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Taxonomy, Production, Isolation, and Biological Activities
YUTAKA KOGUCHI, JUN KOHNO, MAKI NISHIO, KOHEI TAKAHASHI, TORU OKUDA, T ...
2000 Volume 53 Issue 2 Pages
105-109
Published: February 25, 2000
Released on J-STAGE: September 19, 2008
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In our course of screening for novel proteasome inhibitors, TMC-95A and its diastereomers, TMC-95B to D, were isolated from the fermentation broth of
Apiospora montagnei Sacc. TC 1093. TMC-95A inhibited the chymotrypsin-like (ChT-L), trypsin-like (T-L), and peptidylglutamyl-peptide hydrolyzing (PGPH) activities of 20S proteasome with IC
50 values of 5.4 nM, 200 nM, and 60 nM, respectively. TMC-95B inhibited these activities to the same extent as TMC-95A, while the inhibitory activities of TMC-95C and D were 20 to 150 times weaker than that of TMC-95A and B. TMC-95A did not inhibit m-calpain, cathepsin L, and trypsin at 30 μM, suggesting its high selectivity for proteasome. Taxonomy of the producing strain is also described.
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KHISAL A. ALVI, BIPIN G. NAIR, JOHN RABENSTEIN, GRACE DAVIS, DWIGHT D. ...
2000 Volume 53 Issue 2 Pages
110-113
Published: February 25, 2000
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Two inhibitors of CD45 tyrosine phosphatase, dihydrocarolic acid (
1) and penitricin D (
2), were isolated from a fermentation broth of the fungus
Aspergillus niger and purified by HSCCC (high speed countercurrent chromatography) followed by HPLC. The structures were determined by NMR. The inhibitory activities of both compounds were specific to tyrosine phosphatases.
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BONG-SIK YUN, IN-KYOUNG LEE, JONG-PYUNG KIM, ICK-DONG YOO
2000 Volume 53 Issue 2 Pages
114-122
Published: February 25, 2000
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In our continuous investigation for free radical scavengers from extracts of fruit body of basidiomycetes, we have isolated four new
p-terphenyl compounds, designated as curtisians A-D, from the methanolic extract of the fruit body of
Paxillus curtisii. These compounds were isolated by silica gel and Sephadex LH-20 column chromatographies, preparative-TLC and HPLC, consecutively. The structures of curtisians were assigned as
p-terphenyls with substituents of acetyl, benzoyl, phenylbutyryl, 3-hydroxybutyryl and 3-acetoxybutyryl. Curtisians A, B, C and D exhibited inhibitory activity against lipid peroxidation with IC
50 values of 0.15, 0.17, 0.24 and 0.14μg/ml, respectively.
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I. Taxonomy, Fermentation, Isolation, Physico-chemical Properties and Biological Activities
BUNJI SATO, HIDEYUKI MURAMATSU, MICHIYO MIYAUCHI, YASUHIRO HORI, SHIGE ...
2000 Volume 53 Issue 2 Pages
123-130
Published: February 25, 2000
Released on J-STAGE: September 19, 2008
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Using the characteristic morphological changes of mammalian cells, we screened novel antimitotic substances and found that a strain of
Streptomyces sp. No.9885 produced FR182877. This substance was isolated from the culture broth by ethyl acetate extraction, silica gel column chromatography and ODS column chromatography. Structural studies on FR182877 suggested that it had a unique hexacyclic structure encompassing its highly strained double bond. FR182877 exhibited potent antitumor activities against murine ascitic tumor and solid tumor
in vivo.
