaceutical composition or extract which contains them, and their medical use, especially the use in the prevention or treatment of the diseases associated with hyperglycemia, hyperlipidemia and platelets aggregation.

Abstract: A method for producing sophorolipids having spermicidal and/or antiviral properties by synthesizing the sophorolipid by fermentation of Candida bombicola in a fermentation media to form a natural mixture of lactonic sophorolipids compounds and non-lactonic sophorolipids compounds and utilizing the natural mixture as a spermicidal and/or antiviral agent, and/or separating the lactonic sophorolipids from the natural mixture to form a lactonic fraction and mixing all remaining fractions to form a non-lactonic fraction and utilizing the lactonic fraction and/or the non-lactonic fraction as an spermicidal and/or antiviral agent, and sophorolipid compounds for use as spermicidal and/or antiviral agents.

Abstract: The present invention discloses novel saponin derivatives for use with nucleic acids that induce an immune response when administered to animals and humans. The novel saponin derivatives disclosed comprise (a) a saponin aglycone core, wherein the aglycone core is covalently linked to one or more oligosaccharide chains; (b) a positively charged cationic chain, and optionally (c) a naturally occurring or synthetic lipophilic chain. Pharmaceutical and veterinary compositions comprising one or more of the novel saponin derivatives and saponin derivative/polynucleotide complexes are also disclosed. Disclosed as well are methods of using the novel saponin derivatives to deliver a polynucleotide molecule to cells of an animal, to stimulate or generate an immune response in an animal, and to generate a detectable immune response in an animal.

Abstract: A therapeutic agent for a cancer comprising a therapeutically effective amount of an active ingredient, wherein the therapeutic agent is used referring to an ability of acting on NK cell antigen receptor NKR-P1 of NKT cell as an index of the ability to activate the NKT cell.

Abstract: Polysaccharides, which are widely used as an anticoagulation drugs, especially heparin, are clinically administered only by intravenous or subcutaneous injection because of their strong hydrophilicity and high negative charge. Amphiphilic heparin derivatives were synthesized by conjugation to bile acids, sterols, and alkanoic acids, respectively. These heparin derivatives were slightly hydrophobic, exhibited good solubility in water, and have high anticoagulation activity. These slightly hydrophobic heparin derivatives are efficiently absorbed in the gastrointestinal tract and can be used in oral dosage forms. Methods of using these amphiphilic heparin derivatives and similarly modified macromolecules for oral administration are also disclosed.

Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Abstract: A medicinal composition comprising at least one compound which can interact with a target cell, the at least one compound being a glycoalkaloid of general formula (I) wherein: the composition is essentially without free sugars of the type which inhibit the interaction between the at least one glycoalkaloid and a target cell.

Abstract: The invention discloses the use of a number of saponins and sapogenins, notably those of steroidal structure, in the treatment of cognitive disfunction and similar conditions. Methods of treatment, and pharmaceutical compositions are also disclosed.

Abstract: In the present invention, it is discovered that a compound of formula (I) has a potent effect for treatment of osteoporosis, arthritis and ruptured disc: in which R1 represents hydrogen atom or alkyl group and R2 represents hydrogen atom r cinnamoyl group. Therefore, the compound of formula (I) can be used for prevention and treatment of osteoporosis, arthritis and ruptured disc. Thus, the present invention provides a pharmaceutical preparation containing as an effective component a compound of formula (I) 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: Compositions and methods for treating a tumor, neoplastic disease or infectious disease in a subject are based on superantigens in the form of polypeptides including fusion polypeptides or conjugates, homologues, and fragments, all of which induce a tumoricidal response when administered directly into tumor or an organ sheath or body cavity affected by the tumor. Nucleic acid constructs encoding the foregoing polypeptides are also used in antitumor therapy. The above agents may be administered in sustained release or controlled release vehicles at or near sites of tumors in a tumor-bearing subject.

Abstract: This invention is related to methods and compositions comprising rosmarinic acid. More specifically, the present invention comprises compositions comprising borneol, rosmarinic acid and at least one ginsenoside.

