• Title/Summary/Keyword: Selective hydrolysis

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Selective Inhibitory Effect of New Phosphodiesterase Inhibitors on PDE Isozymes in Guinea pig Cardiac Muscle

  • Lee, Sun-Kyeong;Kwon, Kwang-Il;Zee, Ok-Pyo
    • Archives of Pharmacal Research
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    • v.12 no.4
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    • pp.276-281
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    • 1989
  • Selective inhibition of seven new PDE inhibitors on cyclic nucleotide PDE isozymes was investigated. Three PDE isozymes (PDE I, II and III) of guinea pig left ventricular muscles were used. All tested agents inhibited cyclic AMP hydrolysis by PDE III IN A concentration-dependent manner. Some agents represented more potent and selective inhibitory effect on PDE III than that of imazodan.

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Production of Chiral Epoxides: Epoxide Hydrolase-catalyzed Enantioselective Hydrolysis

  • Choi, Won-Jae;Choi, Cha-Yong
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.10 no.3
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    • pp.167-179
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    • 2005
  • Chiral epoxides are highly valuable intermediates, used for the synthesis of pharmaceutical drugs and agrochemicals. They have broad scope of market demand because of their applications. A major challenge in modern organic chemistry is to generate such compounds in high yields, with high stereo- and regio-selectivities. Epoxide hydrolases (EH) are promising biocatalysts for the preparation of chiral epoxides and vicinal diols. They exhibit high enantioselectivity for their substrates, and can be effectively used in the resolution of racemic epoxides through enantioselective hydrolysis. The selective hydrolysis of a racemic epoxide can produce both the corresponding diols and the unreacted epoxides with high enantiomeric excess (ee) value. The potential of microbial EH to produce chiral epoxides and vicinal diol has prompted researchers to explore their use in the synthesis of epoxides and diols with high ee values.

Rhodamine B Hydrazide Revisited: Chemodosimetric Hg2+-selective Signaling Behavior in Aqueous Environments

  • Kim, Kyoung-Nam;Choi, Myung-Gil;Noh, Jae-Hyun;Ahn, Sang-Doo;Chang, Suk-Kyu
    • Bulletin of the Korean Chemical Society
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    • v.29 no.3
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    • pp.571-574
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    • 2008
  • The well-known Cu2+-selective chemodosimetric behavior of rhodamine B hydrazide was successfully switched to selectivity for Hg2+. The fluorescence signaling is remarkably selective toward Hg2+ ions compared to other common biologically and environmentally important metal ions, including Cu2+ ions. The detection limit was 0.2 mM in an acetate-buffered aqueous 10% methanol solution at pH 5. The OFF-ON type of signaling is due to the selective Hg2+-induced hydrolysis of the lactam ring of the hydrazide as has been reported for the standard Cu2+-signaling process of the same compound. A simple change in medium resulted in clear switching of selective signaling from Cu2+ to Hg2+, which extends the applicability of the easily accessible hydrazide derivative.

Alkaline Hydrolysis Behavior of Poly(trimethylene terephthalate) Fibers Annealed by Passing on the Plate Heater (열처리에 의한 폴리(트리메틸렌 테레프탈레이트) 섬유의 알칼리 가수분해 거동)

  • Hong, Sung-Hak;Choi, Chang-Nam;Choi, Hee;Lee, Seok-Young;Song, Min-Kyu;Kim, Yong
    • Textile Coloration and Finishing
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    • v.15 no.3
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    • pp.132-139
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    • 2003
  • PTT[Poly(trimethylene terephthalate)] fibers was annealed by passing on the plate heater to illuminate the effects of annealing on the alkaline hydrolysis behavior properties with varying the treatment temperature for 0.5 second. The L010 and crystallinity were increased with increases in temperature. With the increases of the temperature, the dynamic viscoelastic behaviors were analyzed to be reduction in $T_{max}(tan\;\delta)$. The weight loss in alkaline solution was two times more rapid for the PTT annealed at $200^\circ{C}$ than the control samples. The kinetics of hydrolysis was confirmed that the hydrolysis of the PTT fibers in the alkaline solution was started from the surface of the fibers and selective to the amorphous region in continuation, on the basis of the results of the increase in crystallinity and the decrease in dye uptake at the initial stage of the hydrolysis.

Lipase Catalyzed Kinetic Resolution of rac-2-(3-Methoxy-4-methylphenyl) propan-1-ol and rac-2-(3-Hydroxy-4-methylphenyl)propyl propanoate for S-(+)-Xanthorrhizol

  • Shafioul, Azam Sharif Mohammed;Cheong, Chan-Seong
    • Bulletin of the Korean Chemical Society
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    • v.33 no.2
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    • pp.409-414
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    • 2012
  • Xanthorrhizol is a bisabolane type of natural sesquiterpene, the major component of essential oils of Curcuma xanthorrhiza. 2-(3-Methoxy-4-methylphenyl)propan-1-ol and 2-(3-hydroxy-4-methyl phenyl)propan-1-ol could be essential building block for enantioselective synthesis of xanthorrhizol. Enantioselective (c = 53%, E = $80{\pm}3$) for R-(+)-2-(3-hydroxy-4-methylphenyl) propan-1-ol and (c = 58%, E = $27{\pm}1$) for R-(+)-2-(3-methoxy-4-methylphenyl) propan-1-ol resolution processes were developed via lipase-catalyzed reaction. We found lipase Aspergillus oryzae (AOL) and Porcine pancreas (PPL) are selective to transesterification and hydrolysis in organic and aqueous phase. Modified demethylated substrate is appropriate for enantioselective hydrolysis reaction without any additives. Enantiopure chiral alcohol was crystallized from ethyl acetate/n-hexane co-solvent system. Gram scale resolved chiral intermediate will facilitate the synthesis of the unnatural S-(+)-xanthorrhizol, the corresponding isomer of the natural one.

