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Syed Mashhood Ali*,Mamoru Koketsu,Fahmeena Asmat 대한화학회 2006 Bulletin of the Korean Chemical Society Vol.27 No.9
A detailed spectroscopic study (1H NMR, COSY, ROESY) of complexation of venlafaxine hydrochloride (VEN) with b-cyclodextrin (b-CD) was carried out in solution. The stoichiometry of the complex was determined to be 1 : 1 and penetration of aromatic ring into b-Cyclodextrin cavity was confirmed from primary rim side, with the help of ROESY spectral data. The structure of the venlafaxine hydrochloride-b-CD complex has been proposed. The association constant was determined to be 234 M-1.
Ali, Syed Mashhood,Koketsu, Mamoru,Asmat, Fahmeena Korean Chemical Society 2006 Bulletin of the Korean Chemical Society Vol.27 No.9
A detailed spectroscopic study ($^1H$ NMR, COSY, ROESY) of complexation of venlafaxine hydrochloride (VEN) with $\beta$-cyclodextrin ($\beta$--CD) was carried out in solution. The stoichiometry of the complex was determined to be 1 : 1 and penetration of aromatic ring into $\beta$-Cyclodextrin cavity was confirmed from primary rim side, with the help of ROESY spectral data. The structure of the venlafaxine hydrochloride-$\beta$-CD complex has been proposed. The association constant was determined to be 234 $M^{-1}$.
Inhibitory effects of 1,3-thiazine derivatives on melanogenesis.
Ha, Sang Keun,Koketsu, Mamoru,Lee, Minjae,Moon, Eunjung,Kim, Sung-Hoon,Yoon, Tae-Jin,Kim, Sun Yeou Pharmaceutical Society of Great Britain 2009 Journal of pharmacy and pharmacology Vol.61 No.12
<P>OBJECTIVES: The aim of this study was to identify a novel skin-depigmenting agent from synthetic 1,3-thiazine derivatives. METHODS: We investigated the inhibitory effects of six kinds of 1,3-thiazine derivative on melanogenesis by examining their effects on tyrosinase activity and melanin biosynthesis in melan-a cells and the zebrafish model. KEY FINDINGS: Of the six compounds, 4-hydroxy-2,6-dimethyl-5,6-dihydro-4H-1,3-thiazine (TZ-6) had the strongest anti-melanogenic effects in cultured melan-a cells (30.4% inhibition at 100 mum). In addition, TZ-6 exhibited an inhibitory effect on mushroom and cellular tyrosinase. Based on the results of Western blotting, TZ-6 reduced the expression of tyrosinase at 100 mum. Additionally, TZ-6 reduced body pigmentation and inhibited tyrosinase activity in the zebrafish model. CONCLUSIONS: The results have provided useful information for the development of a skin whitening agent.</P>
Ahn, Hak Jun,Koketsu, Mamoru,Yang, Eun Mi,Kim, Yong Man,Ishihara, Hideharu,Yang, Hyun Ok Wiley Subscription Services, Inc., A Wiley Company 2006 Journal of cellular biochemistry Vol.99 No.3
<P>We examined the ability of the synthetic selenium compound, 2-(4-methylphenyl)-1,3-selenazol-4-one (hereafter designated 3a), to induce apoptosis in a human ovarian cancer cell line (SKOV3) and a human leukemia cell line (HL-60). Flow cytometry showed that 3a treatment induced apoptosis in both cell lines to degrees comparable to that of the positive control, paclitaxel. Apoptosis was measured by PS externalization, DNA fragmentation and decreased mitochondrial membrane potential (MMP). However, analysis of the mechanism of action revealed differences between the responses of the two cell lines. Treatment with 3a arrested the cell cycle and induced caspase-3 activation in HL-60 cells, but not in SKOV3 cells. In contrast, 3a treatment induced apoptosis through translocation of AIF, a novel pro-apoptotic protein, in SKOV3 cells, but not in HL-60 cells. Collectively, our data demonstrated that 3a induced apoptosis in both cell lines, but via different action mechanisms. J. Cell. Biochem. 99: 807–815, 2006. © 2006 Wiley-Liss, Inc.</P>
( Sang Yoon Choi ),( Yeon Ock Jo ),( Mamoru Koketsu ),( Hideharu Ishihara ),( Sung Hoon Kim ),( Sun Yeou Kim ) 한국응용생명화학회 2009 Applied Biological Chemistry (Appl Biol Chem) Vol.52 No.4
In this study, the inhibitory effects of selenium-containing heterocyclic compound, selenazol derivatives on LPS-induced nitric oxide production in macrophage cells (RAW 264.7) were assessed. Five kinds of selenazol derivatives were shown to exhibit 5.4~41.7% of inhibitory effects at 10 μM. Among them, 2-(4-chlorophenyl)-1,3-selenazol-4-one generally evidenced a high degree of inhibitory activity with IC50=11.8 μM, and this compound also profoundly suppressed iNOS expression in LPS-treated RAW 264.7 cells. These results indicated that 2-(4-chlorophenyl)-1,3-selenazol-4-one might function as an anti-inflammatory agent via the inhibition of iNOS-mediated nitric oxide production.
Choi, Sang-Yoon,Jo, Yeon-Ock,Koketsu, Mamoru,Ishihara, Hideharu,Kim, Sung-Hoon,Kim, Sun-Yeou The Korean Society for Applied Biological Chemistr 2009 Applied Biological Chemistry (Appl Biol Chem) Vol.52 No.4
In this study, the inhibitory effects of selenium-containing heterocyclic compound, selenazol derivatives on LPS-induced nitric oxide production in macrophage cells (RAW 264.7) were assessed. Five kinds of selenazol derivatives were shown to exhibit $5.4{\sim}41.7%$ of inhibitory effects at $10{\mu}M$. Among them, 2-(4-chlorophenyl)-1,3-selenazol-4-one generally evidenced a high degree of inhibitory activity with $IC_{50}=11.8{\mu}M$, and this compound also profoundly suppressed iNOS expression in LPS-treated RAW 264.7 cells. These results indicated that 2-(4-chlorophenyl)-1,3-selenazol-4-one might function as an anti-inflammatory agent via the inhibition of iNOS-mediated nitric oxide production.