• Title/Summary/Keyword: YS 55

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Pharmacological Characterization of Synthetic Tetrahydroisoquinoline Alkaloids, YS 51 and YS 55, on the Cardiovascular System

  • Chang, Ki-Churl;Kang, Young-Jin;Lee, Young-Soo;Chong, Won-Seog;Choi-Yun, Hey-Sook;Lee, Duck-Hyong;Ryu, Jae-Chun
    • The Korean Journal of Physiology and Pharmacology
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    • v.2 no.4
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    • pp.461-469
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    • 1998
  • Tetrahydroisoquinoline (THI) alkaloids can be considered as cyclized derivatives of simple phenylethy-lamines, and many of them, especially with 6,7-disubstitution, demonstrate relatively high affinity for catecholamines. Two -OH groups at 6 and 7 positions are supposed to be essential to exert ?${\beta}-receptor$ activities. However, it is not clear whether -OH at 6,7 substitution of THIs also shows ?${\alpha}-adrenoceptor$ activities. In the present study, we investigated whether -OH or $-OCH_3$ substitutions of 6,7 position of THIs differently affect the ?1-adrenoceptor affinity. We synthesized two 1-naphthylmethyl THI alkaloids, $1-{\beta}-naphthylmethyl-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline$ HBr (YS 51) and $1-{\beta}-naphthylmethyl-6, 7-dimethoxy-1,2,3,4-tetrahydroisoquinoline$ HCl (YS 55), and their pharmacological actions on ?${\alpha}_1-adrenoceptor$ were compared. YS 51 and YS 55, concentration-dependently relaxed endothelium-denuded rat thoracic aorta precontracted with phenylephrine (PE, 0.1 ${\mu}M$) in which $pEC_{50}$ were $5.89{\pm}0.21$ and $5.93{\pm}0.19$, respectively. Propranolol (30 nM) did not affect the relaxation-response curves to YS 51 and YS 55. Concentration-response curves to PE were shifted to right by the pretreatment with YS 51 or YS 55. The $pA_2$ values of YS 51 and YS 55 showed $6.05{\pm}0.24$ and $5.88{\pm}0.16$, respectively. Both probes relaxed KCl (65.4 mM)-contracted aorta and inhibited $CaCl_2-induced$ contraction of PE-stimulated endothelium- denuded rat thoracic aorta in $Ca^{2+}-free$ solutions. In isolated guinea pig papillary muscle, 1 and 10 ${\mu}M$ YS 51 increased contractile force about 4- and 8- fold over the control, respectively, along with the concentration-dependent increment of cytosolic $Ca^{2+}$ ions. While, 10 ${\mu}M$ YS 55 reduced the contractile force about 50 % over the control and lowered the cytosolic $Ca^{2+}$ level, in rat brain homogenates, YS 51 and YS 55 displaced $[^3H]prazosin$ binding competitively with Ki 0.15 and 0.12 ${\mu}M$, respectively. However, both probes were ineffective on $[^3H]nitrendipine$ binding. Therefore, it is concluded that two synthetic naphthylmethyl-THI alkaloids have considerable affinity to ?1-adrenenoceptors in rat aorta and brain.

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Molecular Cloning and Expression of a Xylanase Gene from Alkalophilic Bacillus sp.

  • Yu, Ju-Hyun;Kang, Yun-Sook;Park, Young-Seo;Bai, Dong-Hoon
    • Journal of Microbiology and Biotechnology
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    • v.1 no.4
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    • pp.251-255
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    • 1991
  • A 16 kilobase (kb) HindIII fragment of alkalophilic Bacillus sp. YC-335 containing a gene for xylanase synthesis was inserted at the HindIII site of pBR322 and cloned in Escherichia coli HB101. After subcloning of recombinant plasmid pYS52, the 1.5 kb fragment was found to code for xylanase activity, and the hybrid plasmid was named pYS55. The DNA insert of the plasmid was subjected to restriction enzyme mapping, which showed that pYS55 had single site for PuvII and SstI in the 1.5 kb insert fragment. Southern hybridization analysis revealed that the cloned gene was hybridized with chromosomal DNA from alkalophilic Bacillus sp. YC-335. About 64% of the enzyme activity was observed in the extracellular and periplasmic space of E. coli HB10l carrying pYS55.

