19 results on '"Sakai, Masaru"'
Search Results
2. Influential factors of long-term and seasonal 137Cs change in agricultural and forested rivers: Temperature, water quality and an intense Typhoon Event.
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Tsuji, Hideki, Nishikiori, Tatsuhiro, Ito, Shoko, Ozaki, Hirokazu, Watanabe, Mirai, Sakai, Masaru, Ishii, Yumiko, and Hayashi, Seiji
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WATER quality ,AGRICULTURE ,TYPHOONS ,HEAT of reaction ,SUSPENDED solids ,WATER temperature ,LEACHING - Abstract
In this study, the effect of temperature, water quality, and the impact of an intense typhoon event on change in
137 Cs concentration in the water of agricultural and forested rivers near the Fukushima Daiichi nuclear power plant (Japan) was evaluated using monthly stationary observations obtained under baseflow conditions 2.8–10.6 years after the nuclear accident in 2011. The dissolved137 Cs concentration fluctuated seasonally with water temperature in all rivers, and the increase in dissolved137 Cs concentration for unit increase in temperature was higher in forested rivers than in agricultural rivers. The relationship between water temperature and the apparent distribution coefficient of137 Cs well followed the van 't Hoff equation in the two agricultural rivers, where the enthalpy of reaction was estimated as −15.6 and −19.6 kJ mol−1 . The van 't Hoff equation was not well followed for a forested river, where the suspended solids mainly comprised organic matter, suggesting that the dominant process determining dissolved137 Cs concentrations in forested rivers is not only water temperature effect on ion exchange, but rather the input of137 Cs and K+ (competing with137 Cs for exchange sites on mineral particles) into the water phase via litter leaching. Suspended solids concentrations in agricultural rivers correlated negatively with137 Cs concentrations in suspended solids, suggesting an increased proportion of coarse particles or the input of soils with low137 Cs concentration from decontaminated agricultural land. At some sites,137 Cs concentrations in dissolved form and in suspended solids were reduced sharply in association with the passage of Typhoon Hagibis in October 2019, suggesting that Typhoon Hagibis caused large-scale surface erosion that removed the source of137 Cs. [Display omitted] • Trend of137 Cs concentration in river water was analyzed based on 8 years monitoring. • Seasonal change in dissolved137 Cs concentration was mostly affected by temperature. • Typhoon Hagibis caused reduction in particulate/dissolved137 Cs in some rivers. •137 Cs concentration in forested river was poorly regressed by the van't Hoff equation. • The137 Cs reaction enthalpy in two agricultural rivers was −15.6 and −19.6 kJ mol−1 . [ABSTRACT FROM AUTHOR]- Published
- 2023
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3. Catchment-scale deer exclusion changes longitudinal patterns of macroinvertebrate communities through soil runoff mitigation.
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Sakai, Masaru
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COMMUNITIES , *SEDIMENTATION & deposition , *RESTORATION ecology , *SUSPENDED sediments , *DEER - Abstract
Deer overpopulation is occurring worldwide, and deer-induced soil runoff into streams increases levels of suspended sediment and fine sedimentation. While deer-induced fine sedimentation in depositional habitats including first- and fourth-order streams is known to alter macroinvertebrate communities, effects of drifting suspended sediment in erosional habitats between the stream orders are poorly understood. Here, habitat and macroinvertebrate community structures in first- to third-order streams were compared between deer-excluded and grazed catchments of a Japanese headwater system. Fine sediment cover on the streambed was significantly greater in the grazed catchments than the deer-excluded catchment only for first-order streams, while macroinvertebrate community structure differed distinctly between the deer-excluded and grazed catchments at all stream orders. Burrowing collector-gatherers, which inhabit fine streambed sediments, were less abundant in first-order streams in the deer-excluded catchment than the grazed catchments, while clinging collector-filterers, which are vulnerable to suspended sediment inputs, were more abundant in second- and third-order streams of the deer-excluded catchment than the grazed catchments. These results suggest that the effect of deer exclusion on stream ecosystems varies with longitudinal changes in sediment deposition and transport capacity. Hydro-geomorphological processes are thus fundamental to assessing the restoration of forest-stream ecosystems, particularly in spatiotemporally dynamic headwater systems. [ABSTRACT FROM AUTHOR]
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- 2023
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4. Fallout volume and litter type affect 137Cs concentration difference in litter between forest and stream environments.
