CHEMOTHERAPY
Online ISSN : 1884-5894
Print ISSN : 0009-3165
ISSN-L : 0009-3165
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Volume 33, Issue 11
Displaying 1-7 of 7 articles from this issue
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  • MODE OF ANTIMICROBIAL ACTIVITY OF AZTHREONAM (SQ 26, 776) ON GRAM-NEGATIVE ORGANISMS
    MICHIO OGAWA, NAOKI TAKATA, TAKESADA MORI, KAZUFUMI MITSUI, TAKESHI KI ...
    1985 Volume 33 Issue 11 Pages 963-968
    Published: November 25, 1985
    Released on J-STAGE: August 04, 2011
    DOIhttps://doi.org/10.11250/chemotherapy1953.33.963
    JOURNAL FREE ACCESS
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    The mode of antibacterial action of azthreonam (SQ 26, 776), a new synthetic monobactam, was investigated using E.coli K 12, P.aeruginosa KM 338 and S.marcescens IFO 12648, and was compared with that of cefazolin.
    The potent antibacterial activity of azthreonam against E.coli K 12 and S.marcescens IFO 12648 is concluded to be due to its high permeability of the outer membrane and the stability to hydrolysis by β-lactarnase. Compared with cefazolin, azthreonam also showed a stronger antimicrobial activity against P.aeruginosa KM 338, which is attributed to the higher permeability, the better stability to hydrolysis by β-lactamase and the higher sensitivity to the target enzymes of P.aeruginosa KM 338.
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  • STUDIES OF NITROSOUREA DERIVATIVES OF SUCROSE, 6-[[[(2-CHLOROETHYL) NITROSOAMINO] CARBONYL] AMINO]-6-DEOXYSUCROSE (NS-1C) AND 6'-[[[(2-CHLOROETHYL) NITROSOAMINO] CARBONYL] AMINO]-6'-DEOXYSUCROSE (NS-1D)
    I. ANTITUMOR EFFECTS ON MURINE TUMORS
    AKIRA TANOH, KEN-ICHI EDANAMI, KANKI KOMIYAMA, IWAO UMEZAWA, TETSUO SU ...
    1985 Volume 33 Issue 11 Pages 969-977
    Published: November 25, 1985
    Released on J-STAGE: August 04, 2011
    DOIhttps://doi.org/10.11250/chemotherapy1953.33.969
    JOURNAL FREE ACCESS
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    The antitumor activities of 6-[[[(2-chloroethyl)-nitrosoamino] carbonyl] amino]-6-deoxysucrose (NS-1C) and 6'-[[[(2-chloroethyl)-nitrosoamino] carbonyl] amino]-6'-deoxysucrose (NS-1D), novel watersoluble nitrosourea derivatives, against L 1210 leukemia, Lewis lung carcinoma, B-16 melanoma, IMC-carcinoma, sarcoma-180 and colon-38 were studied.
    Both NS-1C and NS-1D possessed significant antitumor activities against the above tumors. All mice with L 1210 leukemia cells were cured and survived for over 60 days when they were given a single injection of NS-1C or NS-1D at their optimal doses on day 1 after tumor inoculation. They were also effective against solid tumors.In particular, almost all mice with Lewis lung carcinoma and sarcoma-180 survived for over 60 days when they were given a single injection on day 1 and their activities were superior to 2-[3-(2-chloroethyl)-3-nitrosoureido]-D-glucopyranose (chlorozotocin) in ip treatment of Lewis lung carcinoma and to 1-(4-amino-2-methylpyrimidin-5-yl) methyl-3-(2-chlotoithyl)-3-nitrosourea (ACNU) in iv treatment of sarcoma-180.
    These findings suggest that both NS-1C and NS-1D possess
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  • STUDIES OF NITROSOUREA DERIVATIVE OF SUCROSE, 6'-[[(2-CHLOROETHYL) NITROSOAMINO] CARBONYL] AMINO-6'-DEOXYSUCROSE (NS-1D)
    II. EFFECTS ON MURINE PERIPHERAL BLOOD AND BONE MARROW
    AKIRA TANOH, KEN-ICHI EDANAMI, KANKI KOMIYAMA, IWAO UMEZAWA, TETSUO SU ...
    1985 Volume 33 Issue 11 Pages 978-983
    Published: November 25, 1985
    Released on J-STAGE: August 04, 2011
    DOIhttps://doi.org/10.11250/chemotherapy1953.33.978
    JOURNAL FREE ACCESS
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    The bone marrow toxicity of a new derivative of nitrosourea, 6'-[[[(2-chloroethyl) nitrosoamino] carbonyl]amino]-6'-deoxyaucrose (NS-1D) was studied in comparison with other nitrosoureas (ACNU, chlorosotocin and TA-077). When the drugs were injected ip into CDF1 mice at the optimal dose against L 1210 leukemia, the minimum counts of peripheral white blood cells (WBC) were observed three days after injection with all four drugs.The lowest WBC reductions were slight in mice treated by NS-1D and chlorosotocin (about 65% of the control), and these counts rapidly recovered.
