24 results on '"Tomii Y"'
Search Results
2. CURRENT STATUS AND CHALLENGES IN JCOG DATA CENTER (DC) AND OPERATIONS OFFICE (OPS)
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Nakamura, K., Fukuda, H., Shibata, T., Kaba, H., Takashima, A., Tomii, Y., Murooka, A., Toshima, H., Abe, J., Katayama, H., Kunieda, F., Kimura, A., Kanato, K., Mizusawa, J., and Yamashita, N.
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- 2012
3. Uptake and intracellular activity of NM394, a new quinolone, in human polymorphonuclear leukocytes
- Author
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Ozaki, M, primary, Komori, K, additional, Matsuda, M, additional, Yamaguchi, R, additional, Honmura, T, additional, Tomii, Y, additional, Nishimura, I, additional, and Nishino, T, additional
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- 1996
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4. Effect of plasma on nitriding of Fe-18Cr-9Ni alloy
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Kuwahara, H., primary, Matsuoka, H., additional, Tamura, I., additional, Takada, J., additional, Kikuchi, S., additional, and Tomii, Y., additional
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- 1992
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5. In vivo evaluation of NM441, a new thiazeto-quinoline derivative
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Ozaki, M, primary, Matsuda, M, additional, Tomii, Y, additional, Kimura, K, additional, Segawa, J, additional, Kitano, M, additional, Kise, M, additional, Shibata, K, additional, Otsuki, M, additional, and Nishino, T, additional
- Published
- 1991
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6. In vitro antibacterial activity of a new quinolone, NM394
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Ozaki, M, primary, Matsuda, M, additional, Tomii, Y, additional, Kimura, K, additional, Kazuno, K, additional, Kitano, M, additional, Kise, M, additional, Shibata, K, additional, Otsuki, M, additional, and Nishino, T, additional
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- 1991
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7. Thermoelectric properties and phase transition of (ZnxCu 2-x)V2O7
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Sotojima, K., Ryosuke, O. Suzuki, Amezawa, K., and Tomii, Y.
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vanadium oxide ,Seebeck coefficient ,layered structure ,electrical resistivity ,phase diagram - Abstract
The phase stability and thermoelectric properties of the layered structure of (ZnxCu2-x)V2O7 solid solutions were studied for x ≥ 0.2. X-ray diffraction measurements, compositional studies, and thermal analysis verified that the low-temperature form of the (ZnxCu2-x)V2O7 solid solution (monoclinic structure, C2/c) was stable for 0.2 ≤ x ≤ 2 when heated below 863K in air. On heating, phase transformation occurred at least at 0.2 ≤ x ≤ 2 at a nearly constant temperature of approximately 873 K; above this temperature, a high-temperature form of the (ZnxCu2-x)V2O7 solid solution was formed. The Seebeck coefficients of the low-temperature (ZnxCu2-x)V2O7 solid solution exhibited large negative values in the range of approximately -520 to -700 μV/K, and the electrical resistivity increased with Zn addition. The maximum power factor of 1.99 x 10^[-7] W/mK2 was obtained at 823K for the low-temperature form of the (Zn0.2Cu1.8)V2O7 solid solution.
8. Images in cardiovascular medicine. Acute morphological change in an extracranial carotid artery dissection on transoral carotid ultrasonography.
- Author
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Nagasawa H, Tomii Y, Yokota C, Toyoda K, Matsuoka H, Suzuki R, Minematsu K, Nagasawa, Hikaru, Tomii, Yasuhiro, Yokota, Chiaki, Toyoda, Kazunori, Matsuoka, Hideki, Suzuki, Rieko, and Minematsu, Kazuo
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- 2008
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9. Validation of a modified enrichment broth for efficient screening of group B Streptococcus in pregnant women.
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Tanno D, Saito K, Tomii Y, Nakatsuka Y, Uechi K, Ohashi K, Yamadera Y, Hata A, Toyokawa M, and Shimura H
- Abstract
We validated a modified enrichment broth that changes its color when group B Streptococcus (GBS) grows. No GBS was detected in any of the non-yellow samples. Thus, the non-yellow samples were considered GBS-negative without conducting further examinations, potentially reducing medical costs and workload., Competing Interests: Declaration of competing interest All authors report no conflicts of interest relevant to this article., (Copyright © 2024. Published by Elsevier B.V.)
