著者
KIMBERLY D. MCBRIEN RONALD L. BERRY SUSAN E. LOWE KIM M. NEDDERMANN ISIA BURSUKER STELLA HUANG STEVEN E. KLOHR JOHN E. LEET
出版者
JAPAN ANTIBIOTICS RESEARCH ASSOCIATION
雑誌
The Journal of Antibiotics (ISSN:00218820)
巻号頁・発行日
vol.48, no.12, pp.1446-1452, 1995-12-25 (Released:2006-04-19)
参考文献数
6
被引用文献数
22 or 0

The new cytotoxic agents rakicidins A and B were isolated from cultured broth of a Micromonospora sp. Spectroscopic and amino acid analysis has shown that rakicidin A is a new cyclic lipopeptide, consisting of 4-amino-penta-2, 4-dienoic acid, 3-hydroxy-2, 4, 16-trimethylheptadecanoic acid, sarcosine, and 3-hydroxyasparagine. Rakicidin B differs by one methylene group in the lipid side chain. These compounds exhibited cytotoxicity against the Ml09 cell line.
著者
TORU KINO HIROSHI HATANAKA SUSUMU MIYATA NORIAKI INAMURA MICHIHISA NISHIYAMA TOSHIMI YAJIMA TOSHIO GOTO MASAKUNI OKUHARA MASANOBU KOHSAKA HATSUO AOKI TAKENORI OCHIAI
出版者
JAPAN ANTIBIOTICS RESEARCH ASSOCIATION
雑誌
The Journal of Antibiotics (ISSN:00218820)
巻号頁・発行日
vol.40, no.9, pp.1256-1265, 1987-09-25 (Released:2006-04-19)
参考文献数
16
被引用文献数
241 or 0

The immuno-pharmacological profile of a novel immunosuppressive agent, FK-506 produced by a streptomycete, is presented here. We proceeded to test the effect of the agent on various in vitro immune systems. It showed that mixed lymphocyte reaction, cytotoxic T cell generation, the production of T cell-derived soluble mediators such as interleukin 2 (IL-2), interleukin 3 and gamma-interferon and the expression of the IL-2 receptor were suppressed by this agent. The IC50 values of FK-506 and ciclosporin (CS) in all tests were approximately 0.1nM and 10nM, respectively. Therefore, the novel agent, FK-506 suppressed in vitro immune systems at about hundred times lower concentration than CS.
著者
CLAUDE VÉZINA ALICIA KUDELSKI S. N. SEHGAL
出版者
JAPAN ANTIBIOTICS RESEARCH ASSOCIATION
雑誌
The Journal of Antibiotics (ISSN:00218820)
巻号頁・発行日
vol.28, no.10, pp.721-726, 1975 (Released:2006-04-12)
参考文献数
6
被引用文献数
244 or 0

A streptomycete was isolated from an Easter Island soil sample and found to inhibit Candida albicans, Microsporum gypseum and Trichophyton granulosum. The antibioticproducing microorganism was characterized and identified as Streptomyces hygroscopicus. The antifungal principle was extracted with organic solvent from the mycelium, isolated in crystalline form and named rapamycin. Rapamycin is mainly active against Candida albicans; minimum inhibitory concentration against ten strains ranged from 0.02 to 0.2 μg/ml. Its apparent activity against Microsporum gypseum and Trichophyton granulosum is lower because of its instability in culture media on prolonged incubation required by these fungi. No activity was observed against gram-positive and gram-negative bacteria. Acute toxicity in mice is low.
著者
MASARU YOSHIDA MASAMI EZAKI MICHIZANE HASHIMOTO MICHIO YAMASHITA NOBUHARU SHIGEMATSU MASAKUNI OKUHARA MASANOBU KOHSAKA KOKI HORIKOSHI
出版者
JAPAN ANTIBIOTICS RESEARCH ASSOCIATION
雑誌
The Journal of Antibiotics (ISSN:00218820)
巻号頁・発行日
vol.43, no.7, pp.748-754, 1990-07-25 (Released:2006-04-19)
参考文献数
12
被引用文献数
46 or 0

