[Biological abilities and identification of the polyene antifungal antibiotic, perspective for protection from fungi biodeterioration].

The producer of the antifungal polyene antibiotic, aimed to protect against fungial biodeterioration, has been isolated from the soil due to a target search. Based on the morphological, cultural, and biochemical abilities, the producer is related to the Streptomyces genus. It has been shown by chromatographic, spectral, physical, and chemical methods that the antibiotic synthesized by the isolated culture consists of two main components--the polyene hexaene antibiotic with a high antifungal activity and a non-polyene antibiotic with antibacterial activity. The antifungal activity of the low purified hexaene antibiotic is comparable with the antifungal activity of the well-known highly purified antibiotics--amphotericin B, clotrimazole, and itrakonazol. This antibiotic inhibits the synthesis of the biodeterioration factors in fungi, i.e., pigments and organic acids.

[Alirinomycin C--a novel macrolide antibiotic from Streptomyces felleus VIZR 8]. / Alirinomitsin C--novyi makrolidnyi antibiotik iz Streptomyces felleus VIZR 8.

The culture of Streptomyces felleus VIZP 8 producing new macrolide antibiotic alirinomycin C was isolated in the screening of new insecticide substances. Antibiotic was related to the carbomycin-cirramycin group. Physico-chemical and biological properties investigation and identification were performed in comparison with other antibiotics of the same group, described in literature.

[The cis-trans isomerization of aromatic heptaenes catalyzed by sulfur and phosphorus compounds]. / Tsis-trans-izomerizatsiia aromaticheskikh geptaenov, kataliziruemaia soedineniiami sery i fosfora.

It was shown that sulfur and phosphorus compounds (sodium thiosulfate, sodium tripolyphosphate, sodium hexametaphosphate, monosodium phosphate) catalyze cis-trans isomerization of aromatic heptaens. Preparative method of levorin isomerezation at the presence of sodium thiosulfate was elaborated. The isolated product was a fully trans-isomer.

[Organofluorine derivatives of amphotericin B: synthesis and antifungal activity]. / Ftororganicheskie poizvodnye amfoteritsina B: sintez i protivogribkovaia aktivnost'.

Reactions of amphotericin B, a polyene macrolide antibiotic, with acyl perfluorides resulted in formation of its N-perfluoroacyl derivatives. Physicochemical and medicobiological properties of the derivatives were studied. The biological study revealed that the acute toxity (LD50) of the derivatives was 2 times as low as that of the starting antibiotic. The derivatives showed high antifungal activity against a great number of the test cultures.

[Ionol phosphorus organic analogs and stabilization of levorin]. / Ispol'zovaniephosphoroorganicheskikh analogov ionola dlia stabilizatsii levorina.

Stability of levorin isolated and purified with the use of ionole phosphorus organic analogs having in their structure phosphate, phosphonate and phosphonite groups was studied. The compound having in its structure (in addition to tertiary butyl substitutes) the phosphonite group with the P-H bond increasing the compound antioxidant property was shown to have the highest stabilizing effect. The results of the study made it possible to recommend the use of the space complicated phenols with the structure fragments of the P-H bond type as antioxidants in production of levorin.

[The possibility of using the mycelial wastes from the production of antifungal antibiotics as additives to lubricating oils]. / Izuchenie vozmozhnosti ispol'zovaniia mitselial'nykh otkhodov proizvodstva protivogribkovykh antibiotikov v kachestve prisadok k smazochnym maslam.

Antiwear and antitear properties of mycelial waste from production of antifungal antibiotics i.e. levorin, nystatin, mycoheptin, amphotericin B and griseofulvin were studied. It was shown that the waste mycelium from griseofulvin production had the best antiwear and antitear characteristics due to a higher percentage of phosphorus and sulphur in it as compared to the mycelial waste from production of the other antibiotics.

[Fungicidal activity of imbricin and its salts]. / Fungitsidnaia aktivnost' imbritsina i ego solei.