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Sakai, Masaru, Gomi, Takashi, and Negishi, Junjiro N.
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FOREST ecology , *LEACHING , *HETEROGENEITY , *DECIDUOUS plants - Abstract
It is important to understand the changes in the 137 Cs concentration in litter through leaching when considering that 137 Cs is transferred from basal food resources to animals in forested streams. We found that the difference of 137 Cs activity concentration in litter between forest and stream was associated with both litter type and 137 Cs fallout volume around Fukushima, Japan. The 137 Cs activity concentrations in the litter of evergreen conifers tended to be greater than those in the litter of broad-leaved deciduous trees because of the absence of deciduous leaves during the fallout period in March 2011. Moreover, 137 Cs activity concentrations in forest litter were greater with respect to the 137 Cs fallout volume. The 137 Cs activity concentrations in stream litter were much lower than those in forest litter when those in forest litter were higher. The 137 Cs leaching patterns indicated that the differences in 137 Cs activity concentration between forest and stream litter could change with changes in both fallout volume and litter type. Because litter is an important basal food resource in the food webs of both forests and streams, the 137 Cs concentration gradient reflects to possible 137 Cs transfer from lower to higher trophic animals. Our findings will improve our understanding of the spatial heterogeneity and variability of 137 Cs concentrations in animals resident to the contaminated landscape. [ABSTRACT FROM AUTHOR]
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- 2016
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5. Contrasting seasonality of 137Cs concentrations in two stream animals that share a trophic niche.
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Sakai, Masaru, Ishii, Yumiko, Tsuji, Hideki, Tanaka, Asuka, Jo, Jaeick, Negishi, Junjiro N., and Hayashi, Seiji
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CESIUM isotopes ,FOOD contamination ,CARNIVOROUS animals ,AQUATIC animals ,EXCRETION - Abstract
Understanding the seasonality of
137 Cs concentrations in aquatic animals is crucial for reviving local inland fisheries. The seasonality of137 Cs concentrations in animals is expected to vary, even if focal species consume similarly contaminated foods because the137 Cs excretion rate is species-specific, and137 Cs uptake by foraging autochthonous food resources also vary among seasons. Here, we conducted a seasonal monitoring survey of dissolved137 Cs concentrations as an indicator of the contamination level of food resources and measured137 Cs concentrations in two carnivorous aquatic animals (Palaemon paucidens and Rhinogobius sp.) that share a trophic niche in a stream connected to a dam reservoir. The dissolved137 Cs concentration had clear seasonality—high in summer and low in winter. The137 Cs concentrations in the animals revealed a different seasonal pattern—it peaked in October in P. paucidens and peaked in February in Rhinogobius. Overall, the137 Cs concentration was relatively higher in P. paucidens than in Rhinogobius , suggesting that P. paucidens has a lower excretion rate than Rhinogobius. Consequently, the seasonality of the137 Cs concentration in P. paucidens showed temporal changes similar to those of the dissolved137 Cs concentration, which were likely affected by137 Cs uptake through foraging, whereas that in Rhinogobius was controlled by137 Cs excretion. This study shows that the seasonality of137 Cs concentration can differ between sympatric animals that share a trophic niche. Accumulating knowledge and comparing the seasonality of137 Cs concentrations in fisheries species based on the balance between uptake and excretion will be valuable to determine the appropriate seasons to obtain less-contaminated products. [Display omitted] • Two sympatric species that belong to different phyla was compared. • Stable carbon and nitrogen ratios showed that the two species share a trophic niche. • Dissolved137 Cs concentration peaked in summer and dropped in winter. • The two species showed different seasonality of137 Cs concentrations. •137 Cs seasonality varies with interspecific variations of excretion rates in animals. [ABSTRACT FROM AUTHOR]- Published
- 2022
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6. Different cesium-137 transfers to forest and stream ecosystems.
