Abstract: The use of menthyl 2-pyrrolidone-5-carboxylate as an insect repellent, usually by application to a substrate or into an air space. The menthyl 2-pyrrolidone-5-arboxylate can be used as a composition, which may be perfumed. A useful composition comprises a mixture of menthyl 2-pyrrolidone-5-arboxylate and a known insect repellent or a compound shown to be an effective insect repellent on a test described herein.

Abstract: Described are salts of hyperforin and adhyperforin of formula I [A−]m[B]p+  (I) wherein m is an integer from 1 to 3, p is equal to m and gives the total number of positive charges of the residue [B], [A−] is an anion of formula II with n=0 or 1 and [B]p+ is an ion of an alkali metal or an ammonium ion of a salt-forming nitrogen base of formula III wherein R1 through R4 have a variety of meanings including hydrogen, alkyl, cycloalkyl and similar groups which in turn may be substituted with one or more substituents. The salts serve inter alia for enriching or purifying hyperforin and adhyperforin from St. John's Wort extracts. Pharmaceutical preparations containing the salts are used for treating Alzheimer's Disease.

Abstract: Astaxanthin is a potent antioxidant, over 500 times more powerful than Vitamin E and 10 times stronger than other carotenoids such as zeaxanthin, lutein, canthaxanthin and beta-carotene. Astaxanthin has also been shown to enhance and modulate the immune system. Disclosed is a method and treatment for retarding and preventing sunburns. The method comprises administering a source of astaxanthin in a therapeutically effective amount to prevent and retard sunburns.

Abstract: This invention provides analogs of triptycene which are useful as anticancer drugs, as well as for other uses. The potency of these compounds is in a similar magnitude as daunomycin, a currently used anticancer drug. Each compound of the invention produces one or more desired effects (blocking nucleoside transport, inhibiting nucleic acid or protein syntheses, decreasing the proliferation and viability of cancer cells, inducing DNA fragmentation or retaining their effectiveness against multidrug-resistant tumor cells).

Abstract: Significant concentrations of naphthalene were detected in carton nests of Formosan subterranean termites, Coptotermes formosanus Shiraki, collected from Florida, Hawaii, and Louisiana. This is the first report of naphthalene being associated with termites or any other insects. Naphthalene and other compounds associated with termite carton nests may be used to increase termite bait acceptance. New attractant molecules include 2-phenoxyethanol. New feeding stimulants include ergosterol. A list of volatile compounds associated with termite nests is presented, compounds that may be used to detect termite nests.

Abstract: A method for deterring birds from perching, roosting or loafing on plant and structural surfaces by applying to the surfaces a non-toxic composition. The non-toxic composition is one that triggers a physiological aversion mechanism in birds by a visual cue and a post-ingestinal response.

Abstract: Nutriceutical compositions useful as a dietary supplement which have antioxidant/free radical scavengers and also having a cytoprotective effect are disclosed. The compositions contain a cytoprotective and antioxidant/free radical scavenging amount of at least one of D-histidine, L-histidine, a racemic mixture thereof, a non-racemic mixture thereof, and nutriceutically acceptable salts thereof in combination with phytonutrients having antioxidant properties such as canthanaxin, vitamin A and limonene. The compositions can be prepared in capsule form, tablets, sustained release tablets, suspensions and oral rehydration solutions.

Abstract: The present invention provides illudin analogs of the general formula I: wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I, intermediates and processes useful for preparing compounds of formula I, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I.

Abstract: Indane dimer compounds and their pharmaceutical use particularly to achieve smooth muscle relaxing activity and/or mast cell stabilizing activity and/or anti-inflammatory activity are described.

Abstract: A method for inhibiting the activity of the enzyme 5&agr;-reductase in a human subject is provided which comprises administering to the subject a composition comprising the carotenoid astaxanthin. Administration of the composition to inhibit the enzyme is useful to prevent and treat benign prostate hyperplasia (BPH) and prostate cancer in human males.

