Abstract: This invention provides methods of inhibiting the export of a leaderless protein from a cell by contacting the cell with a cardiac glycoside or aglycone derivative. Leaderless proteins include FGF-1, FGF-2, IL-1&agr;, IL-1&bgr; and factor XIIIa. These methods are useful in treatment of conditions, including tumors and diabetes.

Abstract: A stable injectable composition includes a non-aqueous parasitic agent in a therapeutically effect amount, chosen from the group of avermectin, ivermectin, doramectin, abamectin, milbemycin and moxidecting, and an antigen in combination with a liquid carrier that also acts as an adjuvant for use with warm blooded animals and a method for treating parasitic diseases and preventing bacterial and viral diseases in warm blooded animals.

Abstract: Pharmaceutical compositions for oral administration comprising a cyclosporin or macrolide as active ingredient, and a polyethoxylated saturated hydroxy-fatty acid.

Abstract: A preventive and curative agent for inflammatory bowel diseases is disclosed which has as an active ingredient thereof a chromanol glucoside represented by the following general formula (1) (wherein R1, R2, R3, and R4 represent identically or differently either a hydrogen atom or a lower alkyl group, R5 represents a hydrogen atom, a lower alkyl group, or a lower acyl group, X represents a monosaccharide residue or an oligosaccharide residue having the hydrogen atom in the hydroxyl group thereof optionally substituted with a lower alkyl group or a lower acyl group, n represents an integer of 0-6, and m represents an integer of 1-6). Owing to the use, as an active ingredient, of the chromanol glucoside excelling in water solubility and possessing an oxidization resisting action and a free radical resisting action, the agent can conspicuously repress the lesion of an inflammatory bowel disease and prominently ameriolate the condition of disease.

Abstract: Ring-contracted N-demethyl-N-isopropyl-erythromycin-A derivatives having a modified side chain and gastrointestinally effective motilin-agonistic properties and the preparation thereof are described.

Abstract: Purified DNA encoding LCF and the recombinant proteins expressed from such DNA are disclosed. In addition, the invention provides methods for suppressing an LCF-CD4 interaction and screening candidate LCF agonists or antagonists. The invention also provides compositions and methods useful for stimulating proliferation of CD4+ T-cells in a mammal.

Abstract: A method for treatment of prophylaxis of skin against ageing, against inflammation and for protection from photoreaction and oxidative influences which comprise applying a formulation comprising alpha-glucosyl rutin and one or more cinnamic acid derivatives to the skin.

Abstract: This invention provides methods of inhibiting the export of a leaderless protein from a cell by contacting the cell with a cardiac glycoside or aglycone derivative. Leaderless proteins include FGF-1, FGF-2, IL-1.alpha., IL-1.beta. and factor XIIIa. These methods are useful in treatment of conditions, including tumors and diabetes.

Abstract: The present invention provides a pharmaceutical composition comprising an extract or combination of extracts having an antiviral, antibacterial, or immunomodulating property, wherein the extract or combination of extracts is obtained from a combination of plants wherein at least one plant is selected from each of the genuses Labiatae, Caprifoliaceae, and Oleaceae. A preferred extract is obtained from Radix scutellaria, Flos lonicera, and Fructus forsythiae. The present invention further provides a pharmaceutical composition comprising baicalin, chlorogenic acid and forsythiaside in isolated and purified form. The present invention further provides certain novel derivatives of baicalin, chlorogenic acid and forsythiaside. The present invention additionally provides processes for preparing the extracts as well as baicalin, chlorogenic acid, and forsythiaside in isolated and purified forms.

Abstract: Methods of inhibiting the export of a leaderless protein from a cell by contacting the cell with a compound that inhibits the binding of the leaderless protein and a transport molecule are provided. Leaderless proteins include FGF-1, FGF-2, IL-1.alpha., IL-1.beta., CNTF and HIV-tat. These methods are useful in treatment of various conditions, including tumors and diabetes.

Abstract: This invention provides methods of inhibiting the export of a leaderless protein from a cell by contacting the cell with a cardiac glycoside or aglycone derivative. Leaderless proteins include FGF-1, FGF-2, IL-1.alpha., IL-1.beta. and factor XIIIa. These methods are useful in treatment of conditions, including tumors and diabetes.