Streptoverticillium fervens produced a new antibiotic, FR-900848, which has a high specific activity against filamentous fungi. Purified by solvent extraction and column chromatography, the compound appears as colorless crystals. Its structure is C32H43N3O6, which consists of 5'-amino-5'-deoxy-5, 6-dihydrouridine with an unsaturated fatty acid having unprecedented four serial and one isolated cyclopropane rings.
著者
YASUHIRO IGARASHI KATSUYUKI FUTAMATA TSUYOSHI FUJITA AKIRA SEKINE HISATO SENDA HIDEO NAOKI TAMOTSU FURUMAI
出版者
JAPAN ANTIBIOTICS RESEARCH ASSOCIATION
雑誌
The Journal of Antibiotics (ISSN:00218820)
巻号頁・発行日
vol.56, no.2, pp.107-113, 2003-02-25 (Released:2009-01-27)
参考文献数
9
被引用文献数
38 or 0

In the screening of novel antifungal compounds, yatakemycin was found in the culture broth of Streptomyces sp. TP-A0356. Yatakemycin was obtained by solvent extraction of the fermentation broth and chromatographic purification using ODS column and preparative HPLC. The structure of yatakemycin was elucidated by NMR and CID-MS/MS experiments as a novel antibiotic belonging to a family of CC-1065 and duocarmycins known to be DNA alkylating agents. Yatakemycin inhibited the growth of pathogenic fungi such as Aspergillus fumigatus and Candida albicans with the MIC values of 0.01-0.03μg/ml, more potent than amphotericin B (MIC: 0.1-0.5μg/ml) or itraconazole (MIC: 0.03-0.2μg/ml). It also showed potent cytotoxicity against cancer cell lines with the IC50 of 0.01-0.3μg/ml.
著者
S. N. SEHGAL H. BAKER Claude VÉZINA
出版者
JAPAN ANTIBIOTICS RESEARCH ASSOCIATION
雑誌
The Journal of Antibiotics (ISSN:00218820)
巻号頁・発行日
vol.28, no.10, pp.727-732, 1975 (Released:2006-04-12)
参考文献数
7
被引用文献数
42 or 0

Rapamycin is a new antifungal antibiotic produced by Streptomyces hygroscopicus NRRL 5491. It was isolated from the mycelium by solvent extraction, purified by silica gel column chromatography and crystallized as a colorless solid which melts at 183-185°C and has the empirical formula C56H89NO14. From its characteristic ultraviolet absorption spectrum rapamycin can be classified as a triene. It is highly active against various Candida species, especially Candida albicans. Its activity is compared with that of amphotericin B, candicidin and nystatin.
著者
KAYOKO SUZUKAKE-TSUCHIYA MAKOTO HORI NOBUYOSHI SHIMADA MASA HAMADA
出版者
JAPAN ANTIBIOTICS RESEARCH ASSOCIATION
雑誌
The Journal of Antibiotics (ISSN:00218820)
巻号頁・発行日
vol.41, no.5, pp.675-683, 1988-05-25 (Released:2006-04-19)
参考文献数
6
被引用文献数
3 or 0

Deoxypheganomycin D, a specific inhibitor of mycobacteria, inhibits the growth in vitro of Mycobacterium smegmatis ATCC 607 (M. 607) bacteriostatically at concentrations as high as 7×10-5M. It shows no cross-resistance to paromomycin, capreomycin, viomycin, streptothricin, kanamycin and streptomycin. Deoxypheganomycin D at 2.8×10-7M where the cell growth of M. 607 is only partially inhibited does not significantly inhibit DNA, RNA or protein synthesis but leads to marked decrease (13 % of control) in [14C]glycerol-derived radioactivity in cell-walls. In the presence of 7×10-6M deoxypheganomycin D, the influx of leucine but not thymidine is affected while the reverse is true with efflux. The data suggest that the effect of deoxypheganomycin D on M. 607 may be related to both the cell membrane and specific mycobacterial lipid like components of the cell-wall.
著者
KIYOSHI TSUJI JOHN F. GOETZ
出版者
JAPAN ANTIBIOTICS RESEARCH ASSOCIATION
雑誌
The Journal of Antibiotics (ISSN:00218820)
巻号頁・発行日
vol.31, no.4, pp.302-308, 1978 (Released:2006-04-12)
参考文献数
16
被引用文献数
27 or 0