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KEUN KI KIM, JAE GON KANG, SUK SIK MOON, KYU YOUNG KANG
2000 Volume 53 Issue 2 Pages
131-136
Published: February 25, 2000
Released on J-STAGE: September 19, 2008
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An antifungal bacterial strain, isolated from a greenhouse soil sample, inhibits growth of microflora nearby. It was selected for further studies of bacterial antifungal properties. This isolate was identified as a
Pseudomonas sp. based on carbohydrate utilization, and other biochemical and physiological tests. Petri plate assay revealed that the
Pseudomonas sp. exhibited antifungal activity against the plant pathogens,
Pythium ultimum,
Rhizoctonia solani,
Phytophthora capsici,
Botrytis cinerea and
Fusarium oxysporum. Using direct inhibition bioassay on TLC plates after ethyl acetate extraction of the culture filtrate, we correlated antifungal activity with production of antifungal compounds. An antifungal antibiotic was isolated from the culture filtrate and was identified as
N-butylbenzenesulphonamide. ED
50 values of the
N-butylbenzenesulphonamide against
P. ultimum,
P. capsici,
R. solani, and
B. cinerea were 73, 41, 33 and 102 ppm, respectively.
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ISAO MOMOSE, RYUICHI SEKIZAWA, NOBUO HOSOKAWA, HIRONOBU IINUMA, SUSUMU ...
2000 Volume 53 Issue 2 Pages
137-143
Published: February 25, 2000
Released on J-STAGE: September 19, 2008
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Three new sesquiterpenoid aromatic esters designated melleolides K (
1), L (
2) and M (
3) were isolated from the cultured mycelia of
Armillariella mellea (Vahl. ex Fr.) Karst. Structures of these compounds were determined on the basis of various NMR spectral data, chemical transformations and X-ray analysis. Compounds
1,
2 and
3 showed antimicrobial activities.
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TAKAAKI TAGUCHI, KEIKO ITOU, YUTAKA EBIZUKA, FRANCISCO MALPARTIDA, DAV ...
2000 Volume 53 Issue 2 Pages
144-152
Published: February 25, 2000
Released on J-STAGE: September 19, 2008
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The
actVI genetic region of
Streptomyces coelicolor A3 (2) is part of the biosynthetic gene cluster of actinorhodin (ACT), the
act cluster, consisting of six ORFs: ORFB, ORFA, ORF1, ORF2, ORF3, ORF4. A newly devised method of ACT detection with a combination of HPLC and LC/MS was applied to the analysis of the disruptants of each ORE ACT was produced by those of ORFB, ORFA, ORF3, and ORF4. Instead of ACT, the ORF1 disruptant produced 3, 8-dihydroxy-1-methylanthraquinone-2-carboxylic acid (DMAC) and aloesaponarin II as shunt products. The ORF2 disruptant gave 4-dihydro-9-hydroxy-1 -methyl- 10-oxo-3-
H-naphtho-[2, 3-
c]-pyran-3-(
S)-acetic acid, (
S)-DNPA. These results support our previous proposal for stereospecific pyran ring formation in the biosynthesis of ACT, most importantly suggesting that the
actVI-ORF2 product would recognize (
S)-DNPA as a substrate for stereospecific reduction at C-15. The disruptant of ORFA produced (
S)-DNPA together with ACT, suggesting that
actVI-ORFA might play a role such as stabilising the multicomponent, type II PKS complex.
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HELGE BJÖRN BODE, BARBARA WEGNER, AXEL ZEECK
2000 Volume 53 Issue 2 Pages
153-157
Published: February 25, 2000
Released on J-STAGE: September 19, 2008
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The biosynthesis of cladospirone bisepoxide (
1) was investigated by feeding
13C-labeled acetate to growing cultures of the fungus
Sphaeropsidales sp. (strain F-24'707).
13C NMR spectral analysis demonstrated the polyketide origin of both naphthalene units. The origin of two epoxide oxygens was confirmed as from air by cultivation of the strain in an
18O
2-enriched atmosphere. The [
18O]incorporation pattern into palmarumycin C
12 (
11), the putative precursor of
1 led to the hypothesis that the carbonyl oxygen of
1 is derived from water by exchange of an oxygen atom. Inhibition of the biosynthesis of
1 with tricyclazole, an inhibitor of the 1, 8-dihydroxynaphthalene (DHN) melanin biosynthesis, confirmed the connection of both biosynthetic pathways.
