Abstract: A process for preparing 2,6-diaminopurine-2′-deoxyriboside and 2′-deoxyguanosine. These compounds may be used as materials for pharmaceuticals, such as antiviral agents and the like, and particularly as starting materials for antisense oligonucleotides.

Abstract: A process for producing riboflavin glucoside comprises cultivating a microorganism belonging to the genus Bacillus, such as Bacillus brevis, Bacillus cereus, Bacillus circulans, Bacillus coagulans, Bacillus licheniformis, Bacillus megaterium, Bacillus pumilus or Bacillus subtilis, which is capable of producing riboflavin glucosides, in an aqueous medium containing a starch under aerobic conditions. Amongst the preferred strains are Bacillus subtilis RB50::[pRF69]60Ade+ and Bacillus subtilis RB50::[pRF69]60[pRF93]120Ade+. The so-produced riboflavin glucoside can be used as a more soluble substitute for riboflavin to prepare clear drinks and injection solutions.

Abstract: Oligosaccharide compounds that are substrates and inhibitors of glycosyltransferase and glycosidase enzymes and compositions containing such compounds are disclosed. A method of glycosylation is also disclosed. An E. coli transformed with phagemid CMPSIL-1, which phagemid comprises a gene for a modified CMP-sialic acid synthetase enzyme, which transformed E. coli has the ATCC accession No. 68531 is also provided.

Abstract: The invention relates to a novel fermentative process for the preparation of acarbose. By monitoring and controlling the osmolality in the fermentation solution, a substantial improvement in yield from the fermentation is achieved.

Abstract: There is disclosed a process for producing a nucleoside derivative of the formula [I]: ##STR1## characterized by contacting 2',3',5'-O-triacylribonucleoside derivative of the formula [II]: ##STR2## with an ester hydrolase: (i) capable of regio-selectively deacylating the acyl group at 5'-O-position in the formula [II] above, and(ii) having an amino acid sequence encoded by a gene which hybridizes to a nucleotide sequence encoding an amino acid sequence of SEQ ID NO:1.

Abstract: The invention relates to a multifunctional nucleoside didesoxyribosyl or nucleoside deoxyribosyl transferase which has one or more of the following additional activities (desoxy) nucleoside kinase, nucleoside reductase desaminase, or DNA polymerase activity. Utilizing the multifunctional enzyme results in a variety of nucleic acid products. These products can be prepared using sequential reactions in a single batch process wherein the sequential reaction can be caused to occur by varying process conditions in a manner which turns on or off the requisite activities causing the sequential reactions to occur. An example of a product prepared in this manner is dideoxyribofuranoside triphosphate. Certain of the resultant products have pharmaceutical activities, e.g. antiviral agents. Lactobacillus leichmannii (DSM 20076) is a source of the multifunctional nucleoside deoxyribosyl transferase.

Abstract: A process for preparing a sugar nucleotide from a nucleotide by using a yeast cell, characterized in that both a nucleoside diphosphate-sugar pyrophosphorylase and a sugar 1-phosphate are present in the reaction system. According to this process, various sugar nucleotides, which have been prepared only in low productivity by the conventional yeast cell process, can be efficiently prepared.

Abstract: The present invention provides a method of preparing stably and at a high yield a purine nucleoside compound by utilizing an exchange reaction of a nucleic acid base which is carried out in the presence of an enzyme, and also provides a microorganism capable of producing uracil thymine dehydrogenase or dihydrouracil dehydrogenase. In preparing the purine nucleoside compound, a pyrimidine nucleoside compound and a purine base are subjected to a base exchange reaction in an aqueous solution containing phosphate ions in the presence of pyrimidine nucleoside phosphorylase and purine nucleoside phosphorylase. The pyrimidine base formed by the base exchange reaction is converted by a microorganism or an enzyme derived from the microorganism into a compound incapable of acting as substrates of pyrimidine nucleoside phosphorylase and purine nucleoside phosphorylase so as to obtain a desired product of purine nucleoside compound.

Abstract: The present invention relates to a process for preparing sugar nucleotides from nucleotides and sugar derivatives by the use of yeast, characterized in that the reactions are conducted at 20.degree. C. or below. According to this process, even when the preparation is conducted on an enlarged scale, a reduction in the yield of a sugar nucleotide can be inhibited by a very simple means; lowering the reaction temperature 20.degree. C. or below. Thus, the process is an extremely practical one applicable to the mass-production of sugar nucleotides.