Abstract: A liquid pesticidal composition, which is substantially free of water, comprising a hydrophobic pesticide or mixture of pesticides dissolved in an organic solvent and comprising as surfactants (a) a castor oil ethoxylate having 30-50 mol ethoxylate, (b) a branched C8-C18 alcohol ethoxylate having 5-10 mol ethoxylate, and (c) a tristyrenephenol-ethoxylate having 8-30 mol ethoxylate, or its phosphate or salt thereof. The compositions also include gels having a viscosity of 500 to 20,000 mPas and comprising additionally a gelling agent.

Abstract: An anti-stress composition having for its active ingredient astaxanthin and/or its ester. This composition can be in the form of a pharmaceutical, functional food, food or beverage and so forth.

Abstract: Astaxanthin is a potent antioxidant, over 500 times more powerful than Vitamin E and 10 times stronger than other carotenoids such as zeaxanthin, lutein, canthaxanthin and beta-carotene. Astaxanthin has also been shown to enhance and modulate the immune system. Disclosed is a method and treatment for retarding and ameliorating carpal tunnel syndrome (CTS) and tenosynovitis. The method comprises administering a source of astaxanthin in a therapeutically effective amount to prevent, retard and ameliorate carpal tunnel syndrome and tenosynovitis.

Abstract: The invention includes a method of treating neurogenic urinary dysfunction that comprises contacting urinary bladder mucosa of a patient afflicted with neurogenic urinary dysfunction with an effective dose of a homovanilloid compound, in particular a compound selected from the group RTX, TYX, 20-homovanillyl-mezerein or 20-homovanillyl-12-deoxyphorbol-13-phenylacetate. The invention includes treatment of urge incontinence due to detrusor hyperreflexia (DH). The invention also includes treatment of sensory hypersensitivity of the bladder resulting from prostate hypertrophy or interstial cystitis, as well as other neurogenic conditions resulting in increased micturition frequency or decreased bladder capacity, with or without frank incontinence.

Abstract: Medicament for the prophylactic and/or therpeutic improvement of the duration of mammalian muscle function and/or treatment of mammalian muscle disorders or diseases, e.g. equine Exertional Rhabdomyolysis, comprising at least one type of xanthophylles, e.g. astaxanthin, is described. Further, the use of xanthophylles in the preparation of such medicaments, and a method of prophylactic and/or therapeutic improvement of the duration of mammalian muscle function and/or treatment of mammalian muscle disorders or diseases, are disclosed.

Abstract: Nigella sativa derivatives, thymoquinone (TM) and dithymoquinone (DIM) are used in treatment of parental and multi-drug resistant human cancers.

Abstract: An improved process for manufacturing transdermal drug delivery devices and devices made therefrom. The invention provides a heat equilibration process for the manufacture of drug delivery devices which eliminates the need to preload the body contacting layer with a drug. The method has particular application in the manufacture of transdermal drug delivery devices including a drug reservoir comprising drug in excess of saturation.

Abstract: The invention concerns a transdermal patch for the release through the skin of estradiol and a progestogen agent and a process for its production.

Abstract: Administration of a pharmaceutical composition comprising:(a) a vasodilator; and(b) a 15-hydroxyprostaglandindehydrogenase inhibitor is effective for the treatment of male erectile dysfunction.

Abstract: The present invention provides illudin analogs of the general formula (I): ##STR1## where R.sub.1 is (CH.sub.2).sub.n --X--Y or H; n is 0 to 4; X is O or S or N or absent; and Y is an optionally substituted (C.sub.1 -C.sub.8)alkyl, (C.sub.6 -C.sub.10)aryl, (C.sub.6 -C.sub.10)aryl(C.sub.1 -C.sub.4)alkyl or cyclo(C.sub.3 -C.sub.6)alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4;R.sub.2 is absent; or R.sub.1 and R.sub.2 together comprise a 5-7 membered cyclic ring;R.sub.3 is (C.sub.1 -C.sub.4)alkyl or H; R.sub.4 is H, SCH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4)alkyl, O--(C.sub.5 -C.sub.12)aryl or --S--(C.sub.5 -C.sub.12)aryl; R.sub.5 is H, OH or absent; R.sub.6 is (C.sub.1 -C.sub.4)alkyl or absent; R.sub.7 is OH or OSi((C.sub.1 -C.sub.4)alkyl).sub.3 ; orR.sub.6 and R.sub.7 together are ethylenedioxy;R.sub.8 is optionally substituted (C.sub.1 -C.sub.4)alkyl; andthe bonds represented by ----- are individually present or absent.

