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STUDIES ON ANTIBIOTICS FROM THE GENUS BACILLUS. XX
JUN'ICHI SHOJI, HIROSHI HINOO, YOSHIHARU WAKISAKA, KENZO KOIZUMI, MIKA ...
1977 Volume 30 Issue 12 Pages
1029-1034
Published: 1977
Released on J-STAGE: April 12, 2006
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Two new members of polymyxin group antibiotics, polymyxins S
1 and T
1, were isolated from the culture broths of strains identified as
Bacillus polymyxa Rs-6 and
Bacillus polymyxa E-12, respectively. These antibiotics are strongly basic substances, their hydrochloric acid salts are soluble in water and methanol. They are primarily active against Gram-negative bacteria
in vitro and
in vivo though polymyxin T
1 exhibits higher activities against Gram-positive bacteria than other polymyxin group antibiotics.
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STUDIES ON ANTIBIOTICS FROM THE GENUS BACILLUS. XXI
JUN'ICHI SHOJI, TOSHIYUKI KATO, IIIROSHI HINOO
1977 Volume 30 Issue 12 Pages
1035-1041
Published: 1977
Released on J-STAGE: April 12, 2006
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Amino acid analysis on the acid hydrolyzate of polymyxin S
1 revealed its amino acid composition. Isolation of the constituent amino acids and measurement of their optical activities clarified their chiralities: Dab(5L), Thr(3L), Ser(1D) and Phe(1D). The constituent fatty acid was identified with anteisononanoic acid by gas chromatography and mass spectrometry. By the action of polymyxin acylase, deacyl polymyxin S was obtained. Successive EDMAN degradation reaction on deacyl polymyxin S revealed the amino acid sequence. Further evidence for the structure of polymyxin S
1 was obtained by partial acid hydrolysis on tetra-(DNP)-polymyxin S
1.
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STUDIES ON ANTIBIOTICS FROM THE GENUS BACILLUS. XXII
JUN'ICHI SHOJI, TOSHIYUKI KATO, HIROSHI HINOO
1977 Volume 30 Issue 12 Pages
1042-1048
Published: 1977
Released on J-STAGE: April 12, 2006
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Amino acid analysis of the acid hydrolyzate of polymyxin T
1, revealed the amino acid composition. Isolation of the constituent amino acids and measurement of their optical activities clarified their chiralities. These were 2, 4-diaminobutyric acid (6L), Thr(1L), Leu(2L) and Phe(1D). The constituent fatty acid was identified as anteisononanoic acid by gas chromatography and mass spectrometry. Deacylation with polymyxin acylase afforded deacyl polymyxin T. Successive EDMAN degradation on deacyl polymyxin T revealed most of its amino acid sequence. The chemical cleavage reaction for fragmentation of threonyl peptide on penta(DNP)-polymyxin T
1 cleaved it at the C-terminal side of the Thr residue to afford a DNP-octapeptide, whose sequence was clarified by EDMAN degradation. Thus, the structure of polymyxin T
1 was determined.
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I. TAXONOMY OF PRODUCING ORGANISM AND FERMENTATION AND ISOLATION OF PHOLIPOMYCIN
MAMORU ARAI, AKIO TORIKATA, RYUZO ENOKITA, HISAYOSHI FUKATSU, RUMI NAK ...
1977 Volume 30 Issue 12 Pages
1049-1054
Published: 1977
Released on J-STAGE: April 12, 2006
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Pholipomycin is a new member of the phosphoglycolipid family of antibiotics. Taxonomic studies of the producing organism revealed that it has morphologically characteristic aerial mycelia in which two to three spores are borne usually on short and clavate side branches. The species name,
Streptomyces lividoclavatus, has been proposed. Pholipomycin is produced mainly in the solid residue of the fermentation culture broth and is isolated by methanol extraction of the mycelial cake followed by purification on ion-exchange resin and silica gel chromatography.
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II. PHYSICO-CHEMICAL PROPERTIES AND COMPARISON WITH OTHER MEMBERS OF THIS FAMILY OF ANTIBIOTICS
MAMORU ARAI, RUMI NAKAYAMA, KAYOKO YOSHIDA, MICHIKO TAKEUCHI, SUSUMU T ...