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Sakai, Masaru, Gomi, Takashi, Negishi, Junjiro N., Iwamoto, Aimu, and Okada, Kengo
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CESIUM ,FOREST ecology ,ENVIRONMENTAL impact analysis ,SALMONIDAE ,LEACHING - Abstract
Understanding the mechanisms of 137 Cs movement across different ecosystems is crucial for projecting the environmental impact and management of nuclear contamination events. Here, we report differential movement of 137 Cs in adjacent forest and stream ecosystems. The food webs of the forest and stream ecosystems in our study were similar, in that they were both dominated by detrital-based food webs and the basal energy source was terrestrial litter. However, the concentration of 137 Cs in stream litter was significantly lower than in forest litter, the result of 137 Cs leaching from litter in stream water. The difference in 137 Cs concentrations between the two types of litter was reflected in the 137 Cs concentrations in the animal community. While the importance of 137 Cs fallout and the associated transfer to food webs has been well studied, research has been primarily limited to cases in a single ecosystem. Our results indicate that there are differences in the flow of 137 Cs through terrestrial and aquatic ecosystems, and that 137 Cs concentrations are reduced in both basal food resources and higher trophic animals in aquatic systems, where primary production is subsidized by a neighboring terrestrial ecosystem. [ABSTRACT FROM AUTHOR]
- Published
- 2016
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7. Radiocesium leaching from contaminated litter in forest streams.
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Sakai, Masaru, Gomi, Takashi, Naito, Risa S., Negishi, Junjiro N., Sasaki, Michiko, Toda, Hiroto, Nunokawa, Masanori, and Murase, Kaori
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CESIUM isotopes , *RADIOISOTOPES , *LEACHING , *FORESTS & forestry , *CRYPTOMERIA japonica , *CONTAMINATION (Psychology) - Abstract
In Japanese forests suffering from the Fukushima Daiichi Nuclear Power Plant accident, litter fall provides a large amount of radiocesium from forests to streams. Submerged litter is processed to become a vital food resource for various stream organisms through initial leaching and subsequent decomposition. Although leaching from litter can detach radiocesium similarly to potassium, radiocesium leaching and its migration are poorly understood. We examined both radiocesium and potassium leaching to the water column and radiocesium allocation to minerals (glass beads, silica sand, and vermiculite) in the laboratory using soaked litter with and without minerals on a water column. The mineral types did not affect radiocesium leaching from litter, but soaking in water for 1, 7, and 30 days decreased the radiocesium concentration in litter by ×0.71, ×0.66, and ×0.56, respectively. Meanwhile, the 1-, 7-, and 30-day experiments decreased potassium concentration in litter by ×0.17, ×0.11, and ×0.09, respectively. Leached radiocesium remained in a dissolved form when there was no mineral phases present in the water, whereas there was sorption onto the minerals when they were present. In particular, vermiculite adsorbed radiocesium by two to three orders of magnitude more effectively than the other minerals. Because radiocesium forms (such as that dissolved or adsorbed to organic matter or minerals) can further mobilize to ecosystems, our findings will increase our understanding regarding the dynamics of radiocesium in stream ecosystems. [ABSTRACT FROM AUTHOR]
- Published
- 2015
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8. Soil removal as a decontamination practice and radiocesium accumulation in tadpoles in rice paddies at Fukushima.