Abstract: The present invention provides illudin analogs of the general formula I: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I, intermediates and processes useful for preparing compounds of formula I, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I.

Abstract: A non-toxic arthropod control composition is disclosed for application to foliage for plant protection. The composition includes behavior interfering compounds, agricultural oil and/or surface active compounds and diluents. The behavior interfering compounds may be any known conventional compound capable of interrupting or altering the normal behavioral sequences of the target. The agricultural oil can be a vegetable oil.

Abstract: Sarcodictyin A and B, eleutherobin, and bioactive analogs thereof synthesized using solid phase and solution phase chemistries. The synthetic method employs an attachment of common precursors, e.g., compounds 1880 or 200, on a solid support for generating conjugates 230 and 240, followed by standard chemical manipulations. A combinatorial library of sarcodictyins and eletherobin analogs was constructed with modified C-8 ester, C-15 ester and C-4 ketal functionalities and was screened for activity with respect to tubulin polymerization and cytotoxic activity against tumor cells, including Taxol-resistant lines. Compounds 600, 610, 630, 660-700, 730, 760, 850, and 920 were identified to be of equal or superior biological activities as compared to their corresponding natural product.

Abstract: The present invention provides illudin analogs of the general formula (I): ##STR1## where R.sub.1 is (CH.sub.2).sub.n --X--Y or H; n is 0 to 4; X is O or S or N or absent; and Y is an optionally substituted (C.sub.1 -C.sub.8)alkyl, (C.sub.6 -C.sub.10)aryl, (C.sub.6 -C.sub.10)aryl(C.sub.1 -C.sub.4)alkyl or cyclo(C.sub.3 -C.sub.6)alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4; R.sub.2 is absent; or R.sub.1 and R.sub.2 together comprise a 5-7 membered cyclic ring;R.sub.3 is (C.sub.1 -C.sub.4)alkyl or H; R.sub.4 is H, SCH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4)alkyl, O--(C.sub.5 --C.sub.12)aryl or --S--(C.sub.5 -C.sub.12)aryl; R.sub.5 is H, OH or absent; R.sub.6 is (C.sub.1 -C.sub.4)alkyl or absent; R.sub.7 is OH or OSi((C.sub.1 -C.sub.4)alkyl).sub.3 ; orR.sub.6 and R.sub.7 together are ethylenedioxy;R.sub.8 is optionally substituted (C.sub.1 -C.sub.4)alkyl; andthe bonds represented by -- are individually present or absent.

Abstract: Antimicrobial diterpenes and methods of using them.

Abstract: Disclosed is a method of treatment of steroid requiring inflammatory diseases using certain saturated monocyclic and bicyclic terpene compounds. These compounds may be administered in the form of capsules resistant to gastric juice, infusion solutions or intramuscular injection solutions. Because these particular terpene compounds exhibit steroid-like effects but without the harmful side-effects of conventional corticosteroids, the use of corticosteroids is substantially reduced, and in some cases, completely eliminated. Therefore, these terpene compounds are also suitable for long-term therapy and prophylaxis.

Abstract: Liquid, oil-miscible carotenoid preparations which, as double dispersion systems, comprise an aqueous-disperse phase which has a particle diameter of less than 100 .mu.m and in which particles, stabilized by protective colloid, of one or more carotenoids are present in disperse form, in an oil as a dispersion medium.

Abstract: The present invention relates to phytocassanes which are novel diterpene compounds exhibiting an antifungal activity against rice blast fungus, Pyricularia oryzae (Magnaporthe grisea) and rice sheath blight fungus, Rhizoctonia solani, and more specifically, it relates to phytocassanes A, B, C, D, and EL and a process for producing phytocassanes or momilactones, antifungal diterpene compounds, at a high yield.

Abstract: The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.