1977 Volume 30 Issue 12 Pages
1055-1059
Published: 1977
Released on J-STAGE: April 12, 2006
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Physico-chemical characterization of pholipomycin revealed that this antibiotic is a new member of phosphoglycolipid antibiotics. Pholipomycin was differentiated from other members by the products formed on acid hydrolysis as follows: the presence of glucosamine, a 257nm chromophore and moenocinol-type C
25 lipids, but the absence of glucose, 6-deoxyglucosamine and glycine.
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III. BIOLOGICAL PROPERTIES
AKIO TORIKATA, HIROJI YOSHIKAWA, TOSHIAKI KATAYAMA, MAMORU ARAI, MASAK ...
1977 Volume 30 Issue 12 Pages
1060-1063
Published: 1977
Released on J-STAGE: April 12, 2006
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Pholipomycin, a new member of the phosphoglycolipid antibiotics, was primarily active against gram-positive bacteria including clinically isolated resistant bacteria. It differed from other members of the antibiotic family as it also demonstrated activity against gram-negative bacteria. Pholipomycin protected mice from infection with
Staphylococcus aureus and was nontoxic to mice having an LD
50 (i.v.) of 600mg/kg. Besides possessing antimicrobiol activity, pholipomycin, when administered orally, appeared to promote growth in chickens and pigs.
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MITSUYOSHI YAMAMOTO, RYO OKACHI, ISAO KAWAMOTO, TAKASHI NARA
1977 Volume 30 Issue 12 Pages
1064-1072
Published: 1977
Released on J-STAGE: April 12, 2006
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A chemically defined medium was devised in order to study the requirements for fortimicin A production by
Micromonospora olivoasterospora KY 11515. Soluble starch was the best carbon source; NH
4Cl and NH
4NO
3 were suitable nitrogen sources both for the growth and fortimicin production. Amino acids such as L-arginine, L-asparagine, L-aspartic acid and L-glutamic acid showed some stimulatory effects on both growth and antibiotic production of
M. olivoasterospora while L-serine stimulated only antibiotic production and L-citrulline only the growth. K2HPO4, MgSO4•7H2O and CaCO3 were essential especially for the antibiotic production. The most important finding was that vitamin B12, cobalt and nickel showed marked stimulatory effects on fortimicin A production.
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TOTAL SYNTHESIS OF TUBERACTINOMYCIN O
TADASHI TESHIMA, SHINYA NOMOTO, TATEAKI WAKAMIYA, TETSUO SHIBA
1977 Volume 30 Issue 12 Pages
1073-1079
Published: 1977
Released on J-STAGE: April 12, 2006
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Tuberactinomycin O, one of the four congeners of the antituberculous peptide tuberactinomycin, was totally synthesized. The β-ureidodehydroalanine moiety was constructed from β, β-diethoxyalanine with excess urea in acidic medium after a cyclization reaction of a pentapeptide was finished. Cyclization was carried out by means of the 1-succinimidyl ester method. To the cyclic pentapeptide, β-lysine was introduced as the branched moiety and then deprotected to afford tuberactinomycin O which was completely identified with the natural form of the antibiotic.
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VINCENT GROUPE, RICHARD DONOVICK
1977 Volume 30 Issue 12 Pages
1080-1086
Published: 1977
Released on J-STAGE: April 12, 2006
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Whole shaken cultures of 20 random, unidentified actinomycetes were extracted with
n-butanol at pH 4.5, 7.0, and 8.5, respectively. Residues of butanol-extractable materials (BXM) were reconstituted (100×) in buffers and freeze-dried. BXM were surprisingly well tolerated in animals and were screened against influenza A viral pneumonia in mice. One culture yielded BXM-80 which suppressed both chemical (LPS) and viral (NDV) pneumonia in mice as well as inhibited rat foot pad edema induced by carrageenin. Aspirin, Butazolidin, hydrocortisone, indomethacin, and prednisolone, which are known to inhibit carrageenin-induced rat foot pad edema were tested against chemical (LPS) and viral (NDV) pneumonia in mice. Only hydrocortisone and prednisolone suppressed LPS pneumonia. All of these 5 compounds failed to inhibit NDV pneumonia. Microbial products are suggested as a source for new and unique anti-inflammatory agents.