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AIQI FANG, GRACE K. WONG, ARNOLD L. DEMAIN
2000 Volume 53 Issue 2 Pages
158-162
Published: February 25, 2000
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Streptomyces hygroscopicus ATCC 29253 produces rapamycin, elaiophylin and nigericin. Although elaiophylin has no activity against
Candida albicans ATCC 11651, it markedly enhances rapamycin's antifungal activity. Nigericin has only weak activity on its own but it also enhances rapamycin action. Surprisingly, elaiophylin does not enhance nigericin activity on
C. albicans.
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II. Physico-chemical Properties and Structure Elucidation
SENJI TAKAHASHI, TAKAYUKI NAKANO, TSUKASA KOIWA, TOSHIRO NOSHITA, SHIN ...
2000 Volume 53 Issue 2 Pages
163-170
Published: February 25, 2000
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Adxanthromycins A and B are new inhibitors of ICAM-1/LFA-1 mediated cell adhesion molecule isolated from the fermentation broth of
Streptomyces sp. NA-148. The molecular formula of adxanthromycins A and B were determined as C
42H
40O
17 and C
48H
50O
22, respectively by FAB-MS and NMR spectral analyses, and the structures of both compounds were elucidated to be a dimeric anthrone peroxide skeleton containing α-D-galactose by various NMR spectral analyses and chemical degradation.
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LAWRENCE C. CREEMER, HERBERT A. KIRST, JONATHAN W. PASCHAL, THOMAS V. ...
2000 Volume 53 Issue 2 Pages
171-178
Published: February 25, 2000
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In an effort to increase the insecticidal activity of the spinosyn family of naturally occurring macrolides, the 2'-, 3'- and 4'-
O-desmethyl-
O-acetyl analogs and the 2'-, 3'-, and 4'
O-desmethoxy analogs have been synthesized. These analogs were prepared synthetically from the minor spinosyn factors H, J, K, L and Q either
via direct acylation of the corresponding factor or deoxygenation of an intermediate xanthate. The acylated analogs were all more potent insecticides against
Heliothis virescens larvae than their respective parent factors, but not as potent as spinosyns A or D. The deoxy analogs were also more potent insecticides than their respective parent factors. The 2'-desmethoxy analogs showed, for the first time, analogs with insecticidal potency against
H. virescens greater than that of spinosyns A and D, indicating that polarity is not well tolerated in the rhamnose moiety of spinosyn A.
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YOICHI HAYAKAWA, MASAAKI NAKAI, KEIKO FURIHATA, KAZUO SHIN-YA, HARUO S ...
2000 Volume 53 Issue 2 Pages
179-183
Published: February 25, 2000
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THOMAS DEGENKOLB, STEPHAN HEINZE, BRIGITTE SCHLEGEL, KLAUSJÜRGEN ...
2000 Volume 53 Issue 2 Pages
184-190
Published: February 25, 2000
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HAIYIN HE, BO SHEN, JOSEPH KORSHALLA, MARSHALL M. SIEGEL, GUY T. CARTE ...
2000 Volume 53 Issue 2 Pages
191-195
Published: February 25, 2000
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JUNKO WUCHIYAMA, MAKOTO KIMURA, ISAMU YAMAGUCHI
2000 Volume 53 Issue 2 Pages
196-200
Published: February 25, 2000
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VIDULA R. DIKSHIT, PRAGNA D. DESAI
2000 Volume 53 Issue 2 Pages
201-203
Published: February 25, 2000
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II. The Mechanism of Action
BUNJI SATO, HIDENORI NAKAJIMA, YASUHIRO HORI, MOTOHIRO HINO, SEIJI HAS ...
2000 Volume 53 Issue 2 Pages
204-206
Published: February 25, 2000
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KENJI NAGINO, HIROSHI SHIMOHIRA, MASATOSHI OGAWA, KATSUHISA UCHIDA, HI ...
2000 Volume 53 Issue 2 Pages
207-210
Published: February 25, 2000
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HACKRYONG KO, BO YEON KIM, WON KEUN OH, DAE OOK KANG, HYUN SUN LEE, HI ...
2000 Volume 53 Issue 2 Pages
211-214
Published: February 25, 2000
Released on J-STAGE: September 19, 2008
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