Abstract: A microorganism belonging to Beauveria sp. and having ability to produce FKI-1366 substance A and/or FKI-1366 substance B and/or FKI-1366 substance C (Beauveria sp. FKI-1366 FERM BP-08459) is cultured in a medium, accumulating FKI-1366 substance A and/or FKI-1366 substance B and/or FKI-1366 substance C in the culture liquid and isolating FKI-1366 substance A and/or FKI-1366 substance B and/or FKI-1366 substance C from the cultured mass. Since the thus obtained FKI-1366 substance A and/or FKI-1366 substance B and/or FKI-1366 substance C or composition thereof have activity to enhance azole antifungal agent, the substance has an action against various fungal infections such as deep-seated mycosis and other fungal infections in the low concentration within short term. Consequently, the substance is useful for reducing frequency of appearance of resistant microorganisms and overcoming resistance, and is expected as a medicament.

Abstract: The present invention is comprised of culturing microorganism having ability to produce FKI-1083 substance represented by the formula: in a medium, accumulating FKI-1083 substance in the cultured medium, and isolating FKI-1083 substance from the cultured mass. The thus obtained FKI-1083 substance has growth inhibitory activities against microorganisms, nematodes and arthropods, and is useful as anthelmintic and insecticide.

Abstract: In the present invention, a recombination of gene groups of nemadectin aglycon biosynthesis is performed for obtaining C-13 hydroxylnemadectin, to which sugar groups can be attached, and a production strain which produces C-13 hydroxylnemadectin is produced. Further, C-13 glycosylnemadectin producing strain is prepared by introducing aveBI-BVIII genes involving glycosidation of avermectin and biosynthesis of oleandrose. As described, C-13 hydroxylnemadectin and C-13 glycosidated nemadectin can be obtained effectively by using the producing strain prepared by means of the molecular genetic technology, and improvement in the biological activity thereof can be expected.

Abstract: The present invention is comprised of culturing microorganism having ability to produce FKI-1033 substance represented by the formula: in a medium, accumulating FKI-1033 substance in the cultured medium, and isolating FKI-1033 substance from the cultured mass. The thus obtained FKI-1033 substance has ryanodine binding inhibition activity, insecticidal activity and anthelmintic activity, and is expected as useful drugs as agrochemicals, veterinary drugs and medicaments in effectiveness and toxicity.

Abstract: The present invention is comprised of culturing a microorganism having ability to produce K01-B0171-B substance and/or K01-B0171-C substance in a medium, accumulating K01-B0171-B substance and/or K01-B0171-C substance in a culture fluid and isolating K01-B0171-B substance and/or, K01-B0171-C substance from the culture fluid. The obtained K01-B0171-B substance, K01-B0171-C substance or a composition of these substances is expected to be useful as a medicament of antituberculous agent.

Abstract: The present invention relates to agent for suppressing infection and proliferation of human immunodeficiency syndrome virus (HIV-1), which infects immunocompetent cells such as macrophage or dendritic cell and causes destruction of immune system, and use of known compounds, macrolide derivatives for suppression of infection and proliferation of human immunodeficiency syndrome virus in M type macrophage derived from human monocytes. The present invention is useful for treatment of patients with HIV-1 infection by low cost chemotherapeutic agents, and in addition, is clinically used as supplement agent in HAART.

Abstract: The present invention relates to agent for suppressing infection and proliferation of human immunodeficiency syndrome virus (HIV-1), which infects immunocompetent cells such as macrophage or dendritic cell and causes destruction of immune system, and use of known compounds, macrolide derivatives for suppression of infection and proliferation of human immunodeficiency syndrome virus in M type macrophage derived from human monocytes. The present invention is useful for treatment of patients with HIV-1 infection by low cost chemotherapeutic agents, and in addition, is clinically used as supplement agent in HAART.

Abstract: The present invention relates to effective drugs for mycosis caused by so called fungi such as fungi and yeast. The present invention is comprised of culturing a microorganism belonging to genus Streptomyces and having ability to produce K99-5278A substance, K99-5278B substance and K99-5278C substance in a medium, accumulating K99-5278A substance, K99-5278B substance and K99-5278C substance in the cultured medium and isolating K99-5278A substance, K99-5278B substance and K99-5278C substance from the cultured mass. The thus obtained substances can be expected as a novel antifungal agent.

Abstract: Macrolide derivatives having enhancing effect for activities of azole antifungal agents, acting at low concentration and within a short time against fungal infection and reducing the frequency of appearance of resistant microorganisms. One such substance is a compound represented by the formula [I]: wherein R1 is Ac, R2 and R3 are Ac, and R4 is Me; when R1 is H, R2 and R3 are Ac, and R4 is Me; when R1 is H, R2 and R3 are Ac, and R4 is H, when R1 Bzl, R2 and R3 are Bzl, and R4 is Me; when R1 is Ac, R2 and R3 are Pr, and R4 is Me; when R1 is Ac, R2 and R3 are Hex, and R4 is Me; when R1 is Ac, R2 and R3 are Bzl, and R4 is Me; when R1 is H, R2 and R3 are Pr, and R4 is Me; when R1 is H, R2 and R3 are Hex, and R4 is Me; when R1 is H, R2 and R3 are Bzl, and R4 is Me; when R1 is H, R2 is H, R3 is Bzl, and R4 is Me; when R1 is H, R2 and R3 are Hex, and R4 is H, or when R1 is H, R2 and R3 are Hex, and R4 is Et.

