• Title/Summary/Keyword: 결합 친화력

Search Result 67, Processing Time 0.03 seconds

Lanthanum-induced Inhibitions of Microsomal $H^+-ATPase$ in the Roots of Tomato ($La^{3+}$에 의한 토마토 뿌리조직 마이크로솜 $H^+-ATPase$ 활성저해)

  • Cho, Kwang-Hyun;Kim, Young-Kee
    • Applied Biological Chemistry
    • /
    • v.46 no.2
    • /
    • pp.84-89
    • /
    • 2003
  • In order to find a chemical agent which is able to modulate the activity of $H^+-ATPase$, microsomal preparation was obtained from the root tissue of tomato plant and the effect of $La^{3+}$ was measured. The activities of plasma and vacuolar membrane $H^+-ATPase$ were analyzed by the inhibited activities using their specific inhibitors, vanadate and $NO_3-$, respectively. $La^{3+}$ inhibited microsomal ATPases in a dose-dependent manner and the inhibitory effect of $La^{3+}$ was suppressed by both vanadate and $NO_3-$, implying that $La^{3+}$ inhibits both plasma and vacuolar membrane $H^+-ATPase$. The Ki. values of $La^{3+}$which inhibit 50% of the activities of plasma and vacuolar membrane $H^+-ATPase$ were 57 and $78\;{\mu}M$, respectively. The $H^+-ATPase$ of the leaky microsomes made by the treatment of Triton X-100 were also inhibited by $La^{3+}$, suggesting that $La^{3+}$ directly inhibits both enzymes. Meanwhile, the inhibitory effect of $La^{3+}$ was decreased by increasing the concentration of ATP, The effect of ATP was also concentration-dependent and 7 mM ATP completely removed the inhibitory effect of $La^{3+}$. These results imply that $La^{3+}$ inhibits both plasma and vacuolar membrane $H^+-ATPases$ by decreasing the binding affinity of ATP and $La^{3+}$ can be used to control the activity or root $H^+-ATPases$.

Characterization of angiotensin II antagonism displayed by KR-31081, a novel nonpeptide AT1 receptor antagonist (안지오텐신 수용체 길항제 KR-31081의 특성에 관한 연구)

  • Lee, Sung-Hou
    • Journal of the Korea Academia-Industrial cooperation Society
    • /
    • v.10 no.10
    • /
    • pp.2997-3003
    • /
    • 2009
  • The pharmacological profile of KR-31081, a nonpeptide $AT_1$ selective angiotensin receptor antagonist, was investigated by receptor binding studies, functional in vitro assays with rabbit aorta. KR-31081 inhibited the specific binding of $[^{125}I]\;[Sar^1,\;Ile^8]$-angiotensin II to human recombinant $AT_1$ receptor with an 8.6-fold greater potency than losartan ($IC_{50}$: 1.43 and 12.3 nM, respectively), but it did not inhibit the binding of [$^{125}I$] CGP 42112A to human recombinant $AT_2$ receptor ($IC_{50}$: higher than $10{\mu}M$ for both). The Hill coefficient for the competition curve of KR-31081 against $AT_1$ receptor was not significantly different from unity (0.99). Scatchard analysis showed that KR-31081 interacted with human recombinant $AT_1$ receptor in a competitive manner, as with losartan. In functional studies with rabbit aorta, KR-31081 competitively inhibited the contractile response to angiotensin II ($pK_B$ values: 8.66) with 20-70% decrease in the maximum contractile responses, unlike losartan that showed competitive antagonism without any change in the maximum contractile responses to angiotensin II ($pA_2$ values: 7.59). These results suggest that KR-31081 is a highly potent $AT_1$ selective angiotensin II receptor antagonist with a mode of insurmountable antagonism to be developed as the exploratory potential of this compound.