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Sakai, Masaru, Gomi, Takashi, Nunokawa, Masanori, Wakahara, Taeko, and Onda, Yuichi
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BIOACCUMULATION ,CESIUM ,TADPOLES ,RANIDAE ,PHYSIOLOGICAL effects of radioisotopes ,RADIOACTIVE decontamination ,PADDY fields ,INVERTEBRATES - Abstract
We investigated the biological accumulation of radiocesium in tadpoles [Rana (Pelophylax) porosa porosa] in rice paddies with and without decontamination practice at Fukushima. Radiocesium was accumulated in surface part of soils both in the control and decontaminated paddies one year after decontamination. Mean
134 Cs and137 Cs concentrations in tadpoles in the control and decontaminated paddies were 3000 and 4500, and 600 and 890 Bq/kg dry weight, respectively. Radiocesium concentrations in surface soil (0–5 cm depth) and tadpoles in the decontaminated paddy were five times smaller than in the control paddy. These results suggest that decontamination practice can reduce radiocesium concentrations in both soil and tadpoles. However, at the decontaminated paddy, radiocesium concentrations in surface soils became 3.8 times greater one year after decontamination, which indicates that monitoring the subsequent movement of radiocesium in rice paddies and surrounding areas is essential for examining contamination propagation. [Copyright &y& Elsevier]- Published
- 2014
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9. Stability of a Locking Plate and Self-Drilling Screws as Orthodontic Skeletal Anchorage in the Maxilla: A Retrospective Study.
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Hibi, Hideharu, Sakai, Kiyoshi, Oda, Tomoo, Hattori, Hisashi, Ueda, Minoru, and Sakai, Masaru
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Purpose: The aim of this retrospective study was to determine the success rate of an orthodontic skeletal anchorage system consisting of a locking plate and 2 self-drilling screws to intrude the upper molars and detect factors that contribute to its stability. Patients and Methods: The subjects were 32 orthodontic and generally healthy patients who had skeletal anchorage plates placed supraperiosteally and unilaterally or bilaterally. The anchorage plate was considered successful if the plate remained stable throughout the period of intrusion of the upper molar without any movement, persistent pain, or infection and was then retrieved without difficulty. The success rates of the anchorage plate were statistically analyzed on the basis of clinically categorized variables. Results: The 32 patients comprised 6 male and 26 female individuals with ages ranging from 11.4 to 35.1 years. The overall success rate of the total 61 plates was 93.4%. No significant differences were observed among the respective success rates analyzed in accordance with gender, age, side of placement, and length of the screws. The thickness of the bony walls that supported the screws was significantly greater in the success group (mean 1.6 ± SD, 0.2 vs 1.0 ± 0.1 mm, P < .001). Conclusion: Bone thickness is a critical factor in supporting the self-drilling screws and locking plate. Skeletal anchorage combining the plate and 2 screws promises a higher success rate with a thicker bone than with the threshold value of thickness that exists within the 1.1 to 1.4 mm range in the maxillary walls. [Copyright &y& Elsevier]
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- 2010
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10. Untangling radiocesium dynamics of forest-stream ecosystems: A review of Fukushima studies in the decade after the accident.
