[Irumamicin Produced by Streptomyces roseoflavus INA-1278].

The strain Streptomyces roseoflavus INA-1278 is described as a new irumamicin producer. Irumamicin 1278 is different by the antifungal activity from irumamicin produced by the world-known strain Streptomyces subflavus subsp. Irumaensis subps. nov. AM-3603.

[Characteristics and identification of bacteriocins produced by Lactococcus lactis subsp. lactis 194-K].

The Lactococcus lactis subsp. lactis 194-K strain has been established to be able to produce two bacteriocins, one of which was identified as the known lantibiotic nisin A, and the other 194-D bacteriocin represents a polypeptide with a 2589-Da molecular mass and comprises 20 amino acid residues. Both bacteriocins were produced in varying proportions in all of the studied nutrient media, which support the growth of the producer. Depending on the cultivation medium, the nisin A content was 380- to 1123-fold lower in the 194-K stain culture fluid than that of the 194-D peptide. In comparision to to nisin A Bacteriocin 194-D possessed a wide range of antibacterial activity and suppressed the growth of both Gram-positive and Gram-negative bacteria. An optimal medium for 194-D bacteriocin synthesis was shown to be a fermentation medium which contained yeast extract, casein hydrolysate, and potassium phosphate. The biosynthesis ofbacteriocin 194-D by the 194-K strain in these media occurred parallel to producer growth, and its maximal accumulation in the culture fluid was observed at 14-20 h of the strain's growth.

[The structure of antibiotic eremomycin B].

A new biologically active component, antibiotic eremomycin B, was isolated from the culture liquid of Amycolatopsis orientalis subsp. eremomycini, the producing strain for antibiotic eremomycin. Its structure was established by NMR spectroscopy and mass spectrometry. Eremomycin B was shown to differ from eremomycin by the presence of an N-carboxymethyl substituent in the disaccharide eremosamine fragment.

[Antibiotics produced by Photorhabdus luminescens ZMI, a symbiont of entomopathogenic nematodes].

A novel strain of Photorhabdus luminescens ZMI isolated from nematode larvae Heterorhabditis sp. was shown to produce antibiotic complexes with antibacterial and antifungal activities. The antibiotic complexes secreted extracellularly and intracellularly were separated into individual components. Comparison of their properties with the databases for biologically active compounds suggested that component A was identical to 3,5-dihydroxy-4-isopropylstilbene, components B and H belonged to anthraquinone derivatives, component C secreted only extracellularly was likely a novel antibiotic.

[Isolation and study of antibiotic INA-1132 (chlorothricin), produced by actinomycete strain].

Taxonomic properties of strain INA-1132 producing antibiotic INA-1132 are described. The antibiotic showed activity against grampositive bacteria and fungi. The strain was classified as belonging to the genus Streptomyces and by its taxomic characteristics is most close to S. baarnensis. The experiments with the bacterial culture Halobacterium salinarum (previously H. halobium) revealed hypolipidemic activity of the antibiotic, i. e. its ability to inhibit biosynthesis of sterols. Conditions for the production of the antibiotic, methods of its isolation and purification, as well as the results of the chemical structure elucidation are described. By its physicochemical properties the antibiotic is identical to chlorothricin. The structure of antibiotic INA-1132 was ascertained by X-ray analysis. Conformation of the molecule of chlorothricin (antibiotic 1132) was determined for the first time.

[A comparison of the properties of bacteriocins formed by Lactococcus lactis subsp. lactis strains of diverse origin].

Bacteriocins formed by four strains of Lactococcus lactis subsp. lactis have been studied and compared: 729 (a natural strain isolated from milk), 1605 (a mutant of strain 729), F-116 (a recombinant obtained by fusing of protoplasts of the two related strain 729 and 1605), and a nisin-forming strain obtained by adaptive selection at Moscow State University. Antimicrobial activity studies revealed differences between the strains in the effects on individual groups of microorganisms; the activities of the strains were also distinct from that of Nisaplin (a commercial preparation of the bacteriocin nisin). Methods for isolation and purification of bacteriocins have been developed, making it possible to obtain individual components of antibiotic complexes as chromatographically pure preparations. Bacteriocins formed by the strains of Lactococcus lactis subsp. lactis have been identified and differences in their biological and physicochemical properties, established. A novel potent broad-spectrum antibiotic substance distinct from nisin has been isolated from the recombinant strain F-116.