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KENNETH S. ROSENTHAL, DANIEL R. STORM
1977 Volume 30 Issue 12 Pages
1087-1092
Published: 1977
Released on J-STAGE: April 12, 2006
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One of the apparent roles of the outer membrane system in gram-negative bacteria is to function as a selective permeability barrier. A number of antibiotics active against gram-positive bacteria are relatively ineffective against gram-negative bacteria presumably because of the implied barrier function of the outer membrane. This interpretation has been strengthened by studies demonstrating synergism between outer membrane perturbing agents such as EDTA or polymyxin B and specific antibiotics. In the case of polymyxin B, it is not totally clear that synergism with other antimicrobials is due to disruption of the outer membrane permeability barrier or to interactions with the inner membrane. In order to resolve this question, polymyxin B was covalently attached to agarose in order to limit interactions with the outer surface of
E. coli. These studies demonstrate that immobilized polymyxin B acts synergistically with bacitracin, rifampicin, or lysozyme. It is proposed that synergistic effects exhibited by polymyxin B are due to its interaction with the outer membrane system.
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GOHTA MASUDA, SUSUMU TOMIOKA
1977 Volume 30 Issue 12 Pages
1093-1097
Published: 1977
Released on J-STAGE: April 12, 2006
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Biological β-lactam antibiotic-inactivating activities were detected in bacteriuria and suppurating pleural fluids. Clinical specimens were sterilized with membrane filters and the amounts of ampicillin and/or cephalothin which were being inactivated by 1 ml of each filtrate were determined. In general, filtrates which originally yielded
Klebsiella sp. tended to show activity against ampicillin; whereas those yielding
Enterobacter sp. and
Pseudomonas aeruginosa showed activity against cephalothin.
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IN VITRO COMPARISON OF THREE ANTI-PSEUDOMONAL SEMISYNTHETIC PENICILLINS
P. C. FUCHS, C. THORNSBERRY, A. L. BARRY, T. L. GAVAN, E. H. GERLACH, ...
1977 Volume 30 Issue 12 Pages
1098-1106
Published: 1977
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Ticarcillin, carbenicillin and BL-P1908, a new anti-pseudomonal semisynthetic penicillin, were subjected to several
in vitrocomparisons-including minimal inhibitory and lethal concentrations (MIC and MLC), effects of inoculum size, effects of buffering the media and regression analyses of MIC and disc diffusion data. Whereas ticarcillin and carbenicillin showed comparable spectra of activity, with ticarcillin being more active against
Pseudomonas aeruginosa and many
Enterobacteriaceae, BL-P1908 exhibited a quite different spectrum, being much more active than either or the other two drugs against
P. aeruginosa and
Streptococcus faecalis, but virtually inactive against most of the
Enterobacteriaceae. However, the MIC/MLC disparity against
P. aeruginosa was much greater for BL-P1908 than for the other two drugs. The increase in MIC's resulting from increasing the inoculum sizes was comparable for the three drugs. The regression analyses showed good correlations between the disc diffusion and MIC data for all three drugs. Based on the regression analyses we conclude that for the 100-mcg carbenicillin disc the NCCLS recommended zone size breakpoints for
P. aeruginosa should be utilized for all organisms, and that if a single disc should be selected as a representative for these two currently available antipseudomonal penicillins, the 75-mcg ticarcillin disc gave slightly better correlations with the MIC data of both drugs than the 100 mcg carbenicillin disc.
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R. N. JONES, C. THORNSBERRY, A. L. BARRY, P. C. FUCHS, T. L. GAVAN, E. ...
1977 Volume 30 Issue 12 Pages
1107-1114
Published: 1977
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Piperacillin (T-1220) is a new semisynthetic penicillin with an unusually broad spectrum of antimicrobial activity.