Abstract: A method is provided of inhibiting the narrowing of the vascular tubular walls of an animal by the proliferation of endothelial cells in the area of trauma after the vascular tubular walls have been traumatized, the method comprising the administration of a therapeutically effective non-toxic amount of a form of hyaluronic acid selected from the group consisting of hyaluronic acid and pharmaceutically acceptable salts thereof to the animal to inhibit the narrowing of the vascular tubular walls by the proliferation of endothelial cells into the area of trauma.

Abstract: The invention relates to certain stable vaccine compositions comprising a macrocyclic lactone compound, a milbemycin compound, an avermectin compound or mixtures thereof; at least one antigen; a dispersing agent; an adjuvant; a water soluble organic solvent; and saline or water or mixtures thereof. The invention further relates to stable compositions as described above of a macrocyclic lactone compound, a milbemycin compound, an avermectin compound or mixtures thereof, but without an antigen. The invention also relates to a method for preventing or controlling helminthiasis, infection by acarids and arthropod endo-and ectoparasites and bacterial and viral disease in warm-blooded animals by the parenteral administration of compositions of the invention. The invention further relates to a process for the preparation of the invention compositions.

Abstract: A 5-oximino-25-substituted avermectin B1 or B2 monosaccharide of formula I herein has use in the treatment of parasitic infections in animals and humans. The compounds may be prepared from corresponding 5-keto substituted derivatives.

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: Ring-contracted N-demethyl-N-isopropyl-erythromycin-A-spiroacetal compounds corresponding to formula I ##STR1## having gastrointestinally effective motilin-agonistic properties and the preparation thereof.

Abstract: This invention provides methods of inhibiting the export of a leaderless protein from a cell by contacting the cell with a cardiac glycoside or aglycone derivative. Leaderless proteins include FGF-1, FGF-2, IL,-1.alpha., IL-1.beta. and factor XIIIa. These methods are useful in treatment of conditions, including tumors and diabetes.

Abstract: New A83543 components, including fermentation products A83543K, A835430, A83543P, A83543U, A83543V, A83543W and A83543Y and N-demethyl derivatives, and salts thereof, are useful for the control of insects and mites. The pseudoaglycones of the new A83543 components are useful for the preparation of A83543 components. Methods are provided for making the new A83543 components by culturing of Saccharopolyspora spinosa NRRL 18395, NRRL 18537, NRRL 18538, or NRRL 18539, or NRRL 18743 or NRRL 18719 or NRRL 18823 in suitable culture medium. Insecticidal and ectoparasiticidal compositions containing new A83543 components are also provided.

Abstract: 14- or 15-membered-ring macrolide compounds such as clarithromycin, erythromycin B, etc. have a potent antitumor effect on non-small cell lung cancers which are considered the most difficult tumors to be be subjected to surgical operation and chemotherapy, and are useful as a practical therapeutic agent of non-small cell lung cancer.

Abstract: Methods for cancer chemosensitization are provided. Texaphyrins are new chemosensitizers for enhancing the cytotoxicity of chemotherapeutic agents. The enhancement appears to be P-glycoprotein-independent since texaphyrins are effective in both a P-glycoprotein-expressing and a P-glycoprotein -nonexpressing cell line. Methods are provided for the treatment of cancers such as leukemia, lymphoma, carcinoma, and sarcoma using a texaphyrin as a chemosensitizer.

Abstract: Antimicrobial compounds having the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen and C.sub.1 -to-C.sub.4 alkanoyl;R.sup.3 and R.sup.4 are selected from the group consisting of(a) R.sup.3 is hydrogen and R.sup.4 is hydroxy,(b) R.sup.3 is hydroxy and R.sup.4 is hydrogen,(c) R.sup.3 and R.sup.4 taken together are .dbd.O; or selected from the group consisting of hydrogen and hydroxy; andR.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, bromine and chlorine, with the proviso that at least one of R.sup.5 and R.sup.6 must be bromine. Also disclosed are pharmaceutical compositions comprising such compounds, methods of treating bacterial infection by the administration thereof and a process for preparing said compounds.

