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I. PRODUCING ORGANISM AND BIOLOGICAL ACTIVITIES
MAMORU ARAI, TATSUO HANEISHI, NOBUAKI KITAHARA, RYUZO ENOKITA, KATSUHI ...
1976 Volume 29 Issue 9 Pages
863-869
Published: 1976
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Herbicidins A and B, two new antibiotics with selective and contact herbicidal activity, were produced by a new species of
Streptomyces designated as
S. saganonensis. Among tested microorganisms, herbicidins indicated some activity against fungi
in vitro and
Xanthomonas oryzae in vivo. Their characteristic features were brought into relief by their selective and contact killing effect on many dicotyledonous plant as well as their inhibition of germination of the plant seeds, such as Chinese cabbage.
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II. FERMENTATION, ISOLATION AND PHYSICO-CHEMICAL CHARACTERIZATION
TATSUO HANEISHI, AKIRA TERAHARA, HISASHI KAYAMORI, JUNKO YABE, MAMORU ...
1976 Volume 29 Issue 9 Pages
870-875
Published: 1976
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Herbicidins were produced in submerged fermentation by
Streptomyces saganonensis. Isolation of the antibiotics from the culture broth was performed by adsorption on resinous adsorbent followed by elution with aqueous acetone. Herbicidins A and B were separated from each other by counter-current distribution on a Ronor column or by silica gel chromatography. Physico-chemical characterization revealed that herbicidins are new antibiotics having an adenine nucleoside moiety in their structures.
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SATOSHI OMURA, CHIAKI KITAO, HARUO TANAKA, RUIKO OIWA, YOKO TAKAHASHI, ...
1976 Volume 29 Issue 9 Pages
876-881
Published: 1976
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Asukamycin, a new antibiotic, has been isolated from the culture broth of a streptomycete designated as
Streptomyces nodosus subsp.
asukaensis. The antibiotic inhibits the growth of Gram-positive bacteria including
Nocardia asteroides. The empirical formula of
antibiotic asukamycin has been proposed as C
29H
22N
2O
9 (M.W. 542). An acute toxicity of the antibiotic in mice is LD
50 48.5 mg/kg by intraperitoneal injection and it has no effect on mice when it was administered by 450 mg/kg per os.
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YOSHIKI KUMADA, HIROSHI NAGANAWA, HIRONOBU IINUMA, MEIKI MATSUZAKI, TO ...
1976 Volume 29 Issue 9 Pages
882-889
Published: 1976
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In the screening of catechol-O-methyltransferase inhibitors, three compounds were isolated from the culture filtrate of a mushroom,
Inonotus sp. One was 3, 4-dihydroxycinnamic acid (caffeic acid) which had been reported as an inhibitor of this enzyme. The others were the dextrorotatory 2, 6-bis-(3', 4'-dihydroxyphenyl)-3, 7-dioxabicyclo-[3, 3, 0]-octane 4, 8-dione (dehydrodicaffeic acid dilactone) and its antipode. These new compounds inhibited both dopamine β-hydroxylase and dopa decarboxylase and showed hypotensive activity in the SH rat.
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II. STRUCTURE DETERMINATION OF NOCARDICINS A AND B
MASASHI HASHIMOTO, TADAAKI KOMORI, TAKASHI KAMIYA
1976 Volume 29 Issue 9 Pages
890-901
Published: 1976
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The structures of nocardicins A and B, novel monocyclic β-lactam antibiotics produced by a strain of
Nocardia, have been established as
1 and
2, respectively, on the basis of spectroscopic and chemical evidence. They are the first examples of monocyclic β-lactam antibiotics possessing relatively high antimicrobial activity, and are stereochemically and biologically related to penicillins and cephalosporins.
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I. SEPARATION OF CEPHALOSPORIN C DERIVATIVES AND CEPHALOSPORIN ANTIBIOTICS; ISOLATION OF CEPHALOSPORIN C FROM FERMENTATION BROTH
ROGER D. MILLER, NORBERT NEUSS
1976 Volume 29 Issue 9 Pages
902-906
Published: 1976
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Microbonded propylamine silica with a solvent system containing acetic acid, methanol, acetonitrile and water (2:4:7.5:86.5) is suitable for an efficient separation of mixtures containing several closely related cephem derivatives. The same system with preparative columns was used for the isolation of cephalosporin C directly from the filtered broth of
C. acremonium fermentation.
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H. BOJARSKA-DAHLIG, W. SLAWINSKI, D. ROSLIK-KAMINSKA, A. SCHAEFFER, A. ...
