Abstract: Compositions, compounds and methods are described for addressing both toxicity of membrane disruptive anti-microbial agents as well as poor transport of such agents across the blood-brain-barrier (BBB) via the use of molecular appendages including one or more facial amphiphiles. These molecules have in vitro anti-fungal activity that is very similar to that of the native drug but with hemolytic activity and toxicity towards mammalian cells that is greatly reduced.

Abstract: The invention provides semisynthetic derivatives of Nystatin A1, water soluble salts and complexes, pharmaceutical compositions and plant protection products comprising the derivatives and their use, as antifungal antibiotics (Formula 1a).

Abstract: The invention provides, biologically active spinosyns, hybrid spinosyn polyketide synthases capable of functioning in Saccharopolyspora spinosa to produce the spinosyns, and methods of controlling insects using the spinosyns.

Abstract: Provided herein are uses of genes for HOG, Ras and cAMP signal transduction pathways to treat fungal infection. To regulate the HOG pathway of Cryptococcus neoformans, roles of SSK1, TCO2, SSK2, PBS2, HOG1, ENA1 and NHA1 genes were investigated to find that a biosynthesis level of ergosterol is increased when these genes are inhibited. When the genes are inhibited, a large amount of ergosterol is distributed on a fungal cell membrane. Accordingly, since there are many working points of an ergosterol-binding antifungal agent, an efficiency of the ergosterol-binding antifungal agent can be considerably improved. To regulate the Ras and cAMP pathways of Cryptococcus neoformans, roles of RAS1, RAS2, CDC24, GPA1, CAC1, ACA1, PKA1, HSP12 and HSP122 genes were investigated to find that a sensitivity to a polyene- or azole-based drug is increased when these genes are inhibited.

Abstract: The invention provides semisynthetic derivatives of Nystatin A1, water soluble salts and complexes, pharmaceutical compositions and plant protection products comprising the derivatives and their use, as antifungal antibiotics (Formula 1a).

Abstract: The present invention relates to a sorbent comprising a solid support material, the surface of which comprises a residue of a general formula (I), wherein the residue is attached via a covalent single bond to a functional group on the surface of either the bulk solid support material itself or of a polymer film on the surface of the solid support material. Furthermore, the present invention relates to the use of the sorbent according to the invention for the purification of organic molecules, in particular pharmaceutically active compounds, preferably in chromatographic applications.

Abstract: The present invention relates to a novel polyene compound similar to nystatin, a method for preparing the same, and an antifungal drug comprising the novel polyene compound as an active ingredient. Compared to nystatin comprising one sugar, NNP, which is the polyene compound similar to nystatin, displays 300 times higher solubility and ten times lower cytotoxicity while maintaining antifungal activity, and thus can be useful in developing a novel polyene antifungal agent having improved solubility and less toxicity in terms of pharmacokinetics.

Abstract: The present invention relates to a new use of a known medicament. Specifically, the invention relates to methods and compositions for enhancing the therapeutic efficacy of a therapeutic agent by increasing the uptake of the therapeutic agent by target cells, and in particular relates to a pharmaceutical composition comprising a regulating agent of lipid raft/caveolae-dependent endocytic pathway and some therapeutic agents, such as anti-tumor agents. The invention also relates to a method for screening a regulating agent of lipid raft/caveolae-dependent endocytic pathway capable of enhancing the therapeutic efficacy of anti-tumor agents.

Abstract: Described herein are compositions and methods that treat fungal infections of the skin, reduce the severity and duration of symptoms of fungal infections of the skin, and prevent recurrence of fungal infections. The topical compositions described herein are creamy pastes composed of an admixture of an imidazole antifungal and nystatin. The topical compositions can also include optional fillers. The compositions and methods described herein minimize fungal resistance and maximize the number of targeted fungal strains. Additionally, the compounds and methods do not suppress the body's immune system either locally or systemically, thus allowing for a faster restoration of normal skin flora. The compositions and methods described herein are particularly suitable for use in infants and children as well as in immunocompromised individuals, diabetics, and the obese.

Abstract: The present invention relates to novel compositions for treating seeds. Moreover, the present invention is directed to the production of these compositions and the uses of these compositions.