Abstract: This invention relates to the saccharide derivatives of macrocyclic compounds useful for the treatment of resistance to transplantion, autoimmune disease and fungal diseases.

Abstract: Antiparasitic compounds of the formula (I) ##STR1## where the broken lines between the 3-4 and 4-5 positions represent optional bonds and either (i) the 3-4 optional bond is present; the 4-5 optional bond is absent, R.sup.7 is absent and R.sup.6 is halogen atom, an isothiocyanate group, a diazo group, a thioureido group of formula NHCSNR.sup.15 R.sup.16 where R.sup.15 and R.sup.16 are independently H, C.sub.1 -C.sub.8 alkyl, cycloalkyl, aryl or aralkyl groups, an azido group or a C.sub.1 -C.sub.8 alkylcarbonyl-thio group, or (ii) the 4-5 optional bond is present, the 3-4 optional bond is absent, R.sup.6 is absent and R.sup.7 is a mercapto, C.sub.1 -C.sub.8 alkylthio, oxo, optionally substituted oximino or C.sub.1 -C.sub.8 alkylcarbonylthio group; or R.sup.7 is absent and R.sup.6 is CN, with the provisos that the compounds where R.sup.6 is .alpha.-fluoro and R.sup.2 is CH(CH.sub.3).sub.2, CH(CH.sub.3)C.sub.2 H.sub.5, C(CH.sub.3).dbd.CHCH.sub.3, C(CH.sub.3).dbd.CHC.sub.2 H.sub.5 and C(CH.sub.3).dbd.CHCH(CH.sub.

Abstract: Novel macrocyclic 13-membered ring-contracted compounds derived from erythromycins A and B having the Formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein R, R.sup.1, R.sup.2, R.sup.3 and X are specifically defined, having use in treating gastrointestinal disorders associated with hypermotilinemia, pharmaceutical compositions thereof, a method of treating gastrointestinal disorders associated with hypermotilinemia with said pharmaceutical compositions, and processes for the preparation thereof.

Abstract: This invention is directed to novel antiparasitic compounds of formula (I), wherein the broken line represents an optional bond, R.sup.1 and R.sup.4 being absent when this bond is present, R.sup.1, R.sup.3, R.sup.4 are independently H, OH, halo mercapto, oxo, oximino, or an organic radical, R.sup.2 and R.sup.7 are organic radicals, R.sup.6 is H or an organic radical and R.sup.12 is OH, halo, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.9 alkanoyloxy, or oximino optionally O-substituted by a C.sub.1 -C.sub.8 alkyl, alkenyl, alkynyl, aryl, trialkylsilyl, aralkyl or C.sub.1 -C.sub.9 alkanoyl group.

Abstract: New A83543 components, including fermentation products A83543K, A835430, A83543P, A83543U, A83543V, A83543W and A83543Y and N-demethyl derivatives, and salts thereof, are useful for the control of insects and mites. The pseudoaglycones of the new A83543 components are useful for the preparation of A83543 components. Methods are provided for making the new A83543 components by culturing of Saccharopolyspora spinosa NRRL 18395, NRRL 18537, NRRL 18538, or NRRL 18539, or NRRL 18743 or NRRL 18719 or NRRL 18823 in suitable culture medium. Insecticidal and ectoparasiticidal compositions containing new A83543 components are also provided.

Abstract: New A83543 components, including fermentation products A83543K, A83543O, A83543P, A83543U, A83543V, A83543W and A83543Y and N-demethyl derivatives, and salts thereof, are useful for the control of insects and mites. The pseudoaglycones of the new A83543 components are useful for the preparation of A83543 components. Methods are provided for making the new A83543 components by culturing of Saccharopolyspora spinosa NRRL 18395, NRRL 18537, NRRL 18538, or NRRL 18539, or NRRL 18743 or NRRL 18719 or NRRL 18823 in suitable culture medium. Insecticidal and ectoparasiticidal compositions containing new A83543 components are also provided.