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- 2024
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10. A Multicenter Study on the Utility of Selective Enrichment Broth for Detection of Group B Streptococcus in Pregnant Women in Japan.
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Tanno D, Saito K, Tomii Y, Nakatsuka Y, Uechi K, Ohashi K, Hidaka T, Yamadera Y, Hata A, Toyokawa M, and Shimura H
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- Infant, Newborn, Pregnancy, Female, Humans, Pregnant Women, Agar, Vagina, Culture Media, Streptococcus agalactiae genetics, Japan, Rectum, Sensitivity and Specificity, Pregnancy Complications, Infectious diagnosis, Streptococcal Infections diagnosis, Streptococcal Infections prevention & control, Communicable Diseases
- Abstract
Universal screening for Streptococcus agalactiae, Group B Streptococcus (GBS), in pregnant women is important for the prevention of severe infectious diseases in neonates. The subculture method using selective enrichment broth significantly improves GBS detection rates in the United States; however, this method is not widely utilized in Japan mainly because of the lack of large-scale validation. Therefore, we aimed to validate the utility of the subculture method in collaboration with multiple facilities. A total of 1957 vaginal-rectal swab specimens were obtained from pregnant women at 35-37 gestational weeks from March 1, 2020, to August 30, 2020, at Fukushima Medical University Hospital, Aiiku Hospital, Kitano Hospital, and the University of the Ryukyus Hospital. Conventional direct agar plating, subculture using selective enrichment broth, and direct latex agglutination (LA) testing with incubated broth were performed for GBS detection, and discrepant results were confirmed using real-time PCR. The GBS detection rates for direct agar plating, subculture, and direct LA testing were 18.2% (357/1957), 21.6% (423/1957), and 22.3% (437/1957), respectively. The use of selective enrichment broth showed promise for GBS detection with high sensitivity and is therefore recommended for GBS screening to prevent GBS-related infectious diseases in neonates in Japan.
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- 2024
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11. Effects of Undernutrition on Swallowing Function and Activities of Daily Living in Hospitalized Patients: Data from the Japanese Sarcopenic Dysphagia Database.
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Abe S, Kokura Y, Maeda K, Nishioka S, Momosaki R, Matsuoka H, Tomii Y, Sugita S, Shimizu K, Esashi N, and Wakabayashi H
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- Humans, Deglutition, Activities of Daily Living, Retrospective Studies, East Asian People, Nutritional Status, Deglutition Disorders complications, Sarcopenia, Malnutrition complications
- Abstract
This retrospective cohort study examined the effects of undernutrition on swallowing function and activities of daily living in hospitalized patients. Data from the Japanese Sarcopenic Dysphagia Database were used, and hospitalized patients aged ≥20 years with dysphagia were included in the analysis. Participants were assigned to the undernutrition or normal nutritional status group based on the Global Leadership Initiative on Malnutrition criteria. The primary outcome was the Food Intake Level Scale change, and the secondary outcome was the Barthel Index change. Among 440 residents, 281 (64%) were classified under the undernutrition group. The undernutrition group had a significantly higher Food Intake Level Scale score at baseline and Food Intake Level Scale change ( p = 0.001) than the normal nutritional status group. Undernutrition was independently associated with the Food Intake Level Scale change (B = -0.633, 95% confidence interval = -1.099 to -0.167) and the Barthel Index change (B = -8.414, 95% confidence interval = -13.089 to -3.739). This was defined as the period from the date of admission to the hospital until discharge or 3 months later. Overall, our findings indicate that undernutrition is associated with reduced improvement in swallowing function and the ability to perform activities of daily living.
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- 2023
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12. Exploitation of Elevated Extracellular ATP to Specifically Direct Antibody to Tumor Microenvironment.