Synthesis of Metal Oxide Semiconductor Nanostructures and Their Gas Sensing Properties (금속 산화물 반도체 나노구조의 합성과 가스 감응 특성)

  • Choi, Kwon-Il;Lee, Jong-Heun
    • Journal of the Korean Institute of Electrical and Electronic Material Engineers
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    • v.25 no.8
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    • pp.632-638
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    • 2012
  • The prepartion of various metal oxide nanostructures via hydrothermal method, hydrolysis, thermal evaporation and electrospinning and their applications to chemoresistive sensors have been investigated. Hierarchical and hollow nanostructures prepared by hydrothermal method and hydrolysis showed the high response and fast responding kinetics on account of their high gas accessibility. Thermal evaporation and electrospinning provide the facile routes to prepare catalyst-loaded oxide nanowires and nanofibers, respectively. The loading of noble metal and metal oxide catalyst were effective to achieve rapid response/recovery and selective gas detection.

Mechanism of Erectogenic Effect of the Selective Phosphodiesterase Type 5 Inhibitor, DA-8159

  • Doh, Hyoun-Mie;Shin, Chang-Yell;Son, Mi-Won;Ko, Jun-Il;Yoo, Moo-Hi;Kim, Soon-Hoe;Kim, Won-Bae
    • Archives of Pharmacal Research
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    • v.25 no.6
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    • pp.873-878
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    • 2002
  • OA-8159, a new Phosphodiesterase (PDE) 5 inhibitor, has exhibited potent erectogenic potential in a penile erection test in rats and anesthetized dogs. In this study, we investigated the mechanism of its erectogenic activity by measuring the activity of OA-8159 against a various PDE isozymes and assessing cGMP and cAMP formation in a rabbit corpus cavernosum in vitro. DA-8159 inhibited the PDE 5 activity in rabbit and human platelets, which the $IC_{50}$ was 5.84$\pm$1.70 nM and 8.25$\pm$2.90 nM, respectively. The $IC_{50}$ of DA-8159 on PDE 1, PDE2, PDE 3 and PDE 6 were 870$\pm$57.4 nM, $101\pm$5 $\mu$M, 52.0$\pm$3.53 $\mu$M and 53.3$\pm$2.47 nM, respectively. This suggests that DA-8159 is a potent, highly selective, competitive inhibitor of PDE 5-catalyzed cGMP hydrolysis. The rates of cGMP hydrolysis catalyzed by human platelets-derived PDE 5 as a function of the cGMP concentration (5~100 nM) and two-fixed DA-8159 concentration (11.3 and 18.8 nM) were investigated in order to characterize the mode of PDE 5 inhibition by DA-8159. DA-8159 increased the apparent 4K_{m}$ value for cGMP hydrolysis but had no effect on the apparent $V_{max}$, indicating a competitive mode of inhibition. DA-8159 increased the cGMP concentrations in the rabbit corpus cavernosum dose dependently. In the presence of sodium nitroprusside (SNP), DA-8159 significantly sti\mulated the accu\mulation of cGMP when compared to the control level. This indicated that the enhancement of a penile erection by DA-8159 involved the relaxation of the cavernosal smooth \muscle by NO-sti\mulated cGMP accu\mulation. In conclusion, DA-8159 is a selective inhibitor of PDE 5-catalyzed cGMP hydrolysis and the enhancement of a penile erection by DA-8159 is mediated by the relaxation of the cavernosal smooth \muscle by the NO-sti\mulated cGMP accu\mulation.

Characteristic Responses of Biosensor Based on $H^+$-Selective Membrance Electrode (H$^+$ 선택성 막 전극을 이용한 바이오센서의 감응 특성)

  • Kim, Ki-Myo;Park, Sung-Bae;Hwang, Myoung-Seok;Hur, Moon-Hye;Ahn, Moon-Kyu
    • YAKHAK HOEJI
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    • v.40 no.6
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    • pp.625-631
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    • 1996
  • The $H^+$-selective membrane consists of tridodecylamine, 2-nitrophenyl octyl ether and a little amount of additive in carboxylated PVC matrix, where penicillinase(Pcase ) and glutaraldehyde may be covalently attached to the matrix. When the $H^+$-selective electrode was used as a detector of biosensor, calibration curve calculated from Nernst equation was not linear. So we investigated the characteristic responses of the $H^+$-selective electrode to the product H+ from hydrolysis of penicillin-G(Pc-G) and plotted calibration curve correlating potential to concentration of Pc-G linearly. The optimal concentration of buffer solution was theoretically calculated and was also experimented. We tried to explain the linear curve of potential to concentration of Pc-G by using Henderson-Hasselbach equation. This method is more effective in calibration curve plotting than any other previous methods. The results obtained may help in further developing pH electrodes with improved analytical preformance.

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