Abstract: The invention refers to primycin or a primycin component or a combination of primycin components, for use in the treatment or prevention of infections caused by Gram-positive bacteria resistant to methicillin and/or vancomycin and/or mupirocin or by penicillin-resistant streptococci. The invention also covers antibiotic compositions containing these active agents.

Abstract: The present invention relates to polyene macrolide derivatives according to the formula: wherein M is a macrocyclic lactone ring; N is a polyene sugar, substituted or unsubstituted; X is independently selected from O, S, N or NH; R is independently selected from an alkyl, cycloalkyl, heterocycloalkyl aryl, heteroaryl, arylalkyl, and heteroaryalkyl group; and i is an integer from 1 to 3, with the condition that it has a negative charge or the zwitterions character is restored; or a pharmaceutically acceptable salt thereof useful as antibiotics.

Abstract: In a first embodiment the present invention relates to a sorbent comprising a porous inorganic solid support material having on its surface a film of a crosslinked polyvinylamine comprising derivatized amine groups and amine groups binding to the surface of the support material via electron donor/acceptor interactions. In a second embodiment the present invention relates to a sorbent comprising a solid support material, the surface of which comprises a residue of a general formula (I), wherein the residue is attached via a covalent single bond to a functional group on the surface of either the bulk solid support material itself or of a polymer film on the surface of the solid support material. Furthermore, the present invention relates to the use of the sorbents according to the invention for the purification of organic molecules, in particular pharmaceutical active compounds, preferably in chromatographic applications.

Abstract: The present invention relates to a prodrug, comprising a pharmaceutically and/or diagnostically active compound, and one or more bisphosphonate groups, to a process for producing such a prodrug, and to a pharmaceutical composition comprising said prodrug, to be used for the treatment of bone-related disorders such as bone cancer.

Abstract: The present invention relates to a new use of a known medicament. Specifically, the invention relates to methods and compositions for enhancing the therapeutic efficacy of a therapeutic agent by increasing the uptake of the therapeutic agent by target cells, and in particular relates to a pharmaceutical composition comprising a regulating agent of lipid raft/caveolae-dependent endocytic pathway and some therapeutic agents, such as anti-tumor agents. The invention also relates to a method for screening a regulating agent of lipid raft/caveolae-dependent endocytic pathway capable of enhancing the therapeutic efficacy of anti-tumor agents.

Abstract: A complex comprises a polyene macrolide antibiotic and an endotoxin. Methods and devices detect the complex. A polymeric material functionalized with a polyene macrolide antibiotic is employed in the devices.

Abstract: The present invention relates to Stambomycin compounds, their derivatives and their pharmaceutically acceptable salt thereof.

Abstract: A method of ameliorating amphotericin treatment side effects in a mammal that comprises administering a therapeutically effective amount of a formulation that comprises a polyene active ingredient that includes amphotericin B, wherein the amphotericin B compound is present, in terms of polyene content, in an amount greater than 90%, and non-amphotericin B polyene compounds are present in an amount of no greater than 10%, and a pharmaceutically effective carrier; and administering a therapeutically effective amount of said formulation to a subject in need thereof.

Abstract: The present invention provides a compound which is a nystatin derivative having an additional double bond present between C28 and C29 and which is further modified relative to nystatin at one or more of positions C5, C7, C9, C10, C11, C16 or at the amino group of mycosamine.

Abstract: The present invention relates to the use of polyene fungicides for reducing weight loss of crops.

Abstract: A method of controlling or preventing damage to a plant, which comprises applying on the plant or a surrounding area thereof a combination comprising (I) abamectin, and (II) cyflumetofen, in any desired sequence or simultaneously.

Abstract: The present invention relates to an improved anti-fungal composition, to a process for preparing it and to its use as a preservative.

Abstract: The present invention provides antimicrobial nanoparticle conjugates and an efficient method of preparing same. In particular, the invention relates to the preparation of antifungal nanoparticle conjugates comprising amphotericin B covalently immobilized to nanoparticles. The conjugates, and suspensions thereof, can be used to form antifungal coatings with particular application to medical devices and materials.

Abstract: The present invention comprises compositions and formulations comprising amphotericin B, compositions and formulations comprising amphotericin B with one or more excipients, methods of making amphotericin B compositions and formulations, as well as systems for using amphotericin B compositions and formulations. Also provided are pharmaceutical compositions comprising the formulation, methods of administering the pharmaceutical compositions and methods of treating patients with the pharmaceutical compositions.

