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Biomedical subjects

S Kondo

Publications and source records attributed to S Kondo.

At least 883 records · Page 49Linked to original sources
PubMed1990

[Effect of age on the amount of autonomic receptors in the rabbit prostate homogenate].

The amount of autonomic receptors in the old and young rabbit prostate homogenate was measured in order to study the effect of age on the autonomic receptors of the prostate using radioligand binding techniques. For measuring the adrenergic alpha-1, alpha-2, beta-receptors and cholinergic muscarinic receptors, 3H-Prazosin (3H-PZ), 3H-Yohimbine (3H-YOH), 3H-Quinuclidinylbenzilate (3H-QNB) were used, respectively. It was found that both the young and old rabbit prostate has a single class of binding sites for each ligand examined. There was an age-related difference in the distribution of these autonomic receptors (young: alpha 1 = muscarinic greater than alpha 2 greater than beta, old: alpha 1 greater than muscarinic greater than alpha 2 greater than beta). There were more alpha-1 and alpha-2 receptors in the old rabbit prostate, although these differences were not statistically significant. There was no age-related differences in the amount of beta adrenergic and muscarinic receptors. These results demonstrate that the age may affect the distribution of autonomic receptors but not significantly the amount of autonomic receptors of rabbit prostate.

Aging↗
PubMed1990

Synthesis and biological activity of (cyclopentenopyridinium) thiomethylcephalosporins.

Substituted (cyclopentenopyridinium)thiomethyl groups were introduced as C-3 substituents of (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-oxyimino]acetami docephalosporins. Structure-activity relationships of this class of cephalosporins are discussed on the basis of their MIC. The selected compounds, 3a and 4a (ME1221), having an acidic substituent, showed excellent in vivo efficacy and low toxicity.

Animals↗
PubMed1990

A new antipseudomonal cephalosporin CP6162 and its congeners.

The synthesis and biological activity of a series of 3-[2-(5-hydroxy-4-pyridon-2-yl)ethenyl]cephalosporin derivatives are described. They showed very potent activity against Gram-negative bacteria, especially Pseudomonas aeruginosa. (6R, 7R)-7-[(Z)-2-(2-Aminothiazol-4-yl)-2 -(1-carboxy-1-methyl)-ethoxyiminoacetamido]-3-[(Z)-2-(1,5-dihydrox y-4- pyridon-2-yl)ethenyl]ceph-3-em-4-carboxylic acid, CP6162 (8e), was selected for further evaluation as antipseudomonal chemotherapeutic agent.

Animals↗
PubMed1990

Improved antitumor effects of 3'-deamino-3'-morpholino derivatives of pirarubicin.

The preparation and antitumor effects of 3'-deamino-3'-morpholino derivatives of pirarubicin are described. Di-N-alkylation of pirarubicin with bis(2-iodoethyl)ether gave 3'-morpholino-pirarubicin, which was converted into its 13-tosylhydrazone, 13-deoxy derivative and 13-(S)- and 13-(R)-dihydro derivatives. Intraperitoneal administration to murine tumors indicated that the effective dose ranges of the compounds having sp3 carbon at C-13 position were broader than those of the compounds having sp2 carbon. By oral administration, 13-(S)-dihydro isomer was more effective than 13-(R)-dihydro isomer.

Administration, Oral↗
PubMed1990

New aminothiazolylglycylcephalosporins with a 1,5-dihydroxy-4-pyridone-2-carbonyl group. I. Synthesis and biological activity of cephalosporin derivatives leading to MT0703.

A series of new aminothiazolylglycylcephalosporins with a mono- or dihydroxypyridonecarbonyl group at the alpha-amino group of the C-7 substituent have been prepared and antibacterial activity of these compounds was investigated. Among them, the compounds having a 1,5-dihydroxy-4-pyridone-2-carbonyl group showed excellent anti-pseudomonal activity. In particular, (6R,7R)-7-[(RS)-2-(2-aminothiazol-4-yl)-2-(1,5-dihydroxy-4- pyridone-2-carboxamido)- acetamido]-3-[[1-(2-hydroxyethyl)pyridinium-4-yl]thiomethyl]ceph-3 -em- 4-carboxylate (MT0703, 7g) was found to be a well balanced compound with respect to antibacterial activity.

Animals↗
PubMed1990

New aminothiazolylglycylcephalosporins with a 1,5-dihydroxy-4-pyridone-2-carbonyl group. II. Synthesis and antibacterial activity of MT0703 and its diastereomers.