Abstract: The present invention provides methods of treating and preventing mortality associated with heart failure in an African American patient with hypertension and improving oxygen consumption, quality of life and exercise tolerance by administering a therapeutically effective amount of at least one hydralazine compound and at least one of isosorbide dinitrate and isosorbide mononitrate, and, optionally, one or more compounds, such as, for example, a digitalis, a diuretic compound, or a compound used to treat cardiovascular diseases. In the present invention, the hydralazine compound is preferably hydralazine or a pharmaceutically acceptable salt thereof. Preferred methods of the invention comprise administering hydralazine or a pharmaceutically acceptable salt thereof and isosorbide dinitrate.

Abstract: The present invention relates to novel estrogenic compounds. The present invention also relates to methods of treating estrogen deprivation in a subject comprising administering novel estrogenic compounds. Additionally, the present invention relates to methods of synthesizing novel estrogenic compounds.

Abstract: One aspect of the invention is concerned with a method of hormone replacement therapy, which method comprises administering to a person in need of such a therapy an effective amount of an estrogenic component selected from the group consisting of: substances represented by the formula (I) in which formula R1, R2, R3, R4 independently are a hydrogen atom, a hydroxyl group or an alokxy group with 1-5 carbon atoms; each of R5, R6, R7 is a hydroxyl group; and no more than 3 of R1, R2, R3, R4 are hydrogen atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures thereof; said composition containing virtually no progestogen or anti-progestin. Another aspect of the invention relates to a drug delivery system for enteral or parenteral administration that contains at least 1 &mgr;g of the aforementioned estrogenic component and virtually no progestogen or anti-progestin.

Abstract: A method of contraception in mammalian females, which method comprises the parenteral or rectal administration of an estrogenic component and a progestogenic component to a female of childbearing capability in an amount effective to inhibit ovulation, wherein the estrogenic component is selected from the group consisting of substances represented by the following formula (1) 1

Abstract: The present invention relates to extracts from the lridaceae plant Belamcanda chinensis for producing a ready-formulated medicament suited for the selective treatment and/or prophylaxis of sexual hormone-related disorders of the uro-genital tract. The inventive extracts are moreover suited for the treatment and/or prophylaxis of post-menopausal bladder infections and of urinary incontinence. The are moreover indicated for the treatment of benign and malignant prostate hyperplasies. It was moreover found that the ingredient tectorigenin as well as its glycosides, isolated from Belamcanda chinensis, essentially has the same effects as the whole extract.

Abstract: A method of treating polycystic kidney disease is described. The method involves administering soyasaponin Bb to an animal in need thereof.

Abstract: The subject invention provides novel compositions of biologically active glycosylated pregnene compounds which can advantageously be used for treating cancer and stopping cell proliferation.

Abstract: Novel estrogenic compounds of Formula I are provided.

Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule in an amount sufficient to control the aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. The present invention further makes available methods and reagents for ameliorating the consequences of hedgehog loss-of-function, ptc gain-of-function, or smoothened loss-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule, in an amount sufficient to ameliorate the In certain embodiments, the subject compounds, e.g., a cAMP analog, adenylate cyclase agonist, or cAMP phosphodiesterase inhibitor, regulate cAMP levels, which in turn modulates activity of the hedgehog pathway.

Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Abstract: A novel solid pharmaceutical dispersion that improves the bioavailability of poorly water soluble drugs is produced by combining the drug with a polymer carrier such as polyvinylpyrrolidone. The drug is combined with the carrier without the need for using organic solvents or melting temperatures (fusion) through the use of a transition compound such as polyethylene glycol which partially solubilizes the drug and/or plasticizes the polymer.

Abstract: A soya extract having a content of glucoside isoflavones of at least 13% by weight and a content of 0.6 to 1.5 parts by weight of group 3 soya saponins per 1 part by weight of glucoside isoflavones. Also, pharmaceutical compositions containing this extract and methods of administering the extract to treat conditions such as pre- or post-menopausal symptoms, cancer, such as breast or prostate cancer, or alcoholism. The extracts are made by a process which includes the steps of treating ripe whole soya beans or oil-free soya flour with an aliphatic alcohol to obtain a first extract; concentrating the first extract to form a concentrated first extract; purifying the concentrated first extract by treatment with at least one aliphatic hydrocarbon; and extracting active components from the purified concentrated first extract with a water-immiscible aliphatic alcohol to obtain a second extract. Preferably, the final extract is concentrated dried to form the desired soya extract.

Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Abstract: The present invention provides methods, preparations, and uses of a variety of liposomal-digitalis glycoside compositions. The present invention also provides protein-stabilized nanoparticle formulations containing liposomal-digitalis glycosides such as Oleandrin, digitoxin, and digoxin with reduced toxicity, high drug to lipid ratio, long circulating time in the bloodstream and the ability to deliver the drug to tumor sites. In another aspect, the present invention provides an effective method to reduce the growth of cancers or reduce the incidence of metastases.

Abstract: A method for treating or preventing chronic obstructive pulmonary disease (COPD) by using as active agent a non-glucorticoid steroid, analogue thereof, such as dehydroepiandrosterone (DHEA) and dehydroepiandrosterone sulfate (DHEA-S), or their salts, in an amount effective for preventing or treating COPD.

Abstract: Novel analogs of fusidic acid are described with one or more carbohydrate units attached. Certain glycosylated analogs of fusidic acid have enhanced solubility properties in diluents or excipient of choice as compared to unmodified fusidic acid. Certain glycosylated analogs may be employed as chemotherapeutic agents and particular analogs may be useful for fighting anti-microbial infections.

Abstract: A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1′, 2′ or 3′-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.

Abstract: The cosmetic topical formulation of this invention is directed toward diminishing skin wrinkling, fine line, improving skin tone, and combinations thereof. Preferably, the topical formulation contains a matrix metalloproteinase inhibitor, MMPI, and advantageously includes a natural estrogen, e.g., a true estrogen compound, such as 17-beta estradiol, or an estrogen-like steroid, (such as various phytoestrogens found in herbal preparations), as opposed to a synthetic estrogen. Other forms of the cosmetic topical formulation of this invention include combinations of synthetic estrogen and MMP inhibitor. Exemplary synthetic estrogens include, but are not limited to, ethinyl estradiol and clomiphine citrate. The cosmetic topical formulation is safe and effective diminishing wrinkling, and improving skin tone.

Abstract: A composition comprising at least two glycoalkaloids of formula I: 1

Abstract: The invention relates to the identification of sterol glucoside toxins, and provides methods for detecting and detoxifying the compounds, as well as therapeutic methods for treating subjects exposed to such toxins. In alternative embodiments, the toxins may for example include beta-sitostrol-beta-D-glucoside (5-cholesten-24b-ethyl-3b-ol-D-glucoside) or cholesterol glucoside (5-cholesten-3b-ol-3b-D-glucoside).

Abstract: The present invention discloses a cardiotonic composition comprising micronized digoxin, hydrophilic polymer(s) and optionally pharmaceutically acceptable excipient(s) in the form of a tablet that releases not more than 50% digoxin in 5 minutes and at least 85% digoxin in 60 minutes.

Abstract: Longterm elevation of the intracellular Na+/K+ ratio inhibits macromolecule synthesis and proliferation in the majority of cell types studied so far, including vascular smooth muscle cells (VSMC). We report here that inhibition of the Na+,K+ pump in VSMC by ouabain or 1 hour preincubation in K+-depleted medium attenuated apoptosis triggered by serum withdrawal, staurosporine or okadaic acid. In the absence of ouabain, both DNA degradation and caspase-3 activation in VSMC undergoing apoptosis were insensitive to modification of the extracellular Na+/K+ ratio as well as to hyperosmotic cell shrinkage. In contrast, protection of VSMC from apoptosis by ouabain was abolished under equimolar substitution of Na+o with K+o, showing that the anti apoptotic action of Na+,K+ pump inhibition was caused by inversion of the intracellular Na+/K+ ratio.

Abstract: The present invention provides compositions and methods for using cardioprotective or hemodynamic drugs in combination with dichloroacetate enabling usage of cardioprotective or hemodynamic drugs at concentrations higher than used in normal clinical practice without increasing deleterious side effects normally associated with the cardioprotective or hemodynamic drug, thereby conferring added clinical benefit. The present invention teaches administration of DCA with cardioprotective or hemodynamic drugs as an adjunct therapy thereby conferring added clinical benefit to clinically recommended protocols.

Abstract: The invention relates to a composition intended for administration by the oral or topical route and comprising, in a physiologically acceptable medium, DHEA and/or a chemical or biological precursor or derivative of the latter, in combination with at least one NO-synthase inhibitor.

Abstract: A method of controlling preeclampsia includes the steps of providing a supply of digoxin immune Fab (ovine), calculating an appropriate dosage of the digoxin immune Fab (ovine) based on a patient's weight and using an assumed endogenous digitalis-like factor level, administering the appropriate dosage as an intravenous bolus, and repeating the administration of the appropriate dosage on a fixed schedule.