The fungicidal activity of imbricin and its salts against fungal phytopathogens was studied. The biological tests revealed that the compounds had a fungicidal activity and inhibited the development of a number of plant diseases. Imbricin showed a marked fungicidal activity when used as a disinfectant of wheat seeds and in the control of root rot of cucumbers. It was demonstrated that imbricin and its salts had the growth regulating activity in plant cell culture.

[A new metabolite with fungistatic and bacteriostatic activity, produced by strain L-30 of Flavobacterium sp]. / Novyi metabolit s fungistaticheskoi i bakteriostaticheskoi aktivnost'iu, produtsiruemyi shtammom L-30 Flavobacterium sp.

Flavocin, an agent with fungistatic and bacteriostatic activities, was isolated from the culture of Flavobacterium sp. L-30. The data on the physico-chemical and biological properties of flavocin A, the major active component, are presented. The component was identified with metabolites of the genus Flavobacterium and other genera of nonsporulating bacteria. Flavocin was highly efficient in the treatment of various farm crops. The antagonistic effect of flavocin was observed under field conditions in growing sugar beet, barley, spring wheat, potato and grape. Presowing and nonradical exposure to flavocin lowered the affection of the plants with brown patch, scab, soft rot and oidium.

[Stabilization of roseofungin by antioxidants]. / Stabilizatsiia rozeofungina antioksidantami.

Stabilization of roseofungin, a pentaene antibiotic, by antioxidants of different chemical structure was studied. The highest inhibitory effect was observed with the use of antioxidants X-1 (a partially hydrated oxyquinoline) and P-1 (a polyaromatic nitrogen containing compound). The results of the study correlated with the data on nystatin and levorin. The stabilizing effect markedly depended on the temperature: with increasing of the temperature the antioxidant effect decreased. The spectrophotometric study revealed that the decrease of the biological activity of the antibiotic in the presence of the antioxidants was more pronounced than the change of its structure.

[A laboratory method for sensitized isomerization of polyene macrolides]. / Laboratornyi metod sensibilizirovannoi izomerizatsii polienovykh makrolidov.

The study was aimed at the development of a laboratory procedure for isomerization of polyene macrolides in the presence of sensitizers. The reaction was performed with exposure of levorin solutions to the xenon lamp irradiation in the presence of rose bengal B as a sensitizers. It was shown that levoristatin contain in the levorin sample was not degraded under the experimental conditions. The use of a redetermined variant of the Vierordt's methods made it possible to offer a design formula for the estimation of the isolevorin content in solutions in the presence of levorin.

[Synthesis and biological activity of hydrophosphoryl derivatives of amphotericin B]. / Sintez i biologicheskaia aktivnost' gidrofosforil'nykh proizvodnykh amfoteritsina b.

Reactions of amphotericin B, a polyenic macrolide antibiotic, with aromatic aldehydes and H3PO2 resulted in formation of its new hydrophosphoryl derivatives. Physico-chemical and biological properties of the compounds were investigated. The biological studies showed that the hydrophosphoryl derivatives of amphotericin B were low toxic and had antifungal and antiviral activities.

[The characteristics of alirin B1--the basic component of a fungicidal preparation produced by the Bacillus subtilis 10-VIZR strain]. / Kharakteristika alirina B1--osnovnogo komponenta fungitsidnogo preparata, produtsiruemogo shtammom Bacills subtilis 10-VIZR.

Alirin B1, the major active component of a fungicidal complex produced by Bacillus subtilis 10-VIZR was separated. Its physico-chemical and biological properties as well as the amino acid composition were investigated. Alirin B1 was shown to differ from the polypeptide substances described in the literature. The antibiotic was classified as belonging to the bacteriocins.

[Dye-sensitized photoisomerization of polyenic macrolide antibiotics]. / Sensibilizirovannaia krasiteliami fotoizomerizatsiia polienovykh makrolidnykh antibiotikov.

Photoisomerization of levorin A2, a polyenic macrolide, sensitized by various dyes such as thiazines, acridines, xanthenes and phthalocyanines was studied. The use of the dyes made it possible to shift the isomerization process to the visible spectrum region and to increase the quantum yield to 1. The conditions of the triplet-triplet transfer of the sensitized reaction energy were investigated. By its physio-chemical and biological properties the levorin A2 isomer was identical to the levorin A2 isomer resulting from the direct action on the heptaene chromophore. The dye efficiency was demonstrated in regard to other heptaene antibiotics such as trichomycin and candicidin.

