Abstract: The present invention relates to provide an aflatoxin production inhibitor that inhibits aflatoxin production specifically and efficiently, is highly safe, and is practical, and an efficient production method thereof; and a method for controlling aflatoxin contamination that uses the aflatoxin production inhibitor, specifically relating to an aflatoxin production inhibitor that includes at least one of a dioctatin represented by the following formula (I) and a derivative thereof, as an active ingredient: where, in the formula (I), R represents one of hydrogen and a methyl group.

Abstract: The present invention relates to provide an aflatoxin production inhibitor that inhibits aflatoxin production specifically and efficiently, is highly safe, and is practical, and an efficient production method thereof; and a method for controlling aflatoxin contamination that uses the aflatoxin production inhibitor, specifically relating to an aflatoxin production inhibitor that includes at least one of a dioctatin represented by the following formula (I) and a derivative thereof, as an active ingredient: where, in the formula (I), R represents one of hydrogen and a methyl group.

Abstract: To provide dioctatin derivatives, a production process thereof, an aflatoxin production inhibitor containing the dioctatin derivative, and a method of controlling aflatoxin contamination by use of the aflatoxin production inhibitor containing the dioctatin derivative. The present invention provides dioctatin derivatives represented by the following Structural Formula (I): where R1 and R2 each represent CH3—(CH2)n—, (CH3)2CH—CH2— or C6H5—CH2—; n represents an integer of 2 to 6; X1 and X2 each represent CH3 or hydrogen atom; and Y represents 2-amino-2-butenoic acid or amino acid residue, with compounds where R1 and R2 are each CH3(CH2)4—, X2 is a hydrogen atom and Y is 2-amino-2-butenoic acid being excluded.

Abstract: A medicament for prophylaxis or treatment of bone marrow suppression, for treatment of infectious diseases and for increasing the number of leukocytes, which comprise as an active ingredient a sulphostin-related compound represented by general formula (I): wherein n is an integer of 0 to 3, or a pharmacologically acceptable salt thereof.

Abstract: A medicament for prophylaxis or treatment of bone marrow suppression, for treatment of infectious diseases and for increasing the number of leukocytes, which comprise as an active ingredient a sulphostin-related compound represented by general formula (I): wherein n is an integer of 0 to 3, or a pharmacologically acceptable salt thereof.

Abstract: A medicament for prophylaxis or treatment of bone marrow suppression, for treatment of infectious diseases and for increasing the number of leukocytes, which comprise as an active ingredient a sulphostin-related compound represented by general formula (I): 1

Abstract: A sulphostin analogue represented by the general formula, wherein n is an integer of from 0 to 3, provided that a case where n is 2 and steric configurations of C* and P* are S and R, respectively, is excluded, or a pharmaceutically acceptable salt thereof.

Abstract: This invention provides a physiologically active substance having a strong dipeptidyl peptidase IV inhibitory activity. The physiologically active substance sulphostin is obtained by culturing a microorganism belonging to the genus Streptomyces and having an ability to produce the physiologically active substance sulphostin, producing and accumulating this substance in the cultures, and harvesting it from the cultures.

Abstract: Novel amide derivatives of amythiamicin are now provided, which are soluble in water and exhibit antibacterial activities, some of which exhibit an excellent antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA).

Abstract: The invention relates to novel pyrrolidine derivatives represented by formula (1): ##STR1## wherein: R1 represents (1) a lower alkyl group having 1 to 6 carbon atoms, or (2) a 3- to 15-membered mono- or fused cyclic hydrocarbon group which may contain a hetero atom on the ring, or which may be substituted with a substituent(s); each of n and m represents an integer and the sum of n and m is an integer of 0 to 2; each of X and E represents oxygen, NR' (wherein R' is hydrogen or a lower alkyl group having 1 to 6 carbon atoms), sulfur, phenylene, CH.dbd.CH or CH.sub.2 ; A represents an amino acid residue or an imino acid residue, which functional group may be optionally protected, or a glycine residue which may be substituted at the amino moiety thereof; and, Y1 represents a cycloalkyl group having 3 to 8 carbon atoms; or a salt thereof. The pyrrolidine derivatives inhibit a prolyl endopeptidase and are expected to be effective for the treatment of amnesia.

Abstract: The invention relates to novel pyrrolidine derivatives represented by formula (1): ##STR1## wherein: R1 represents (1) a lower alkyl group having 1 to 6 carbon atoms, or (2) a 3- to 15-membered mono- or fused cyclic hydrocarbon group which may contain a hetero atom on the ring, or which may be substituted with a substituent(s); each of n and m represents an integer and the sum of n and m is an integer of 0 to 2; each of X and E represents oxygen, NR' (wherein R' is hydrogen or a lower alkyl group having 1 to 6 carbon atoms), sulfur, phenylene, CH.dbd.CH or CH.sub.2 ; A represents an amino acid residue or an imino acid residue, which functional group may be optionally protected, or a glycine residue which may be substituted at the amino moiety thereof; and, Y1 represents a cycloalkyl group having 3 to 8 carbon atoms; or a salt thereof. The pyrrolidine derivatives inhibit a prolyl endopeptidase and are expected to be effective for the treatment of amnesia.

Abstract: A novel, biologically active substance, poststatin, has been isolated from a culture medium of microorganism belonging to Streptomyces. The novel substance is a peptide compound having a novel structure, wherein the peptide chains have ketone radicals. Thus substance has a high endopeptidase inhibition activity. It is possible to chemically synthesize poststatin related compound having ketone radicals in the peptide chains. These compounds also have an endopeptidase inhibition activity.