Abstract: The present invention relates to an isolated DNA which comprises a DNA sequence encoding avermectin aglycon synthase domains that corresponds to multifunctional enzyme proteins involved in the biosynthesis of a polyketide compound, or its mutants having avermectin aglycon synthase activity, particularly functional modules and submodules in the DNA sequence derived from Streptomyces avermitilis, a polypeptide or mutants thereof encoded by the DNA or the mutants, a vector containing the DNA or the mutants, a host cell transformed with the DNA, the mutants thereof, or the vector, and a method for producing avermectin.

Abstract: The present invention is a process for selective production of beauveriolide I substance or beauveriolide III substance, in which a beauveriolide producing microorganism strain FO-6979 or mutant thereof is cultured in a medium for fungi added with specific amino acid in order to produce beauveriolide I substance or beauveriolide III substance selectively with high yield; beauveriolide I substance or beauveriolide III substance is accumulated selectively in the cultured mass; and beauveriolide I substance or beauveriolide III substance is collected selectively with high yield from said cultured mass.

Abstract: The present invention relates to an isolated DNA which comprises a DNA sequence encoding avermectin aglycon synthase domains that corresponds to multifunctional enzyme proteins involved in the biosynthesis of a polyketide compound, or its mutants having avermectin aglycon synthase activity, particularly functional modules and submodules in the DNA sequence derived from Streptomyces avermitilis, a polypeptide or mutants thereof encoded by the DNA or the mutants, a vector containing the DNA or the mutants, a host cell transformed with the DNA, the mutants thereof, or the vector, and a method for producing avermectin.

Abstract: The present invention is comprised of culturing microorganism having ability to produce FKI-1083 substance represented by the formula: in a medium, accumulating FKI-1083 substance in the cultured medium, and isolating FKI-1083 substance from the cultured mass. The thus obtained FKI-1083 substance has growth inhibitory activities against microorganisms, nematodes and arthropods, and is useful as anthelmintic and insecticide.

Abstract: The present invention relates to a novel FKA-25 substance, which inhibits formation of the foam macrophage originated from mouse, having inhibitory action against formation of the foam macrophage and a process for production thereof. The process includes culturing Pseudobotrytis sp. FKA-25 belonging to genus Pseudobotrytis sp. and having ability to produce FKA-25 substance in a medium, accumulating FKA-25 substance in the cultured medium, and collecting FKA-25 substance from the cultured mass. The obtained FKA-25 substance specifically inhibits the formation of the foam macrophage originated from mouse and is expected to be useful for prevention and treatment of arteriosclerosis and causative diseases therefrom.

Abstract: An electron transport system complex II inhibitor comprising 2-pyridinol derivative represented by the general formula [I] 1

Abstract: The present invention relates to obtain novel FT-0554A substance useful for infectious disease of parasite, especially helminth and more particularly relates to the novel FT-0554A substance represented by the following formula [I] or the tautomer thereof represented by the formula [II] obtained by treating FT-0554 substance represented by the formula [II] under alkaline condition.

Abstract: A microorganism capable of producing substances K97-0239 comprising K97-0239A represented by the following formula [I]: and K97-0239B represented by the following formula [II]: is cultured in a medium and the substances K97-0239 thus accumulated in the medium are collected from the culture medium. The obtained substances have a low toxicity and specifically inhibit the foaming of macrophages. Owing to these characteristics, they are useful in preventing and treating human arteriosclerosis and diseases caused thereby.

Abstract: A microorganism having ability to produce FKI-0076 substance represented by the following formula [I] is cultured in a medium allowing for the accumulation of FKI-0076 substance in the culture liquid. The FKI-0076 substance from can then be isolated the cultured mass. Since the substance has the ability to enhance azole antifungal agents, it provides an action against various fungal infections such as deep-seated mycosis and other fungal infections in low concentration and within a short term. Consequently, the FKI-0076 is useful for reducing the frequency of appearance of resistant microorganisms. Further, usefulness for overcoming resistance is expected.

Abstract: The present invention comprising culturing a microorganism which belongs to genus Streptomyces and has ability to produce K99-5041-C1x substance and/or K99-5041-C2x substance in a medium, accumulating K99-5041-C1x substance and/or K99-5041-C2x substance in the culture fluid, and isolating K99-5041-C1x substance and/or K99-5041-C2x substance form the cultured mass. Since the obtained K99-5041-C1x substance and/or K99-5041-C2x substance exhibit inhibitory activity against lanosterol synthase, these substances are expected to apply clinically for preventive and therapeutic agents caused by accumulation of cholesterol in humans and antifungal agents.

Abstract: The present invention comprising culturing a microorganism which belongs to genus Streptomyces and has ability to produce K99-5041-C1x substance and/or K99-5041-C2x substance in a medium, accumulating K99-5041-C1x substance and/or K99-5041-C2x substance in the culture fluid, and isolating K99-5041-C1x substance and/or K99-5041-C2x substance form the cultured mass. Since the obtained K99-5041-C1x substance and/or K99-5041-C2x substance exhibit inhibitory activity against lanosterol synthase, these substances are expected to apply clinically for preventive and therapeutic agents caused by accumulation of cholesterol in humans and antifungal agents.