1976 Volume 29 Issue 9 Pages
907-914
Published: 1976
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Erythromycin A cyclic 11, 12-carbonate, a compound with high antibacterial activity, forms with L-aspartic acid a salt possessing valuable properties as a potential chemotherapeutic agent. The L-aspartate of erythromycin A cyclic 11, 12-carbonate exhibits strong antibacterial activity, especially against Gram-positive bacteria and shows low toxicity. The serum and the lung tissue levels of the discussed salt after a single dose administration to a rat were measured in comparison with those of erythromycin, its L-aspartate, erythromycin cyclic 11, 12-carbonate and its L-glutamate. The new erythromycin derivative showed definitely superior characteristics to those of the other substances tested. The activity of the L-aspartate of erythromycin A cyclic 11, 12-carbonate in chemotherapy of experimental staphylococcal infection and experimental pneumococcal bronchopneumonia in mice is superior to that of the parent carbonate and erythromycin itself.
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I. SYNTHESIS
HELMUT EGGER, HELLMUTH REINSHAGEN
1976 Volume 29 Issue 9 Pages
915-922
Published: 1976
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A series of new derivatives of the antibiotic pleuromutilin, produced by some Basidiomycetes, was synthesized by chemical modification of natural pleuromutilin. Most of them contain basic functional groups in the side chain at C
14 of the mutilin skeleton. The monotosylate of pleuromutilin was used as a versatile intermediate for displacement by N-, O- and S-nucleophiles.
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II. STRUCTURE-ACTIVITY CORRELATIONS
HELMUT EGGER, HELLMUTH REINSHAGEN
1976 Volume 29 Issue 9 Pages
923-927
Published: 1976
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Structural modification of the antibiotic pleuromutilin has afforded several derivatives with considerably enhanced activity against bacteria and mycoplasmas, and has permitted conclusions to be reached about structure-activity relationships. The carbonyl group in the five-membered ring and the hydroxyl group at C
11 seem to be essential for activity. The vinyl group can be hydrogenated without loss of activity. Chemical modification at C
14 offers the most possibilities for achieving the best activity and solubility properties. Mutilin, and other compounds with a free OH at C
14, are inactive. It was shown that mutilin esters of substituted thioglycolic acids had distinctly superior MIC values, especially in combination with a tertiary amino group in the side chain, the latter group of derivatives having MIC values better than pleuromutilin by a factor of more than 10. Further variation within this group led to the development of 14-deoxy-14-[(2-diethylaminoethyl) thioacetoxy]-mutilin hydrogen fumarate
(81.723 hfu, tiamulin) for extensive investigation of its chemotherapeutic potential.
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STRUCTURE-ACTIVITY RELATIONSHIPS OF α-SULFOCEPHALOSPORINS
HIROAKI NOMURA, ISAO MINAMI, TAKENORI HITAKA, TAKESHI FUGONO
1976 Volume 29 Issue 9 Pages
928-936
Published: 1976
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Synthesis and
in vitro activity of a number of cephalosporins having α-sulfoacyl- or other acyl groups,
e.g., α-carboxyacyl- and α-sulfoaminoacyl- at the 7-position and bearing a variety of heterocyclic thioether or pyridinium moieties at the 3-position are described.
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YOSHIMASA UEHARA, MAKOTO HORI, SHINICHI KONDO, MASA HAMADA, HAMAO UMEZ ...
1976 Volume 29 Issue 9 Pages
937-943
Published: 1976
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Various negamycin analogs were examined for (1) miscoding activity and (2) inhibition of the termination of protein synthesis. Since properties (1) and (2) do not correlate for the investigated compounds they may depend on different structural features of negamycin analogs. The results of biochemical and antimicrobial studies indicate that (a) the natural configuration of the carbon atom carrying the β-amino group is essential, (b) the δ-hydroxyl group is unnecessary, and (c) the acylation of the ε-amino group causes loss of activity.