A practical synthetic method for large scale production of MT0703, (6R,7R)-7-[(RS)-2-(2-aminothiazol-4-yl)-2-(1,5-dihydroxy-4-pyridon e-2- carboxamido)acetamido]-3-[[1-(2-hydroxyethyl)pyridinium-4- yl]thiomethyl]ceph-3-em-4-carboxylate, was established. Its two diastereomers on configuration of the aminothiazolylglycyl moiety were synthesized using chemico-enzymatic method. The S-isomer of MT0703 was found to be more active against Gram-positive and Gram-negative bacteria including beta-lactamase-producing strains than the R-isomer.

Animals↗
PubMed1990

Synthesis and antibacterial activity of novel 2-methyl-1-oxacephalosporins.

New 2-methyl-1-oxacephem compounds having 2-(2-aminothiazol-4-yl)-2-(alkoxyimino)acetamido substituents at C-7 and various C-3 side chains were synthesized starting from (3R,4S)-phenyloxazolinoazetidinone (8). Introduction of the 2 beta-methyl group into the 1-oxacephem nucleus increased the stability to beta-lactamases. OCP-9-176 (7b) having the (1-methylpyridinium-4-yl)thiomethyl group at C-3 showed potent antibacterial activity and a broad spectrum.

Bacteria↗
PubMed1990

The absolute configuration of decilonitrose, a sugar component of decilorubicin, is undoubtedly 2,3,6-trideoxy-3-C-methyl-3-nitro-L-ribo-hexopyranose.

The absolute structure of decilonitrose, a sugar component of an antitumor antibiotic decilorubicin was decided to be 2,3,6-trideoxy-3-C-methyl-3-nitro-L-ribo-hexopyranose by synthesis of its methyl beta-glycoside starting from L-rhamnose through the 3-ulose. In the synthetic route, any configurational ambiguities do not exist.

Anthracyclines↗
PubMed1990

A new aminothiazolylcephalosporin having 1-carboxyethoxyimino group, ME1228.

Aminothiazolylacetamidocephalosporins having 1-carboxyethoxyimino groups were synthesized and found to have excellent antibacterial activities including anti-pseudomonal activity and low toxicities. Among these cephalosporins, ME1228 having (S)-1-carboxyethoxyimino substituent and being combined with an (N-ethyl-4-pyridinio)thiomethyl group at C-3 showed marked therapeutic effects against systemic infections in mice and was selected as the best candidate for further evaluation.

Animals↗
PubMed1990

Punctate porokeratotic keratoderma: some pathogenetic analyses of hyperproliferation and parakeratosis.

An 82-year-old Japanese woman had numerous palmoplantar keratotic plugs and pits, resembling 'music box spines'. Histological examination revealed compact columns of parakeratosis in the horny layer. Ultrastructually, the affected stratum corneum contained numberous variable-sized pyknotic nuclei, and cells in the stratum granulosum contained fewer keratohyalin granules. Autoradiographic analysis by [3H]thymidine [3H]TdR incorporation into epidermal cells of affected skin slices in organ culture revealed that only basal cells below the keratotic plug were stimulated to proliferate. Two-dimensional gel electrophoresis revealed that palmar keratotic plugs contained the keratin filaments that are specifically present in the plantar viable epidermal layer, or other hyperproliferative epithelial cells.

Aged↗
PubMed1990

Direct action of human granulocyte colony-stimulating factor on mature human neutrophils: flow-cytometric analysis.

The direct effects of human granulocyte colony-stimulating factor (G-CSF) on mature neutrophils in vitro were studied using flow cytometry. G-CSF increased the neutrophil forward scatter without recruitment of side scatter, as assessed by flow cytometry. This indicates that G-CSF acts on neutrophils directly and induces the activation of mature neutrophils without degranulation of primary granules.

Colony-Stimulating Factors↗
PubMed1990

Hypertension and cardiovascular diseases in an epidemiological study in Hokkaido, Japan.

The present study describes the results from the 10-year follow-up data of a prospective epidemiological study for hypertension and cardiovascular diseases in two communities of rural agricultural districts in Hokkaido, Japan. The number of incidences of cerebrovascular accidents (CVAs) in persons who were normotensive, borderline hypertensive (BHT), untreated hypertensive (HT), well-controlled HT [blood pressure (BP) less than 150/90 mm Hg], and poorly controlled HT (BP greater than or equal to 150/90 mm Hg) were 0.46, 3.24, 4.17, 3.49, and 12.76 per 1,000 person-years. respectively: CVAs were markedly high in poorly controlled HT persons. The winter-summer mean BP differences in the first year were significantly and positively correlated with the differences in mean BP between the tenth and the first year, and were significantly higher in the progression to hypertension group than in the nonprogression group in both towns. Multivariate analysis indicated that the winter-summer mean BP difference was a significant variable for indication of progression to hypertension. From these results, we concluded that (a) good control of hypertension could considerably prevent CVA, (b) cold environment may contribute to the progression to hypertension, and (c) winter-summer variation in BP may predict the future course of BP.