Abstract: The use of a benzylidenenorcamphor compound of the formula I ##STR1## wherein Phe is a phenyl group which is unsubstituted or substituted by 1 to 5 hydroxyl, alkyl or alkoxy groups having 1 to 10 C atoms, andn is 1 or 2.as sunscreen filters,and also novel compounds of the formula I, their preparation and use as UV filters, in particular in cosmetic or pharmaceutical preparations.

Abstract: A novel hypoglycemically active triterpenoid compound isolated in purified, preferably substantially purified, form from Salacia spp., processes for obtaining the novel triterpenoid compound, compositions comprising the triterpenoid compound and methods for use a hypoglycemic agent, for example, in the treatment of diabetes, are described. In a preferred embodiment, the triterpenoid compound is obtained from Salacia prinoides. As an agent for the treatment of diabetes, the novel triterpenoid is useful for treating insulin-dependent (type I) and/or non-insulin-dependent (type II) diabetes.

Abstract: The present invention relates to a method of inhibiting a protein kinase C-mediated biological response, such as, hyperplasia. The method comprises administering to a mammal a non-tumor promoting 12-deoxyphorbol ester. Phorbol esters suitable for use in the method include 12-deoxyphorbol 13-monoesters wherein the ester is a formate, acetate, propionate, butyrate, pentanoate, hexanoate, benzoate or phenylacetate ester.

Abstract: Fouling of marine structures such as boats by shell bearing sea animals which attach themselves to such structures, such as barnacles, is inhibited by coatings containing lipid soluble, non-toxic, biodegradable substances which prevent the animals from sitting down on the structures. These substances attack the nervous system of the barnacle, neutralize the glue extruded by the barnacle, and otherwise prevent the barnacles from attaching themselves to surfaces immersed in the aqueous marine environment while being benign to the environment. A preferred inhibitor is pepper containing capsaicin. The inhibitor is incorporated into standard marine paints, impregnants, varnishes and the like.

Abstract: The use of active gibberellins for the preparation of a pharmaceutical composition for the treatment of prostatitis. The method results in a decrease in prostate mass.

Abstract: A method of inhibiting viruses in which a virus is contacted with diamondoid alcohol, ketone, ketone derivative, adamantyl amino acid, quaternary salt or combinations thereof which have antiviral properties. These diamondoid derivatives are shown to have antiviral activity against HIV.

Abstract: Antineoplastic illudin analogs are provided of the formula: wherein R.sub.4, R.sub.5 and R.sub.6 are (C.sub.1 -C.sub.4)alkyl, Y is H, (C.sub.1 -C.sub.3)alkyl, (R.sub.4)R.sub.5)(R.sub.6)Si or alkanoyl ((C.sub.1 -C.sub.4)alkylC(O)) and R is CH.sub.2 OH, halo, benzyl optionally substituted with OY, or alkanoylmethyl (CH.sub.2 OC(O)R.sub.7), wherein R.sub.7 is (C.sub.1 -C.sub.4)alkyl, (C.sub.6 -C.sub.2)aryl or N(X).sub.2, wherein each X is H or (C.sub.1 -C.sub.4)alkyl, and the pharmaceutically-acceptable salts thereof.

Abstract: Various first messengers linked to phospholipase C, including acetylcholine and interleukin-1, regulate the production both of the secreted form of the amyloid protein precursor and of amyloid .beta.-protein. Intracellular signals which are responsible for mediating these effects have now been identified, and that activation of phospholipase C may affect APP processing by either of two pathways, one involving an increase in protein kinase C and the other an increase in cytoplasmic calcium levels. The effects of calcium on APP processing appear to be independent of protein kinase C activation. The observed effects of calcium on APP processing are of therapeutic utility in the treatment of Alzheimer-type amyloidosis.

Abstract: Novel compositions comprising an antiandrogenic compound of the formula ##STR1## wherein R is COR.sub.1 wherein R.sub.1 is loweralkyl and a vehicle comprising a metabolism modulator and a polar organic solvent, and a method of controlling the membrane permeation and metabolism of the compound thereof are disclosed.

