-
I. TAXONOMY, FERMENTATION, ISOLATION, PHYSICO-CHEMICAL PROPERTIES AND BIOLOGICAL ACTIVITIES
SUSUMU MIYATA, NOBUTAKA OHHATA, HIDETUGU MURAI, YUKO MASUI, MASAMI EZA ...
1992 Volume 45 Issue 7 Pages
1029-1040
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
WS009 A and B novel endothelin receptor antagonists, have been isolated from the fermentation broth of
Streptomyces sp. No. 89009. These antagonists were purified from the culture filtrate followed by Diaion SP-207, DEAE Toyopearl column chromatography and HPLC. WS009 A and B showed selective activity in an endothelin receptor binding assay with IC
50 of 5.8 × 10
-6M and 6.7 × 10
-7M, respectively. On the basis of spectroscopic and chemical evidence, the structures of WS009 A and B have been established as
1 and
3, and are highly hydroxylated benz[
a]anthraquinone chromophores.
View full abstract
-
II. BIOLOGICAL CHARACTERIZATION AND PHARMACOLOGICAL CHARACTERIZATION OF WS009 A AND B
SUSUMU MIYATA, MICHIZANE HASHIMOTO, KEIKO FUJIE, MIWAKO SHOUHO, KEIZO ...
1992 Volume 45 Issue 7 Pages
1041-1046
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
WS009 A and B, produced by
Streptomyces sp. No. 89009, were found to be competitive and specific antagonists against endothelin (ET)-1 receptors in
in vitro studies and also active in
in vivo studies. Furthermore, WS009 A and B were specific antagonists for vascular ET-1 receptors (ET
A receptors) and significantly prevented the accumulation of intracellular inositol 1, 4, 5-triphosphate (IP
3) in endothelin treated rat aorta tissues.
View full abstract
-
SHINICHIRO TOKI, KATSUHIKO ANDO, ISAO KAWAMOTO, HIROSHI SANO, MAYUMI Y ...
1992 Volume 45 Issue 7 Pages
1047-1054
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
Verticillium sp. SPC-15898 was found to produce novel metabolites, designated ES-242-2--8, which were structurally related to ES-242-1. These compounds were isolated from the culture broth and the physico-chemical and biochemical properties were examined. ES-242-2--8 inhibited [
3H]thienyl cyclohexypiperidine ([
3H]TCP) binding to rat crude synaptic membranes (CSM) with IC
50 values of 0.116, 2.9,
ca. 2.9, 25.3, 1.0, 59, 24, and 13μM, respectively. None of these compounds showed inhibitory effects against the binding of [
3H]kainate to its receptor, which is another subtype of the excitatory amino acid receptor.
View full abstract
-
I. TAXONOMY, FERMENTATION, ISOLATION, PHYSICO-CHEMICAL PROPERTIES AND BIOLOGICAL ACTIVITIES
KENICHI HAYASHI, MICHIZANE HASHIMOTO, NOBUHARU SHIGEMATSU, MOTOAKI NIS ...
1992 Volume 45 Issue 7 Pages
1055-1063
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
Data from several studies suggest that tachykinins may play an important role in the pathophysiology of airway diseases, especially asthma. Our aim is to discover tachykinin antagonists which exhibit therapeutically useful anti-asthmatic activity. In our search for activities inhibiting the binding of [
3H]substance P to guinea-pig lung membrane preparations, we have found that the fermentation product, WS9326A, isolated from
Streptomyces violaceusniger, is a potent tachykinin receptor antagonist.
View full abstract
-
II. BIOLOGICAL AND PHARMACOLOGICAL PROPERTIES OF WS9326A AND TETRAHYDRO-WS9326A (FK224)
MICHIZANE HASHIMOTO, KENICHI HAYASHI, MASAKO MURAI, TAKASHI FUJII, MOT ...
1992 Volume 45 Issue 7 Pages
1064-1070
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
WS9326A binds competitively to [
3H]substance P (NK-1 receptor) binding sites on guinea-pig lung membranes (IC
50 = 3.6 × 10
-6 M), and acts as a tachykinin antagonist in various functional assays.
WS9326A inhibited tracheal constrictions produced by exogenously added substance P and neurokinin A, with IC
50 values of 9.7 × 10
-6 M and 3.5 × 10
-6 M, respectively. WS9326A inhibited neurokinin A-induced bronchoconstriction in a dose dependent manner when administered to guinea-pigs intravenously together with neurokinin A, and was also effective in preventing capsaicin-induced bronchoconstriction, which is known to be caused by release of endogenous tachykinins (substance P and neurokinin A).
