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Predecessor
Volume 53, Issue 9
Displaying 1-17 of 17 articles from this issue
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I. Producing Strain, Fermentation, Isolation, Physico-chemical Properties and Biological ActivityYOSHINORI KANAI, DAISUKE ISHIYAMA, HISATO SENDA, WAKAO IWATANI, HIROKO ...2000 Volume 53 Issue 9 Pages 863-872
Published: September 25, 2000
Released on J-STAGE: September 19, 2008
JOURNAL FREE ACCESSIn the course of a screening program for specific inhibitors of human topoisomerase I using a recombinant yeast, we have discovered four new active compounds. All four compounds were isolated from the culture broth of a fungus, Phoma sp. BAUA2861, and two of them were isolated from the culture broth of a fungus, Penicillium sp. BAUA4206. We designated these compounds as topopyrones A, B, C and D.
Topopyrones A, B, C and D selectively inhibited recombinant yeast growth dependent on expression of human topoisomerase I with IC50 values of 1.22, 0.15, 4.88 and 19.63ng/ml, respectively. The activity and selectivity of topopyrone B were comparable to those of camptothecin. The relaxation of supercoiled pBR322 DNA by human DNA topoisomerase I was inhibited by these compounds, however they did not inhibit human DNA topoisomerase II. Topopyrones A, B, C and D were cytotoxic to all tumor cell lines when tested in vitro. Topopyrone B has potent inhibitory activity against herpesvirus, especially varicella zoster virus (VZV). It inhibited VZV growth with EC50 value of 0.038μg/ml, which is 24-fold stronger than that of acyclovir (0.9μg/rnl). Topopyrones A, B, and C were inhibitory to Grampositive bacteria.View full abstractDownload PDF (1327K) -
II. Structure ElucidationDAISUKE ISHIYAMA, YOSHINORI KANAI, HISATO SENDA, WAKAO IWATANI, HIROKO ...2000 Volume 53 Issue 9 Pages 873-878
Published: September 25, 2000
Released on J-STAGE: September 19, 2008
JOURNAL FREE ACCESSThe structures of novel topoisomerase I inhibitors, topopyrones A, B, C and D were elucidated by spectral analysis of the chemical derivatives. These compounds are an anthraquinone type containing a fused 1, 4-pyrone moiety. Topopyrones A and B contain a chlorine atom, however C and D do not. It was suggested that topopyrones B and D are converted from topopyrones A and C, respectively by Wessely-Moser type rearrangement.View full abstractDownload PDF (366K) -
Production, Isolation, Physico-chemical and Biological PropertiesFLORENZ SASSE, HEINRICH SIEINMETZ, JÜRGEN HEIL, GERHARD HÖFL ...2000 Volume 53 Issue 9 Pages 879-885
Published: September 25, 2000
Released on J-STAGE: September 19, 2008
JOURNAL FREE ACCESSNew cytostatic compounds, tubulysins, were isolated from the culture broth of strains of the myxobacteria Archangium gephyra and Angiococcus disciformis. The compounds are peptides partly consisting of unusual amino acids and are distantly related to the dolastatins. The tubuly sins were not active against bacteria and only little against fungi, but showed high cytostatic activity against mammalian cell lines with IC50 values in the picomolar range. An incubation with 50ng/ml tubulysin A led to a complete disappearance of the microtubuli network of the cells within 24 hours. The more active tubulysin D induced multipolar spindles: At 0.5ng/ml all mitotic cells showed more than four spindle poles.View full abstractDownload PDF (700K) -
NOBUO HOSOKAWA, HIROSHI NAGANAWA, MASA HAMADA, HIRONOBU IINUMA, TOMIO ...2000 Volume 53 Issue 9 Pages 886-894
Published: September 25, 2000
Released on J-STAGE: September 19, 2008
JOURNAL FREE ACCESSNew triene-ansamycins designated thiazinotrienomycins F (TT-F) and G (TT-G) and a new diene-ansamycin, benzoxazomycin, were isolated from a culture broth of Streptomyces sp. MJ672-m3 and their structures were elucidated by spectroscopic analyses. The Mean Graphs of TT-G suggests that the tumor growth inhibitory activities are almost as strong as TT-B, in respect of GI50 and TGI against several human cancer cell lines.View full abstractDownload PDF (463K) -
LIBRADA M. CAÑEDO HERNÁNDEZ, JESÚS ANGEL DE LA FU ...2000 Volume 53 Issue 9 Pages 895-902
Published: September 25, 2000
Released on J-STAGE: September 19, 2008