Reverse phase high performance liquid chromatography (HPLC) was used as a rapid means of monitoring the erythromycin and the tetracycline fermentation processes. The sample preparation process for tetracycline in the fermentation broth includes simple dilution and filtration through a Millipore filter prior to injection into the HPLC column. Fermentation broth samples showed no interference, and excellent separation for selective determination of tetracycline, 4-epitetracycline, anhydrotetracycline, chlortetracycline, and 4-epianhydrotetracycline was obtained. The relative standard deviation for the HPLC analysis for tetracycline is about one percent and the correlation coefficient between the HPLC and the spectrophotometric assay methods is better than 0.994.The sample preparation procedure for erythromycin determination in fermentation broth requires solvent cleanup and extraction processes. The chromatographic analysis takes approximately 25 minutes, and the HPLC method is capable of separating and quantifying erythromycins A, B, C, and various epimers and degradation compounds. The correlation coefficient between the HPLC and the microbiological assay method is 0.970.
著者
MIKIO SAWADA TOMOYOSHI HOSOKAWA TSUNEO OKUTOMI KUNIO ANDO
出版者
JAPAN ANTIBIOTICS RESEARCH ASSOCIATION
雑誌
The Journal of Antibiotics (ISSN:00218820)
巻号頁・発行日
vol.26, no.11, pp.681-686, 1973-11-25 (Released:2006-04-12)
参考文献数
15
被引用文献数
24 or 0

Ascofuranone significantly reduced serum lipid levels of rats fed with normal diet 6 hours after a single oral administration of 108 mg/kg. When the antibiotic was orally given for consecutive 10 days to normolipidemic rats, the treatment resulted in marked reduction of serum cholesterol, triglycerides, phospholipids and free fatty acids without affecting organ weight gain, serum total protein, albumin/globulin ratio and serum transaminases. Reduction was also noted with cardiac cholesterol content but liver total sterol and fecal sterol excretion were unchanged. Acute toxicity of ascofuranone is weak to mice and rats and the antibiotic did not induce hepatomegaly which is the main side effect of a positive control agent, ethyl-p-chlorophenoxyisobutyrate.
著者
JUNJI MAGAE JUNICHI HAYASAKI YUKO MATSUDA MITSUYUKI HOTTA TOMOYOSHI HOSOKAWA SEIKICHI SUZUKI KAZUO NAGAI KUNIO ANDO GAKUZO TAMURA
出版者
JAPAN ANTIBIOTICS RESEARCH ASSOCIATION
雑誌
The Journal of Antibiotics (ISSN:00218820)
巻号頁・発行日
vol.41, no.7, pp.959-965, 1988-07-25 (Released:2006-04-19)
参考文献数
20
被引用文献数
34 or 0