Abstract: A method of regulating a preeclamptic/eclamptic patient's sodium/potassium ATPase activity includes the administration of digoxin immune Fab (ovine). It is theorized that an endogenous digitalis-like factor present in preeclamptic and eclamptic patients inhibits the functioning of sodium/potassium ATPase, resulting in elevated level of intracellular sodium and calcium levels. These elevated intracellular sodium and calcium levels lead to intravascular volume contraction and vasoconstriction. Digoxin immune Fab (ovine) binds with the endogenous digitalis-like factor to prevent it from interfering with the functioning of the sodium/potassium ATPase, thereby allowing the patient's intracellular sodium and calcium to return to a more normal level.

Abstract: A composition for medicinal treatment by means of topical administration is described, which contains an aromatase inhibitor, in addition to conventional constituents of topical forms of administration. The active ingredient or the composition containing this active ingredient is especially suitable for the prophylaxis and for the treatment of mastalgia.

Abstract: The present invention relates (a) to new compounds represented by Formula I: 1

Abstract: The present invention relates to a composition including DHEA and/or a chemical or biological precursor or derivative of the latter, characterized in that it additionally comprises at least one metalloproteinase inhibitor.

Abstract: A compound, method and composition for treating a host infected with a hepatitis C viral comprising administering an effective hepatitis C treatment amount of a described 4′-disubstituted nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.

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: Compounds having an ansamycin anitibiotic, or other moiety which binds to hsp90, coupled to a targeting moiety which binds specifically to a protein, receptor or marker can provide effective targeted delivery of the ansamycin antibiotic leading to the degradation of proteins and death of the targeted cells. These compositions may have different specificity than the ansamycin alone, allowing for a more specific targeting of the therapy, and can be effective in instances where the ansamycin alone has no effect. Thus, these compounds provide an entirely new class of targeted chemotherapy agents with application, depending on the nature of the targeting moiety, to treatment of a variety of different forms of cancer. Such agents can further be used to promote selective degradation of proteins associated with the pathogenesis of others diseases, including antigens associated with autoimmune disorders and pathogenic proteins associated with Alzheimer's disease.

Abstract: The present invention relates to a composition containing a sapogenin, and/or a sapogenin ester, and to the use of a sapogenin and/or a sapogenin ester to manufacture a composition that is suitable for topical application to the skin, and in a method wherein sapogenin and/or a sapogenin ester are used as agents for the of smoothing out wrinkles and fine lines, in particular expression wrinkles and fine lines. The sapogenin may be used/provided in the form of a natural extract containing it. A preferred sapogenin is diosgenin.

Abstract: This invention provides methods of treating muscle spasm and/or pain by treatment with a cardiac glycoside or aglycone derivative. These methods are useful in treatment of conditions associated with muscle pain.

Abstract: The present invention is directed to compositions and methods for inducing, promoting or otherwise facilitating pain relief. More particularly, the present invention relates to the use of a compound which either directly or indirectly prevents, attenuates or reverses the development of reduced opioid sensitivity, together with a compound which activates the opioid receptor that is the subject of the reduced opioid sensitivity, in methods and compositions for the prevention or alleviation of pain, especially in neuropathic conditions and even more especially in peripheral neuropathic conditions such as painful diabetic neuropathy (PDN).

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

Abstract: A pharmaceutical or veterinary composition comprises a non-corticosteroids, and/or salts thereof, and an anti-muscarinic (anti-cholinergic) agent, and\or pharmaceutically or veterinarilly acceptable salts thereof. The composition is provided in various formulations and in the form of a kit. The products of this patent are useful in the prophylaxis and treatment of various respiratory, lung and malignant diseases.

Abstract: Methods are provided for treating arrhythmia in a manner that minimizes undesirable side effects, comprising administration of a therapeutically effective minimal dose of an A1 adenosine receptor agonist with a therapeutically effective minimal dose of a beta blocker, calcium channel blocker, or a cardiac glycoside.

Abstract: The present invention relates to the use of a sapogenin, chosen from diosgenin and hecogenin, and/or of a plant extract containing at least one of these sapogenins. A preferred use is the treatment of oligoseborrheic dry skin. Another preferred use is the treatment of dry scalp. Compositions containing these sapogenins are also described.