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Yoshihiko Fujita,Masahiko Kimura,Hiroki Sato,Toshikazu Takata,Nobufumi Ono,Kazuto Nishio 대한약학회 2016 Archives of Pharmacal Research Vol.39 No.6
Rotaxanes comprise a class of interlocked moleculescontaining a wheel threaded onto an axle with blockinggroups on the ends to keep thewheel fromsliding off.Here,weshow that [2][bis(2-(3,5-dimethylphenylcarbonyloxy)ethyl)ammoniumtrifluoromethanesulfonate]-[dibenzo-24-crown-8]rotaxane (TRO-A0001), a rotaxane compound, exerted agrowth inhibitory effect on several human cancer cell lines.AnMTT assay revealed an IC50 of 14-830 nMfor TRO-A0001 inthese cells. Neither the wheel nor the axle part alone inhibitedtumor cell growth, suggesting that the complete rotaxanemolecule with its unique ‘‘intramolecular mobility’’ is requiredto inhibit cell growth. Annexin-V/PI staining provided evidenceof the induction of apoptosis, which was further confirmedby the observation of poly (ADP-ribose) polymerasecleavage. Furthermore, a cell cycle analysis using flowcytometry showed that TRO-A0001 treatment resulted in G1arrest in glioblastoma T98G and melanoma G361 cells. Animmunoblot analysis revealed that in both cell lines, TROA0001treatment caused the induction of p21/Cip1, therebydown-regulating Cdks 2, 4 and 6 and reducing Cyclins D1 andE. The results presented in this study demonstrate cytotoxicityof the rotaxane compound and its potential as a lead compoundfor the development of a chemotherapeutic agent againstcancer.
SAFB1, an RBMX-binding protein, is a newly identified regulator of hepatic SREBP-1c gene
( Yasushi Omura ),( Yoshihiko Nishio ),( Tadashi Takemoto ),( Chikako Ikeuchi ),( Osamu Sekine ),( Katsutaro Morino ),( Yasuhiro Maeno ),( Toshiyuki Obata ),( Satoshi Ugi ),( Hiroshi Maegawa ),( Hiros 생화학분자생물학회 2009 BMB Reports Vol.42 No.4
Satoshi Ugi,Hiroshi Maegawa,Katsutaro Morino,Yoshihiko Nishio,Toshiyuki Sato,Seiki Okada,Yasuo Kikkawa,Toshihiro Watanabe,Hiromu Nakajima,Atsunori Kashiwagi 대한당뇨병학회 2016 Diabetes and Metabolism Journal Vol.40 No.4
Background: Management of postprandial hyperglycemia is a key aspect in diabetes treatment. We developed a novel system to measure glucose area under the curve (AUC) using minimally invasive interstitial fluid extraction technology (MIET) for simple monitoring of postprandial glucose excursions. In this study, we evaluated the relationship between our system and continuous glucose monitoring (CGM) by comparing glucose AUC obtained using MIET with that obtained using CGM for a long duration. Methods: Twenty diabetic inpatients wearing a CGM system were enrolled. For MIET measurement, a plastic microneedle array was applied to the skin as pretreatment, and hydrogels were placed on the pretreated area to collect interstitial fluid. Hydrogels were replaced every 2 or 4 hours and AUC was predicted on the basis of glucose and sodium ion levels. Results: AUC predicted by MIET correlated well with that measured by CGM (r=0.93). Good performances of both consecutive 2- and 4-hour measurements were observed (measurement error: 11.7%±10.2% for 2 hours and 11.1%±7.9% for 4 hours), indicating the possibility of repetitive measurements up to 8 hours. The influence of neither glucose fluctuation nor average glucose level over the measurement accuracy was observed through 8 hours. Conclusion: Our system showed good relationship with AUC values from CGM up to 8 hours, indicating that single pretreatment can cover a large portion of glucose excursion in a day. These results indicated possibility of our system to contribute to convenient monitoring of glucose excursions for a long duration.