FK224 (tetrahydro-WS9326A; catalytic hydrogenation of WS9326A gave FK224) was more potent than WS9326A in the [
3H]substance P receptor binding assay using guinea-pig lung membrane (IC
50 = 1.0 × 10
-7 M).
View full abstract
-
KAZUSHIGE TANAKA, SHIGERU MATSUTANI, KOICHI MATSUMOTO, TADASHI YOSHIDA
1992 Volume 45 Issue 7 Pages
1071-1078
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
Thielocin A1β, a novel phospholipase A
2 inhibitor, was isolated from
Thielavia terricola RF-143. It inhibited various phospholipase A
2s in a dose-dependent manner. Among these, group II phospholipase A
2 from rat was most sensitive to thielocin A1β (IC
50 = 0.0033 μM). The inhibition of phospholipase A
2 by thielocin A1β was independent of Ca
2+ and substrate concentration. In addition, the inhibition of rat group II phospholipase A
2 was noncompetitive (
Ki=0.0068 μM) and reversible. Furthermore, thielocin Al β quenched the relative fluorescent intensity of
Naja naja venom phospholipase A
2 and in a dose-dependent manner; 50% quench was noted with a molar ratio of thielocin A1β/ enzyme of 2.2. These observations indicated that inhibition of phospholipase A
2 by thielocin A1β may result from direct interaction with the enzyme.
View full abstract
-
I. TAXONOMY, FERMENTATION, ISOLATION AND BIOLOGICAL ACTIVITIES
TAKAAKI AOYAGI, MASAHIRO HATSU, FUKIKO KOJIMA, CHIGUSA HAYASHI, MASA H ...
1992 Volume 45 Issue 7 Pages
1079-1083
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
We found benarthin, a new inhibitor of pyroglutamyl peptidase, in the fermentation broth of
Streptomyces xanthophaeus MJ244-SF1. It was purified by column chromatography and centrifugal partition chromatography (CPC) and then was isolated as a colorless powder. The binding of benarthin was competitive with substrate and its inhibition constant (
Ki) was 1.2 × 10
-6M.
View full abstract
-
II. PHYSICO-CHEMICAL PROPERTIES AND STRUCTURE DETERMINATION
MASAHIRO HATSU, HIROSHI NAGANAWA, TAKAAKI AOYAGI, TOMIO TAKEUCHI
1992 Volume 45 Issue 7 Pages
1084-1087
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
Benarthin, a new inhibitor of pyroglutamyl peptidase (PG-peptidase), has been isolated from the culture broth of
Streptomyces xanthophaeus MJ244-SF1. The structure of benarthin was determined to be L-(2, 3-dihydroxybenzoyl)argininyl-L-threonine by analysis of spectral properties and through chemical studies.
View full abstract
-
III. SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS
MASAHIRO HATSU, MAKOTO TUDA, YASUHIKO MURAOKA, TAKAAKI AOYAGI, TOMIO T ...
1992 Volume 45 Issue 7 Pages
1088-1095
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
Benarthin, a new inhibitor of pyroglutamyl peptidase (PG-peptidase), has been isolated from the culture filtrate of
Streptomyces xanthophaeus MJ244-SF1. The structure of benarthin has been determined to be L-(2, 3-dihydroxybenzoyl)arginyl-L-threonine. This structure was confirmed by the total synthesis of benarthin. Moreover, we synthesized benarthin derivatives to obtain information on the relationship between structure and inhibitory activity. The results indicated that the catechol group of benarthin is the essential moiety for the inhibition of PG-peptidase.
View full abstract
-
I. PRODUCTION, ISOLATION, STRUCTURAL ELUCIDATION AND BIOLOGICAL ACTIVITY OF OBSCUROLIDES A1 TO A4
HUBERT HOFF, HANNELORE DRAUTZ, HANS-PETER FIEDLER, HANS ZÄHNER, J ...
1992 Volume 45 Issue 7 Pages
1096-1107
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
A novel class of butyrolactones, named obscurolides, was isolated from the culture nitrate of
Streptomyces viridochromogenes by chemical screening methods. The structural elucidation of the obscurolides A
1 to A
4 (
1-4) is described. The carboxy group of the 4-aminobenzoic acid moiety of obscurolide A
1 (
1) is reduced in the other compounds. The isolated natural products have been proved to be diastereomeric mixtures by a partial racemization at C-7 which belongs to an allylic alcohol system. The obscurolides showed a weak inhibitory activity against calcium/calmodulindependent and independent phosphodiesterases from bovine.
