Studies on prodrugs. VIII. Preparation and characterization of (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl esters of sulbactam and its analogs.
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Biomedical subjects
Publications and source records attributed to F Sakamoto.
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The presence of neuron-specific enolase (NSE) and S-100 protein, which are nerve specific proteins, was immunohistochemically investigated on the cutaneous nerves. NSE was found in the axons of the cutaneous nerve bundles and the terminal axons in the Meissner and Pacinian corpuscles of the normal human and macaque skin. S-100 protein was found in the Schwann cells, lamellar cells of the Meissner corpuscles, and inner core cells of the Pacinian corpuscles. After denervation of the ulnar nerve on macaque, NSE on axons of the cutaneous nerves and Meissner and Pacinian corpuscles was completely disappeared in the 5th digit. However, S-100 protein was still maintained in the Schwann cells and Meissner and Pacinian corpuscles in the same digit. From these results, we conclude that the comparative immunohistochemical staining of NSE and S-100 protein is simple and reliable method to demonstrate the cutaneous nerves in normal and pathological conditions.
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Macromelanosomes in a spindle and epithelioid cell nevus, which occurred in the electron beam-damaged skin of a woman with mycosis fungoides, were ultrastructurally investigated. The melanosomes in the spindle and epithelioid cells were varied in size but uniformly spherical in shape and composed of a core and cortex structure. Electron-lucent bodies were observed in the small melanosomes as well as in the macromelanosomes. Positive dopa-oxidase reaction was revealed on the cortex of these melanosomes and partly on their electron-lucent bodies. The electron-lucent bodies were not vesicular structures but were aggregates of filamentous elements, which had a continuity with fibrous structures in the melanosome cortex. It is concluded that the electron-lucent bodies may be one of the matrices of melanization. Anomalously large accumulations of these bodies and concentrical melanization seem to lead to the formation of macromelanosomes.
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Normal human skin, malignant melanoma, nevocellular nevus, blue nevus, nevus of Ota and mongolian spot were immunohistochemically investigated on the localization of S-100 protein and neuron specific enolase (NSE). Tissues were fixed with buffered-formalin, processed with routine procedure and examined by the ABC technique. All cases of malignant melanoma and nevocellular nevus showed a relatively high amount of S-100 protein, but NSE was scantly demonstrated on about the half cases of these tumors. Blue nevus, nevus of Ota and mongolian spot revealed the presence of a small amount of S-100 protein and NSE on the half cases. Normal melanocytes were devoid of S-100 protein and NSE. Our results suggest that S-100 protein is the useful marker for diagnosis of malignant melanoma, and immunoreactive intensity for S-100 protein represents the differentiation of neural crest derived melanogenic cells and tumors.
Several N-(oxoalkyl)norfloxacin derivatives (3a-g) were synthesized and evaluated for antibacterial activity in vitro and in vivo. Most of the compounds exhibited in vitro activity comparable to that of norfloxacin for Gram-positive bacteria, whereas their activity was lower than for Gram-negative bacteria. N-(2-Oxopropyl)norfloxacin (3b) liberated norfloxacin in the blood after oral administration in mice, and the serum level of norfloxacin was about 3-fold higher than that of norfloxacin itself. Thus, 3b showed high antibacterial activity in vivo.
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Content of thiol and disulphide groups was cytofluorometrically measured on guinea pig keratinocytes, which were separated into three fractions. Free keratinocytes were obtained by the treatment of EDTA and trypsin. After the treatment keratinocytes were separated into three fractions by centrifugation on a continuous colloidal silica (Percoll) density gradient. Cells in each fraction were stained with N-(7-dimethylamino-4-methyl-3-coumarinyl)maleimide, and measured by cytofluorometry. Thiol concentration was low in basal cells, and higher in both spinous and granular cells. Disulphide group content was low and fairly constant in them. Human peripheral lymphocytes and guinea pig spleen lymphocytes were used to examine the influence of EDTA-trypsin treatment. No remarkable loss of either thiol or disulphide groups was found in them after the treatment.
A locally invasive tumor developed in a 71-year-old woman on the right retroauricular skin, involving cartilage and parotid glands. Histologically, the tumor displayed characteristic features of basal cell epithelioma accompanied by stromal fibrosis. Histochemically, an apocrine pattern in enzyme reactions was detected in tumor cells. Ultrastructurally, the tumor cells showed the features of apocrine-type secretory cells and ductlike structures, and the peripheral cells revealed the characteristics of myoepithelial cells. A large number of myofibroblasts was observed in the connective tissue surrounding the tumor nests. From these findings, the woman's tumor was considered to represent a basal cell tumor with apocrine differentiation.
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Cefmenoxime (CMX), a new semisynthetic antibiotic, was administrated in 29 cases diagnosed as complicated urinary tract infection. All patients received drip injection of 2 g (twice a day) for 5 days. Clinical results were excellent in 1 patient (3.4%), good in 15 patients (51.8%) and poor in 13 patients (44.8%). Effectiveness rate was 55.2%. In bacteriological response, out of 35 strains 27 (77.1%) strains were eradicated and 8 (22.9%) strains persisted. As for side effects, except one case of transient diarrhea after administration, no noteworthy reactions were observed. Laboratory abnormalities attributed to CMX treatment consisted of 4 cases of elevated serum transaminase and 2 cases of elevated serum creatinine.
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