In vitro comparisons of this drug with 6 other beta-lactam antimicrobics (ticarcillin, carbenicillin, ampicillin, cephalothin, cefamandole and cefoxitin) were conducted. These included minimal inhibitory concentrations (MIC) against 394 bacterial isolates, the minimal lethal concentrations (MLC) against 79 of those, as well as the effect of inoculum size on the MIC and MLC of the drugs. Piperacillin had significantly greater activity than did the other penicillins against
Pseudomonas species and
Klebsiella pneumoniae. Against
P. aeruginosa piperacillin was 8- and 16-fold more active than ticarcillin and carbenicillin, respectively. The MLC of piperacillin rarely differed from the MIC by more than one log
2 dilutions except against
P. aeruginosa in which the MLC was 4-fold greater or more than the MIC of 45% of isolates tested. Ticarcillin, carbenicillin and cefoxitin showed minimal inoculum size effects. Cefamandole results showed the greatest inoculum size variation with 55% and 37% of isolates showing an 8-fold increase in MIC and MLC respectively by increasing inoculum from 10
5 to 10
7 CFU/ml. Piperacillin was intermediately effected having 25% of strains >8-fold increase in MIC.
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EUGENE S. WAGNER, BARRY LINDLEY, MADONNA TALBERT
1977 Volume 30 Issue 12 Pages
1115-1118
Published: 1977
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Benzylpenicillin, 5.2%
14C-enriched, was incubated with human whole blood. The erythrocyte component was washed and exhaustively dialyzed and found to contain 6.3% of the original radioactivity. None of the penicillin was found to bind to the cell membrane. Dialysis of the cell contents indicated that none of the penicillin binds irreversibly to the proteins within the cell. Infrared examination of the contents of the cell leads to the
conclusion that benzylpenicillin (a monovalent anion) enters the erythrocyte and is hydrolyzed to benzylpenicilloic acid (a divalent anion). This structural change prevents the antibiotic from migrating out of the cell.
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G. LABER, E. SCHÜTZE
1977 Volume 30 Issue 12 Pages
1119-1122
Published: 1977
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Tiamulin concentrations have been determined in the serum of chickens, turkeys and swine after a single oral administration of various doses. The compound peaked between 2 and 4 hours after drug supply. In the highest dose used (50 mg/kg body weight), mean concentrations of 3.5, 2.9, 4.5μg/ml for chickens, turkeys and swine, respectively, could be obtained. In poultry, the levels declined between 12 and 24 hours to values not useful for calculation. In swine at 24 hours after administration measurable values could still be detected.
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KENSUKE TOBE, TAKESHI NISHINO, YOSHIMI HIRAI, SHOZO NAKAZAWA
1977 Volume 30 Issue 12 Pages
1123-1126
Published: 1977
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YOSHIO ABE, SUSUMU NAKAGAWA, TAKAYUKI NAITO, HIROSHI KAWAGUCHI
1977 Volume 30 Issue 12 Pages
1127-1129
Published: 1977
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STREPTOMYCES SP. STRAIN NO. K-342">III. REACYLATION OF 4"-DEPROPIONYL MARIDOMYCIN III INTO MARIDOMYCIN V (MARIDOMYCIN K) BY STREPTOMYCES SP. STRAIN NO. K-342
MASARU UYEDA, SHINYA MORI, MASAKO MORITA, TERUMI OGATA, MARIKO MORI, M ...
1977 Volume 30 Issue 12 Pages
1130-1131
Published: 1977
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R. J. MEHTA, M. K. FOX, D. J. NEWMAN, C. H. NASH
1977 Volume 30 Issue 12 Pages
1132-1133
Published: 1977
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TETSUO SAWAI, KIYOTAKA MATSUBA, SABURO YAMAGISHI
1977 Volume 30 Issue 12 Pages
1134-1136
Published: 1977
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SHINICHI KONDO, KENZABURO YOSHIDA, TAKAKO IKEDA, KATSUHARU IINUMA, YOS ...
1977 Volume 30 Issue 12 Pages
1137-1139
Published: 1977
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J. A. CHAN, T. T. WEI, C. C. KALITA, D. J. WARNICK, A. L. GARRETSON, A ...
1977 Volume 30 Issue 12 Pages
1140-1142
Published: 1977
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SHINICHI KONDO, MASASHI MIYAMOTO, HIROSHI NAGANAWA, TOMIO TAKEUCHI, HA ...
1977 Volume 30 Issue 12 Pages
1143-1145
Published: 1977
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KUNIMOTO HOTTA, YOSHIRO OKAMI, HAMAO UMEZAWA
1977 Volume 30 Issue 12 Pages
1146-1149
Published: 1977
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SHINICHI KONDO, TSUYOSHI MIYASAKA, KENZABURO YOSHIDA, KATSUHARU IINUMA ...
1977 Volume 30 Issue 12 Pages
1150-1152
Published: 1977
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