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Photochemical properties of a Rhodopsin for Light Energy Conversion obtained from Yellow Sea in Korea

  • Kim, So Young;Jung, Kwang-Hwan
    • Rapid Communication in Photoscience
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    • v.2 no.2
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    • pp.52-55
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    • 2013
  • Proteorhodopsin (PR) is a photoinduced proton pump found abundantly in ocean and fresh water habitat, and has an important role in photoenergy conversion to bioenergy in the living cells. Numerous sequences that encode PR protein variants were discovered by environmental genome sequencing and they indicated the high sequence similarity. A new-type of PR (YS-PR) which had been discovered from the surface of Yellow Sea was found to have only 5 amino acid differences from the previously known green-light absorbing PR (GPR) protein, but showed different photochemical properties. This YS-PR showed a 10 nm red-shifted absorption maximum, when compared with GPR. It also showed slower photocycling rate than GPR. However, the photoconversion rate of YS-PR was fast enough to pump protons. Four different amino acids out of 5 were similar to Blue-light absorbing PR (BPR), suggesting that those residues might be responsible for the observed spectral and photoconverting properties.

Comparison of Inodilator Effect of Higenamine, YS49, YS51, Tetrahydroisoquinoline Analogs, and Dobutamine in the Rat

  • Chong, Won-Seog;Lee, Young-Soo;Kang, Young-Jin;Lee, Duck-Hyung;Ryu, Jae-Chun;Yun-Choi, Hye-Sook;Chang, Ki-Churl
    • The Korean Journal of Physiology and Pharmacology
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    • v.2 no.3
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    • pp.323-330
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    • 1998
  • Tetrahydroisoquinoline (THI) alkaloids can be considered as cyclized derivatives of simple phenylethylamines. Many of them, especially with 6,7-disubstitution, demonstrate a relatively high affinity for catecholamines. Present study examines the pharmacological action of limited series of THI, using rats' isolated atria and aorta. In addition, a $[^3H]$ prazosin displacement binding study with THI compounds was performed, using rat brain homogenates to investigate whether these probes have ?${\alpha}$-adrenoceptor affinity. We also compared the vascular relaxation potency of these probes with dobutamine. YS 49, YS 51, higenamine and dobutamine, concentration-dependently, relaxed endothelium-denuded rat thoracic aorta precontracted with phenylephrine (PE, 0.1 ${\mu}M$) in which $pEC_{50}$ were $5.56{\pm}0.32$ and $5.55{\pm}0.21$, $5.99{\pm}1.16$ and $5.57{\pm}0.34$, respectively. These probes except higenamine also relaxed KCl (65.4 mM)-contracted aorta. In isolated rat atria, all THIs and dobutamine increased heart rate and contractile force. In the presence of propranolol, the concentration response curves of YS 49 and YS 51 shifted to the right and resulted in $pA_2$ values of $8.07{\pm}0.84$ and $7.93{\pm}0.11$, respectively. The slope of each compound was not deviated from unity, indicating that these chemicals are highly competitive at the cardiac ?${\beta}-adrenoceptors$. YS 49, YS 51, and higenamine showed ?${\alpha)-adrenoceptor$ affinity in rat brain, in which the dissociation constant $(K_i)$ was 2.75, 2.81, and 1.02 ${\mu}M$, respectively. It is concluded, therefore, that THI alkaloids have weak affinity to ${\alpha)_1-adrenoceptor$ in rat aorta and brain, respectively, while these probes show relatively high affinity for cardiac ${\beta}-adrenoceptors$. Thus, these chemicals may be useful in the treatment of congestive heart failure.