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Sakai, Masaru, Tsuji, Hideki, Ishii, Yumiko, Ozaki, Hirokazu, Takechi, Seiichi, Jo, Jaeick, Tamaoki, Masanori, Hayashi, Seiji, and Gomi, Takashi
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RESERVOIR sedimentation ,ECOSYSTEM dynamics ,ECOLOGICAL disturbances ,CESIUM isotopes ,RADIOACTIVE fallout ,FUKUSHIMA Nuclear Accident, Fukushima, Japan, 2011 ,FOREST soils ,NUCLEAR energy - Abstract
Forest-stream ecosystems are widespread and biodiverse terrestrial landscapes with physical and social connections to downstream human activities. After radiocesium is introduced into these ecosystems, various material flows cause its accumulation or dispersal. We review studies conducted in the decade after the Fukushima nuclear accident to clarify the mechanisms of radiocesium transfer within ecosystems and to downstream areas through biological, hydrological, and geomorphological processes. After its introduction, radiocesium is heavily deposited in the organic soil layer, leading to persistent circulation due to biological activities in soils. Some radiocesium in soils, litter, and organisms is transported to stream ecosystems, forming contamination spots in depositional habitats. While reservoir dams function as effective traps, radiocesium leaching from sediments is a continual phenomenon causing re-contamination downstream. Integration of data regarding radiocesium dynamics and contamination sites, as proposed here, is essential for contamination management in societies depending on nuclear power to address the climate crisis. [Display omitted] • Various material flows in forest-stream ecosystems cause radiocesium migrations. • Studies in forest-stream ecosystems after the Fukushima accident were reviewed. • Radiocesium accumulates in organic forest soils and depositional stream environments. • Integrating biotic and abiotic processes are essential for contamination management. [ABSTRACT FROM AUTHOR]
- Published
- 2021
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11. Orthodontic Anchorage System Using a Locking Plate and Self-Drilling Screws.
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Hibi, Hideharu, Ueda, Minoru, Sakai, Masaru, and Ikemori, Yoshiyuki
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- 2006
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12. Developing a food web-based transfer factor of radiocesium for fish, whitespotted char (Salvelinus leucomaenis) in headwater streams.
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Haque, Md. Enamul, Gomi, Takashi, Sakai, Masaru, and Negishi, Junjiro N.
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FOOD contamination , *FOOD chains , *TRANSFER factor (Immunology) , *MONOCHAMUS scutellatus , *PREDATION - Abstract
We developed a food web-based transfer factor ( TF web ) to study contaminant movements from multiple prey items to a predator based on the dietary contributions of prey items with their respective contamination levels. TF web was used to evaluate the transfer of 137 Cs into whitespotted char ( Salvelinus leucomaenis ) from the trophic structure of a stream–riparian ecosystem in headwater streams draining a Japanese cedar forest. We also examined the applicability of this method by comparing sites with different contamination levels but similar surrounding environments in Fukushima and Gunma. All samples were collected from August 2012 to May 2013. The dietary contributions from both aquatic and terrestrial prey items to whitespotted char were analyzed using stable carbon and nitrogen isotope ratios. 137 Cs activity concentrations in char ranged from 704 to 6082 Bq kg −1 -dry in Fukushima and from 193 to 618 Bq kg −1 -dry in Gunma. Dominant prey taxa such as mayflies ( Ephemera japonica ), spider crickets (Rhaphidosphoridae gen. spp.), and freshwater crabs ( Geothelphusa dehaani ), each of them accounted for 3–12% of the fish diet, based on lower and upper estimates, respectively. TF web ranged from 1.12 to 3.79 in Fukushima and from 1.30 to 4.30 in Gunma, which suggested bioaccumulation from prey items to predator. Widely used ecological parameters TF s by media–char and TTF by single prey–char showed high variability with both dilution and accumulation. TF web is applicable for 137 Cs transfer in predator-prey systems with complex food web structures of stream-riparian ecosystems. [ABSTRACT FROM AUTHOR]
