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Ito N.,Gunma University | Shibuguchi N.,Analytical Research | Ishikawa R.,Gunma Prefectural College of Health Sciences | Tanaka S.,Takasaki University of Health and Welfare | And 3 more authors.
Bioscience, Biotechnology and Biochemistry | Year: 2013

Calcineurin (CN) is a Ca2+/calmodulin (CaM) dependent serine/threonine protein phosphatase and plays important role in several cellular functions in both higher and lower eukaryotes. Here we report inhibition of CN by linear alkylbenzene sulfonate. The clue to the finding was obtained while identifying the inhibitory material leaching from acrylonitrile butadiene rubber used for packing. Using standard dodecylbenzene sulfonate (C12-LAS), we obtained strong inhibition of CN with a half maximal inhibitory concentration of 9.3μM, whereas analogs such as p-octylbenzene sulfonate and SDS hardly or only slightly affected CN activity. Three alkaline phosphatases, derived from shrimp, bacteria, and calf-intestine, which exhibit similar enzymatic activities to CN, were not inhibited by C12-LAS at concentrations of up to 100μM. Furthermore, C12-LAS did not inhibit Ca2+/CaM-dependent myosin light chain kinase activity when tested at concentrations of up to 36μM. The results indicate that C12-LAS is a potent selective inhibitor of CN activity. Source


Tian F.,University of Shanghai for Science and Technology | Li Y.,East China University of Science and Technology | Xing J.,East China University of Science and Technology | Tian H.,CAS Zhengzhou Research Institute | And 3 more authors.
Materials Letters | Year: 2014

Anatase titanium dioxide nanosheets with exposed highly active {001} facets are very important for photo-catalysis because of their superior catalytic properties. However, pores are always found to be present on the nanosheets in transmission electron microscopy (TEM) observation, which would degrade their catalytic performance. The origin of the pores is as yet unclear. In this study we use TEM to investigate the origin and nature of the pores. It is found that, instead of chemicals used in the preparation process, it is irradiation damage from the electron beam results in the pores. © 2014 Published by Elsevier B.V. Source


Ishida M.,Global Formulation Research | Ishida M.,Pharmaceutical Science and Technology Core Function Unit | Uchiyama J.,New Chemical Entity Demand Chain Unit | Isaji K.,Analytical Research | And 5 more authors.
Drug Development and Industrial Pharmacy | Year: 2014

The applicability of porous spherical silica (PSS) was evaluated as core particles for pharmaceutical products by comparing it with commercial core particles such as mannitol (NP-108), sucrose and microcrystalline cellulose spheres. We investigated the physical properties of core particles, such as particle size distribution, flow properties, crushing strength, plastic limit, drying rate, hygroscopic property and aggregation degree. It was found that PSS was a core particle of small particle size, low friability, high water adsorption capacity, rapid drying rate and lower occurrence of particle aggregation, although wettability is a factor to be carefully considered. The aggregation and taste-masking ability using PSS and NP-108 as core particles were evaluated at a fluidized-bed coating process. The functional coating under the excess spray rate shows different aggregation trends and dissolution profiles between PSS and NP-108; thereby, exhibiting the formation of uniform coating under the excess spray rate in the case of PSS. This expands the range of the acceptable spray feed rates to coat fine particles, and indicates the possibility of decreasing the coating time. The results obtained in this study suggested that the core particle, which has a property like that of PSS, was useful in overcoming such disadvantages as large particle size, which feels gritty in oral cavity; particle aggregation; and the long coating time of the particle coating process. These results will enable the practical fine particle coating method by increasing the range of optimum coating conditions and decreasing the coating time in fluidized bed technology. © 2014 Informa Healthcare USA, Inc. Source


Teleha C.A.,High Output Synthesis | Branum S.,High Output Synthesis | Zhang Y.,High Output Synthesis | Reuman M.E.,High Output Synthesis | And 10 more authors.
Organic Process Research and Development | Year: 2014

The preparation of a novel chemokine receptor type 2 (CCR-2) antagonist is described on a 135 g scale. The synthesis of an all-carbon bicyclic core was accomplished using a radical cyclization strategy using chiral precursors, wherein elaboration led to N-Boc carboxylic acid in good yield. After amidation using a traditional coupling reaction, a reductive amination using enantiomerically enriched 3-methoxy-4-pyranone led to the final compound. Although several steps of the syntheses involved reagents that would not be preferred in process and chromatography was used to provide the free-base diastereomer of the final succinate salt, the overall route went through stable intermediates that could be used for future scale-up. This lab-scale synthesis struck a balance between a quick scale-up and a more thorough process review of all possible methods and routes. © 2014 American Chemical Society. Source


Teleha C.A.,High Output Synthesis | Branum S.,High Output Synthesis | Zhang Y.,High Output Synthesis | Reuman M.E.,High Output Synthesis | And 10 more authors.
Organic Process Research and Development | Year: 2014

The preparation of a chemokine receptor type 2 (CCR-2) antagonist bearing a cyclopenta[b]furan core is described on a 600 g scale. Compared to our previously reported synthesis of the all-carbon core CCR-2 antagonist with a similar peripheral 3-methoxypyran appendage, our work required a redesign of the original Discovery Chemistry route and took advantage of a side product seen in the diastereoselective alkylation reaction. Elaboration by reduction and oxy-cyclization eventually led to the required N-Boc acid method. After amidation using a traditional coupling reaction, a reductive amination using enantiomerically enriched 3-methoxy-4-pyranone led to the final compound. Although several steps of the syntheses involved reagents such as selenium and chromium that would not be used in a large-scale process setting, the overall route went through intermediates that could certainly be used for future scale-up campaigns. The synthesis provided a method to make lab-scale quantities of the final succinate salt to support tox/toleration studies. Relative to the Discovery Chemistry route, this lab-scale route featured novel intermediates that could open new avenues for future research in this area. © 2014 American Chemical Society. Source

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