-
YASUNOBU MURAKAMI, SHINICHIRO KATO, MIIKO NAKAJIMA, MICHIKO MATSUOKA, ...
1996 Volume 49 Issue 9 Pages
839-845
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
Formobactin, a new free radical scavenger, was isolated from the culture of
Nocardia sp. strain ND20. The structure of formobactin was determined to be a member of the nocobactin group antibiotics. Formobactin inhibited lipid peroxidation in rat brain homogenate. Formobactin also showed the activity to suppress L-glutamate toxicity in neuronal hybridoma N18-RE-105 cells.
View full abstract
-
TETSURO FUJITA, NORIMITSU HAMAMICHI, MASATOSHI KIUCHI, TOHRU MATSUZAKI ...
1996 Volume 49 Issue 9 Pages
846-853
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
Mycestericins D, E, F and G were isolated from the culture broth of
Mycelia sterilia ATCC 20349 as potent immunosuppressants. Mycestericins F and G were identical with dihydromycestericins D and E, respectively. Their absolute configurations were determined by use of the modified MOSHER'S method and by comparison of the CD spectra of their benzoate derivatives with those of synthetic analogs. Mycestericins D, E, F and G suppressed the proliferation of lymphocytes in the mouse allogeneic mixed lymphocyte reaction.
View full abstract
-
URSULA MOCEK, LAURI SCHULTZ, TIM BUCHAN, CHARLES BAEK, LARRY FRETTO, J ...
1996 Volume 49 Issue 9 Pages
854-859
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
Five new quinone pigments have been discovered from the fermentation broth of
Aspergillus,
Humicola and
Botryotrichum species isolated from different soil samples. These compounds inhibit serine proteases of the coagulation pathway. Their structures which differ in the identity and position of a 5-carbon side chain on the indole moiety have been elucidated based on NMR and FAB-MS experiments.
View full abstract
-
I. Taxonomy of Producing Organism, Fermentation and Biological Activity
KIN SING LAM, GRACE A. HESLER, DONALD R. GUSTAVSON, RONALD L. BERRY, K ...
1996 Volume 49 Issue 9 Pages
860-864
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
Strain C39217-R109-7 (ATCC 53791) is an actinomycete strain isolated from a soil sample collected at Puerto Viejo, Peru. It produces a new antitumor antibiotic, designated pyrrolosporin A. Taxonomic studies on its morphological, cultural and physiological characteristics identified this producing strain as
Micromonospora sp. C39217-R109-7. Pyrrolosporin A shows antimicrobial activity against Gram-positive bacteria and it is weakly active against Gram-negative bacteria. Pyrrolosporin A prolongs the life span of mice inoculated with P388 leukemia cells.
View full abstract
-
II. Isolation, Physico-chemical Properties, Spectroscopic Study and X-ray Analysis
DANIEL R. SCHROEDER, KIMBERLY L. COLSON, STEVE E. KLOHR, MIKE S. LEE, ...
1996 Volume 49 Issue 9 Pages
865-872
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
Pyrrolosporin A (
1) is a new macrolide antitumor antibiotic possessing an unusual spiro-a-acyltetronic acid moiety. The antibiotic was isolated from the fermentation broth of
Micromonospora sp. by vacuum liquid chromatography, crystallization and reversed phase HPLC (CIS). The structure was determined by a combination of NMR, MS, IR, UV, X-ray analysis and degradation studies.
View full abstract
-
HISAYOSHI KOBAYASHI, MICHIO NAMIKOSHI, TAKESHI YOSHIMOTO, TOSHIHIRO YO ...
1996 Volume 49 Issue 9 Pages
873-879
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
A bioassay method detecting deformations of mycelia germinated from conidia of
Pyricularia oryzae P-2b, has been modified to give quantitative estimations. The method was first developed using antimitotic agents which showed characteristic curling effect. Morphological deformations include curling, swelling, hyper-divergency, beads shape and so on, and inhibition of the germination was also observed. For quantitative estimations, indices were introduced for the hyphal growth inhibition and a quantity of conidia in each assay cell and concentration of test solutions were adjusted. Details of the modified method and the application to screening assay of marine fungi isolated in Yap Islands are described. Eight strains of 109 tested showed morphological deformations, and chaetoglobosin A was isolated from the broth filtrate of a strain assigned to
Chaetomium sp.