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- 2017
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13. Effects of organic solvents on drug incorporation into polymeric carriers and morphological analyses of drug-incorporated polymeric micelles
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Harada, Yoshiko, Yamamoto, Tatsuhiro, Sakai, Masaru, Saiki, Toshiharu, Kawano, Kumi, Maitani, Yoshie, and Yokoyama, Masayuki
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ORGANIC solvents , *DRUG carriers , *MICELLES , *POLYMERS , *CAMPTOTHECIN , *EVAPORATION (Chemistry) , *CHLOROFORM , *PHARMACOKINETICS - Abstract
Abstract: We incorporated an anticancer agent, camptothecin (CPT), into polymeric micelle carriers by using two different solvents (TFE and chloroform) in the solvent-evaporation drug incorporation process. We observed significant differences in the drug-incorporation behaviors, in the morphologies of the incorporated drug and the polymeric micelles, and in the pharmacokinetic behaviors between the two solvents’ cases. In particular, the CPT-incorporated polymeric micelles prepared with TFE as the incorporation solvent exhibited more stable circulation in blood than those prepared with chloroform. This contrast indicates a novel technological perspective regarding the drug incorporation into polymeric micelle carriers. Morphological analyses of the inner core have revealed the presence of the directed alignment of the CPT molecules and CPT crystals in the micelle inner core. This is the first report of the morphologies of the drug incorporated into the polymeric micelle inner cores. We believe these analyses are very important for further pharmaceutical developments of polymeric micelle drug-carrier systems. [ABSTRACT FROM AUTHOR]
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- 2011
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14. Synthesis, further biological evaluation and pharmacodynamics of newly discovered inhibitors of TNF-α production
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Matsui, Toshiaki, Kondo, Takashi, Nakatani, Shingo, Omawari, Nagashige, Sakai, Masaru, Mori, Hideaki, Ogata, Akihito, Kato, Junya, Ohno, Hiroyuki, Obata, Takaaki, Nakai, Hisao, and Toda, Masaaki
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PHENETHYLAMINES , *PHOSPHATES , *METABOLISM - Abstract
(1S,2R)-2-Acylamino-1-methyl-2-phenylethyl phosphate derivatives 2a, 2b, 3a, and 5a, which are conformationally restricted and metabolically stable analogues of (2R)-2-acylamino-2-phenylethyl phosphate derivatives 1a and 1b, are a new class of inhibitors of TNF-α production. More efficient alternative synthesis of a key intermediate, (1R,2S)-1-amino-1-(3-methoxyphenyl)propan-2-ol hydrochloride (9), was achieved using one-step, three-component coupling of 3-methoxyphenyl boronic acid (13), (5S)-2,2,5-trimethyl-1,3-dioxolan-4-ol (14), and amino diphenyl methane (15), [as reported in J. Am. Chem. Soc. 1998, 120, 11798]. Evaluation of the hypotensive activity of these compounds was done to assess one of their side effects. Among the compounds tested, the above-mentioned four compounds (2a, 2b, 3a, and 5a) were identified as inhibitors with both sufficient potency and an acceptable safety margin regarding their hypotensive activity. The pharmacodynamics of these compounds were also investigated. Single-dose pharmacokinetic data for compounds 2a, 2b, 3a, and 5a are displayed. These compounds were estimated to be mainly metabolized by the liver in the species tested based on their in vitro stability in tissue homogenates and plasma. A representative compound, 2a, showed good linearity of its plasma concentration after intravenous injection. [Copyright &y& Elsevier]
- Published
- 2003
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15. Discovery of Novel Phosphonic Acid Derivatives as New Chemical Leads for Inhibitors of TNF-α production
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Matsui, Toshiaki, Takahashi, Shinya, Matsunaga, Naoki, Nakamura, Kazunori, Omawari, Nagashige, Sakai, Masaru, Kamoshima, Wataru, Terai, Kouichiro, Ohno, Hiroyuki, Obata, Takaaki, Nakai, Hisao, and Toda, Masaaki
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PHOSPHONIC acids , *TUMOR necrosis factors , *CHEMICAL inhibitors - Abstract