Abstract: The present invention is drawn to methods for the synthesis of sialyl Lewis.sup.x derivatives modified at the C-2 and/or C-6 position of GlcNAc employing chemoenzymatic synthesis. The derivatives find use in the treatment and prevention of diseases.

Abstract: The present invention is drawn to methods for the synthesis of Lewis.sup.a derivatives modified at the C-2 and/or C-6 position of GlcNAc employing chemo-enzymatic synthesis. The derivatives find use in the treatment and prevention of diseases.

Abstract: The present invention relates to novel aminooligosaccharide derivative and pharmaceutically acceptable non-toxic salts thereof, which possess potent saccharide hydrolase inhibition and antibacterial activities. The invention also relates to a process for preparing the same and to pharmaceutical compositions containing the same as active ingredients. In accordance with the present invention, the inventors isolated novel aminooligosaccharide derivative from a soil microorganism categorized as Streptomyces sp., and discovered that it can be applied as potent inhibitors for saccharide hydrolases and antibacterial agents as well.

Abstract: The present invention provides compositions comprising at least one complement moiety and at least one carbohydrate moiety, and methods of producing such compositions. In particular, the compositions of the invention comprise complement proteins related to the complement receptor type I, and further comprise ligands for intracellular molecules, such as selectins. In a preferred embodiment, the compositions comprise a complement-related protein in combination with the Louis X antigen or the sialyl Lewis X antigen. The compositions of the invention have use in the diagnosis or therapy of disorders involving complement activity and inflammation. Pharmaceutical compositions are also provided for treating or reducing inflammation mediated by inappropriate complement activity and intercellular adhesion.

Abstract: The invention is directed to methods of converting high mannose type glycosylation patterns to hybrid or complex type glycosylation patterns.

Abstract: The object of this invention is to provide a biosorbent for heavy metals having polyaminosaccharide sodiumphosphate as main ingredient prepared from microbial biomass using Aspergillus, Penicillium, Trichoderma or Micrococcus genus originating from industrial fermentations and biological treatment plants.

Abstract: Oligosaccharide compounds that are substrates and inhibitors of glycosyltransferase and glycosidase enzymes and compositions containing such compounds are disclosed. A method of glycosylation is also disclosed. An E. coli transformed with phagemid CMPSIL-1, which phagemid comprises a gene for a modified CMP-sialic acid synthetase enzyme, which transformed E. coli has the ATCC accession No. 68531 is also provided.

Abstract: A method for producing uridine diphosphate N-acetylglucosamine comprising culturing osmo-tolerant yeasts in aerobic conditions in a medium having inorganic salt concentration of about 2-8%.

Abstract: Indolopyrrolocarbazole derivatives, such as, for example, 12,13-dihydro-1,11-dihydroxy-13-(.beta.-D-glucopyranosyl)-5H-indolo[2,3-a] pyrrolo[3,4-c]carbazole-5,7-(6H)-dione or 6-amino derivative thereof, are produced by glycosylating a precursor compound by cultivating with Microtetraspora sp. A34549, Saccharothrix aerocolonigenes ATCC 39243 or mutants thereof, in a nutrient medium containing the precursor compound.

Abstract: Disclosed is a method for producing saccarides of definite chain length, such as glucose, maltose, malto-oligosaccharides and isomalto-oligosaccharides with a high purity. Saccharides such as starch, dextran and cellulose, and hydrolyzates thereof, are subjected to modification of the anomeric carbon at the reducing end of the molecule without modification of the non-reducing end of the molecule. The modification may be oxidation, for example by bromine to produce a carboxylic acid at the anomeric carbon, or amination, for example by phenylhydrazine to produce an osazone or osone of the saccharide. After modification, the modified saccharide can be adsorbed on an ion exchange resin and then repeatedly cleaved with a suitable enzyme, such as .beta.-amylase, to produce the desired saccharide of definite chain length.

Abstract: The present invention provides an efficient method for the production of ceramides and hybrid ceramides via the selective N-acylation of glycosphingolipids by reacting an organic acid or ester thereof with a lysosphingolipid in the presence of a lipase in an organic medium.