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Mimoto F, Tatsumi K, Shimizu S, Kadono S, Haraya K, Nagayasu M, Suzuki Y, Fujii E, Kamimura M, Hayasaka A, Kawauchi H, Ohara K, Matsushita M, Baba T, Susumu H, Sakashita T, Muraoka T, Aso K, Katada H, Tanaka E, Nakagawa K, Hasegawa M, Ayabe M, Yamamoto T, Tanba S, Ishiguro T, Kamikawa T, Nambu T, Kibayashi T, Azuma Y, Tomii Y, Kato A, Ozeki K, Murao N, Endo M, Kikuta J, Kamata-Sakurai M, Ishii M, Hattori K, and Igawa T
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- Animals, Humans, Mice, Tumor Microenvironment, Adenosine Triphosphate metabolism, Antibodies metabolism, Extracellular Space metabolism
- Abstract
The extracellular adenosine triphosphate (ATP) concentration is highly elevated in the tumor microenvironment (TME) and remains tightly regulated in normal tissues. Using phage display technology, we establish a method to identify an antibody that can bind to an antigen only in the presence of ATP. Crystallography analysis reveals that ATP bound in between the antibody-antigen interface serves as a switch for antigen binding. In a transgenic mouse model overexpressing the antigen systemically, the ATP switch antibody binds to the antigen in tumors with minimal binding in normal tissues and plasma and inhibits tumor growth. Thus, we demonstrate that elevated extracellular ATP concentration can be exploited to specifically target the TME, giving therapeutic antibodies the ability to overcome on-target off-tumor toxicity., Competing Interests: Declaration of Interests All authors except for J.K. and M.I. are employees of Chugai Pharmaceutical Co., Ltd. K. Ohara, K.A., H.K., H.K., T.I., E.T., M.M., Y.A., Y.S., K.H., T.K., T.M., M.N., S.K., S.T., T.B., M.E., and F.M. own stock in the company. H.K., K.T, S.S., M.K., T.I., S.T., H.K., A.H., F.M., T.K., and M.H. are inventors on intellectual property related to this work. J.K. and M.I. receive research support from Chugai Pharmaceutical Co., Ltd. This study was funded by Chugai Pharmaceutical Co., Ltd., (Copyright © 2020 The Author(s). Published by Elsevier Inc. All rights reserved.)
- Published
- 2020
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13. Protective Effects of 2',3'-Dihydroxy-4',6'-dimethoxychalcone Derived from Green Perilla Leaves against UV Radiation-Induced Cell Injury in Human Cultured Keratinocytes.
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Takada-Takatori Y, Tomii Y, Takemasa S, Takeda Y, Izumi Y, Akaike A, Tsuchida K, and Kume T
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- Animals, Cell Line, Cell Survival drug effects, Heme Oxygenase-1 metabolism, Humans, Keratinocytes, NF-E2-Related Factor 2, Perilla, Plant Extracts pharmacology, Reactive Oxygen Species metabolism, Skin metabolism, Chalcones pharmacology, Ultraviolet Rays adverse effects
- Abstract
Skin exposure to UV rays causes the production of reactive oxygen species (ROS), and it is a major risk factor for various skin disorders and diseases. In particular, exposure to UV-A is a major cause of photoaging. We have previously isolated 2',3'-dihydroxy-4',6'-dimethoxychalcone (DDC) from green perilla leaves as an activator of the nuclear factor erythroid 2-related factor-2 (Nrf2)-antioxidant response element (ARE) and demonstrated the protective effects of DDC both in vitro and in vivo in PC12 cells and Parkinson's disease models, respectively. In this study, we used HaCaT cells to examine the effects of DDC on ROS production and cell damage induced by UV-A. Our results indicated that UV-A irradiation in HaCaT cells increased ROS production in an energy-dependent manner. In addition, cell viability decreased in an energy-dependent manner 24 h after UV-A irradiation. However, treatment with DDC 24 h prior to UV-A irradiation significantly suppressed UV-A radiation-induced ROS production. In addition, DDC showed cytoprotective effects when used 24 h before and after UV-A irradiation. Treatment with DDC for 24 h also increased the expression levels of heme oxygenase-1 (HO-1) in a concentration-dependent manner. Pretreatment with the HO-1 inhibitor followed by DDC treatment before UV-A irradiation for 24 h reduced ROS production and the cytoprotective effect. These results suggest that DDC increases the expression levels of HO-1 and protects HaCaT cells through the suppression of UV radiation-induced ROS production.