New chiral stationary phase with macrocyclic glycopeptide antibiotic eremomycin chemically bonded to silica.

A new chiral stationary phase (CSP) was prepared by attachment of macrocyclic glycopeptide antibiotic eremomycin to the epoxy-activated silica under mild conditions. In contrast to CSP with immobilized vancomycin, which is a close structural analogue of eremomycin, the prepared CSP reveals high enantioselectivity for separation of amino acids enantiomers. It was demonstrated by the example of ristocetin A CSP that method of the immobilization of macrocyclic glycopeptide antibiotics affects remarkably the resulting enantioselectivity.

[Echinomycin production by Actinomadura sp. INA 654].

An actinomycete strain designated as Actinomadura sp. INA 654 was isolated from a chernozem soil sample in the Voronezh Region by the soil sample treatment with millimetric waves (EHF band). The strain produced an antibiotic complex of 2 components, named A-654-I and A-654-II. Investigation of their physico-chemical properties showed that A-654-I was identical to echinomycin, a heteropeptide lactone of the quinoxaline group with antitumor activity, while A-654-II proved to be likely a new natural compound. Production of echinomycin by a representative of the Actinomadura genus was detected for the first time. Up to now, only representatives of the Streptomyces genus were known to produce echinomycin.

[Antibiotic properties of the strains of the basidiomycete Lentinus edodes (Berk.) sing].

Antibiotic properties of the extracts from the fermentation broth and mycelium of 15 strains of the edible and medicinal basidiomycete L. edodes were studied and it was shown that the extracts were active against grampositive and gramnegative bacteria, yeasts and mycelial fungi, including dermatophytes and phytopathogens. The strains differed by the set of the organisms susceptible to the action of the extracts. Strains of L. edodes combining marked antibiotic properties and high yields of water soluble polysaccharides were screened. The active compounds were detected by preparative TLC. Two of them were identified with UV- and mass spectrometry as lentinamycin B and erytadenine (lentinacin). Lentinamycin B was found to be the main component responsible for the antibiotic activity of the L. edodes strains.

[Screening of microbial secondary metabolites inhibiting cholesterol biosynthesis with the use of hepatoblastoma G2]. / Otbor mikrobnykh vtorichnykh matabolitov--ingibitorov biosinteza kholesterina s pomozh'iu kul'tury kletok gepatoblastomy G2.

The culture of hepatoblastoma G2 (Hep G2) cells is proposed as an effective model for screening of microbial metabolites--inhibitors of sterol biosynthesis. This model can be applied at early stages of screening procedures and is quite effective for testing of crude extracts of producers' culture broth. The test is based on measurement inhibition of the radiolabelled precursors incorporation in cholesterol and separate fractions of lipids by microbial metabolites in Hep G2 cells. That allows not only to reveal inhibitors of cholesterol biosynthesis, but also to evaluate mechanism of action, including ability to inhibit the synthesis of cholesterol ethers. The cholesterol biosynthesis inhibition was tested at 150 microbial cultures (actinomycetes and imperfect fungi), isolated from soil. The ability to inhibit 14C-acetate incorporation into cholesterol was found in 15-20% of microbial cultures possessing antifungal activity of extracts (culture broth and mycelium).

[An antibiotic complex produced by Streptomyces werraensis 1365T strain]. / Antibioticheskii kompleks, obrazuemyi shtammom Streptomyces werraensis 1365 T.

An antibiotic complex comprising four components (A, B, C, and X) was extracted from a native solution and mycelium of Streptomyces werraensis 1365T. The components were purified by column and thin-layer (TLC) chromatographic procedures to study their physicochemical and biological properties. The results were used to identify the substances isolated. The preliminary data allowed us to identify the components X, A, and B as the previously described compounds undecylprodigiosin, anisomycin, and copiamycin, respectively, whereas component C is a natural compound, which probably has never been described.

[Development of a new method for preparing biologically active compounds based on the typed strain Streptomyces werraensis]. / Razrabotka novogo metoda polucheniia biologicheski aktivnykh soedinenii na osnove tipovogo shtamma Streptomyces werraensis.

