Yasuo Fukagawa

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A new arylsulfatase designated Es-1, which desulfated etoposide 4'-sulfate and p-nitrophenyl sulfate, was isolated from Streptomyces griseorubiginosus S980-14 and purified to protein homogeneity by ammonium sulfate fractionation, ion exchange column chromatography, and chromatofocusing. The enzyme was active in monomeric form with an approximate molecular(More)
Accurate and precise component analysis of eurystatin analogs in fermentation broth was devised by HPLC methods with and without 2,4-dinitrophenylhydrazonation. Detailed optimization of fermentation conditions and strain improvement by HPLC analysis significantly increased the eurystatin productivity of Streptomyces eurythermus. Chemically defined(More)
Eurystatins A and B, which are produced by Streptomyces eurythermus R353-21, potently inhibited Flavobacterium prolyl endopeptidase (PED) with IC50 values of 0.004 and 0.002 micrograms/ml, respectively, while no inhibition was observed against another 5 proteases, even at 100 micrograms/ml. The protective effect of eurystatins A and B against scopolamine (3(More)
Rats were made dependent on morphine by mixing the drug with their only source of food. Naltrexone (0.5 mg/kg) injection precipitated a syndrome of withdrawal signs including weight loss. Pretreatment with the selective kappa agonist, U-50,488H (1.0, 30.0 or 10.0 mg/kg), generally had no effects on the signs of morphine withdrawal. In other subjects,(More)
Morphine dependence was induced by treatment with morphine-admixed food (0.25mg/g of food) for 7 days. Withdrawal was precipitated by injecting naloxone (0.5mg/kg, s.c.). Rats treated with morphine exhibited body weight loss upon the naloxone injection. When morphine-dependent rats were injected subcutaneously with morphine, codeine, meperidine and(More)
Chronic treatment with naloxone (Nx) or naltrexone (Ntx) induces paradoxical analgesia. In the present study, the effects of chronic treatment with opioid receptor antagonists, such as nor-binaltorphimine (nor-BNI) for kappa and naltrindole (NTI) for delta receptors, on analgesic response using the hot plate test and on morphine physical dependence in rats(More)
Chronic treatment of rats with naloxone for 5 days increased the analgesic threshold (hot plate latency). Further, when rats were treated with morphine-admixed food for 3 days after the chronic naloxone treatment the withdrawal signs precipitated by naloxone were significantly greater in the naloxone-pretreated rats than in saline-pretreated rats. These(More)
New 5-lipoxygenase inhibitors, designated epocarbazolins A and B, were isolated from the culture broth of Streptomyces anulatus T688-8. These compounds showed potent rat 5-lipoxygenase inhibitory activity with weak antibacterial activity. Structural studies revealed that epocarbazolins are new carbazole antibiotics having a novel substitution pattern and an(More)
BMY-28864 (BMS-181184), a water-soluble pradimicin derivative, specifically bound on the yeast cell surface in the presence of calcium, which was considered to be the initial step that triggered chain reactions leading to the fungicidal action. Close cause-effect relationships of the cell wall binding of BMY-28864 with its antifungal activity and potassium(More)