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Evaluation of YasufukuYs Constitutive Model for Compacted Weathered Granite Soil (다짐풍화화강토에 대한 Yasufuku 구성모델의 평가)

  • ;;Li Guang Fan
    • Journal of the Korean Geotechnical Society
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    • v.15 no.5
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    • pp.43-55
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    • 1999
  • This study evaluated Yasufuku's constitutive model in terms of its capability to accurately consider the observed behavior of Iksan compacted weathered granite soil for various stress-paths. The strains calculated from the model are in reasonable agreement with those measured, but some discrepancies occur. The largest differences between measured and calculated strains occur for axial strain of proportional loading with increasing stress. Yasufuku's constitutive model can consider the observed behavior of Iksan compacted weathered granite soil with accuracy for conventional triaxial compression and for p'-constant loading with increasing stress ratio.

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Geochemical Characterization of Rock-Water Interaction in Groundwater at the KURT Site (물 암석 반응을 고려한 KURT 지하수의 지구화학적 특성)

  • Ryu, Ji-Hun;Kwon, Jang-Soon;Kim, Geon-Young;Koh, Yong-Kwon
    • Journal of Nuclear Fuel Cycle and Waste Technology(JNFCWT)
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    • v.10 no.3
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    • pp.189-197
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    • 2012
  • Geochemical composition of fracture filling minerals and groundwater was investigated to characterize geochemical characteristics of groundwater system at the KURT site. Minerals such as calcite, illite, laumontite, chlorite, epidote, montmorillonite, and kaolinite, as well as I/S mixed layer minerals were detected in the minerals extracted from the fracture surfaces of the core samples. The groundwater from the DB-1, YS-1 and YS-4 boreholes showed alkaline conditions with pH of higher than 8. The electrical conductivity (EC) values of the groundwater samples were around $200{\mu}S/cm$, except for the YS-1 borehole. Dissolved oxygen was almost zero in the DB-1 borehole indicating highly reduced conditions. The Cl- concentration was estimated around 5 mg/L and showed homogeneous distribution along depths at the KURT site. It might indicate the mixing between shallow groundwater and deep groundwater. The shallow groundwater from boreholes showed $Ca-HCO_3$ type, whereas deep groundwater below 300 m from the surface indicated $Na-HCO_3$ type. The isotopic values observed in the groundwater ranged from -10.4 to -8.2‰ for ${\delta}^{18}O$ and from -71.3 to -55.0‰for ${\delta}D$. In addition, the isotope-depleted water contained higher fluoride concentration. The oxygen and hydrogen isotopic values of deep groundwater were more depleted compared to the shallow groundwater. The results from age dating analysis using $^{14}C$ indicated relatively younger (2000~6000yr old) groundwater compared to other european granitic groundwaters such as Stripa (Sweden).

Comparison of principle components and quality of eggs by laying hen breeds (산란계 품종별에 따른 계란의 주요 성분과 품질 비교)

  • Kim, Byung Ki;Ha, Jae Jung;Yi, Jun Koo;Oh, Dong Yep;Jung, Dae Jin;Choi, Seong Bok;Hwang, Eun Gyoung;Kim, Soo Jung;Lee, Jea Young
    • Journal of the Korean Data and Information Science Society
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    • v.27 no.5
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    • pp.1307-1316
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    • 2016
  • This study was to execute the random arrangement of total 120 heads (10 heads per treatment plot ${\times}$ 3 repeats ${\times}$ 4 treatment plots) for four breeds [Blue arakana commercial Fowl (BC), Yeonsan silky fowl (YS), Korean native fowl (KN), White leghorn fowl (WL)] with the initiation of laying hens at 32 weeks old in order to comparatively analyze egg quality and composition by sorts of laying hens. In case of evaluation of the quality of eggs, this study has shown that BC had higher degree of Haugh unit coefficient (82.82) and in case cholesterol content of eggs, BC had significantly low content as 317.55mg/100g, but YS had rather higher content as 381.30mg/100g. Furthermore, this study has found out that BC had significantly low Oleic acid (C18:1n9) and WL had higher Amino acid content by breeds than those of other breeds (p<0.05).