JOURNAL FREE ACCESSTwo new indolocarbazole alkaloids, 4'-N-methyl-5'-hydroxystaurosporine (2) and 5'-hydroxystaurosporine (3), were isolated together with the known staurosporine (1) from the culture broth of a marine Micromonospora sp. (strain L-31-CLCO-002). The fermentation, structural data and cytotoxic activities of these compounds against various tumor cell lines are given.View full abstractDownload PDF (517K) -
EUI-IL HWANG, BONG-SIK YUN, YOUNG-KOOK KIM, BYOUNG-MOG KWON, HONG-GI K ...2000 Volume 53 Issue 9 Pages 903-911
Published: September 25, 2000
Released on J-STAGE: September 19, 2008
JOURNAL FREE ACCESSPhellinsin A, a novel chitin synthases inhibitor was isolated from the cultured broth of fungus PL3, which was identified as Phellinus sp. PL3. Phellinsin A was purified by solvent partition, silica gel, ODS column chromatographies, and preparative HPLC, consecutively. The structure of phellinsin A was assigned as a phenolic compound on the basis of various spectroscopic analyses including Uy IR, Mass, and NMR. Its molecular weight and formula were found to be 358 and C18H14O8, respectively. Phellinsin A selectively inhibited chitin synthase I and II of Saccharomyces cerevisiae with an IC50 value of 76 and 28μg/ml, respectively, in our cell free assay system. This compound showed antifungal activity against Colletotrichum lagenarium, Pyricularia oryzae, Rhizoctonia solani, Aspergillus fumigatus, and Trichophyton mentagrophytes.View full abstractDownload PDF (660K) -
I. Taxonomy, Fermentation, Isolation, Physico-chemical Properties and Biological PropertiesAKIHIKO FUJIE, TOSHIRO IWAMOTO, HIDEYUKI MURAMATSU, TERUMI OKUDAIRA, K ...2000 Volume 53 Issue 9 Pages 912-919
Published: September 25, 2000
Released on J-STAGE: September 19, 2008
JOURNAL FREE ACCESSFR901469 is a novel antifungal antibiotic produced by an unidentified fungus No.11243. This compound was isolated from the culture broth by solvent extraction, HP-20 and YMC ODS gel column chromatography, and lyophilization. FR901469 is a white powder which melts at 182-187°C and possesses the molecular formula C71H116N14O23. This compound has good water solubility. FR901469 inhibited the activity of 1, 3-β-glucan synthase from Candida albicans with an IC50 value of 0.05μg/ml, and displayed greater inhibitory activity than other 1, 3-β-glucan synthase inhibitors such as, WF11899A, echinocandin B, aculeacin A, and papulacandin B.View full abstractDownload PDF (656K) -
II. In Vitro and In Vivo ActivitiesAKIHIKO FUJIE, TOSHIRO IWAMOTO, HIDEYUKI MURAMATSU, TERUMI OKUDAIRA, I ...2000 Volume 53 Issue 9 Pages 920-927
Published: September 25, 2000
Released on J-STAGE: September 19, 2008
JOURNAL FREE ACCESSFR901469 is a water-soluble macrocyclic lipopeptidolactone (C71H116N14O23) that has inhibitory activity against 1, 3-β-glucan synthase and exhibits in vitro and in vivo antifungal activity against both Candida albicans and Aspergillus fumigatus. The MICs of FR901469 against Candida albicans FP633 and Aspergillus fumigatus FP1305 in a micro-broth dilution test were 0.63 and 0.16μg/ml, respectively. FR901469 showed excellent efficacy by subcutaneous injection against both Candida albicans and Aspergillus fumigatus in a murine systemic infection mode, with ED50s of 0.32 and 0.2mg/kg, respectively. This compound also showed potent anti-Pneumocystis activity in the nude mice model with experimental Pneumocystis pneumonia. The hemolytic activity of FR901469 towards mouse red blood cells is about 30-fold weaker than that of amphotericin B.View full abstractDownload PDF (457K) -
YASUHIRO IGARASHI, YUKO KUWAMORI, KEIICHI TAKAGI, TOSHIHIKO ANDO, RYOS ...2000 Volume 53 Issue 9 Pages 928-933
Published: September 25, 2000
Released on J-STAGE: September 19, 2008
JOURNAL FREE ACCESSA new antifungal antibiotic xanthoepocin was isolated from the culture broth of Penicillium simplicissimum IFO5762. Xanthoepocin was obtained from the culture fluid by solvent extraction and chromatographic purification. It showed antibiotic activity against Grampositive bacteria and yeasts.View full abstractDownload PDF (363K) -
YUAN-QING TANG, ISABEL SATTLER, RALF THIERICKE, SUSANNE GRABLEY, XIAO- ...2000 Volume 53 Issue 9 Pages 934-943
