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Biomedical subjects

M Komiya

Publications and source records attributed to M Komiya.

At least 19 recordsLinked to original sources

Antigenicities of enteropathogenic Escherichia coli, lysozyme, and alpha-1-antichymotrypsin on macrophages of genitourinary malacoplakia.

Seven cases of genito-urinary malacoplakia were analyzed histologically, ultrastructurally and immunohistochemically in a comparison with two cases of xanthogranulomatous pyelonephritis. Immunohistochemically, von Hansemann cells and Michaelis-Guttmann bodies, both hallmarks for the diagnosis of malacoplakia, showed a common antigenicity for enteropathogenic Escherichia coli as cytoplasmic granules of varying sizes. These microscopic manifestations corresponded ultrastructurally to a series of phagolysosomal degradations of coliform bacilli. Serogroups against E. coli OK antigens, which were positive for malacoplakic cells, were not confined to a particular group. Macrophages of xanthogranulomatous pyelonephritis did not show the E. coli antigenicity. Antigenicity of lysozyme and alpha-1-antichymotrypsin on the von Hansemann cells was equivocal, but these enzymes were strongly positive on macrophages of xanthogranulomatous pyelonephritis. The macrophages of both malacoplakia and xanthogranulomatous pyelonephritis were positive for antihuman macrophage antibody. These results indicate that malacoplakia depends mainly on infection by a non-specific strain of enteropathogenic E. coli and may arise from defective digestive enzyme activity of infiltrating macrophages. Immunohistochemical analysis using antisera against E. coli OK antigens, lysozyme and alpha-1-antichymotrypsin was useful in identifying the prediagnostic stage of malacoplakia and in differentiating the lesion from xanthogranulomatous pyelonephritis.

Adult

Cefadroxil concentrations in human serum, gingiva, and mandibular bone following a single oral administration.

Cefadroxil concentrations in human serum, gingiva, and mandibular bone were measured by a paper disk method following a single 500-mg oral dose. The mean peak concentrations in serum, gingiva, and mandibular bone occurred at the identical time, 3 hours, and were 12.92 micrograms/mL, 6.50 micrograms/g, and 2.67 micrograms/g, respectively. Mean cefadroxil concentration ratios of gingiva/serum and mandibular bone/serum at the peak time were 0.54 and 0.21, respectively. Mean concentrations in gingiva and mandibular bone at the peak time exceeded the minimum inhibitory concentrations for 90% of clinically isolated strains of a alpha-hemolytic streptococci.

Absorption

Amoxicillin concentration in pus from abscess caused by odontogenic infection.

1. Amoxicillin concentration in pus from odontogenic infection was assayed and the concentrations were compared with MIC (minimum inhibitory concentration) of alpha-hemolytic streptococci isolated from odontogenic infection. 2. Measurable amoxicillin concentrations in serum and pus were found in all instances (n = 16). 3. The mean peak concentrations in serum and pus were found at identical times, 1.5 hr after administration, which were 5.92 and 0.90 micrograms/ml, respectively. 4. The mean concentration ratio of pus/serum at the peak time was 0.15. 5. All amoxicillin concentrations in pus at the peak time exceeded the MIC for 90% of alpha-hemolytic streptococci (0.25 micrograms/ml).

Administration, Oral

Cephalexin concentrations in radicular granuloma following a single oral administration of 250- or 500-mg cephalexin.

1. Cephalexin concentrations in radicular granuloma and serum following a single oral administration of 250- or 500-mg cephalexin were measured by a paper disk method. 2. The highest concentration of cephalexin in radicular granuloma following administration of 250-mg cephalexin to nonfasting patients was observed at 2 hr, and was 1.62 micrograms/g. The mean cephalexin concentration ratio of radicular granuloma/serum at 2 hr was 0.35. 3. The highest concentrations of cephalexin in radicular granuloma following administration of 500-mg cephalexin to nonfasting and fasting patients occurred at 2 and 1.5 hr, and was 3.35 and 3.42 micrograms/g, respectively. Mean cephalexin concentration ratios of radicular granuloma/serum at 2 and 1.5 hr were 0.32 and 0.30, respectively. 4. All mean cephalexin concentrations in radicular granuloma following administration of 500-mg cephalexin to both fasting and nonfasting patients exceeded MIC for 90% (2 micrograms/ml) of clinically isolated strains of alpha-hemolytic streptococci. However, those concentrations obtained by 250-mg cephalexin did not exceed it.