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- 2019
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14. Ventricular Temperatures in Idiopathic Normal Pressure Hydrocephalus (iNPH) Measured with DWI-based MR Thermometry.
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Kuriyama N, Yamada K, Sakai K, Tokuda T, Akazawa K, Tomii Y, Tamura A, Kondo M, Watanabe I, Ozaki E, Matsui D, Nakagawa M, Mizuno T, and Watanabe Y
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- Aged, Algorithms, Case-Control Studies, Feasibility Studies, Female, Humans, Hydrocephalus, Normal Pressure cerebrospinal fluid, Hydrocephalus, Normal Pressure surgery, Image Processing, Computer-Assisted statistics & numerical data, Male, Neuroimaging statistics & numerical data, ROC Curve, Sensitivity and Specificity, Thermometry statistics & numerical data, Ventriculoperitoneal Shunt methods, Body Temperature physiology, Cerebral Ventricles physiopathology, Diffusion Magnetic Resonance Imaging statistics & numerical data, Hydrocephalus, Normal Pressure physiopathology
- Abstract
Purpose: The brain produces intense heat as a result of cerebral metabolism and cerebral blood flow, and the generated heat is removed mainly through circulation of the intracranial blood vessels and cerebrospinal fluid (CSF). Because magnetic resonance (MR) images are constructed from analysis of the spin of various molecules, the diffusion coefficient can be used as a parameter that reflects the temperature of water molecules. We used diffusion-weighted imaging (DWI)-based MR imaging to measure the temperature of the CSF around the lateral ventricles in patients with idiopathic normal pressure hydrocephalus (iNPH)., Methods: Our study included 33 cases of iNPH (Group N, mean age, 75.1 years) and 40 age-matched controls (Group C, mean age, 74.5 years). We calculated CSF temperature in the ventricular domain using the conversion formula to evaluate the feasibility of iNPH study., Results: The mean temperatures were significantly higher in Group N (37.6°C ± 0.4°C) than Group C (36.7°C ± 0.5°C; P < 0.01). The cut-off value of 37.2°C (more than the mean + 2 standard deviations [SD] of the values in Group C) showed sensitivity of 72.4% and specificity of 77.5% for distinguishing the 2 groups. We confirmed improved CSF temperature in the lateral ventricles in all patients examined both before and after shunting., Conclusions: Elevated ventricular temperatures in patients with iNPH (Group N) may represent a disturbance in heat balance. Our results showed that thermometry using DWI-based MR imaging can help in the noninvasive and consistent evaluation of CSF temperature and may thus provide a useful supplementary brain biomarker for iNPH.
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- 2015
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15. Optimizing the Physicochemical Properties of Raf/MEK Inhibitors by Nitrogen Scanning.
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Aoki T, Hyohdoh I, Furuichi N, Ozawa S, Watanabe F, Matsushita M, Sakaitani M, Morikami K, Takanashi K, Harada N, Tomii Y, Shiraki K, Furumoto K, Tabo M, Yoshinari K, Ori K, Aoki Y, Shimma N, and Iikura H
- Abstract
Substituting a carbon atom with a nitrogen atom (nitrogen substitution) on an aromatic ring in our leads 11a and 13g by applying nitrogen scanning afforded a set of compounds that improved not only the solubility but also the metabolic stability. The impact after nitrogen substitution on interactions between a derivative and its on- and off-target proteins (Raf/MEK, CYPs, and hERG channel) was also detected, most of them contributing to weaker interactions. After identifying the positions that kept inhibitory activity on HCT116 cell growth and Raf/MEK, compound 1 (CH5126766/RO5126766) was selected as a clinical compound. A phase I clinical trial is ongoing for solid cancers.
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- 2014
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16. Fluorine Scanning by Nonselective Fluorination: Enhancing Raf/MEK Inhibition while Keeping Physicochemical Properties.