Published: September 25, 2000
Released on J-STAGE: September 19, 2008
JOURNAL FREE ACCESSFour new lactone compounds, named feigrisolides A to D (1 to 4), have been isolated from Streptomyces griseus. The chemical structures were determined by detail analysis of their spectroscopic data and chemical transformations. Structurally, the feigrisolides A (1) and B (2) are hepta-lactones, feigrisolide C (3) and D (4) are 16-membered macrodiolides. Biological studies showed that feigrisolide B (2) exhibited strong antibacterial, as well as medium cyctotoxic, and antiviral activities. Feigrisolides A (1), C (3) and D (4) are medium inhibitors of 3α-hydroxysteroid-dehydrogenase (3α-HSD) inhibiting activity.View full abstractDownload PDF (764K) -
JIN-FENG HU, DIRK WUNDERLICH, ISABEL SATTLER, ALBERT HÄRTL, INA P ...2000 Volume 53 Issue 9 Pages 944-953
Published: September 25, 2000
Released on J-STAGE: September 19, 2008
JOURNAL FREE ACCESSChemical screening with extracts of Streptomyces sp. (strain GT 61150) resulted in the detection, isolation, and structure elucidation of two new acyl α-L-rhamnopyranosides (1 and 2) and three new rhamnosyllactones A, B1 and B2 (3-5). Rhamnosyllactones B1 and B2 were obtained as a 5:1 mixture. The structures were confirmed by spectroscopic analysis, especially 2D-NMR techniques. The rhamnosyltransferase of our strain is able to connect the sugar moiety to heteroaromatic carboxylic acids and enols. The metabolites 1 and 4/5 as well as previously reported acylrhamnosides 6-11 inhibit the enzyme 3α-hydroxysteroid-dehydrogenase (3α-HSD).View full abstractDownload PDF (576K) -
OH SUNG KWON, SANG HO PARK, BONG-SIK YUN, YU RYANG PYUN, CHANG-JIN KIM2000 Volume 53 Issue 9 Pages 954-958
Published: September 25, 2000
Released on J-STAGE: September 19, 2008
JOURNAL FREE ACCESSA diketopiperazine (1) has been isolated from the culture broth of Penicillium sp. F70614 and its structure has been determined to be cyclo(dehydroala-L-Leu) by various spectroscopic analyses. This compound selectively inhibited yeast α-glucosidase and porcine intestinal α-glucosidase with IC50 values of 35 and 50 μg/ml, respectively. However, it did not show significant inhibitory effects against almond β-glucosidase, Aspergillus α-galactosidase, Escherichia coli β-galactosidase and jack bean α-mannosidase.View full abstractDownload PDF (320K) -
TAKAYUKI SAWADA, MASAHIRO AONO, SEIICHI ASAKAWA, AKIRA ITO, KATSUYA AW ...2000 Volume 53 Issue 9 Pages 959-966
Published: September 25, 2000
Released on J-STAGE: September 19, 2008
JOURNAL FREE ACCESSA novel antibacterial substance, AB0022A, was isolated from the cellular slime mold Dictyostelium purpureum K1001. It inhibited the growth of Gram-positive bacteria, and its MICs ranged from 0.39 to 50 μg/ml. Because AB0022A was a highly substituted aromatic compound, we could not determine its structure based on only its physico-chemical and spectral data. We therefore used a dehalogenated derivative from AB0022A and deduced that its structure was l, 9-dihydroxy-3, 7-dimethoxy-2-hexanoyl-4, 6, 8-trichlorodibenzofuran. To confirm this structure, we synthesized the compound having the deduced structure. The synthetic compound was identical to naturally occurring AB0022A.View full abstractDownload PDF (554K) -
YUTAKA KOGUCHI, MAKI NISHIO, SHIN-ICHI SUZUKI, KOHEI TAKAHASHI, TETSUO ...2000 Volume 53 Issue 9 Pages 967-972
Published: September 25, 2000
Released on J-STAGE: September 19, 2008
JOURNAL FREE ACCESSDownload PDF (316K) -
BRIGITTE SCHLEGEL, UDO LUHMANN, ALBERT HÄRTL, UDO GRÄFE2000 Volume 53 Issue 9 Pages 973-974
Published: September 25, 2000
Released on J-STAGE: September 19, 2008
JOURNAL FREE ACCESSDownload PDF (131K) -
MARIKO NAKAMURA, SETSUKO KUNIMOTO, HATSUYA KAWASHIMA, TOMIO TAKEUCHI, ...2000 Volume 53 Issue 9 Pages 975-978
Published: September 25, 2000
Released on J-STAGE: September 19, 2008
JOURNAL FREE ACCESSDownload PDF (671K) -
KENJI UEDA, SHIHO KAWAI, HIRO-OMI OGAWA, AZUSA KIYAMA, TERUYOSHI KUBOT ...2000 Volume 53 Issue 9 Pages 979-982
Published: September 25, 2000
Released on J-STAGE: September 19, 2008
JOURNAL FREE ACCESSDownload PDF (531K)
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