Abstract: A composition for preventing or limiting the attack and infestation of trees by pine bark beetles, by inhibiting the response of the beetles to their aggregation pheromones. The composition comprises a green leaf volatile selected from six carbon alcohols, aldehydes, their derivatives such as acetates, and mixtures thereof. The green leaf volatile may be employed alone or in combination with an additional, known inhibitor of the pheromone response of the beetle.

Abstract: A compound having the formula ##STR1## which is useful as an antifungal agent and for the treatment and control of several agricultural phytopathogens, including Phytophthora infestans, is disclosed.

Abstract: A method of inhibiting certain tumor cell growth in a subject is provided comprising contacting the tumor with a therapeutic amount of an illudin S or illudin M analog having the structure ##STR1## wherein the analog is capable of inhibiting tumor cell growth without excessive toxicity to the subject and whereinR.sub.1 is hydrogen;R.sub.2 is methyl; andR.sub.3 is hydroxy.

Abstract: A therapeutic method is provided to inhibit tumor cell growth in a subject in need of said therapy is provided, comprising parenterally administering a therapeutic amount of a compound in a pharmaceutically acceptable carrier, wherein said compound has the structure: ##STR1## wherein R is selected from the group consisting of: ##STR2## and wherein said tumor cell is sensitive to inhibition by said compound and is selected from the group consisting of a myeloid leukemia cell, a T-cell leukemia cell, a lung carcinoma cell, an ovarian carcinoma cell, and a breast carcinoma cell.

Abstract: An herbal treatment for plant growth comprising a water solution of extracts of the type withdrawn at elevated temperature from Artemesia plants and the like, applicable to the root structure of plants and as an external spray.

Abstract: The present invention relates to a method of inhibiting the protein kinase C-mediated biological response inflammation. The method comprises administering to a mammal a non-tumor promoting 12-deoxyphorbol ester. Phorbol esters suitable for use in the method include 12-deoxyphorbol 13-monoesters wherein the ester is a formate, acetate, propionate, butyrate, pentanoate, hexanote, benzoate or phenylacetate ester. The invention also relates to novel 12-deoxyphorbol 13-monoesters, wherein the ester can be a formate, propionate, butyrate or pentanoate ester, and to pharmaceutical compositions comprising same.

Abstract: The present invention provides a method of inhibiting neoplasia and tumor promotion. The method comprises administering to a mammal, particularly a human, in need thereof an effective amount of a 12-deoxyphorbol ester, particularly a 12-deoxyphorbol 13-monoester such as 12-deoxyphorbol 13-acetate (prostratin) and 12-deoxyphorbol 13-phenylacetate (dPP).

Abstract: A method of regulating phosphorylation of proteins involved in controlling processing or function of key proteins found in intracellular neurofibrillary tangles and extracellular amyloid plaques associated with Alzheimer disease comprising introducing an effective amount of a kinase modulator or phosphatase modulator, the modulator capable of increasing or decreasing the rate of proteolytic processing, or modulating the function, of said key proteins.

Abstract: The invention relates to carbacyclin derivatives of Formula I ##STR1## wherein the various substituents are defined herein, including, inter alia,if R.sub.2 is a hydrogen atom, their salts with physiologically compatible bases, their cyclodextrin clathrates, and their use as medicinal agents.

Abstract: Described is the use of a mixture of aldehydes and ketones having the structures: ##STR1## containing from 45-60 mole percent of the compound having the structure: ##STR2## from 15-20 mole percent of the compound having the structure: ##STR3## and from 25-35 mole percent of the compound having the structure: ##STR4## in repelling Aedes aegyptae.

Abstract: Agents which modulate or affect the intracellular trafficking and processing of proteins in the mammalian cell can be utilized to affect the trafficking and processing of APP, thereby inhibiting production of Alzheimer type amyloidosis. Particularly useful agents are chloroquine and its related derivatives such as primaquine.

Abstract: The present invention relates to a method for desensitizing a subject animal, which comprises administering to the subject animal a therapeutically effective desensitizing amount of resiniferatoxin for desensitizing the subject animal to neurogenic inflammation, to chemically and thermally induced pain and to responses involving sensory afferent pathways sensitive to capsaicin and to responses involving the hypothalamic temperature control region, and a pharmaceutically acceptable carrier therefor.