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Hyohdoh I, Furuichi N, Aoki T, Itezono Y, Shirai H, Ozawa S, Watanabe F, Matsushita M, Sakaitani M, Ho PS, Takanashi K, Harada N, Tomii Y, Yoshinari K, Ori K, Tabo M, Aoki Y, Shimma N, and Iikura H
- Abstract
A facile methodology effective in obtaining a set of compounds monofluorinated at various positions (fluorine scan) by chemical synthesis is reported. Direct and nonselective fluorination reactions of our lead compound 1a and key intermediate 2a worked efficiently to afford a total of six monofluorinated derivatives. All of the derivatives kept their physicochemical properties compared with the lead 1a and one of them had enhanced Raf/MEK inhibitory activity. Keeping physicochemical properties could be considered a benefit of monofluorinated derivatives compared with chlorinated derivatives, iodinated derivatives, methylated derivatives, etc. This key finding led to the identification of compound 14d, which had potent tumor growth inhibition in a xenograft model, excellent PK profiles in three animal species, and no critical toxicity.
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- 2013
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17. Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity.
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Ishii N, Harada N, Joseph EW, Ohara K, Miura T, Sakamoto H, Matsuda Y, Tomii Y, Tachibana-Kondo Y, Iikura H, Aoki T, Shimma N, Arisawa M, Sowa Y, Poulikakos PI, Rosen N, Aoki Y, and Sakai T
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- Allosteric Regulation, Animals, Cell Line, Tumor, Enzyme Activation drug effects, Extracellular Signal-Regulated MAP Kinases metabolism, Feedback, Physiological drug effects, Female, Humans, MAP Kinase Kinase 1 chemistry, MAP Kinase Kinase 1 metabolism, Mice, Mice, Inbred BALB C, Mice, Nude, Phosphorylation, Protein Binding, Protein Processing, Post-Translational, Proto-Oncogene Proteins genetics, Proto-Oncogene Proteins B-raf chemistry, Proto-Oncogene Proteins c-raf chemistry, Proto-Oncogene Proteins c-raf metabolism, Proto-Oncogene Proteins p21(ras), Xenograft Model Antitumor Assays, ras Proteins genetics, Antineoplastic Agents pharmacology, Coumarins pharmacology, MAP Kinase Kinase 1 antagonists & inhibitors, MAP Kinase Signaling System drug effects, Proto-Oncogene Proteins B-raf metabolism
- Abstract
Tumors with mutant RAS are often dependent on extracellular signal-regulated kinase (ERK) signaling for growth; however, MEK inhibitors have only marginal antitumor activity in these tumors. MEK inhibitors relieve ERK-dependent feedback inhibition of RAF and cause induction of MEK phosphorylation. We have now identified a MEK inhibitor, CH5126766 (RO5126766), that has the unique property of inhibiting RAF kinase as well. CH5126766 binding causes MEK to adopt a conformation in which it cannot be phosphorylated by and released from RAF. This results in formation of a stable MEK/RAF complex and inhibition of RAF kinase. Consistent with this mechanism, this drug does not induce MEK phosphorylation. CH5126766 inhibits ERK signaling output more effectively than a standard MEK inhibitor that induces MEK phosphorylation and has potent antitumor activity as well. These results suggest that relief of RAF feedback limits pathway inhibition by standard MEK inhibitors. CH5126766 represents a new type of MEK inhibitor that causes MEK to become a dominant-negative inhibitor of RAF and that, in doing so, may have enhanced therapeutic activity in ERK-dependent tumors with mutant RAS., (©2013 AACR.)
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- 2013
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18. Effects of 24-hour blood pressure and heart rate recorded with ambulatory blood pressure monitoring on recovery from acute ischemic stroke.