Abstract: The present invention discloses a new .alpha.-keto amide derivative or a salt thereof represented by the formula (1): ##STR1## wherein X represents (1) a peptide residue or amino acid residue in which the functional group may be protected, (2) a hydrogen atom or (3) an amino-protective group, Y represents a peptide residue or amino acid residue in which the functional group may be protected, E represents a substituent on the alkylene (C.sub.n H.sub.2n-1) and is a halogen, lower alkoxy or hydrogen, A represents a carbonyl group or mono- or di-substituted methylene (the substituent being a hydroxy, lower alkoxy, phenylimino or benzylimino), and n represents an integer of 2 to 6.The compound of the present invention is effective in inhibiting prolyl endopeptidase activity and useful as an active ingredient of an enzyme inhibitor.

Abstract: A novel, biologically active substance, poststatin, has been isolated from a culture medium of microorganism belonging to Streptomyces. The novel substance is a peptide compound having a novel structure, wherein the peptide chains have ketone radicals. Thus substance has a high endopeptidase inhibition activity. It is possible to chemically synthesize poststatin related compound having ketone radicals in the peptide chains. These compounds also have an endopeptidase inhibition activity.

Abstract: Benastatins A and B which are novel and physiologically active substances having the formula ##STR1## wherein R represents --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, exhibit a potent immunomodifier activity, a glutathione transferase inhibition activity and an anti-microorganism activity and are therefore extremely useful for various drugs.

Abstract: Disclosed is a 3-(4'-aminobutylamino) propylaminobleomycin having low pulmonary toxicity, which expressed by the following general formula[BX]--NH--(CH.sub.2).sub.3 --A--(CH.sub.2).sub.4 --Bwherein [BX] represents a residue remaining after removing a hydroxyl group from the carboxyl group of bleomycinic acid, A represents a group of the formula ##STR1## in which R.sub.1 represents (i) a hydrogen atom, (ii) an alkyl group having 1 to 10 carbon atoms, or (iii) a methyl which may be substituted by at least one of a phenyl group and a cycloalkyl group having 5 to 13 carbon atoms, said substituents being each optionally further substituted more than one position by one or more substituents selected from the class consisting of a halogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms, and benzyloxy group; and R.sub.2 represents a lower alkyl group having 1 to 4 carbon atoms or a benzyl group, B represents a group of the formula ##STR2## in which R.sub.3 and R.

Abstract: Plipastatin represented by the general formula ##STR1## wherein R.sub.1 is --C.sub.13 H.sub.27 or --C.sub.14 H.sub.29 ; and R.sub.2 is Ala or Val, or salts thereof, which is prepared by culturing a Plipastatin-producing strain belonging to the genus Bacillus to produce and accumulate Plipastatin in a cultured broth and then isolating Plipastatin from the cultured broth. Plipastatin exhibits an enzyme inhibiting activity against phospholipase A.sub.2, C and D and which will be useful as an immunosuppressive agent or as a type I anti-allergic agent.

Abstract: An aminopropylaminobleomycin represented by the following formula or a salt thereof, which is minimized in side effects such as pulmonary toxicity:[BX]--NH--(CH.sub.2).sub.3 --A--)CH.sub.2).sub.3 --Bwherein[BX] represents the acyl group of bleomycinic acid whose formula differs from that of bleomycin acid by the removal of the hydroxyl group from the carboxyl group of said acid;A represents a group of the general formula ##STR1## wherein R.sub.1 is a lower alkyl or benzyl,R.sub.2 is a lower alkyl or benzyl,R is a lower alkylene, andn is 0 or 1; andB represents a group of the formula ##STR2## wherein (i) R.sub.3 is hydrogen and R.sub.4 is(a) benzyl substituted by one or more halogen atoms, provided that the benzyl is substituted by two halogen atoms when R.sub.

Abstract: An aminopropylaminobleomycin represented by the following formula or a salt thereof, which is minimized in side effects such as pulmonary toxicity:[BX]--NH--(CH.sub.2).sub.3 --A--(CH.sub.2).sub.3 --Bwherein[BX] represents the acyl group of bleomycinic acid whose formula differs from that of bleomycin acid by the removal of the hydroxyl group from the carboxyl group of said acid;A represents a group of the general formula ##STR1## wherein R.sub.1 is a lower alkyl or benzyl,R.sub.2 is a lower alkyl or benzyl,R is a lower alkylene, andn is 0 or 1; andB represents a group of the formula ##STR2## wherein (i) R.sub.3 is hydrogen and R.sub.4 is(a) benzyl substituted by one or more halogen atoms, provided that the benzyl is substituted by two halogen atoms when R.sub.

Abstract: A promising carcinostatic (amido)N-substituted bleomycin represented by the following formula, or a salt thereof and a process for the preparation thereof: ##STR1## wherein BM represents a moiety of bleomycin skeleton; X represents an alkyl of 1 to 18 carbon atoms, an aminoalkyl of 1 to 12 carbon atoms, a lower alkyl having a halogen, phenyl indolyl, 5- or 6-membered heterocyclic group, or (lower)alkylamino (the alkyl group may have a substituent group) as a substituent, naphthyl, thiazolyl, or N-phenyl(lower)alkylpiperazinyl; and R represents a terminal amino residue of the bleomycin.