Acute Disease↗
PubMed1990

Protective effect of dl-alpha-tocopherol on the cytotoxicity of ultraviolet B against human skin fibroblasts in vitro.

The effect of dl-alpha-tocopherol on ultraviolet light, 280-320 nm (UVB)-induced damage of human skin fibroblasts was studied by measuring the colony-forming ability, unscheduled DNA synthesis (UDS) and malondialdehyde (MDA) production. Regarding the cell toxicity, the values of the mean lethal dose (D0) of UV in fibroblast strains from 5 normal subjects were examined. D0 increased dose-dependently when the cells were cultured in the presence of dl-alpha-tocopherol at the concentration of 10-1000 micrograms/ml. UDS induced by 500 J/m2 UVB irradiation was not altered by treatment of 100 micrograms/ml dl-alpha-tocopherol. MDA did not increase after 500 J/m2 UVB irradiation in the fibroblasts cultured with 100 micrograms/ml dl-alpha-tocopherol, while MDA in the fibroblasts cultured without dl-alpha-tocopherol increased after irradiation. These results suggest that dl-alpha-tocopherol protects human skin fibroblasts against the cytotoxic effect of UVB, and its mechanism seems to be related to inhibition of UV-induced lipid peroxidation or to the antioxidation effect of dl-alpha-tocopherol.

Adolescent↗
PubMed1990

[Transverse strength and acoustic emission characteristics of commercial denture base resins].

Transverse strength and acoustic emission (AE) characteristics were measured by the transverse test in deionized water at 37 degrees C on commercial denture base resins (five heat-cured type resins and one polysulfone). Difference in flexural property of five heat-cured denture base resins was not shown from the transverse deflection according to JIS, but high toughness of polysulfone was recognized in transverse deflection, flexural strength, flexural modulus, flexural rigidity, flexural proof stress, and fracture energy. The five heat-cured denture base resins showed a low AE activity, but the polysulfone resin high AE activity. Significant rates of AE for polysulfone were detected at a kgf of approximately 50-60% the maximum load. The presence of Kaiser effect in its cycle transverse test was confirmed.

Acoustics↗
PubMed1990

Both granulocyte-macrophage colony-stimulating factor and monocytic colony-stimulating factor are produced by the human T-cell line, HUT 102.

We present the first report of a T-helper cell line, HUT 102, constitutively producing both granulocyte-macrophage colony-stimulating factor (GM-CSF) and monocytic colony-stimulating factor (M-CSF), as detected by sensitive enzyme-linked immunosorbent assays and Northern blot analysis. However, neither amplification nor structural change of the GM-CSF and M-CSF genes was detected by Southern blot analysis. In the case of HUT 102, in which human T-lymphotropic leukemia virus type I (HTLV-I) is integrated, the viral protein, which acts as a trans-acting transcriptional activator, may induce the production of both GM-CSF and M-CSF.

Cell Line↗
PubMed1990

[Rothmund-Thomson's syndrome--a case demonstrating prominent hyperkeratosis and literature review].

A patient, 21-year-old japanese man demonstrating many of the changes seen in the Rothmund-Thomson's syndrome is presented. In particular the hyperkeratosis palmo-plantar hyperkeratosis and warty hyperkeratosis on the hand and feet are prominent clinical features in this patient. The literatures describing hyperkeratosis in the Rothmund-Thomson's syndrome are reviewed and the clinical feature as well as diagnostic value of the hyperkeratosis is discussed.

Adult↗
PubMed1990

Resection of intrahepatic bile duct carcinoma with hilar bile duct and portal vein invasion--a case report.

A case of resected intrahepatic bile duct cancer with hilar bile duct and portal vein invasion is presented. Percutaneous transhepatic biliary drainage was performed to alleviate jaundice and evaluate the biliary system. Intraductal tumor extension was determined, and an accurate histological diagnosis was made in biopsy material obtained under percutaneous transhepatic cholangioscopy. Preoperative surgical planning was carried out on the basis of an evaluation of the findings of ultrasonography, computed tomography, arteriography, portography and percutaneous transhepatic cholangioscopy. Curative surgery, which included right hepatic lobectomy with total caudate lobectomy and combined resection and reconstruction of the portal vein, was performed. Bilioenteric continuity was re-established by a Roux-en-Y jejunal loop. The histological diagnosis was moderately differentiated tubular adenocarcinoma originated in the right posterior branch of the intrahepatic bile duct. Postoperative recovery was very good, and the patient has now been enjoying a good active social life for the past three years with no signs of tumor recurrence. This case report discusses the accurate diagnosis and rational surgical treatment for intrahepatic bile duct carcinoma with hilar invasion.

Adenoma, Bile Duct↗