Adult

Pharmacologic properties of a novel Ca2+ entry blocker, AJ-2615, in vitro.

We studied the in vitro vascular relaxant properties of AJ-2615, (+/-)-N-[6,11-dihydrodibenzo[b,e]-thiepin-11-yl]-4-[4- fluorophenyl]-1-piperazinebutanamide monomaleate, a novel compound with long-lasting antihypertensive activity. AJ-2615 inhibited the high K(+)-induced contractile response in rat aorta with an IC50 of 2.08 x 10(-8) M. It was 13 times less potent than nifedipine and 3, 10, and 15 times more potent than verapamil, diltiazem, and fluanarizine, respectively. AJ-2615 also inhibited the high K(+)-induced 45Ca influx in rat aorta at almost the same concentration as that for inhibition of the contractile response. The inhibition of 45Ca influx was reversed by Bay k 8644, a Ca2+ channel agonist. The effects of AJ-2615 on the contractile response and Ca2+ influx persisted for at least 120 min after AJ-2615 was removed from the medium. These results indicate that AJ-2615 acts directly on the potential-dependent Ca2+ channel in a long-lasting manner. AJ-2615 inhibited [3H]prazosin binding to dog aortic membranes (IC50 = 1.25 x 10(-8) M) and phenylephrine-induced contractile response in superior mesenteric artery (SMA) of rabbits (IC50 = 3.87 x 10(-8) M), indicating that AJ-2615 has potent alpha 1-adrenoceptor blocking activity. AJ-2615 at 10(-6) M did not inhibit the caffeine-induced contractile response in rabbit SMA in Ca(2+)-free medium, nor did it inhibit calmodulin (CAM) activity.(ABSTRACT TRUNCATED AT 250 WORDS)

3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethy

Concentrations of lomefloxacin in radicular cyst and oral tissues following single or multiple oral administration.

Concentrations of lomefloxacin in serum, the wall and fluid of radicular cyst, gingiva, and jawbone following single or multiple oral administration were measured. The highest concentrations of lomefloxacin in serum, cyst wall, cyst fluid, gingiva, and jawbone occurred at 3 h after multiple administration, and were 2.31 micrograms/ml, 4.06 micrograms/g, 1.54 micrograms/ml, 4.72 micrograms/g and 2.79 micrograms/g, respectively. The mean concentration ratios of wall/serum, fluid/serum, fluid/wall, gingiva/serum, and jawbone/serum at the highest concentrations were 1.74, 0.73, 0.47, 2.52 and 1.20, respectively. Although most lomefloxacin concentrations in cyst and oral tissues following single oral administration did not exceed the MICs for 80% of clinically isolated strains of alpha-hemolytic streptococci, Staphylococcus aureus and Niesseria spp., most of those obtained after multiple oral administration exceeded the MICs except in the case of fluid.

Adult

An ultrathin frozen section is suitable for demonstrating cytochrome c oxidase activity at electron microscopic level.

Cytochrome c oxidase activity in rat liver was demonstrated in 40 microns sections and ultrathin frozen sections (100-200 nm in thickness), using the diaminobenzidine method. Electron microscopic observations showed strong activity in 81.9 +/- 13.1% of mitochondria along the edge, and 29.9 +/- 21.2% in the center of 40 microns sections. On the other hand, all mitochondria possessed strong activity in ultrathin frozen sections under the same experimental condition. In the ultrathin frozen section, the mitochondrial membranes, as well as the plasma membrane, were broken. The present study indicates that the ultrathin frozen section is suitable for demonstrating cytochrome c oxidase activity at electron microscopic level.

Animals

Cefaclor concentrations in human serum, gingiva, mandibular bone, and dental follicle following a single oral administration.