This bioassay is a cheap, quick and easy method to be applied to the primary screening for antimitotic and antifungal substances from natural sources.
View full abstract
-
III. Strain and Fermentation Study
FLAVIA MARINELLI, LUCIANO GASTALDO, GIORGIO TOPPO, CLAUDIO QUARTA
1996 Volume 49 Issue 9 Pages
880-885
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
GE37468A is a new thiazolyl peptide antibiotic acting on Elongation Factor Tu, produced by fermentation of
Streptomyces sp. ATCC 55365. The low (<10mg/liter) and poorly reproducible antibiotic productivity of the original soil isolate hampered the development of a scalable fermentation process. A tenfold increase of GE37468A productivity was achieved by selection of spontaneous morphochromatic variants, which appeared at high frequency in the wild type population. The higher producing ATCC 55365/O/5 colony was tyrosinase defective and blocked in the aerial mycelium differentiation (Amy
-Mel
- phenotype). The fermentation process of this stable and purified strain was rapidly optimized to achieve a further fourfold improvement in a fed-batch process.
View full abstract
-
II. Structure Elucidation and Total Synthesis
RYUJI UCHIDA, KAZURO SHIOMI, TOSHIAKI SUNAZUKA, JUNJI INOKOSHI, AI NIS ...
1996 Volume 49 Issue 9 Pages
886-889
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
The structures of new protein farnesyltransferase inhibitors, kurasoins A and B, were elucidated by NMR study. Kurasoins A and B are acyloin compounds having in common a 3-hydroxy-lpheny-1-2-butanone moiety, to which
p-hydroxyphenyl and 3-indolyl moieties respectively, are connected at C-4. The structures were confirmed by total synthesis.
View full abstract
-
V. Endopeptidase Inhibitory Activity of Poststatin Analogues
MAKOTO TSUDA, YASUHIKO MURAOKA, MACHIKO NAGAI, TAKAAKI AOYAGI, TOMIO T ...
1996 Volume 49 Issue 9 Pages
890-899
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
Thirty analogues of poststatin were synthesized, and their inhibitory activities against prolyl endopeptidase, human leukocyte elastase and cathepsin B were measured. The α-ketone was essential and the
S configuration was preferable to the
R configuration in the β-substituted-β-amino-α-oxopropionic acid moiety of poststatin analogues for endopeptidase inhibitory activity. The analogue in which the D-leucine residue of poststatin was replaced by L-leucine showed strong inhibitory activity to cathepsin B. Introduction of an aromatic group into the P
4 position and proline into the P
2 position increased inhibitory activity to elastase. Benzyloxycarbonyl-L-homophenylalanyl-(
RS)-3-amino-2-oxovaleryl-D-leucyl-L-valine was about 6 times more active to prolyl endopeptidase than natural poststatin.
View full abstract
-
VI. Endopeptidase Inhibitory Activity of Poststatin Analogues Containing Pyrrolidine Ring
MAKOTO TSUDA, YASUHIKO MURAOKA, TETSUYA SOMENO, MACHIKO NAGAI, TAKAAKI ...
1996 Volume 49 Issue 9 Pages
900-908
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
Several pyrrolidine-containing analogues of poststatin were synthesized and examined for their inhibitory activity against prolyl endopeptidase and cathepsin B
in vitro. Replacement of the postine residue with 2-oxo-2-(2-pyrrolidinyl)acetic acid increased the selectivity and inhibitory activity against prolyl endopeptidase. Benzyloxycarbonyl-L-phenylalanyl-(
S)-2-oxo-2-(2-pyrrolidinyl)acetyl-D-phenylalanine was about 46 times as active to prolyl endopeptidase as natural poststatin.