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Tomii Y, Toyoda K, Suzuki R, Naganuma M, Fujinami J, Yokota C, and Minematsu K
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- Aged, Aged, 80 and over, Female, Humans, Hypertension physiopathology, Male, Middle Aged, Blood Pressure physiology, Blood Pressure Monitoring, Ambulatory, Brain Ischemia physiopathology, Heart Rate physiology, Stroke physiopathology
- Abstract
Background and Purpose: This study used ambulatory blood pressure (BP) monitoring to generate BP and heart rate (HR) profiles soon after stroke onset and evaluated the association between determined values and 3-month stroke outcomes., Methods: We analyzed 24-hour ambulatory BP monitoring records from 104 patients with acute ischemic stroke. Ambulatory BP monitoring was attached at the second and eighth hospitalization days (Days 1 and 7). Both BP and HR were characterized using baseline, mean, maximum, and minimum values and coefficient of variation during 24-hour recording periods. Outcomes at 3 months were assessed as independence according to a modified Rankin Scale score of ≤2 and poor according to the score of ≥5., Results: Sixty-six (63%) patients achieved independence and 12 (11%) had poor outcomes. Mean ambulatory BP monitoring values changed from 150.5±19.5/85.7±11.3 mm Hg on Day 1 to 139.6±19.3/80.0±11.7 mm Hg on Day 7. After multivariate adjustment, mean values of systolic BP (OR, 0.63; 95% CI, 0.45-0.85), diastolic BP (0.61; 0.37-0.98), pulse pressure (0.55; 0.33-0.85), and HR (0.61; 0.37-0.98) recorded on Day 1 as well as mean HR on Day 7 (0.47; 0.23-0.87) were inversely associated with independence and mean values of systolic BP (1.92; 1.15-3.68), diastolic BP (5.28; 1.92-22.85), and HR (4.07; 1.83-11.88) on Day 1 as well as mean HR on Day 7 (4.92; 1.36-36.99) were positively associated with a poor outcome., Conclusions: All of systolic BP, diastolic BP, pulse pressure, and HR on Day 1 and HR on Day 7 assessed using ambulatory BP monitoring were associated with outcomes of patients with stroke at 3 months.
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- 2011
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19. Synthesis and antibacterial activity of novel 7-substituted-6-fluoro-1- fluoromethyl-4-oxo-4H-[1,3thiazeto[3,2-a]quinoline-3-carboxylic acid derivatives.
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Matsuoka M, Segawa J, Amimoto I, Masui Y, Tomii Y, Kitano M, and Kise M
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- Animals, Anti-Bacterial Agents pharmacology, Anti-Bacterial Agents therapeutic use, Carboxylic Acids pharmacology, Carboxylic Acids therapeutic use, Circular Dichroism, Crystallography, X-Ray, Escherichia coli Infections drug therapy, Escherichia coli Infections microbiology, Gram-Negative Bacteria drug effects, Gram-Positive Bacteria drug effects, Male, Mice, Microbial Sensitivity Tests, Molecular Conformation, Quinolines pharmacology, Quinolines therapeutic use, Staphylococcal Infections drug therapy, Staphylococcal Infections microbiology, Anti-Bacterial Agents chemical synthesis, Carboxylic Acids chemical synthesis, Quinolines chemical synthesis
- Abstract
A series of 7-substituted-6-fluoro-1-fluoromethyl-4-oxo-4H- [1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid derivatives (2a-1) was prepared and evaluated for antibacterial activity. These compounds were obtained by deacylation of 4-benzoyloxy-2-(1-chloro-2-fluoroethyl)thio-6,7- difluoroquinoline-3-carboxylate (10) and subsequent intramolecular cyclization followed by substitution with cyclic amines and then hydrolysis. The intramolecular cyclization reaction of 18, one of the diastereomers (17, 18) revealed that the cyclization reaction proceeded through an inversion to afford (-)-11a in good chemical and optical yield. The enantiomers of 2a were prepared from the enantiomers of 11a, which were obtained by the optical resolution of the racemate using high-performance liquid chromatography (HPLC). Compounds 2a,b showed excellent in vitro and in vivo antibacterial activity against both gram-negative and gram-positive bacteria including quinolone and Methicillin-resistant Staphylococcus aureus.
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- 1999
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20. In vitro and in vivo activities of NS-718, a new lipid nanosphere incorporating amphotericin B, against Aspergillus fumigatus.