1. Cefaclor concentrations in human serum (n = 59), gingiva (n = 46), mandibular bone (n = 39), and dental follicle (n = 42) following a single oral administration of cefaclor (500 mg) were measured by the paper disk method. 2. The peak times of serum, gingiva, mandibular bone, and dental follicle were 1.5, 2, 2, and 1.5 hr, respectively. 3. The mean peak concentrations of serum, gingiva, mandibular bone, and dental follicle were 7.58 micrograms/ml, 3.71, 1.59 and 2.42 micrograms/g, respectively. 4. The concentration ratios of gingiva/serum, mandibular bone/serum, and dental follicle/serum at peak times of the tissues were 0.49, 0.18, and 0.32, respectively. 5. Mean cefaclor concentrations in gingiva, mandibular bone, and dental follicle at peak times exceeded MIC for 90% for clinically isolated strains of alpha-hemolytic Streptococci.

Administration, Oral

Formation of reductive metabolite, 2-sulfamoylacetylphenol, from zonisamide in rat liver microsomes.

Zonisamide (1,2-benzisoxazole-3-methanesulfonamide) was metabolized to its reductive product, 2-sulfamoylacetylphenol, in rat liver microsomes under anaerobic conditions. The rate of NADPH-dependent reaction was much more rapid than that of NADH-dependent reaction. Furthermore, synergistic effect of NADH on NADPH-dependent reaction was not observed. The optimal formation of 2-sulfamoylacetylphenol from zonisamide in the presence of NADPH was observed around pH 7.0. Cimetidine showed an inhibitory effect on the formation of 2-sulfamoylacetylphenol in a dose-dependent manner. The reductive metabolism of zonisamide was almost completely inhibited by carbon monoxide, and was increased by pretreatment of rats with phenobarbital and pregnenolone 16 alpha-carbonitrile but not by pretreatment with ethanol, 3-methylcholanthrene and imidazole. These results suggest that phenobarbital- and pregnenolone 16 alpha-carbonitrile-inducible form(s) of cytochrome P-450 is responsible for the reductive metabolism of zonisamide to 2-sulfamoylacetylphenol in rat liver microsomes.

Anaerobiosis

Improvement of 5-HT3 receptor binding assay: enhancement of specific [3H]quipazine binding with Triton X-100-treated membranes from rat cortex.

The 5-hydroxytryptamine (5-HT)3 receptor binding assay using [3H]quipazine was examined. It was impossible to obtain specific [3H]quipazine binding with the membrane fractions from rat cortex prepared by the usual procedure. When the membranes were pretreated with detergent Triton X-100, the ratio of specific [3H]quipazine binding markedly increased, depending upon the concentration of Triton X-100 in the range of 0.01-0.1% (w/v). At a concentration of more than 0.05%, the specific binding reached a maximum of 55 to 60% of the total binding. The specific [3H]quipazine binding to the Triton X-100-treated membranes was reversible and was potently inhibited by several 5-HT3 antagonists, while 5-HT1, 5-HT2 receptor antagonists and other receptor-specific ligands had no effect on the binding. Scatchard analysis indicated a single class of binding sites with a Kd of 0.62 nM and Bmax of 97 fmol/mg protein. Thus, the Triton X-100-treated membranes retained the characteristics of 5-HT3 binding sites, making it possible to use [3H]quipazine for a 5-HT3 receptor binding assay with a high ratio of specific binding.

Animals

Cephalexin concentrations in human serum, gingiva, and mandibular bone following a single oral administration.

1. Cephalexin concentrations in human serum, gingiva, and mandibular bone after a single oral administration of cephalexin (500 mg) were measured by the paper disc method. 2. The peak times of serum, gingiva, and mandibular bone were approximately 90, 120 and 120 min, respectively. 3. The peak concentrations of serum, gingiva, and mandibular bone were 10.58 micrograms/ml, 5.57 micrograms/g and 2.12 micrograms/g, respectively. 4. The concentration ratio of gingiva/serum and mandibular bone/serum peak time of serum were 0.47 and 0.18, respectively. 5. Cephalexin concentrations in gingiva and mandibular bond did not exceed the MIC80s for clinically isolated strains of Staphylococcus aureus spp., alpha-Streptococci and Peptostreptococcus spp.