Abstract: A compound of formula (VIII) ##STR1## is added to a culture media containing Microtetraspora sp. A34549 or Saccharothrix aerocolonigenes ATCC 39243.

Abstract: A process for irreversible regio- and stereoselective enzyme catalyzed acylation of alcohols using enol esters as acylating reagents is disclosed. The present invention permits the selective modification of hydroxyl group(s) of chiral and meso alcohols, including sugars, organometallics, and glycosides. The enol freed upon transesterification rapidly tautomerizes to the corresponding volatile aldehyde or ketone thereby preventing the reverse reaction from occurring.

Abstract: There are provided a novel .alpha.2.fwdarw.3 sialyltransferase expressed by a cloned gene from animal cells, a cDNA encoding the .alpha.2.fwdarw.3 sialyltransferase, a method for detecting or suppressing the expression of an .alpha.2.fwdarw.3 sialyltransferase by use of said cDNA, a recombinant vector containing said cDNA, a cell containing said vector, and their production processes.

Abstract: Addition of certain tryptophan analogs to the culture medium during fermentation of a rebeccamycin-producing strain of Saccharothrix aerocolonigenes results in production of new rebeccamycin analogs having advantageous antitumor properties.

Abstract: Anhydrous crystals of 4-carbamoyl-1-.beta.-D-ribofuranosyl imidazolium-5-olate are disclosed. The crystals possess (1) water content of 0.5% by weight or less (the Karl Fisher method), and (2) specific IR spectrum absorption peaks in the neighborhoods of 3580, 1852, 1630, 1575, and 1554 cm.sup.-1. They are stable against heat and high humidity conditions and can easily be manufactured by using ethanol. The compound has superior immuno-suppressing activity and is thus made into preparations for oral administration.

Abstract: A method for the hydrolysis of only the lacto-N-biosidic (Gal.beta.1-3GlcNAc.beta.1-) linkages at the non-reducing termini of sugar compounds, characterized by the use of glycosidase that is specific for only the lacto-N-biosidic linkage in said sugar compounds. And disclosed is a reagent for use in hydrolysis of only the lacto-N-biosidic linkage at the non-reducing termini of sugar compounds.

Abstract: There are provided a novel .alpha.2.fwdarw.3 sialyltransferase expressed by a cloned gene from animal cells, a cDNA encoding the .alpha.2.fwdarw.3 sialyltransferase, a method for detecting or suppressing the expression of an .alpha.2.fwdarw.3 sialyltransferase by use of said cDNA, a recombinant vector containing said cDNA, a cell containing said vector, and their production processes.

Abstract: A new antitumor antibiotic designated BMY-41219 is produced by fermentation of Saccharothrix aerocolonigenes ATCC 39243. The BMY-41219 antibiotic exhibits antitumor activity.

Abstract: An antitumor antibiotic designated BMY-41219 is produced by fermentation of Saccharothrix aerocolonigenes ATCC 39243. The BMY-41219 antibiotic exhibits antitumor activity.

Abstract: A method for modifying eukaryotic and prokaryotic proteins to extend their in vivo circulatory lifetimes. In the preferred embodiment, enzymatic and/or chemical treatments are used to produce a modified protein carrying one or more covalently attached trisaccharide, sialic acid.fwdarw.galactose.fwdarw.N-acetylglucosamine.fwdarw.(SA.fwdarw.Gal.fwd arw.GlcNAc.fwdarw.), or tetrasaccharide (SA.fwdarw.Gal.fwdarw.GlcNAc.fwdarw.GlcNAc.fwdarw.) moieties. The method can be applied to any natural or recombinant protein possessing asparagine-linked oligosaccharides or to any non-glycosylated protein that can be chemically or enzymatically derivatized with the appropriate carbohydrate units. Following injection into an animal, the modified glycoproteins are protected from premature clearance by cells of the liver and reticulo-endothelial system which recognize and rapidly internalize circulating glycoproteins with carbohydrate chains containing terminal Gal, GlcNAc, fucose or mannose residues.

Abstract: The invention relates to a process for the enzymatic synthesis of 2-deoxy-.beta.-D-galactosides. The enzyme galactosyltransferase is able to catalyze the transfer of 2-deoxygalactose residues from the donor substrate uridine 5'-diphospho-2-deoxy-D-galactose to N-acetylglucosamine or aspartyl-N-acetylglucosamine or, in the presence of lactose, to terminal glucose.

