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K Nishimura

Publications and source records attributed to K Nishimura.

At least 1,117 records · Page 62Linked to original sources

Activation of macrophages by quinonyl-N-acetylmuramyl dipeptide.

The effect of 6-O-QS-10-N-acetylmuramyl-L-valyl-D-isoglutamine methyl ester (quinonyl-MDP-66) on various functions of macrophages was examined. Mouse peritoneal macrophages, when treated either in vitro or in vivo with quinonyl-MDP-66 suspended in phosphate-buffered saline, showed a capacity for cytolysis and cytostasis against tumor targets and released H2O2 in the presence of phorbol myristate acetate. The macrophages induced by quinonyl-MDP-66 also had both antibody-dependent cell-mediated cytotoxicity and phagocytic activity against erythroid targets. The fact that synthetic quinonyl-MDP-66 stimulates the macrophages to become more cytotoxic than do other MDP analogs suggests that the lipophilic residue (QS-10) in quinonyl-MDP-66 may be important for the development of this activity.

Acetylmuramyl-Alanyl-Isoglutamine↗

An adult case with rhabdomyosarcoma of the liver.

An autopsy case of primary rhabdomyosarcoma of the liver in a 70-year-old man is described. The case could not be clinically differentiated from hepatocellular carcinoma. The tumor showed typical features of rhabdomyosarcoma; phosphotungstic acid hematoxylin (PTAH)-positive myofibrils and cross-striations were observed in the cytoplasm of highly plemorphic tumor cells.

Aged↗

[Therapeutic efficacy of KS-R1, an ampicillin suppository, against experimental infections in mice].

In experimental infections induced with S. aureus, S. pneumoniae, E. coli, K. pneumoniae, P. mirabilis and H. influenzae in mice, the therapeutic efficacies of ampicillin (ABPC) after its rectal administration were compared with those obtained after its oral and subcutaneous administration, and the following results were obtained. Generally, in experimental intraperitoneal infections of mice, the effects of ABPC after rectal administration were inferior to those after subcutaneous administration and superior to those after oral administration. In experimentally induced intraperitoneal and urinary tract infection of E. coli KC-14, similar results were obtained. The plasma levels were reflected as the difference between various administration in the therapeutic efficacies observed with ABPC.

Administration, Oral↗

Macrophage activation with ubiquinones and their related compounds in mice.

The effect of ubiquinones (Q-2, -7 and -10) and their related compounds (QSA-1, -4, -6, -10 and -18) on macrophage functions was investigated. All compounds tested in this study, except QSA-4 and -6, augmented macrophage-mediated functions such as cytolysis, cytostasis and H2O2 release. Furthermore, QSA-10 and QSA-10(H2) were also shown to increase antibody-dependent cell-mediated cytotoxicity. However, QSA-10(Phenol), which lacks a quinone ring, was not observed these activities. It was suggested that quinone ring might be important for the expression of macrophage activation.

Animals↗

[Pharmacokinetics of an ampicillin suppository (KS-R1) in mice, rats and rabbits].

KS-R1, a new suppository of ampicillin (ABPC) sodium, was rectally administered to study its absorption, excretion and distribution in mice, rats and rabbits. Concentrations of ABPC in plasma when 12.5 and 25.0 mg/kg of KS-R1 were rectally administered to experimental animals reached the peak levels rapidly. The values were 7.3 and 13.9 micrograms/ml in mice, 7.7 and 15.9 micrograms/ml in rats, and 14.1 and 35.3 micrograms/ml in rabbits, respectively. All of these values were about 3.5 times as high as those attained by oral administration of the same doses. Concentrations of ABPC in tissues when 25.0 mg/kg of KS-R1 was rectally administered to rats reached the peak level rapidly, as in the concentration in plasma. The concentrations distributed into various tissues were found as follows; liver not equal to kidney greater than spleen greater than heart greater than lung. Urinary recoveries of ABPC after rectal administration of 12.5 and 25.0 mg/kg were 23.4 and 28.4% (0 approximately 12 hours) in rats while 79.4 and 75.4% (0 approximately 6 hours) in rabbits, respectively. When 25.0 mg/kg of KS-R1 was administered to rats, 10.7% of the dose was excreted into bile during 6 hours after administration. The relative bioavailabilities of KS-R1, calculated on the basis of AUC and urinary recovery after parenteral administration of ABPC sodium, were 81.0 to 87.5% in mice, 37.6 to 45.9% in rats and 75.6 to 101% in rabbits, which were 1.5 to 2.8 times higher than those of ABPC orally administered.

Administration, Oral↗

[Absorption and excretion of an ampicillin suppository (KS-R1) in dogs].

KS-R1, a new suppository of ampicillin (ABPC) sodium, was compared with the widely used oral ABPC and parenteral ABPC sodium in terms of absorption and excretion in mature and infant Beagle dogs. Plasma levels of ABPC in mature dogs when administered rectally with 12.5 and 25.0 mg/kg of KS-R1 reached the respective peaks of 8.0 and 13.5 micrograms/ml in 10 to 20 minutes. Thereafter, the plasma levels declined with biological half-lives of 0.72 and 0.93 hours, respectively. During the first 6 hours after administration of 12.5 mg/kg, 14.3% of the dose was excreted in urine. The relative bioavailability of KS-R1, calculated on the basis of AUC and urinary recovery after intramuscular administration of ABPC sodium, was 23.1% to 28.9%, compared with 31.1% to 50.2% in the case of oral ABPC. Plasma levels of ABPC in infant dogs rectally administered with 12.5 mg/kg of KS-R1 reached 11.9 microgram/ml in 10 minutes, and then declined with biological half-life of 1.24 hours. During the first 6 hours after rectal administration, 31.9% of the dose was recovered in the urine. The relative bioavailability of KS-R1 in infant dogs was 53.8% to 58.0%, which was better than that of mature dogs and was equal to that of oral ABPC. In the case of multiple doses of KS-R1 to mature dogs, no remarkable difference was found in concentration in plasma, and no accumulation of ABPC was demonstrated. Macroscopically, no remarkable abnormality was found at all around the sites of continuous administration.

Administration, Oral↗

[Effects of rectal administration of an ampicillin suppository (KS-R1) on cecal microflora and cecal weight in mice].

KS-R1 is a new rectal preparation of ampicillin (ABPC) sodium. Changes of cecal microflora, changes of cecal weight and ABPC concentrations in the cecum after rectal administration of KS-R1 to mice were compared with those after oral and subcutaneous administration of ABPC. When KS-R1 was administered to mice by 25.0 mg/kg 3 times a day for 10 days continuously, a little changes were observed in the number of Enterobacteriaceae, Staphylococcus and Lactobacillus in the cecum. However, at the fifth day after completing the rectal administrations, normal level of microflora was gained. This change of microflora closely resemble those in case when ABPC sodium was administered subcutaneously. On the other hand, when ABPC was administered orally, changes of microflora were large, i.e. the number of Enterobacteriaceae and Streptococcus increased remarkably, the number of Fusobacterium increased and the number of Staphylococcus and Bacteroides decreased. Recovery of normal level of microflora was late. The cecal weight did not show changes but the increase observed in the case when ABPC was orally administered. This increase was due to the increase of moisture in the cecum. The concentrations of ABPC in the cecum when administered by 25.0 mg/kg were in the order of oral administration greater than rectal administration (KS-R1) greater than subcutaneous administration. The highest concentrations were respectively 219.6, 54.1 and 5.1 micrograms/g. Changes of microflora in the cecum was great in proportion to the concentrations of ABPC.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Oral↗