View full abstract
-
VII. N-Cycloalkylamide Analogues
MAKOTO TSUDA, YASUHIKO MURAOKA, MACHIKO NAGAI, TAKAAKI AOYAGI, TOMIO T ...
1996 Volume 49 Issue 9 Pages
909-920
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
Poststatin analogues containing (
S)-2-oxo-2-(2-pyrrolidinyl)acetyl moiety in P
1 were synthesized and examined for their inhibitory activity against prolyl endopeptidase and cathepsin B
in vitro. Introduction of non-peptidyl cycloalkylamine component in P'
1 was effective and P
3-acyl groups must be widely modifiable for prolyl endopeptidase inhibition. Acyl-L-phenylalanyl-(
S)-2-oxo-2-(2-pyrrolidinyl)acetyl-cycloalkylamide type compounds showed IC
50 value of nano to subnano g/ml as prolyl endopeptidase inhibitor and were shown no significant inhibitory activities against cathepsin B, a cysteine protease.
View full abstract
-
AILEEN ALLSOP, GERALD BROOKS, PETER D. EDWARDS, ARUN C. KAURA, ROBERT ...
1996 Volume 49 Issue 9 Pages
921-928
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
A series of 6-(substituted oxyethyl)penem esters having the (
5S) stereochemistry which are potent inhibitors of
Escherichia coli leader peptidase is described. Structure-activity relationships are discussed.
View full abstract
-
HLROSHI TOMODA, YUICHI YAMAGUCHI, NORIKO TABATA, TATSUYA KOBAYASHI, RO ...
1996 Volume 49 Issue 9 Pages
929-931
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
-
I. Producing Strain, Fermentation, Isolation, and Biological Activities
RYUJI UCHIDA, KAZURO SHIOMI, JUNJI INOKOSHI, ROKURO MASUMA, TOMOYA KAW ...
1996 Volume 49 Issue 9 Pages
932-934
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
-
Novel Minor Congeners of Monensins from Streptomyces cinnamonensis
STANISLAV POSPISIL, PETR SEDMERA, VLADIMIR HAVLICEK
1996 Volume 49 Issue 9 Pages
935-937
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
-
FATTORI RAIMONDO, PELLACINI FRANCO, ROMAGNANO SLEFANO, FRONZA GIOVANNI ...
1996 Volume 49 Issue 9 Pages
938-940
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
-
FERENC SZTARICSKAI, ZOLTÁN DINYA, MARIA M. PUSKÁS, GYULA ...
1996 Volume 49 Issue 9 Pages
941-943
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
-
I. Synthesis and β-Lactamase Inhibitory Activity of 2β-Alkoxycarbonyl Penicillanic Acid Sulfones
EDUARDO L. SETTI, NARENDER A. V. REDDY, OLUDOTUN A. PHILLIPS, DAVID P. ...
1996 Volume 49 Issue 9 Pages
944-946
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
-
JUNG-SIK KIM, KAZUO SHIN-YA, JUN EISHIMA, KAZUO FURIHATA, HARUO SETO
1996 Volume 49 Issue 9 Pages
947-948
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
-
SHIGERU HIRAMOTO, NOBUHIRO KINOSHITA, SHIGEO HATANAKA, HARUO SETO
1996 Volume 49 Issue 9 Pages
949-952
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
-
NAOKI MATSUMOTO, TOSHIO TSUCHIDA, MASATO MARUYAMA, RYUICHI SAWA, NAOKO ...
1996 Volume 49 Issue 9 Pages
953-954
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
-
SHIN-DUK KIM, IN-JA RYOO, CHANG-JIN KIM, WON-GON KIM, JONG-PYUNG KIM, ...
1996 Volume 49 Issue 9 Pages
955-957
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS
-
DAISUKE KOMAGATA, SHINJI FUJITA, NORIYUKI YAMASHITA, SEIICHI SAITO, TO ...
1996 Volume 49 Issue 9 Pages
958-959
Published: September 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
FREE ACCESS