Pharmacological Characterization of KR-31125, a Novel Nonpeptide AT1 Receptor Antagonist (안지오텐신 수용체 길항제 KR-31125의 특성에 관한 연구)

  • Lee, Sung-Hou
    • Journal of Life Science
    • /
    • v.20 no.6
    • /
    • pp.831-837
    • /
    • 2010
  • KR-31125 (2-butyl-5-dimethoxymethyl-6-phenyl-7-methyl-3-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-3H-imidazo[4,5-b]pyridine) is a potent inhibitor of angiotensin II type 1 ($AT_1$) receptors in human recombinant $AT_1$ receptors and rabbit aorta. These in vitro studies revealed that KR-31125 inhibited specific [$^{125}I$] [$Sar^1$, $Ile^8$]-angiotensin II binding to human recombinant $AT_1$ receptors in a concentration dependent manner with an $IC_{50}$ value of $19.72{\pm}2.65$ nM. However, no interaction with $AT_2$ receptors was detected as displayed by the competition binding of [$^{125}I$] CGP 42112A to human recombinant $AT_2$ receptor. The binding action was also confirmed as a competitive mode that was identical to the previously studied compound, losartan. In addition, KR-31125 caused a nonparallel shift to the right in the concentration response curves to angiotensin II with a 30-80% decrease in the maximum contractile responses ($pK_B$: 7.63). Compared to the previous studies with losartan that showed a parallel right shift in the maximum contractile responses to AII ($pA_2$: 7.59), KR-31125 presented a different mode of action with a similar potency to losartan. These results demonstrate that KR-31125 is a highly potent and $AT_1$ selective angiotensin II receptor antagonist that can be applied to the fields of new diagnostic and research tools with upcoming in vivo study results.

An Experimental Study on the Engineering Properties of Lightweight Aggregate Concrete (경량골재 콘크리트의 공학적 성질에 관한 실험적 연구)