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Otsubo T, Maesaki S, Hossain MA, Yamamoto Y, Tomono K, Tashiro T, Seki J, Tomii Y, Sonoke S, and Kohno S
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- Amphotericin B administration & dosage, Amphotericin B pharmacokinetics, Animals, Antifungal Agents administration & dosage, Antifungal Agents pharmacokinetics, Aspergillosis, Allergic Bronchopulmonary microbiology, Colony Count, Microbial, Drug Carriers, Immunocompromised Host, Lipids, Male, Microspheres, Rats, Rats, Sprague-Dawley, Amphotericin B pharmacology, Antifungal Agents pharmacology, Aspergillosis, Allergic Bronchopulmonary drug therapy, Aspergillus fumigatus drug effects
- Abstract
We evaluated the in vitro and in vivo potencies of a new lipid nanosphere that incorporates amphotericin B (AmB), NS-718, against Aspergillus fumigatus. The in vitro activity of NS-718 (the MIC at which 90% of strains are inhibited [MIC90], 0.25 microgram/ml) against 18 isolates of A. fumigatus was similar to that of deoxycholate AmB (D-AmB; Fungizone; MIC90, 0.25 microgram/ml), but NS-718 was more potent than liposomal AmB (L-AmB; AmBi-some; MIC90, 1.0 microgram/ml). The in vivo efficacy of NS-718 in a rat model of invasive pulmonary aspergillosis was compared with those of D-AmB and L-AmB. A low dose (1 mg/kg of body weight) of L-AmB was ineffective (survival rate, 0%), although equivalent doses of D-AmB and NS-718 were more effective (survival rate, 17%). However, a higher dose of NS-718 (3 mg/kg) was more effective (survival rate, 100%) than equivalent doses of D-AmB and L-AmB (survival rate, 0%). To explain these differences, pharmacokinetic studies showed higher concentrations of AmB in the plasma of rats treated with NS-718 than in the plasma of those treated with D-AmB. Our results suggest that NS-718, a new preparation of AmB, is a promising antifungal agent with activity against pulmonary aspergillosis.
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- 1999
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21. Structure-antibacterial activity and cytotoxicity relationships of thiazolo and thiazetoquinolone derivatives.
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Ozaki M, Segawa J, Kitano M, Tomii Y, Honmura T, Matsuda M, Kise M, and Nishino T
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- 4-Quinolones, Animals, Cell Line, Cell Survival drug effects, Cricetinae, Cricetulus, Structure-Activity Relationship, Thiazoles pharmacology, Anti-Infective Agents pharmacology, Bacteria drug effects
- Abstract
In the course of our search for derivatives with potent antibacterial activity and low cytotoxicity, we have studied the relationships among the structure, antibacterial activity and cytotoxicity of thiazoloquinolone and thiazetoquinolone derivatives (the term quinolone as used in this paper includes the quinolone, 1,8-naphthyridine and pyridopyrimidine nuclei). The antibacterial activities and cytotoxicity of these derivatives were compared with those of norfloxacin, ofloxacin, enoxacin and ciprofloxacin. The antibacterial activities of the thiazoloquinolone derivatives were more potent than those of the dihyrothiazoloquinolone derivatives, and comparable to that of ciprofloxacin. All of the thiazoloquinolone derivatives were highly cytotoxic against mammalian cells, but some of the dihyrothiazoloquinolone derivatives were less cytotoxic, being comparable in cytotoxicity to the reference drugs. The thiazetoquinolone derivatives were less cytotoxic than the thiazoloquinolone derivatives, and one of them, 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3]thiazeto[3,2-a] quinoline-3-carboxylic acid, showed the most potent antibacterial activity of all compounds tested in this study, as well as a very low cytotoxicity. The antibacterial activity and cytotoxicity of this compound were similar to that of ciprofloxacin.
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- 1996
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22. Studies on pyridonecarboxylic acids. IV. Synthesis and antibacterial activity evaluation of S-(-)- and R-(+)-6-fluoro-1-methyl-4-oxo-7- (1-piperazinyl)-4H-[1,3] thiazeto[3,2-a]quinoline-3-carboxylic acids.