2-(Acylamino)benzylphosphonic acid 6 derived from an artificial substrate of sphingomyelinase was found to show inhibitory activity of TNF-α production. Structural optimization was started with the chemical modification of 6. The discovery of another chemical leads 7, 8, 10 and 16 for the development of structurally new inhibitors of TNF-α production is reported. [Copyright &y& Elsevier]
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- 2002
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16. Highly potent inhibitors of TNF-α production. Part I: Discovery of new chemical leads and Their structure–Activity relationships
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Matsui, Toshiaki, Kondo, Takashi, Nishita, Yoshitaka, Itadani, Satoshi, Nakatani, Shingo, Omawari, Nagashige, Sakai, Masaru, Nakazawa, Shuichi, Ogata, Akihito, Mori, Hideaki, Terai, Kouichiro, Kamoshima, Wataru, Ohno, Hiroyuki, Obata, Takaaki, Nakai, Hisao, and Toda, Masaaki
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TUMOR necrosis factors , *CHEMICAL inhibitors , *STRUCTURE-activity relationships - Abstract
Discovery of new chemical leads of inhibitors for TNF-α production starting from the chemical modification of 1 is reported. Further biological studies of 1 to disclose the site of its action strongly suggested that 1 inhibits LPS-induced TNF-α expression in the liver and spleen of mice. Structure–activity relationships (SARs) are also discussed and full details including the chemistry are reported. [Copyright &y& Elsevier]
- Published
- 2002
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17. Highly potent inhibitors of tnf-α production. Part II: metabolic stabilization of a newly found chemical lead and conformational analysis of an active diastereoisomer
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Matsui, Toshiaki, Kondo, Takashi, Nishita, Yoshitaka, Itadani, Satoshi, Tsuruta, Hiroshi, Fujita, Setsuko, Omawari, Nagashige, Sakai, Masaru, Nakazawa, Shuichi, Ogata, Akihito, Mori, Hideaki, Kamoshima, Wataru, Terai, Kouichiro, Ohno, Hiroyuki, Obata, Takaaki, Nakai, Hisao, and Toda, Masaaki
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TUMOR necrosis factors , *CHEMICAL inhibitors , *DIASTEREOISOMERS - Abstract
Design and synthesis of metabolically stabilized inhibitors of TNF-α production, which could be new drug candidates, are reported. Conformational analysis of an active diastereoisomer was performed based on biological evaluations of the conformationally fixed indane derivatives 17 and 18. Structure–activity relationships (SARs) based on biological evaluations of the optically active derivatives are also discussed. Full details including chemistry are reported. [Copyright &y& Elsevier]
- Published
- 2002
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18. Highly potent inhibitors of TNF-α production. Part 2: identification of drug candidates
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Matsui, Toshiaki, Kondo, Takashi, Nishita, Yoshitaka, Itadani, Satoshi, Tsuruta, Hiroshi, Fujita, Setsuko, Omawari, Nagashige, Sakai, Masaru, Nakazawa, Shuichi, Ogata, Akihito, Mori, Hideaki, Ohno, Hiroyuki, Obata, Takaaki, Nakai, Hisao, and Toda, Masaaki
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METHYL groups , *PHARMACOLOGY - Abstract
Metabolic stabilization of the chemical lead 1, which is a structurally novel inhibitor of TNF-α production, was accomplished by introducing a (1S)-methyl group into the optically active backbone. As a result, 2, 3 and 4 were identified as drug candidates and evaluated pharmacologically. The analysis of an active conformer was also carried out. [Copyright &y& Elsevier]
- Published
- 2002
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19. Highly Potent Inhibitors of TNF-α Production. Part 1: Discovery of Chemical Leads
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Matsui, Toshiaki, Kondo, Takashi, Nishita, Yoshitaka, Itadani, Satoshi, Nakatani, Shingo, Omawari, Nagashige, Sakai, Masaru, Nakazawa, Shuichi, Ogata, Akihito, Ohno, Hiroyuki, Obata, Takaaki, Nakai, Hisao, and Toda, Masaaki
- Subjects
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PHOSPHATES , *TUMOR necrosis factors - Abstract
The discovery of 2-acylamino-2-phenylethyl disodium phosphates and as structurally novel inhibitors of TNF-α production is reported. Structure–activity relationships (SARs) are also discussed. [Copyright &y& Elsevier]
- Published
- 2002
- Full Text
- View/download PDF
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