Abstract: A method for the topical or systemic treatment of disorders mediated by proteases which result in skin or mucosal lesions, and in particular, pemphigus, cicatricial pemphigoid, bullous pemphigoid, lichen planus, and canker sores, is disclosed wherein the host is treated with an effective amount of N-acetyl ysteine or a derivative thereof, or its pharmaceutically acceptable salt, optionally in a pharmaceutically acceptable diluent or carrier for systemic or topical delivery.

Abstract: A vitamin C supplement comprising ascorbic acid, ascorbyl palmitate, niacinamide ascorbate, calcium ascorbate, magnesium ascorbate, potassium ascorbate, and sodium ascorbate which together can be administered to a human to avoid the transitory initial suppression of human NK cell activity which is present when ascorbic acid alone is administered. Also included is xylitol, lysine acetate, tetrasodium pyrophosphate, ribose, cysteine, and hesperidin which further prolongs the biological activity of ascorbic acid and promotes the uptake of ascorbic acid by human tissue.

Abstract: Texaphyrins are provided for use as radiation sensitizers. Advantageous properties of texaphyrins for use as a radiation sensitizer include: i) a low redox potential which allows radiation-induced hydrated electrons to flow to texaphyrin rather than neutralizing hydroxyl radicals, allowing hydroxyl radicals to cause cellular damage, ii) a relatively stable texaphyrin radical that reacts readily to covalently modify neighboring molecules causing further cellular damage, iii) intrinsic biolocalization, and iv) indifference to the presence or absence of O.sub.2. These properties allow texaphyrins to be particularly effective for treating the hypoxic areas of solid neoplasms. Methods of treatment for an individual having a neoplasm or atheroma include the use of a texaphyrin as a radiation sensitizer and as an agent for photodynamic tumor therapy, or the use of a texaphyrin for internal and for external ionizing radiation. Novel texaphyrins are provided.

Abstract: A stable topical formulation with good active ingredient release characteristics, comprising at least one macrolide antibiotic which is lipophilized with at least one former of oppositely charged ions which is selected from the group consisting of alkyl sulfates, alkylsulfonates, and alkyl salicylates, RX, where R represents a linear and/or branched alkyl group with 6-32 C atoms, and X represents a sulfate, sulfonate, or salicylate group.

Abstract: Stable parenteral antitumor formulations contain elsamitrucin salt, a stabilizer and a buffer. The formations are optionally stored in sealed containers under air or nitrogen headspace.

Abstract: A therapeutic agent for hemorrhoidal diseases, comprising, as an active ingredient, a diester phosphate compound of the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each is a hydrogen atom or a methyl, or a pharmacologically acceptable salt thereof, and a method for treating hemorrhoidal diseases, comprising administering a pharmaceutically effective amount of said diester phosphate compound or a pharmacologically acceptable salt thereof.

Abstract: A stable topical formulation with good active ingredient release characteristics, comprising at least one macrolide antibiotic which is lipophilized with at least one former of oppositely charged ions which is selected from the group consisting of alkyl sulfates, alkylsulfonates, and alkyl salicylates, RX, where R represents a linear and/or branched alkyl group with 6-32 C atoms, and X represents a sulfate, sulfonate, or salicylate group.

Abstract: This invention relates to the antibiotics LL-14E605.beta. and O-methyl-LL-14E605.beta. derived from the microorganism Sebekia benihana which are useful as antibacterial agents.

Abstract: Ring-contracted N-demethyl-N-isopropylerythromycin A derivatives with gastrointestinally effective motilin-agonistic properties, a method for preparing such compounds, and pharmaceutical compositions containing them.

Abstract: Avermectin derivatives are disclosed which incorporate two fluorine atoms at the 4' monosaccharide position, the 4" disaccharide position or the 23 position. Avermectin aglycone derivatives are also disclosed which incorporate two fluorine atoms at position 13 or 23. These difluoro avermectin analogs are derived from corresponding ketones and enones which in turn are prepared by chemical modification of naturally occurring avermectins. These compounds are used as antiparisitic, insecticidal and antihelmintic agents in humans and animals and compositions containing such compounds as the active ingredient thereof are also disclosed.