- Author
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Segawa J, Kazuno K, Matsuoka M, Amimoto I, Ozaki M, Matsuda M, Tomii Y, Kitano M, and Kise M
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- Bacillus subtilis drug effects, Crystallography, X-Ray, Escherichia coli drug effects, Microbial Sensitivity Tests, Pseudomonas aeruginosa drug effects, Staphylococcus aureus drug effects, Stereoisomerism, Structure-Activity Relationship, Anti-Infective Agents chemical synthesis, Anti-Infective Agents pharmacology, Fluoroquinolones, Piperazines chemical synthesis, Piperazines pharmacology, Quinolones chemical synthesis, Quinolones pharmacology
- Abstract
Optically active isomers of 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H- [1,3] thiazeto [3,2-alpha] quinoline-3- carboxylic acid (NM394, 3) were prepared through optical resolution of their racemic intermediate ( +/- )-1 by high-performance liquid chromatography (HPLC). The absolute configuration at the C-1 position in the thiazeto-quinolone ring of ( - )-3 was confirmed by X-ray analysis ( - )-4 to be S. The in vitro antibacterial activity of ( - )-3 was 2--8 times that of (+)-3.
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- 1995
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23. Studies on pyridonecarboxylic acids. III. Synthesis and antibacterial activity evaluation of 1,8-disubstituted 6-fluoro-4-oxo-7-piperazinyl-4H-[1,3]thiazeto[3,2- a]quinoline-3-carboxylic acid derivatives.
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Segawa J, Kazuno K, Matsuoka M, Shirahase I, Ozaki M, Matsuda M, Tomii Y, Kitano M, and Kise M
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- Animals, Anti-Bacterial Agents pharmacology, Bacterial Infections drug therapy, Bacterial Infections microbiology, Carboxylic Acids pharmacology, Gram-Negative Bacteria drug effects, Gram-Positive Bacteria drug effects, Male, Mice, Microbial Sensitivity Tests, Anti-Bacterial Agents chemical synthesis, Carboxylic Acids chemical synthesis, Pyridones chemistry
- Abstract
A series of 1,8-disubstituted 6-fluoro-4-oxo-7-piperazinyl-4H-[1,3]thiazeto[3,2-a]quinoline-3- carboxylic acid derivatives was prepared and evaluated for antibacterial activity. In the 7-piperazinyl series, addition of a fluorine at C-8, which increased the in vitro activity for the 1-hydrogen and 1-methyl analogues and decreased it for the 1-phenyl analogue, improved the in vivo activity of all the analogues. Introduction of a methoxy group at C-8 of the 1-methyl-7-piperazinyl analogue also improved its in vivo antibacterial activity. The effect of 8-substituents on the in vitro and in vivo antibacterial activity of the 1-methyl-7-(4-methyl-1-piperazinyl) series is also discussed.
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- 1995
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24. Preventive procedure of dysuria after radical hysterectomy by adnexal flap fixation to the bladder.
- Author
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Yamaguchi R, Nishikawa Y, Tsubomoto S, Ueha K, and Tomii Y
- Subjects
- Adult, Female, Follow-Up Studies, Humans, Methods, Middle Aged, Pressure, Urinary Bladder physiology, Urinary Bladder, Neurogenic etiology, Urinary Bladder, Neurogenic prevention & control, Urination Disorders etiology, Adnexa Uteri surgery, Hysterectomy methods, Postoperative Complications prevention & control, Urinary Bladder surgery, Urination Disorders prevention & control
- Abstract
To prevent postoperative dysuria, which occurs inevitably after the radical hysterectomy, several surgical procedures have been tried. The principal method is to suture adnexal flaps to the bladder trigone and fundus. Of four procedures so far tried sequentially, the best one was to fix the bladder trigone and to support it with round ligament flaps sutured with the bladder fundus covered by tubal flaps (Type IV). In follow-up studies, Type IV proved more preferable than the other three types or the non-sutured control group in regard to the following aspects: (1) days necessary for the disappearance of residual urine, (2) appearance of urinary sensation, (3) acquirement of urinary sensation, (4) incidence of urinary incontinence, (5) residual urine/bladder capacity ratio, (6) cystometric findings, and others. Effectiveness of our procedures, particularly of Type IV, may be ascribed to the supported bladder trigone and fundus by sutured tissues and to the acquirement of urinary sensation, rather than to the restoration of nervous contact between the bladder and the micturition center in the spinal cord.
- Published
- 1976
- Full Text
- View/download PDF
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