View full abstract
-
JE-TAE WOO, CHIKARA SHINOHARA, KAORU SAKAI, KEIJI HASUMI, AKIRA ENDO
1992 Volume 45 Issue 7 Pages
1108-1116
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
Four new analogues of concanamycin family, designated concanamycins D, E, F and G, were isolated from the mycelium of
Streptomyces sp. A1509 by solvent extraction, silica gel column chromatography and HPLC. Structures of these compounds were identified by the combination of spectroscopic analyses. All of these compounds were structurally related to concanamycins A, B and C, which had been isolated previously, and inhibited the acidification of rat liver lysosomes at 10
-11-10
-9 concentration. The structure-activity study showed that the 18-membered macrolide ring and the 6-membered hemiketal ring portions of the molecules of concanamycin family are responsible for potent inhibitory activity.
View full abstract
-
I. PRODUCTION, ISOLATION, PHYSICO-CHEMICAL PROPERTIES AND BIOLOGICAL ACTIVITIES
DAISUKE KOMAGATA, TSUTOMU SAWA, YASUHIKO MURAOKA, CHIAKI IMADA, YOSHIR ...
1992 Volume 45 Issue 7 Pages
1117-1121
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
TA-3037A, a new inhibitor of glutathione
S-transferase was discovered in the fermentation broth of
Streptomyces sp. TA-3037. It was purified by chromatography followed by solvent extraction and then isolated as yellow needles. TA-3037A has the molecular formula of C
16H
11NO
4. It was competitive with the substrate, and the inhibition constant (
Ki) was 4.9 μM.
View full abstract
-
II. STRUCTURE DETERMINATION
DAISUKE KOMAGATA, YASUHIKO MURAOKA, RYUICHI SAWA, YOSHIKAZU TAKAHASHI, ...
1992 Volume 45 Issue 7 Pages
1122-1124
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
TA-3037A, a new inhibitor of glutathione
S-transferase, has been isolated from the culture broth of
Streptomyces sp. TA-3037. The structure of TA-3037A was defined as (
Z)-3-benzylidene-3, 4-dihydro-2-oxo-2
H-1, 4-benzoxazine-5-carboxylic acid by an analysis of spectral properties and chemical studies of TA-3037 A and its derivatives.
View full abstract
-
I. TAXONOMY OF THE PRODUCING ORGANISM, FERMENTATION AND BIOLOGICAL ACTIVITY
JAMES P. KARWOWSKI, MARIANNA JACKSON, ROBERT J. THERIAULT, GRANT J. BA ...
1992 Volume 45 Issue 7 Pages
1125-1132
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
Tirandalydigin is a new tetramic acid antibiotic which was discovered in a screen designed to find compounds with activity against pathogenic anaerobic bacteria. It was named tirandalydigin because it possesses structural features that are common to both tirandamycin and streptolydigin. The producing culture, strain AB 1006A-9, is a
Streptomyces and was compared to the streptomycetes that synthesize tirandamycin and streptolydigin. It is closely related to the former culture and was named
Streptomyces tirandis subsp.
umidus. Tirandalydigin has MICs in the range of 0.5 to 32 μg/ml against many pathogenic anaerobes, streptococci, enterococci and legionellae.
View full abstract
-
MASAYA NAKAGAWA, YOICHIRO TODA, KAZUO FURIHATA, YOICHI HAYAKAWA, HARUO ...
1992 Volume 45 Issue 7 Pages
1133-1138
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
A new antitumor antibiotic, designated AL081, was obtained from the culture filtrate of an actinomycete identified as
Streptomyces gannmycicus, and found to be identical with viridenomycin by direct comparison. The structure of the antibiotic was determined by NMR spectral analysis including a variety of two-dimensional techniques to be a novel 24-membered macrocyclic polyene lactam. Viridenomycin prolonged the survival periods of mice bearing P388 leukemia and B16 melanoma cells.
View full abstract
-
TOSHIAKI SUNAZUKA, KAZUO TSUZUKI, HIDETOSHI KUMAGAI, HIROSHI TOMODA, H ...
1992 Volume 45 Issue 7 Pages
1139-1147
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
Simple and efficient syntheses of 1233A analogs were developed and the inhibitory activity of the analogs against hydroxymethylglutaryl coenzyme A (HMG-CoA) synthase was determined. Study of the structure-activity relationships revealed that not only the geometry in β-lactone moiety but also the length of the carbon side chain is important for inhibitory activity against HMG-CoA synthase.
View full abstract
-
HIDETOSHI TOKUYAMA, MASAHIKO ISAKA, EIICHI NAKAMURA, RYOICHI ANDO, YAS ...
1992 Volume 45 Issue 7 Pages
1148-1154
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
A number of derivatives of the cyclopropenone antibiotic penitricin have been synthesized by the reaction of metalated cyclopropenone acetals with electrophiles. Studies on the antimicrobial structure-activity relationships indicated that the penitricin skeleton, hydroxymethylcyclopropenone, is indispensable for antimicrobial activity. These compounds were also found to display cytotoxic activity.