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FATEMAH KAMAL, EDWARD KATZ
1976 Volume 29 Issue 9 Pages
944-949
Published: 1976
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The biosynthesis of etamycin by
Streptomyces griseoviridus was investigated with the precursors,
14C-L-leucine and
14CH
3-L-methionine, during short-term incubations. Both radioisotopes are rapidly incorporated into the antibiotic without significant lag. D-Leucine, but not L-leucine, inhibits etamycin formation. The kinetics of incorporation of
14C-L-leucine as well as the inhibitor studies suggest that L-leucine is the direct precursor of the D-enantiomer present in the antibiotic peptide. Chloramphenicol has been shown to inhibit protein synthesis by
S. griseoviridus without reduction of etamycin formation, indicating that a non-ribosomal mechanism of synthesis is involved in etamycin biogenesis. When L-ethionine was employed, both the formation of antibiotic and protein were blocked.
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KOJI FURUNO, SHUZO MATSUBARA, KUNIO ANDO, SHIGEO SUZUKI, KOZO HIRATA
1976 Volume 29 Issue 9 Pages
950-953
Published: 1976
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Kanamycin-induced renal impairment in dehydrated rats was spared by the administration of sodium D-glucaro-1, 4-lactone. In the plasma elimination and urinary excretion studies, n-glucarate-treated rats showed quick removal of the antibiotic from the body as compared with non-treated rats. Organ distribution study clearly demonstrated the potent nephrotoxicity of kanamycin and the reduction effect of D-glucarate against the nephrotoxicity. The
drug level in the kidney in non-treated rats was more than two orders of magnitude higher than those in other organs such as the liver, lung and spleen, and remained high for 48 hours after antibiotic administration. In D-glucarate-treated rats the kidney content of the drug was diminished as compared with non-treated rats just after the antibiotic administration, followed by a gradual decline with time.
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CLASS FUNGI IMPERFECTI, COLLECTED IN THE VIETNAMESE EMOCRATIC REPUBLIC
L. KRIZKOVÁ, L. MARVANOVÁ, P. NEMEC, J. BALANOVÁ, ...
1976 Volume 29 Issue 9 Pages
954-957
Published: 1976
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From soil samples collected in the jungles of Ninh Binh Province of the Vietnamese Democratic Republic, 97 isolates belonging to 54 species of
Fungi imperfecti were obtained and screened for the production of antibiotics. The isolates were identified as belonging to the orders
elanconiales, Moniliales, Sphaeropsidales and
Mycelia sterilia. In the species studied a very high incidence of antiprotozoal activities were observed.
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K. SAMBAMURTHY, P. ELLAIAH
1976 Volume 29 Issue 9 Pages
958-965
Published: 1976
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An extensive screening of soil samples from Kerala State, India, gave a new streptomycete,
Streptoverticillium quilonensis. Its taxonomy is described in detail.
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V. P. MARSHALL, E. A. REISENDER, P. F. WILEY
1976 Volume 29 Issue 9 Pages
966-968
Published: 1976
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NOVEL OXIDATION PROCEDURE FOR SYNTHESES OF 7α-METHOXYCEPHALOSPORINS AND 6α-METHOXYPENICILLINS
HIROAKI YANAGISAWA, MASAMI FUKUSHIMA, AKIKO ANDO, HIDEO NAKAO
1976 Volume 29 Issue 9 Pages
969-972
Published: 1976
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R. M. DEMARINIS, J. V. URI, J. A. WEISBACH
1976 Volume 29 Issue 9 Pages
973-975
Published: 1976
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A. K. GANGULY, B. K. LEE, R. BRAMBILLA, R. CONDON, O. SARRE
1976 Volume 29 Issue 9 Pages
976-977
Published: 1976
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HIROSHI SANO, TSUTOMU TSUCHIYA, SHIGERU KOBAYASHI, MASA HAMADA, SUMIO ...
1976 Volume 29 Issue 9 Pages
978-980
Published: 1976
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JÁN FUSKA, ALZBETA FUSKOVÁ
1976 Volume 29 Issue 9 Pages
981-982
Published: 1976
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KAZUHIKO TAKAHASHI, KOICHI TAMOTO, JIRO KOYAMA
1976 Volume 29 Issue 9 Pages
983-985
Published: 1976
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