  • ;R. N. Swanmy
    • Magazine of the Korean Society of Agricultural Engineers
    • /
    • v.39 no.1
    • /
    • pp.75-82
    • /
    • 1997
  • 건설기술과 산업의 발전에 따라 구조물은 대형화되어 가고, 건설공사의 급격한 팽창으로 골재 수용량이 급증함에 따라 천연골재자원은 점차 부족현상을 면치 못할 처지에 있다. 또한, 무리한 천연골재의 채취는 자연환경을 훼손시킬 뿐만 아니라 자연보호 측면에서도 심각한 공해문제로 대두되고 있어 공급량 부족현상은 날로 심화되고 있다. 이에 세계 몇몇 나라에세는 산업부산물을 이용한 골재 생산으로 공해예방과 폐기물 활용방법을 연구하고 있다. 산업부산물중 플라이 애쉬 생산량은 전 세계적으로 매년 약 2억여톤에 달하고 있으나 이중 일부만 활용되고 있는 실정이다. 이와같은 부산물을 활용하기 위한 일환으로 산업부산물인 PFA(Pulverized Fuel Ash)로 만든 인공경량골재의 년생산량이 영국은 600,000$m^3$, 미국은 300,000$m^3$이며, 매년 증가주세에 있다. 고성능 경량골재 콘크리트는 단위중량의 증가없이 내구성과 강도를 향상시켜 실용화 측면에서 경제적인 효과가 있으며, 플라이 애쉬로 만든 경량골재는 시멘트와의 친화력이나 접착면에서 우수한 것으로 알려져 있다. 본 시험에 사용한 골재는 플라이 애쉬로 만든 인공경량 조골재와 강모래이고, 결합제로서 프틀랜드 시멘트를 사용하였다. 부수적인 결합재로서는 플라이 애쉬, 슬래그, 실리카 흄을 사용하였으며, 고성능 경량골재 콘크리트를 개발코자 재령 28일과 180일의 압축강도가 각각 50MPa와 60MPa가 되도록 배합설계를 하였다. 본 연구에서는 플라이 애쉬, 슬래그, 시리카 흄과 같은 산업부산물을 혼입했을때 경량골재 콘크리트의 압축강도, 휨강도, 동탄성계수, 공극체적, 공극률, 단위중량, 공극 크기별 분포등의 변화를 실험적으로 구명하여 재반 구조용 콘크리트에 활용하기 위한 기초자료를 마련코저 한다.있어 특정한 발육단계의 난포 사망기전을 연구하기 어렵다. 또한 난포는 생체 내에서 다양한 호르몬을 동시에 분비하기 때문에 특정한 난소국부호르몬이 사망기전에 미치는 영향을 조사하기 힘든 점이 있다. 최근 들어 난포체외배양이 다양하게 개발되면서, 이러한 어려운 점을 극복할 수 있게 되었다. 본 논문은 각 발육단계의 난포를 절단해 체외배양하면서, apoptosis DNA 절단 현상을 이용하여 각종 난소국부 호르몬들이 난포발육단계별로 사망기전에 미치는 영향을 요약해 보였다. 난포는 발육하면서 점차 복잡한 호르몬 경로를 생존을 위해 필요로 한다. Prevulatory난포생존에 필요한 난소국부호르몬들은 early antral 단계의 난포에서는 그 미치는 영향이 감소되다가 preantral단계의 난포에서는 영향을 전혀 미치지 못했다. 단지 예외는 cGMP처리로써, 세포내 cGMP수준을 일정하게 유지시켜주는 것이 난포발육단계에 무관하게 생존에 중요한 인자로, 장래 연구는 난포 세포내의 cGMP수준을 조절하는 기작을 규명하는데 있을 것이다.인정되지 않았다. 7. 농지보전 처리구인 배수구와 초생수로구는 비처리구에 비해 낮은 침두 유출량과 낮은 토양유실량을 나타내었다.구보다 14% 절감되는 것으로 나타났다.작용하는 것으로 사료된다.된다.정량 분석한 결과이다. 시편의 조성은 33.6 at% U, 66.4 at% O의 결과를 얻었다. 산화물 핵연료의 표면 관찰 및 정량 분석 시험시 시편 표면을 전도성 물질로 증착시키지 않고, Silver Paint 에 시편을 접착하는 방법으로도 만족한 시험 결과를 얻을 수 있었다.째, 회복기 중에 일어나는 입자들의 유입은 자기폭풍의 지속시간을 연장시키는 경향을 보이며 큰 자기폭풍일수록 현저했다. 주상에서 관측된 이러한 특성은 서브스톰 확장기 활동이 자기폭풍의 발달과 밀접한 관계가

  • PDF

Sequential Fractionation of Heavy metals from Mine Tailings and Two Series of Agricultural Soils (광미장과 두개의 농업토양통 토양으로 부터의 중금속의 연속 분획)

  • Chung, Doug-Young;Lee, Do-Kyoung
    • Korean Journal of Soil Science and Fertilizer
    • /
    • v.32 no.4
    • /
    • pp.375-382
    • /
    • 1999
  • In order to investigate the contamination characteristics of the heavy metals in the mine tailings of abandoned gold mine and its surrounding agricultural soils, a sequential extraction procedure of increasing reactivity in the dissolution processes of the heavy metals(Cd, Cu, and Pb) which were associated with solid and/or solution phase in soils was attempted to partition into six particulate fractions : exchangeable, bound to carbonate, bound to Fe-Mn oxides, bound to organic matter, residual, and soluble. Among indigenous heavy metals in the mine tailings, Pb was the most abundant and Cu and Cd were followed by. Fractionation result of Pb obtained from the triplicate samples of the mine tailings were in the order of Fe-Mn oxide> Carbonate> Residual> Organic> Exchangeable> Soluble, while Wolgok series were Exchangeable > Fe-Mn oxide > Carbonate> Organic> Residual> Soluable. However the other heavy metals studied were not followed this trend. The fractionation results of mine tailing and agricultural soils demonstrated that different geochemical fractions were operationally defined by an extraction sequence that generally followed the order of decreasing solubility. Therefore potential mobility and bioavailability of heavy metals as toxic pollution sources can be evaluated when studying the pollution levels of heavy metals in soils.