Abstract: Chitin-containing material is heat-treated in organic solvent or in the solvent with water, and then .beta.-1, 4 glycoside decomposing enzyme is added for decomposing the chitin-containing material by enzyme reaction. Or, chitin-containing material is ultrasonicated in organic solvent or in the solvent with water, and then chitin-containing material is decomposed by enzyme reaction of .beta.-1, 4 glycoside decomposing enzyme. Further, chitin-containing material is exposed in the solution containing urea and/or surfactant, and then chitin-containing material is let co-exist with .beta.-1, 4 glycoside decomposing enzyme under the presence or non-presence of urea and/or surfactant for decomposing chitin-containing material. Or, at the time of exposing chitin-containing material in the solution containing urea and/or surfactant, the solution is heated and the .beta.-1, 4 glycoside decomposing enzyme is added for decomposing chitin-containing material.

Abstract: Fermentation of the microorganism Streptomyces sp. MA6751 (ATCC No. 55043) in the presence of the Angiotensin II (A II) receptor antagonist ##STR1## yields an N2-glucuronide analog which is also an A II antagonist useful in the treatment of hypertension and congestive heart failure and other indications known to respond to A II antagonists.

Abstract: A method of purifying ferment-produced riboflavin, wherein the impure riboflavin is suspended in water or dilute aqueous acid, and the suspension is heated at a temperature of from 75.degree. to 130.degree. C. for from 0.3 to 3 hours with stirring, during which time crystal transformation takes place, after which the mixture is cooled and the purified product is isolated in known manner.

Abstract: A process is described which uses a "cold" gas shock to accelerate microprojectiles wherein particles are presented to the gas shock on a planar surface perpendicular to the plane of expansion of the gas shock wave. Several different apparatus capable of accomplishing this method are described.

Abstract: Antibacterially active compositions are prepared from a proteolytic enzymatic digestate of glycopeptides obtained from a protein isolate enriched with soya glycoprotein 7S or with bean glycoprotein II. The glycopeptide digestate is treated with endo-.beta.-N-acetylglucosaminidase H to obtain oligosaccharide compositions which then also may be treated with exo-.alpha.-mannosidase to obtain further oligosaccharide compositions.

Abstract: The present invention relates to an improved process for the preparation of 1-desoxynojirimycin. 1-Desoxynojirimycin can be reacted by alkylation on the nitrogen atom to give various saccharase inhibitors which are used therapeutically in the treatment of diabetes mellitus.

Abstract: This invention provides a process for producing 3'-deoxy-'-fluorothymidine, which comprises allowing 3'-deoxy-'-fluoro-5'-mesylthymidine (the stating material) to react with an acetylating agent, selected from the group consisting of alkali metal salts of acetic acid, amine salts of acetic acid and ammonium acetate, in an aprotic, ploar solvent to form the 5'-acetyl derivative, and ammonium acetate, in an aprotic, polar solvent to form the 5'-acetyl derivative, and eliminating the 5'-acetyl group from this intermediate, thereby giving the objective 3'-deoxy-'-fluorothymidine.According to the process of this invention described above, the 5'-mesyl derivative can be efficiently acetylated, and 3'-deoxy-'-fluorotymidine can be obtained in a high yield.

Abstract: Addition of bromine to the culture medium during fermentation of a rebeccamycin-producing strain of Saccharothrix aerocolonigenes results in production of a new rebeccamycin derivative having advantageous antineoplastic properties.

Abstract: An enzyme preparation is obtained containing a nuclease that is produced by a fungus such as Trichoderma, Aspergillus and Fusarium and which remains active even after heating at 100.degree. C. for 30 minutes. This enzyme preparation may be effectively used when it is necessary to decompose nucleic acids at elevated temperature over a prolonged period.

Abstract: A process for the fermentative production of the deoxyribonucleoside thymidine and/or its corresponding base thymine by aerobically cultivating a strain of the genus Brevibacterium, in particular one of the strains NCIMB 40117 and 40116. The produced thymidine may be used as an intermediate in the production of azidothymidine and active ingredient in a composition for use in the treatment of auto imune deficiency syndrome (AIDS). Biologically pure cultures of strain NCIMB 40014 and variants and mutants derived therefrom are claimed per se.