Abstract: The present invention provides novel glycopeptides antibiotic derivatives comprising a sugar residue (I) represented by the formula: (wherein n is an integer of 1 to 5: Sugs are each independently a monosaccharide, (Sug)n is a divalent sugar residue formed by binding of same or different 1 to 5 monosaccharides; RA1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, or optionally substituted cycloalkyl; and RE is OH or NHAc (Ac is acetyl)) is bound to an aromatic ring of the fourth amino acid residue in the glycopeptide skeleton. These derivatives have antibacterial activity against vancomycin-resistant bacteria.

Abstract: In certain aspects, the present disclosure provides for novel, water-soluble polyene macrolides and salts or solvates thereof and methods of making the water-soluble polyene macrolides. Also provided are compositions and methods for inhibiting, preventing, and/or treating fungal and parasitic diseases in a subject.

Abstract: The present invention describes natamycin comprising needle shaped crystals.

Abstract: The present invention relates to compounds which are nystatin derivatives and are anti-fungal agents.

Abstract: This invention provides cross-linked glycopeptide-cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.

Abstract: The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.

Abstract: Disclosed are drug delivery compositions comprising an oligonucleotide-modified nanoparticle and a therapeutic agent. Specifically, disclosed are compositions comprising a number of oligonucleotide molecules in a ratio to therapeutic agent molecules to allow a sufficient transportation of the therapeutic agent molecules into a cell. The therapeutic agents include both hydrophobic and hydrophilic. Different attachments of therapeutic agents in a composition are also described.

Abstract: The present invention relates to an improved anti-fungal composition, to a process for preparing it and to its use as a preservative.

Abstract: The present invention concerns a process for improving the preservation of a bakery product by natamycin. A composition comprising natamycin in the form of a natamycin-cyclodextrin complex is provided and the composition is applied onto a bakery product as an antifungal agent. The invention also concerns a bakery product comprising an effective antifungal amount of natamycin. Another aspect of the invention is an antifungal natamycin composition and the use thereof, which composition has a modified antifungal activity. Further, the invention concerns a process for modifying the antifungal activity of natamycin.

Abstract: The present invention discloses a new polyene diester and its preparation. This polyene diester has a structure of Formula 1, which is used as prodrugs by introducing diester group to polyene antibiotics, and these prodrugs exhibit antifungal or antiviral activities through releasing parent polyenes by esterase in vivo. The new derivatives have good antimicrobial activity and better safety. These new derivatives are useful for the antifungal and antiviral treatment.

Abstract: The present invention relates to Stambomycin compounds, their derivatives and their pharmaceutically acceptable salt thereof.

Abstract: Natamycin is separated and recovered from a fermentation broth containing biomass and natamycin by adjusting the pH of a natamycin-containing suspension first to dissolve the natamycin in a solvent then adjusting the pH again to precipitate the dissolved natamycin which is used as an antifungal used to protect products susceptible to fungal spoilage.

Abstract: The present invention comprises compositions and formulations comprising amphotericin B comprising less than 10% degradants, compositions and formulations comprising amphotericin B with one or more excipients, methods of making amphotericin B compositions and formulations, as well as systems for using amphotericin B compositions and formulations. Also provided are pharmaceutical compositions comprising the formulation, methods of administering the pharmaceutical compositions and methods of treating patients with the pharmaceutical compositions.

Abstract: Novel avermectin derivatives of the formula (I) in which —C22R1-A-C23R2, R3, R4 and R5 have the meanings given in the description, processes for preparing these compounds and their use for controlling animal pests, and also novel intermediates and their preparation.

Abstract: A method for increasing breast meat yield in avians by treating the poultry with an effective amount of natamycin. The effective amount of natamycin can be added to the avian's feed wither directly or in the form of a premix containing a carrier.

Abstract: This invention is directed to the use of spinosyn or a physiologically acceptable derivative or salt thereof for improved production of fish; controlling ectoparasite infestations in aquaculture raised fish; and fish feed formulations.