  • PDF

Alterations of Binding Capacities of Dopamine Receptors After Treatment with Haloperidol and Sulpiride in Rat Brain (Haloperidol 및 Sulpiride 투여후 백서 뇌내 Dopamine 수용체 결합력의 변화)

  • Hahn, Kyu-Hee;Ahn, Yun-Young
    • Korean Journal of Biological Psychiatry
    • /
    • v.2 no.1
    • /
    • pp.63-69
    • /
    • 1995
  • The effects of chronic treatment with haloperidol and sulpiride on the binding capacities of dopamine(DA) receptor were examined in rat striatum and olfactory tubercle. Additionally, the stereotypy scores were assessed after apomorphine administration. Rats were treated with haloperidol(0.5mg/kg/day) or sulpiride(40mg/kg/day) for four weeks. Apomorphine(0.5mg/kg) was injected after three-day washout from neuroleptics, and stereotypy scores were assessed. Haloperidol group showed high scores of stereotyped behavior in comparison with control and sulpiride groups. With control group, sulpiride group displayed similar stereotyped behaviors. Saturation analysis of the binding of [$^3H$]spiperone to striatal membranes showed that the Bmax of haloperidol and sulpiride groups increased significantly in comparison with that of control group. The $K_D$ decreased significantly after sulpiride treatment in striatum. Although sulpiride produces the same proliferation of DA receptor, the low stereotypy scores of sulpiride group indirectly suggest that sulpiride acts differently from haloperidol in brain DA system. The Bmax increased remarkably following both treatment with haloperidol and sulpiride in olfactory tubercle. Also, the increase in $K_D$ was significant after treatment with haloperidol and sulpiride in olfactory tubercle. Moreover, the $K_D$ of control group in olfactory tubercle was more than twice the $K_D$ of control group in striatum. The $K_D$ was 86.2 in striatum and 37.5 pM in olfactory tubercle. The present finding indicates that sulpiride also induces the proliferation of DA receptor in olfactory tubercle and may interact with some DA receptor subtype with high affinity profile. The different affinities of the control groups of striatum and olfactory tubercle suggest that striatal DA receptor subtypes labeled by [$^3H$]spiperone could differ from those of olfactory tubercle.

  • PDF

Expression of Recombinant Hybrid Peptide Gaegurin4 and LL37 using Fusion Protein in E. coli (Glutathione S-Transferase에 융합한 재조합 Hybrid Peptide Gaegurin-LL37의 대장균에서의 발현)

  • Bayarbat, Ishvaanjil;Lee, Jae-Hag;Lee, Soon-Youl
    • Microbiology and Biotechnology Letters
    • /
    • v.40 no.2
    • /
    • pp.92-97
    • /
    • 2012
  • Antimicrobial peptides (AMPs) are important components of living organisms acting against Gram-negative and Gram-positive bacterial and fungal pathogens. Cathelicidin human peptides have a variety of biological activities that can be used in clinical applications. AMPs are not produced naturally in large quantities, and chemical synthesis is also economically impractical, especially for long peptides. Therefore, as an alternative, heterologous expression of AMPs by recombinant techniques has been studied as a means to reduce production costs. E. coli is an excellent host for the expression of AMPs, as well as other recombinant proteins, because of the low cost involved and its easy manipulation. However, overexpression of AMPs in E. coli has been shown to cause difficulties resulting from the toxicity of the subsequently produced AMPs. Therefore, fusion expression was theorized to be a solution to this problem. In this study, AMPs were expressed as fused proteins with the glutathione S-transferase (GST) binding protein to protect against the toxicity of AMPs when expressed in E. coli. The LL37, and hybrid gaegurin and LL37 (GGN4(1-16)-LL37(17-32), which we designated as GL32, peptides were expressed as GST-fusion proteins in E. coli and the fusion proteins were then purified by affinity columns. The purified peptides were obtained by removal of GST and were confirmed by western blot analysis. The purified antimicrobial peptides then demonstrated antimicrobial activities against Gram-negative and Gram-positive bacterial strains.