Abstract: Salbostatin, a compound of the formula I ##STR1## acts as a glycosidase inhibitor and is suitable for use in pharmacy and in plant protection.

Abstract: Fermentation of the microorganism Streptomyces sp. MA6751 (ATCC No. 55043) in the presence of the Angiotensin II (A II) receptor antagonist ##STR1## yields an N2-tetrazole .beta.-glucuronide analog which is also an A II antagonist useful in the treatment of hypertension and congestive heart failure and other indications known to respond to A II antagonists.

Abstract: A process for obtaining N-acetylneuraminic acid from N-acetylglucosamine is disclosed. The process is carried out in a reactor which contains both N-acylglucosamine-2-epimerase (E.C. 5.1.3.8) which isomerizes GlcNAc into ManNAc, and N-acetylneuraminic acid pyruvate lyase (E.C. 4.1.3.3) which catalyzes the reaction of the resulting ManNAc with pyruvic acid to give Neu5Ac. GlcNAc and Pyr are fed into the reactor and Neu5Ac is obtained in the outflow. The process is preferably carried out continuously and in particular in an enzyme membrane reactor at pH 7.5 and 25.degree. C., especially using residence times of 0.2 to 10 h, and with an excess of GlcNAc in comparison with Pyr which is subsequently added if necessary. Epimerase and lyase are preferably present in the reactor in a ratio of activities which is equivalent to the reciprocal value of the quotient of the conversion rates.

Abstract: This invention relates to novel proteins useful for enhancing pulmonary surfactant activity, methods and materials for obtaining said proteins and compositions containing one or more of the proteins.

Abstract: The invention relates to a process for the conversion of corrinoids produced by microorganisms into cyanocorrinoids by reaction with cyanides. According to the invention a fermentation broth obtained by disruption of microorganism cells in a known manner, preferably by heat treatment in the presence or absence of sulfite ions, optionally after purification steps known per se, is contacted with a suitable adsorbent or ion exchange resin, the corrinoids adsorbed on the surface of the adsorbent or ion exchange resin are treated with an aqueous solution containing cyanide ions or a compound capable of supplying cyanide ions, in an amount providing cyanide ions in a 1.1 to 2.0-fold molar excess related to the corrinoids, the adsorbent or ion exchange resin is washed with water, and the cyanocorrinoids obtained is eluted in a known manner, preferably with aqueous ethanol.

Abstract: A new antitumor antibiotic designated BMY-41950 is produced by fermentation of Streptomyces staurosporeus ATCC 55006 or Streptomyces hygroscopicus ATCC 53730. The BMY-41950 antibiotic exhibits both antimicrobial and antitumor activities.

Abstract: The present invention relates to methods for producing ribavirin utilizing microorganisms and a method for producing ribose-1-phosphoric acid which is a precursor of ribavirin. The methods involve contacting certain microorganisms with orotidine, orotidic acid, or salts thereof, and inorganic phosphoric acid or a salt thereof (to produce ribose-1-phosphoric acid), and further with 1,2,4-triazole-3-carboxamide or a salt thereof (to produce ribavirin) in an aqueous solvent.

Abstract: A method of controlling the regioselectivity of the glycosidic bond between glycosyl donor and glycosyl acceptor in the enzymatic production of an oligosaccharide compound which either consists of or is a fragment or an analog of the cabohydrate part in a glycoconjugate, by reverse hydrolysis or transglycosidation reactions, is described. The synthesis is carried out in that a donor substance which is a mono- or oligosaccharide or a glycoside thereof, is caused to react, in the presence of a glycosidase, with an acceptor substance which is an O-, N-, C- or S-glycoside consisting of a monosaccharide, oligosaccharide or a saccharide analog and at least one aglycon which is O-, N-, C- or S-glycosidically bonded in 1-position, the .alpha. or .beta.-configuration being selected on the glycoside bond between the glycosyl group and the aglycon in the acceptor substance, and the oligosaccharide compound being separated from the reaction mixture.

Abstract: There is herein described an invention for promoting the rate and improving the quality of wound healing by topically applying insulin-like growth factor-II to the wound.