Adolescent

Concentrations of ampicillin in human serum and mixed saliva following a single oral administration of lenampicillin, and relationship between serum and mixed saliva concentrations.

The concentrations of ampicillin in serum and mixed saliva after a single oral administration of lenampicillin (500 mg) were determined by the paper disc method. The samples of serum and mixed saliva were obtained at 1, 2, 3 and 4 h after administration. The highest concentrations of ampicillin in serum and mixed saliva occurred 1 h after administration of lenampicillin, and were 11.55 and 0.060 micrograms/ml, respectively. A significant correlation coefficient between the concentrations of ampicillin in serum and mixed saliva, r = 0.71, P less than 0.001, was found.

Administration, Oral

Josamycin concentrations in human dental granuloma after a single oral administration of josamycin.

1. Josamycin concentrations in human serum and dental granuloma after a single oral administration of josamycin (600 mg) were assayed by an agar diffusion (paper disc) method. 2. The mean peak josamycin concentrations in serum and dental granuloma occurred at an identical time, approximately 90 min, and were 0.88 micrograms/ml and 1.61 micrograms/g, respectively. 3. The mean concentration ratio of dental granuloma to serum at the peak time was 2.24. 4. Josamycin concentration in dental granuloma at the peak time exceeded MIC80 for clinically isolated strains of Streptococcus group A, Peptostreptococcus spp., and Bacteroides spp.

Administration, Oral

Ampicillin concentrations in human serum and periodontal membrane following a single oral administration of talampicillin.

1. Ampicillin concentrations in human serum and periodontal membrane after a single oral administration of talampicillin (500 mg) were assayed by the agar diffusion (paper disc) method. 2. The peak times of serum and periodontal membrane were identical, being 150 min after administration. 3. The peak concentrations of serum and periodontal membrane were 7.81 micrograms/ml and 4.11 micrograms/g, respectively. 4. The mean ratio of periodontal membrane to serum concentration at the peak time was 0.53.

Administration, Oral

Ampicillin concentrations in human dental granuloma after a single oral administration of talampicillin.

Ampicillin concentrations in human serum and dental granulomas of 31 patients were determined after a single oral dose of talampicillin (equivalent to 500 mg of ampicillin) was administered to each. The specimens were taken at 1.5, 2.0, 2.5, 3.0, and 3.5 h after the administration of talampicillin. The mean peak ampicillin concentrations in serum and dental granulomas occurred at identical times, 2.5 h, and were 8.29 micrograms/ml (range, 1.81 to 13.20 micrograms/ml) and 2.94 micrograms/g (range, 1.14 to 7.16 micrograms/g), respectively. The mean dental granuloma/serum ampicillin concentration ratio at the peak time (2.5 h) was 0.42 (range, 0.29 to 0.56). Ampicillin concentrations in dental granulomas exceeded most of the MICs for the bacteria commonly isolated from odontogenic infection.

Administration, Oral

Ampicillin concentrations in human serum, gingiva, mandibular bone, dental follicle, and dental pulp following a single oral administration of bacampicillin.

Ninety-six patients who underwent the extraction of impacted mandibular third molars in a nonfasting state were given a single oral dose of bacampicillin preoperatively. Specimens of serum from venous blood (n = 107), gingiva (n = 57), mandibular bone (n = 68), dental follicle (n = 56), and dental pulp (n = 43) were obtained during the operation and assayed for ampicillin content. The mean peak concentrations in serum, gingiva, mandibular bone, dental follicle, and dental pulp all occurred approximately 90 minutes after administration. The concentration ratios of the tissues to the corresponding serum at the peak time were 0.50, 0.20, 0.34, and 0.61, respectively. Bacampicillin showed good absorption by the intestine, and sufficient concentrations of the resulting metabolite, ampicillin, were found in the oral tissues.

Administration, Oral