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Biomedical subjects

K Ninomiya

Publications and source records attributed to K Ninomiya.

At least 181 records · Page 10Linked to original sources

Biologic activity of MCNU: a new antitumor agent.

A novel nitrosourea derivative, methyl-6-[[[(2-chloroethyl)nitrosoamino]carbonyl]-amino]-6-deoxy-alpha-D-glucopyranoside (MCNU), is a water-soluble compound in which a methoxyl group is attached to the C-1 position and an N-(2-chloroethyl)-N-nitrosoureido group is attached to the C-6 position of the glucose moiety. MCNU exhibited a marked life-prolongation or growth-inhibitory effect against mouse L1210 leukemia, adenocarcinoma 755, Nakahara-Fukuoka sarcoma, Lewis lung carcinoma, and B16 melanoma. Ip, oral, or iv administration of MCNU was markedly effective against L1210 leukemia, and the therapeutic ratio by ip administration was larger than that of chlorozotocin or CCNU. The life-prolongation effect of MCNU against established Lewis lung carcinoma was similar to that of methyl-CCNU. The bone marrow toxicity of MCNU was less than that of CCNU but considerably more than that of chlorozotocin.

Adenocarcinoma↗

Alkyl streptozotocin analogues with improved biological activities.

Alkyl 16alpha- and -beta-glycosides of a series of N3-alkyl homologues of streptozotocin were synthesized from glucosamine hydrochloride. These compounds, when tested against ascites Sarcoma 180, Ehrlich ascites carcinoma, or leukemia L1210, exhibited potent antitumor activities, and antibacterial and diabetogenic activities were eliminated. Furthermore, the acute toxicities of these compounds were lower than that of streptozotocin. The methyl, ethyl, n-propyl, and n-butyl glycosides of streptozotocin, whether alpha- or beta-anomers, all showed higher antitumor activities than streptozotocin itself. The most active compound was found to be the methyl beta-streptozotocin.

Animals↗

[Antibacterial and bactericidal activity of tinidazole against anaerobic bacteria comparing with metronidazole (author's transl)].

Antibacterial activity of tinidazole (1-2-(ethylsulfonyl)-2-methyl-5-nitroimidazole) against anaerobic bacteria including Peptococcus, Peptostreptococcus, Eubacterium, Propionibacterium, Bacteroides and Fusobacterium was studied by agar dilution method comparing with metronidazole. In addition to this work, bactericidal effect of tinidazole and metronidazole against P. prevotii, B. fragilis ss. fragilis and F. varium was examined by quantitative culture method after incubation in GAM broth containing of 4 MIC, 2 MIC, 1 MIC and 1/2 MIC of both drugs against each of three strains for 1, 3, 6, 12 and 24 hours. All the strains of Peptococcus and Peptostreptococcus including P. anaerobius, P. saccharolyticus, P. prevotii and Ps. anaerobius and others were susceptible to a concentration of 6.25 mcg/ml of this drug. A concentration of 3.13 mcg/ml inhibited all strains of Bacteroides including B. fragilis ss. fragilis (12 strains), ss. vulgatus (5 strains), ss. thetaiotaomicron (4 strains) and ss. distasonis (2 strains). To this concentration all strains of Fusobacterium including F. varium (20 strains), F. mortiferum (2 strains) and other Fusobacterium sp. (5 strains) were susceptible. On the contrary, Propionibacterium acnes (6 strains) was resistant to 100 mcg/ml or more of tinidazole and metronidazole. The antibacterial activity of tinidazole was stronger against Bacteroides than that of metronidazole, while almost equal against Peptococcus, Peptostreptococcus, Eubacterium and Fusobacterium. Tinidazole was bactericidal against F. varium in a concentration of 2 MIC till 24 hours of incubation but did not show such an activity on B. fragilis ss. fragilis in same concentration even after 12 hours of incubation. On the other hand, metronidazole was bactericidal against B. fragilis ss. fragilis while was not against F. varium. Against P. prevotii bactericidal activity of both drugs was similar. Tinidazole as well as metronidazole is an excellent chemotherapeutic agent against anaerobic bacteria excluding Propionibacterium acnes and Bifidobacterium adolescentis.

Actinomycetaceae↗