    Bone marrow cellularity, bone marrow CFU-s and CFU-c were also investigated after injection of drugs.The bone marrow cellularity of NS-1D showed the lowest level one day after injection, recovered immediately and reached the normal level one week after injection. On the other hand, the bone marrow cellularities of the other nitrosoureas showed a minimum on day 3 and they also recovered rapidly like that of NS-1D, but one of them remained slightly depressed. Similar observations were obtained with CFU-c but CFU-s showed remarkable depression with all four nitrosoureas.
    These results indicated that the bone marrow toxicity of NS-1D was less and its recovery was more rapid than with other nitrosoureas.
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  • DISULFIRAM-LIKE REACTIONS RESULTING FROM ADMINISTRATION OF CEPHEMS WITH METHYLTETRAZOLETHIOL
    AN ANALYSIS OF LIVER ACETALDEHYDE DEHYDROGENASE ACTIVITY
    HISASHI NAKAHATA, YUICHI HIRAI, YOSHIHIRO KUMASAKA, TADASHI MIYAZAWA, ...
    1985 Volume 33 Issue 11 Pages 984-987
    Published: November 25, 1985
    Released on J-STAGE: August 04, 2011
    DOIhttps://doi.org/10.11250/chemotherapy1953.33.984
    JOURNAL FREE ACCESS
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    The mechanism of disulfiram-like reactions due to cephems with methyltetrazolethiol (LMOX and CPZ) was studied.
    Rats were intraperitoneally injected with these cephems (500mg/kg) for three days.
    After overnight fasting, blood samples were obtained following administration of 20% ethanol (2g/kg). the blood ethanol, acetaldehyde concentration, and liver acetaldehyde dehydrogenase activity (Enzyme 1, 2) were determined.
    In both groups of LMOX and CPZ blood ethanol concentration was not changed, but blood acetaldehyde contentration was markedly increased.
    Additionally, strong inhibition of acetaldehyde dehydrogenase activity was observed. And the activity of enzyme 1 which mainly metabolized acetaldehyde was reduced more strongly than that of enzyme 2.
    Therefore, it is concluded that disulfiram-like reactions due to cephems with methyltetrazolethiol could be caused by inhibition of liver acetaldehyde dehydrogenase activity, especially enzyme 1.
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  • DISULFIRAM-LIKE REACTIONS RESULTING FROM ADMINISTRATION OF CEPHEMS WITH METHYLTETRAZOLETHIOL IN THE RATS WITH LIVER DYSFUNCTION
    HISASHI NAKAHATA, YUICHI HIRAI, YOSHIHIRO KUMASAKA, TADASHI MIYAZAWA, ...
    1985 Volume 33 Issue 11 Pages 988-993
    Published: November 25, 1985
    Released on J-STAGE: August 04, 2011
    DOIhttps://doi.org/10.11250/chemotherapy1953.33.988
    JOURNAL FREE ACCESS
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    The influence of liver dysfunction on the disulfiram-like reactions due to cephems with methyltetrasolethiol was studied.
    The rats with fatty liver and cirrhosis were made by the administration of CCl4. Normal, fatty liver, and cirrhosis rats were injected intraperitoneally with these cephems (500mg/kg) for three days.After overnight fasting blood samples were obtained after 20% ethanol loading (2g/kg).Then, blood ethanol and acetaldehyde concentrations were determined.
    After the administration of latamoxef and cefoperazone with methyltetrazolethiol blood acetaldehyde concentration in fatty liver groups increased more remarkably than that in control groups. But after the administration of ceftizoxime without methyltetrazolethiol these findings were not observed.
    To investigate this mechanism, in cirrhosis rats liver acetaldehyde dehydrogenase activity was determined after the administration of cefoperazone.The activity (especially enzyme 1 which mainly metabolized acetaldehyde) was inhibited more strongly in cirrhosis groups than that in control groups.
    Based on these data, it is concluded that the degree of disulfiram-like reactions could be enhanced under the conditions of liver dysfunction.
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  • [title in Japanese]
    1985 Volume 33 Issue 11 Pages 994-995
    Published: November 25, 1985
    Released on J-STAGE: August 04, 2011
    DOIhttps://doi.org/10.11250/chemotherapy1953.33.994
    JOURNAL FREE ACCESS
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  • [title in Japanese]
    1985 Volume 33 Issue 11 Pages 995-1039
    Published: November 25, 1985
    Released on J-STAGE: August 04, 2011
    DOIhttps://doi.org/10.11250/chemotherapy1953.33.995
    JOURNAL FREE ACCESS
    Download PDF (7694K)
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