• 제목/요약/키워드: YS 55

검색결과 13건 처리시간 0.023초

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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    • 제2권4호
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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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    • 제1권4호
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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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    • 제2권2호
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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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    • 제2권3호
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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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다짐풍화화강토에 대한 Yasufuku 구성모델의 평가 (Evaluation of YasufukuYs Constitutive Model for Compacted Weathered Granite Soil)

  • 정진섭;이광찬
    • 한국지반공학회논문집
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    • 제15권5호
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    • pp.43-55
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    • 1999
  • 본 연구는 익산다짐풍화 화강토를 사용하여 여러가지 응력경로 시험을 실시하고 관측된 거동을 정확하게 예측할 수 있는 능력으로서 Yasufuku구성모델을 평가하였다. Yasufuku구성모델로 계산된 변형률은 측정치와 대부분 잘 일치하지만 약간의 차이를 나타내기도 하였다. 측정한 변형률과 계산한 변형률 사이에 가장 큰 차이를 보인곳은 증가하는 응력을 갖는 비례하중이 작용할 때 축변형률에 대하여 일어났다. Yasufuku 구성모델은 익산다짐풍화 화강토의 거동을 일정 구속압력하에서 축하중이 작용할 때와 p'-일정하중이 작용할 때 정확하게 추정할 수 있었다.

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

  • 류지훈;권장순;김건영;고용권
    • 방사성폐기물학회지
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    • 제10권3호
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    • pp.189-197
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    • 2012
  • KURT 지하수의 지구화학적 특성을 조사하기 위하여 단열충전광물과 지하수의 지구화학적 성분이 조사되었다. KURT내의 시추공들로부터 얻어진 시추코아로부터 방해석(calcite), 일라이트(illite), 로먼타이트(laumonite), 녹니석(chlorite), 녹염석(epidote), 몬모릴로나이트(montmorillonite), 카올리나이트(kaolinite) 및 일라이트와 스멕타이트(smectite)의 혼합층상광물 등이 감정되었다. 시추공 DB-1, YS-1, YS-4에서 채취한 대부분의 지하수는 pH 8이상의 알칼리 환경을 보여주었으며 YS-1을 제외한 두 관측공의 전기전도도는 약 2$200{\mu}S/cm$를 나타냈으며 이들 시추공에서 천부지하수는 $Ca-HCO_3$$Ca-Na-HCO_3$ 유형 이였으며 심부 250m이하에서는 $Na-HCO_3$ 유형을 나타냈다. DB-1 공의 심부지하수에서 낮은 용존산소량(DO)와 Eh값의 감소를 측정하였으며 이는 환원환경을 지시한다. KURT의 지하수 시료의 $Cl^-$ 이온의 농도는 5 mg/L 이하이며 전 샘플링구간에서 커다란 변화 없이 일정하게 나타났다. 이러한 현상은 KURT 지역의 천부와 심부지하수가 혼합(mixing)되어 $Cl^-$의 농도가 깊이에 따라 큰 변화가 없는 것으로 해석된다. 지하수 시료의 ${\delta}^{18}O$${\delta}D$ 분석 값은 각각 -10.4~-8.2‰과 -71.3~-55.0‰의 범위로 지하수가 순환수 기원임을 보여준다. 긴 순환경로를 거친 심부지하수의 수소, 산소 동위원소 값은 천부지하수에 비해 감소하며 이러한 값은 일반적으로 높은 불소농도를 동반하였다. 이는 불소함량이 높은 지하수가 물-암석 반응에 의해 생성되었음을 보여준다. KURT 지역에서 채취한 지하수의 $^{14}C$를 이용한 연대측정분석에서 지하수의 체류시간(residence time)이 약 2,000~6,000년으로 측정되었다. 이러한 체류시간은 KURT 지역의 화강암에 존재하는 지하수가 다른 유럽의 화강암지역(예, 스트리파 지역, 스웨덴)보다 상대적으로 지하수의 연령이 오래되지 않은 것으로 측정되었다.

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

  • 김병기;하재정;이준구;오동엽;정대진;최성복;황은경;김수정;이제영
    • Journal of the Korean Data and Information Science Society
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    • 제27권5호
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    • pp.1307-1316
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    • 2016
  • 본 논문은 계란에 대한 소비자들의 인식을 향상시키기 위해 산란계 종류에 따른 계란품질과 성분조성을 실험 및 분석하였다. 산란개시 32주령에 있는 4개 품종의 청색란실용계 (BC), 연산오골계 (YS), 재래닭 (KN), 백색레그혼 (WL) 총 120수 (각 처리구당 10수 ${\times}$ 3반복 ${\times}$ 4처리구)를 임의 배치하여 생산된 계란의 성분을 분석하였다. 계란의 품질 평가의 경우, BC가 다른 품종에 비하여 호우닛 계수 (82.82),난각강도 (0.37mm) 및 난각두께 ($40.58kg/cm^2$)가 유의적으로 높게 나왔으며, 계란의 콜레스테롤 함량은 BC가 317.58mg/100g로 가장 낮았지만, YS는 381.30mg/100g으로 매우 높게 나타났다 (p<0.05). 그리고 계란의 지방산 조성에서 oleic acid (C18:1n9)함량은 BC가 다른 품종보다 매우 낮았으며, 아미노산의 경우에는 Thronine과 Proline을 제외한 모든 성분에서 대체로 WL종이 다른 품종보다 더 높게 나타났다 (p<0.05).

재조합 Saccharomyces cerevisiae에서 Inulinase와 Invertase의 발현과 분비에 미치는 배양조건의 영향

  • 남수완;신동하;김연희
    • 한국미생물·생명공학회지
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    • 제25권3호
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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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난연성 AZ31-xCa 마그네슘합금의 열간압연 특성 (Hot Rolling Properties of Non-combustible AZ31-xCa Magnesium Alloys)

  • 임창동;유봉선;이진수;김완철
    • 한국소성가공학회:학술대회논문집
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    • 한국소성가공학회 2004년도 제5회 압연심포지엄 신 시장 개척을 위한 압연기술
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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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    • 제3권4호
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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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