Abstract: A method for treating fungal infections in a mammal that includes administering a therapeutically effective amount of a composition comprising substantially pure amphotericin B and a pharmaceutically acceptable carrier. Amphotericin BHP is associated with decreased toxicity in mammals and cells measured by cell viability and expression of cytokine markers. Thus, this method allows for reduced adverse reactions when using amphotericin B products.

Abstract: The present invention provides a compound of formula (I?) which is a nystatin derivative having an additional double bond present between C28 and C29 and which is further modified relative to nystatin at one or more of positions C5, C7, C9, C10, C11, C16 or at the amino group of mycosamine. These compounds are used as anti-fungal agents.

Abstract: The invention provides a nucleic acid molecule comprising: (a) a nucleotide sequence as shown in SEQ ID No. 35; or (b) a nucleotide sequence which is the complement of SEQ ID No. 35; or (c) a nucleotide sequence which is degenerate with SEQ ID No. 35; or (d) a nucleotide sequence hybridising under conditions of high stringency to SEQ ID No. 35, to the complement of SEQ ID No. 35, or to a hybridisation probe derived from SEQ ID No. 35 or the complement thereof; or (e) a nucleotide sequence having at least 80% sequence identity with SEQ ID No. 35; or (f) a nucleotide sequence having at least 65% sequence identity with SEQ ID No. 35 wherein said sequence preferably encodes or is complementary to a sequence encoding a nystatin PKS enzyme or a part thereof.

Abstract: The present invention discloses a new polyene diester and its preparation. This polyene diester has a structure of Formula 1, which is used as prodrugs by introducing diester group to polyene antibiotics, and these prodrugs exhibit antifungal or antiviral activities through releasing parent polyenes by esterase in vivo. The new derivatives have good antimicrobial activity and better safety. These new derivatives are useful for the antifungal and antiviral treatment.

Abstract: Seven novel antibiotic substances could be produced by cultivation of a microbial strain which has been isolated from a soil sample and which is designated as Microbispora sp. A 34030 (deposited under an access number FERM BP-10505 in terms of Budapest Treaty). These seven antibiotic substances are named as bispolide A1, bispolide A2, bispolide A3, bispolide B1, bispolide B2a, bispolide B2b and bispolide B3, respectively. These bispolides are each novel compounds which have a chemical structure as collectively represented by the general formula (III) shown below. These bispolides have each a high antibacterial activity against a variety of bacteria, particularly Gram-positive bacteria and their antibiotic-resistant strains, and hence these bispolides each are effective and useful for therapeutically treating bacterial infections of Gram-positive bacteria in human and animals.

Abstract: The present invention describes natamycin comprising needle shaped crystals.

Abstract: The use of macrolide polyene antibiotics or derivatives or analogues thereof as culture supplement for the propagation of virus is described. Further pharmaceutical compositions comprising a virus and a macrolide polyene antibiotic or a derivative or analogue thereof and methods for using of macrolide polyene antibiotics for transfection and infection of cells as well as the use of macrolide poylene antibiotics for the isolation of virus from clinical samples are disclosed.

Abstract: The invention relates to novel polyenes having formula (I), wherein: R1 represents alkyl C1-C3; and R2 represents a functional group selected from CH3— or CONH2— (methyl- or primary amide-). The aforementioned polyenes have a biocide action on organisms comprising cell membranes that contain ergosterol, e.g., fungi or parasites. Said compounds can be obtained using a method that consists in cultivating a producing micro-organism under conditions that enable the production thereof. In addition, the invention also relates to a mechanism for the in vitro production of amidated polyenes, consisting in incubating carboxylated polyenes with cell-free extracts (or proteinaceous fractions) of the producers of same in the presence of ATP/Mg++ and an amide- group donor compound (preferably glutamine).

Abstract: The present invention provides new polyene macrolide derivatives which show very low toxicity while retaining high antifungal activity as compared with amphotericin B (AmB). These polyene macrolide derivatives comprise a polyene macrolide backbone having at least one free amino group, wherein the amino group is doubly alkylated with at least one hydrocarbon group carrying a total of at least two basic groups.

Abstract: Ipomoeassin compounds derived from morning glory plant material (especially Ipomoea sp. from Suriname) are useful as anti-cancer agents. The novel compounds also are useful for treating neurodegenerative disorders (such as Alzheimer's disease) in human patients.