View full abstract
-
TSUTOMU OIKAWA, MARIKO SHIMAMURA, HIROMI ASHING, OSAMU NAKAMURA, TOSHI ...
1992 Volume 45 Issue 7 Pages
1155-1160
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
The effect of staurosporine, a potent inhibitor of protein kinases, on embryonic angiogenesis was studied in an
in vivo assay system involving chorioallantoic membranes of growing chick embryo. Staurosporine inhibited embryonic angiogenesis in a dose-related manner, the ID
50 value being 71pmol/egg. Staurosporine dose-dependently suppressed the proliferation of vascular endothelial cells, an important event involved in the angiogenesis process. The IC
50 value was 0.88nM. In contrast, staurosporine did not affect the migration of vascular endothelial cells. These results suggest that staurosporine affected embryonic angiogenesis probably by inhibiting endothelial cell proliferation. In addition, these results might support the notion that certain protein kinase(s) could be implicated in induction of angiogenesis and also that staurosporine would be a useful compound for studying a mode of action of angiogenesis occurring in various diseases, including tumor development.
View full abstract
-
RONALD J. PARRY, NAIQUAN YANG
1992 Volume 45 Issue 7 Pages
1161-1166
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
Stable mutants that are blocked in the production of the polyketide antibiotic furanomycin were generated by treatment of
Streptomyces threomyceticus (ATCC 15795) with a combination of
N-methyl-
N'-nitro-
N-nitrosoguanidine (NTG) and ultraviolet light. On the basis of their cosynthetic properties in mixed culture, the mutants were grouped into eleven phenotypic classes. The polarity of the cosynthetic reactions for seven classes of mutants was revealed by filtrate feeding experiments. This allowed them to be arranged in the most probable linear sequence of metabolic blocks. One of the remaining groups of mutants exhibited no cosynthetic behavior and is believed to be blocked in a gene that regulates furanomycin biosynthesis.
View full abstract
-
TOSHIO OHTA, ERI HASHIMOTO, MAMORU HASEGAWA
1992 Volume 45 Issue 7 Pages
1167-1175
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
A gene encoding sannamycin B-glycyltransferase (
sms13) of
Streptomyces sannanensis IFO 14239 was identified by cloning and complementation of
S. sannanensis mutant SN13 which is blocked at the interconversion of sannamycins B and A. The cloned DNA fragment also permitted the conversion of fortimicin B to A both in
S. sannanensis SN13 and
Streptomyces lividans TK23. DNA sequences similar to
sms13 were detected in all five producers of the fortimicin-group antibiotics,
Micromonospora olivasterospora ATCC 21819 (fortimicin-producer),
Micromonospora sp. strain SF-2098 ATCC 31580 (SF-2052),
Dactylosporangium matsuzakiense ATCC 31570 (dactimicin),
Streptomyces tenjimariensis ATCC 31603 (istamycin), and
Saccharopolyspora hirsuta ATCC 20501 (sporaricin). This suggests that these genes of similar function from different genera were derived from a common ancestral gene.
View full abstract
-
DECARESTRICTINES, A NEW FAMILY OF INHIBITORS OF CHOLESTEROL BIOSYNTHESIS FROM PENICILLIUM: III. DECARESTRICTINES E TO M
SUSANNE GRABLEY, PETER HAMMANN, KLAUS HÜTTER, REINHARD KIRSCH, HE ...
1992 Volume 45 Issue 7 Pages
1176-1181
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
-
SHO-ZOU KAWADA, YOSHINORI YAMASHITA, YOUICHI UOSAKI, KATSUSHIGE GOMI, ...
1992 Volume 45 Issue 7 Pages
1182-1184
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
-
E. V. FOMICHOVA, G. B. FEDOROVA, N. P. POTAPOVA, G. S. KATRUKHA
1992 Volume 45 Issue 7 Pages
1185-1186
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
-
JOHN P. DIRLAM, JON BORDNER, WALTER P. CULLEN, MARK T. JEFFERSON, LAUR ...
1992 Volume 45 Issue 7 Pages
1187-1189
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
-
ERNST EGERT, MATHIAS NOLTEMEYER, JOHANNES SIEBERS, JÜRGEN ROHR, A ...
1992 Volume 45 Issue 7 Pages
1190-1192
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS
-
Eui NAKAYAMA, KOICHI FUJIMOTO, SHIGEKI MURAMATSU, JUNYA IDE
1992 Volume 45 Issue 7 Pages
1193-1194
Published: July 25, 1992
Released on J-STAGE: April 19, 2006
JOURNAL
FREE ACCESS