The regulatory function of a DNA fragment responsible for actinomycin resistance in the typed strain Streptomyces werraensis ATCC 1365, which produces a macrotetrolide antibiotic, was studied. Metabolic changes made this strain capable of producing an antibiotic complex, which comprises four biologically active compounds absent from the parent culture.

[Isolation and identification of antibiotics produced by Actinoplanes brasiliensis INA 3802]. / Vydelenie i identifikatsiia antibiotikov, produtsiruemykh shtammom Actinoplanes brasiliensis INA 3802.

In the screening programme for new antibiotics produced by Actinoplanes brasiliensis an antibiotic complex A-3802 was isolated and studied in detail. It had a marked therapeutic effect in the treatment of staphylococcal sepsis in albino mice and was low toxic. Two components of the complex i.e. A-3802-IV-3 and A-3802-IV-4 were identified with the lantibiotics actagardin and its diamide disulfoxide. Antibiotics A-3802-V-4 and A-3802-VI-7 were shown to be new antibiotics of the same group.

[A conjugate of ristomycin A ristosaminylaglycon-polymyxin B: the spectrum of its antimicrobial action and its membranolytic activity]. / Kon''iugat ristozaminilaglikon ristomitsina A--polimiksin B: spektr antimikrobnogo deistviia i membranoliticheskaia aktivnost'.

Antimicrobial activity of a conjugate based on two antibiotics, i.e. ristomycin A and polymyxin B was studied. The conjugate was shown to have a broad antimicrobial spectrum. In concentrations of 5 to 30 micrograms/ml it inhibited the growth of gram-positive and gram-negative bacteria and in concentrations of 5 to 40 micrograms/ml it inhibited the growth of the pathogenic clinical strains. An insignificant membranolytic action of the conjugate with respect to membranes of the susceptible bacteria and no hemolytic action on human red blood cells were detected.

[Rubomycin Q1--an anthracycline metabolite from Streptomyces coeruleorubidus 2679, a strain producing rubomycin C]. / Rubomitsin Q1--antratsiklinovyi metabolit iz rubomitsin c-produtsiruiushchego shtamma Streptomyces coeruleorubidus 2679.

In the programme of screening of biologically active secondary metabolites produced by Streptomyces coeruleorubidus 2679 a new reddish-violet component (rubomycin Q1) with antibacterial and cytotoxic activity was isolated from the culture fluid of the organism. Some physico-chemical and biological properties of a chromatographically pure rubomycin Q1 were investigated. It was shown with the use of 1H NMR, UV, IR and mass spectrometry that rubomycin Q1 was an anthracycline antibiotic (9,10-anhydro-13-desoxycarminomycin).

[Induction of antibiotic formation by inactive cultures of actinomycetes. A mutant strain of Streptomyces helvaticus, a new producer of bruneomycin]. / Induktsiia obrazovaniia antibiotikov neaktivnymi kul'turami aktinomitsetov. Mutantnyi shtamm Streptomyces helvaticus-- novyi produtsent bruneomitsina.

After exposure of an inactive actinomycete to ethidium bromide a stable mutant producing an antibiotic on a solid medium was isolated. The exposure to methylnitrosoguanidine provided the isolation of a more productive variant synthesizing the antibiotic in a liquid medium. By UV, IR, NMR and mass spectroscopy the antibiotic was identified as bruneomycin (streptonigrin). The taxonomic investigation of the culture showed that it belongs to Streptomyces helvaticus which is a new culture producing bruneomycin (streptonigrin). Previously it did not synthesize the antibiotic.

Structure of microcin C51, a new antibiotic with a broad spectrum of activity.

The structure of microcin C51, a new antibiotic produced by E. coli, has been determined. This antibiotic was shown to be a 1.18 kDa nucleotide peptide. It consists of a heptapeptide with formylmethionine as the N-terminus and a C-terminal asparagine linked with nebularin-5'-monophosphate through the three-methylene bridge. The OH-group of threonine is substituted. The peptide chain of microcin C51 synthesized on ribosomes is the longest among the known biologically active nucleotide peptides.