[Component composition of the pentaene antibiotic roseofungin]. / Komponentnyi sostav pentaenovogo antibiotika rozeofungina.

The component composition of the pentaene antibiotic roseofungin was studied by the phase reversal high performance liquid chromatography in the Millichrom apparatus. A 62 x 2 mm column filled with the Separon 5 C18 sorbent was employed. The composition of the mobile phase was determined experimentally by testing various solvent mixtures (methanol-water, methanol-acetate buffer, 0.05 M, pH 4.7, acetonitrile acetate buffer) with different contents of the organic solvent under conditions of isocratic and gradient elution. The optimal separation of the complex was achieved with the use of the mixture of acetonitrile and acetate buffer (45:55) as the mobile phase. Roseofungin was detected at 360 nm. The assay of the roseofungin experimental lots showed that roseofungin mainly contained three components with identical UV spectra. Their contents ranged within 8-17, 45-57 and 25-30 per cent respectively. Some of the samples additionally contained minor components whose quantity did not exceed 20 per cent.

[Askostatin--a fungicide from Streptomyces viridovulgaris]. / Askostatin--fungitsid iz Streptomyces viridovulgaris.

Askostatin is a fungicide isolated from the culture of Streptomyces viridovulgaris. It was separated by the countercurrent distribution procedure into components A and B. By the mass and NMR spectra and the biological findings the components were identified with cycloheximide and isocycloheximide respectively.

[Aleicid, a new natural insecticide isolated from a culture of Streptomyces aurantuacus. Component composition, physicochemical and biological properties of the aleicid major components]. / Aleitsid, novyi prirodnyi insektitsid, vydelennyi iz kultury Streptomyces aurantuacus. Komponentnyi sostav. Fiziko-khimicheskie i biologicheskie svoistva osnovnykh komponentov aleitsida.

The component composition of aleicid, a complex product with insecticidal activity was studied. It was shown by TLC and HPLC that aleicid is a complex of components two of which are basic. The major components of aleicid were identified with pyericidines of groups B and C.

[The component composition of a new natural insecticide isolated from a Streptomyces lipmani culture]. / Komponentnyi sostav novogo prirodnogo insektitsida, vydelennogo iz kul'tury Streptomyces lipmani.

The component composition of a complex product named liocid was studied by the methods of counter-current distribution and column chromatography. The product was shown to be a multicomponent mixture containing hydrocarbons, fatty acids, phospholipids, higher tetrolides and o-phthalic ester.

[High performance liquid chromatography in studies of component composition of polyene macrolides]. / Ispol'zovanie vysokoéffektivnoi zhidkostnoi khromatografii dlia izucheniia komponentnogo sostava polienovykh makrolidov.

The published data on the use of HPLC in studies on the chemistry of polyene macrolide antibiotics are summarized and the conditions for HPLC, the use of various sorbents, the impact of the ratio of the organic solvents and buffer solutions, etc. are discussed comparatively. Several aspects of the use of HPLC are indicated i.e. the identification of polyene antibiotics (heptaenes, pentaenes and hexaenes), the standardization and investigation of the antibiotic homogeneity and quality, the purification of the antibiotics and the determination of the amphotericin B content in tissues and plasma.

[Determination of nystatin component composition using HPLC and TLC with densitometry]. / Opredelenie komponentnogo sostava nistatina metodami VEZhKh i TSKh s ispol'zovaniem densitometrii.

The component composition of nystatin produced by an improved strain of Streptomyces noursei was determined by HPLC on Milichrom chromatograph (USSR). It was shown that the antibiotic consisted of nystatins A1, A2, A3 and B and admixture substances. The data appeared to be in good agreement with the results of the complex TLC investigation, by using densitometry. The component composition of the samples was evidenced by SIEAP mass spectrometry. Physiochemical and biological characteristics of separate components are presented.