Ascofuranone demonstrated antitumor activity against FM3A murine mammary carcinoma, implanted in the peritoneal cavity of syngeneic mice, C3H/He. It was more effective by treatment prior to implantation than by that after implantation. Treatment with ascofuranone also increased splenic cytotoxicity and phagocytic activity of host animal cells. Moreover, ascofuranone induced inflammatory cells in the peritoneal cavity which are mainly composed of polymorpho-nuclear leukocytes and macrophages. These cells are more potent in cytotoxicity against FM3A cells than with resident peritoneal cells. The antitumor activity of ascofuranone was suppressed by ip administration of silica, just prior to tumor implantation. These results suggest that the prophylactic antitumor activity of ascofuranone is expressed through the activation of phagocytes. Ascofuranone also suppressed pulmonary metastasis of B16 melanoma and Lewis lung carcinoma. Treatment after tumor implantaion failed to suppress the metastasis. Single treatment of ascofuranone 4 days prior to implantation decreased the metastasis of Lewis lung carcinoma but not that of B16, whereas single treatment of ascofuranone 24 hours prior to the tumor implantation decreased the metastasis of B16 but not that of Lewis lung carcinoma.
著者
HIROSHI SASAKI TOMOYOSHI HOSOKAWA MIKIO SAWADA KUNIO ANDO
出版者
JAPAN ANTIBIOTICS RESEARCH ASSOCIATION
雑誌
The Journal of Antibiotics (ISSN:00218820)
巻号頁・発行日
vol.26, no.11, pp.676-680, 1973-11-25 (Released:2006-04-12)
参考文献数
15
被引用文献数
43 or 0

A new antibiotic with hypolipidemic activity, ascofuranone, C23H29C1O5, and related substance, ascofuranol, C23H31C1O5, were isolated from the filter cake of the fermented broth of Ascochyta viciae LIBERT, an ascochlorin-producing fungus, and their structures were elucidated. They possess 3-substituted-5-chloro-orcylaldehyde moiety with novel sesquiterpenyl side chains.
著者
JEAN-JACQUES SANGLIER VALERIE QUESNIAUX THEODOR FEHR HANS HOFMANN MARION MAHNKE KLAUS MEMMERT WALTER SCHULER GERHARD ZENKE LILIANE GSCHWIND CLAUDINE MAURER WOLFGANG SCHILLING
出版者
JAPAN ANTIBIOTICS RESEARCH ASSOCIATION
雑誌
The Journal of Antibiotics (ISSN:00218820)
巻号頁・発行日
vol.52, no.5, pp.466-473, 1999-05-25 (Released:2008-09-19)
参考文献数
20
被引用文献数
52 or 105

A novel class of macrolides for which the name sanglifehrins is proposed, has been discovered from actinomycete strains based on their high affinity binding for cyclophilin A (CypA), an immunophilin originally identified as a cytosolic protein binding cyclosporin A (CsA). The sanglifehrins were produced by Streptomyces sp. A92-308110. They were isolated and purified by extraction and several chromatographic, activity-guided steps. Sanglifehrins A and B exhibit a 10-20 fold higher affinity for CypA than CsA, whereas the affinity of sanglifehrins C and D for CypA is comparable to that of CsA. Sanglifehrins exhibit a lower immunosuppressive activity than CsA when tested in the mixed lymphocyte reaction. Their in vitro activity indicates that they belong to a novel class of immunosuppressants.
著者
AKIRA TSUJI HIDEKI HIROOKA IKUMI TAMAI TETSUYA TERASAKI
出版者
JAPAN ANTIBIOTICS RESEARCH ASSOCIATION
雑誌
The Journal of Antibiotics (ISSN:00218820)
巻号頁・発行日
vol.39, no.11, pp.1592-1597, 1986 (Released:2006-04-19)
参考文献数
18
被引用文献数
12 or 0

Transport of a new cephalosporin developed for oral use, FK089, has been studied with the rat everted small intestine in vitro. Uptake was found to be pH-dependent with the maximum rate at an acidic pH below 5 and with a 5-fold lower rate at pH 7.0. The shape of the pH-rate profile was very similar to that of cefixime and different from that of pH-lipophilicity profile of FK089. The saturation kinetics of the uptake of FK089 were demonstrated at pH 5.0. By correcting the nonsaturable rate process, the kinetics of the mutual inhibition of FK089 uptake by cefixime and cefixime uptake by FK089 were all consistent with competitive type inhibition. The results indicate that carrier-mediated transport is responsible for transport of cephem antibiotics without an α-amino group in the side chain at the 7-position of the cephem nucleus in the intestinal brush-border membrane.