Abstract: Kedarcidin chromophore, a non-protein chromophore isolated from kedarcidin antitumor antibiotic, is obtained from purified or partially purified kedarcidin by solvent extraction and chromatographic procedures. The chromophore is characterized and found to contain substantially all of the antitumor activity of kedarcidin.

Abstract: An antitumor substance BE-12406 or a pharmaceutically acceptable salt thereof, which is represented by the general formula ##STR1## and a method of producing the novel substance.

Abstract: Compositions for inhibiting protein kinase C, comprising an inhibitory amount of a compound having the formula: ##STR1## wherein Q is a hydrophobic group; wherein X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, which may be substituted by one or more halogens or C.sub.1 -C.sub.3 alkyl groups,wherein Y is ##STR2## wherein W is a halogen; wherein R.sub.1 and R.sub.2 may be the same or different and are selected from hydrogen, lower alkyl groups having from 1 to 7 carbon atoms, aralkyl, and aryl groups, andwherein Z is a phosphate or an organic group, and a pharmaceutically acceptable carrier material; and a method for inhibiting protein kinase C using such compositions.

Abstract: Novel ring-contracted macrolides which enhance gastrointestinal motility and novel methods and compositions for treating gtastrointestinal disorders in animals with these macrolides and with certain other previously known ring-contracted macrolides are provided.

Abstract: Compositions for inhibiting protein kinase C, comprising an inhibitory amount of a compound having the formula: ##STR1## wherein Q is a hydrophobic group; wherein X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, which may be substituted by one or more halogens or C.sub.1 -C.sub.3 alkyl groups,wherein Y is ##STR2## wherein W is a halogen; wherein R.sub.1 and R.sub.2 may be the same or different and are selected from hydrogen, lower alkyl groups having from 1 to 7 carbon atoms, aralkyl, and aryl groups, andwherein Z is a phosphate or an organic group, and a pharmaceutically acceptable carrier material; and a method for inhibiting protein kinase C using such compositions.

Abstract: Novel lysine esters used as absorption enhancing agents for gastrointestinally and rectally administered drugs. Also provided are processes for preparation of said lysine ester compounds as well as pharmaceutical formulations and methods for their use as absorption enhancing agents.

Abstract: A ganglioside mixture, comprised of the gangliosides GM.sub.1, GD.sub.1a, GD.sub.1b and GT.sub.1b, has been found to possess significant analgesic or pain relieving activity. The mixture is, therefore, useful for treating pain due to various peripheral neuropathies and the mixture is more effective than the individual gangliosides which comprise the mixture.

Abstract: Adminiculum increasing the antitumor activities of mitomycin C and doxorubicin hydrochloride and decreasing the side effects associated with their use comprising an aqueous or aqueous organic solvent extract of a crude preparation of Astragali radix, Cinnamomi cortex, Rehmanniae radix, Paeoniae radix, Cnidii rhizoma, Atractylodis lanceae rhizoma, Angelicae radix, Ginseng radix, Hoelen and Glycyrrhizae radix, a method for preparing said adminiculum and a method for its use. In addition, compositions and methods for treating tumor-bearing patients are disclosed.

Abstract: A new salt of the macrolide antibiotic Josamycin with (-)-cis-1,4-epoxypropionylphosphonic acid, of formula (I) ##STR1## The salt (I), prepared from Josamycin base and phosphomycin, possesses favorable antimicrobial and pharmacokinetics properties.

Abstract: The novel glycopeptide antibiotic A-51568B is produced by submerged, aerobic fermentation of Nocardia orientalis NRRL 15232. A-51568B demonstrates antibiotic activity against gram-positive bacteria.

Abstract: An agent and treatment for a subject susceptible to septic shock. The subject is treated with a PKC inhibitor, preferably wit a PKC inhibitor selected from the group consisting of lipid analogues. Preferred among the lipid analogues are sphingosine and its analogues. The inhibitors of this invention are administered, preferably by infusion in a suitable pharmaceutical carrier, in a range of 0.1 to 50 mg/Kg body weight preferably in the range of 0.5 to 25 mg/Kg body weight and most preferably in the range of 1 to 5 mg/Kg body weight.