재조합 Saccharomyces cerevisiae에서 Inulinase와 Invertase의 발현과 분비에 미치는 배양조건의 영향

  • 남수완;신동하;김연희
    • Microbiology and Biotechnology Letters
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    • v.25 no.3
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    • pp.258-265
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    • 1997
  • The effects of medium pH and culture temperature on the expression and secretion of inulinase and invertase were investigated with recombinant Saccharomyces cerevisiae cells. These cells were obtained by transformation of 2$\mu$-based plasmids pYI10 and pYS10 which contain Kluyveromyces marxianus inulinase gene (INU1A) and S. cerevisiae invertase gene (SUC2), respectively, in the downstream of GAL1 promoter. The expression level and localization of inulinase and invertase were not affected significantly by the initial medium pH: secretion efficiencies of inulinase and invertase into the medium were about 90% and 60%, respectively, in the pH ranges of 4.0 to 6.5. However, the expression and secretion of both enzymes were strongly dependent on the culture temperature. The highest expression (7.7 units/mL) and secretion (6.7 units/mL) of inulinase were observed at 28$\circ$C and 30$\circ$C. As a consequence of decreased localization of inulinase in the periplasmic space, the secretion efficiency increased from 68% at 20$\circ$C, to 95% at 35$\circ$C,. The total expression level and secretion efficiency of invertase increased from 19 units/mL and 55% at 20$\circ$C to 25 units/mL and 68% at 35$\circ$C, respectively. Irrespective of the culture temperature, the invertase activity in the cellular fraction (periplasmic space and cytoplasmic fractions) was kept constant at around 33-45%.

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Hot Rolling Properties of Non-combustible AZ31-xCa Magnesium Alloys (난연성 AZ31-xCa 마그네슘합금의 열간압연 특성)

  • Yim C. D.;You B. S.;Lee J. S.;Kim W. C.
    • Proceedings of the Korean Society for Technology of Plasticity Conference
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    • 2004.08a
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    • pp.55-62
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    • 2004
  • In this study, the effects of Ca content and processing variables on hot rolling properties of gravity cast AZ31-xCa alloys were evaluated systematically. The number and length of side crack were decreased with increasing preheating temperature and decreasing reduction ratio per pass and Ca content. The UTS and YS were not strongly dependent on the Ca content but the elongation decreased with increasing Ca content. The decrease of elongation in Ca containing alloys was least when the sheets were fabricated under preheating temperature of $400^{\circ}C$ and reduction ratio per pass of $15\%$. The sheets had the sound external features with little side cracks by homogenization of gravity cast AZ31-xCa alloys before hot rolling. In the cases of AZ31-xCa alloys containing under $1wt.\%$ Ca, the annealed sheets after homogenization and hot rolling had the similar tensile properties to those of AZ31 sheet.

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Sequence Analysis and Expression of Xylanase Gene (xynY) from Alkalophilic Bacillus sp. YC-335

  • Park, Young-Seo;Yum, Do-Young;Kim, Jin-Man;Bai, Dong-Hoon
    • Journal of Microbiology and Biotechnology
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    • v.3 no.4
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    • pp.224-231
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    • 1993
  • The nucleotide sequence of the xylanase gene (xynY) from alkalophilic Bacillus sp. YC-335 was determined and analyzed. An open reading frame of 1, 062 base pairs for xynY gene was observed and encoded for a protein of 354 amino acids with a molecular weight of 38, 915. S1 nuclease mapping showed that the transcription initiation sites of the xynY gene were different in Bacillus sp. YC-335 and Escherichia coli HB101 (pYS55). S1 mapping also showed that -10 region of the xynY gene recognized by RNA polymerases of E. coli and Bacillus sp. YC-335 were TACAGT and TATGAT , respectively. A ribosome binding site sequence with the free energy of -17.0 Kcal/mol was observed 9 base pairs upstream from the unusual initiation codon, TTG. The proposed signal sequence consisted of 27 amino acids, 2 of which were basic amino acid residues and 21 were hydrophobic amino acid residues. When the amino acid sequences of xylanases were compared, Bacillus sp. YC-335 xylanase showed more than 50% homology with xylanases from B. pumilus, B. subtilis, and B. circulans.

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