Characterization of PET films coated with organic-inorganic hybrid coating system containing surface modified zirconia (표면 개질된 지르코니아를 함유한 유-무기 하이브리드 코팅액으로 도포된 PET 필름의 특성)

  • Lee, Soo;Kim, Sang Yup;Kim, Young Jun
    • Journal of the Korean Applied Science and Technology
    • /
    • v.35 no.3
    • /
    • pp.595-605
    • /
    • 2018
  • In recent years, researches on organic-inorganic coating films have conducted a nanocomposite system composed of organic resin matrices having excellent flexibility and chemical stability and inorganic materials having excellent mechanical properties. The o-phenylphenoxyethyl acrylate (OPPEA) used as the acrylate monomer has a high refractive index of 1.58, and the bisphenol A ethoxylate diacrylate (BAEDA) has a low refractive index but improves the chemical stability of the organic resin. In addition, zirconia used as an inorganic material exhibits excellent durability and optical properties. In this study, the BAEDA contents in acrylate monomer were controlled to produce a film with suitable optical transparency. And optimum conditions were established by comparing the changes in surface properties of PET films detected with pencil hardness tester, Abbe's refractometer, and UV-vis spectrophotometer. The hydrophobicity and the dispersibility of zirconia in acrylate monomer were much improved after modification with ${\gamma}$-methacryloxypropyltrimethoxysilane (MPS), which is a silane coupling agent. And the existence of ester C=O bond peak at $1716cm^{-1}$ introduced by MPS through FT-IR ATR spectrophotometer confirmed the completion of surface modification of zirconia with MPS. In addition, the presence of silicon atom on the surface modified zirconia was also proved using X-ray fluorescence spectrometer. When the photocurable hybrid coating was prepared by introducing chemically modified zirconia into acrylate monomer, the refractive index of this coated PET film was improved by 1.2%, compared to the only acrylate coated PET film. The homogeneous distribution of zirconia in acrylate coating layer on PET film was also identified through SEM/EDS mapping analysis technique.

Production and Evaluation of Anti-Gastrin Serum for Radioimmunoassay (방사면역측정을 위한 항 Gastrin 혈청의 생산 및 평가)

  • Park, Hyoung-Jin;Kwon, Hyeok-Yil;Lee, Yun-Lyul;Shin, Won-Im;Suh, Sang-Won;Oh, Yang-Suk
    • The Korean Journal of Physiology
    • /
    • v.23 no.1
    • /
    • pp.89-98
    • /
    • 1989
  • In order to produce antibody for use in radioimmunoassay of gastrin in physiological concentration, four rabbits of New Zealand white were immunized with synthetic human gastrin-17-I conjugated to hemocyanin with EDC. Among them, only one rabbit produced antibody that could bind 50% of $^{125}I-gastrin$ at a final dilution of 1:25,000. $^{125}I-gastrin$ was prepared with synthetic human gastrin-17-I and $NaI^{125}$ by lactoperoxidase technique. The product was then purified on a column of Sephadex Gl5/G5O (7:3, w/w) followed by a column of DEAE sephadex A-25. The specific radioactivity of the purified $^{125}I-gastrin$ was in the range of 347-1429 ${\mu}Ci/nmole$ when determined by the self-displacement method. The effective affinity constant $(K_{eff})$, total binding sites (N), heterogeneity index $({\alpha})$ and average affinity constant $(K_{0})$ of the anti-gastrin serum calculated from Scatchard plot as well as Sips plot were $1.77{\times}10^{11}/M$, 255 nM, 0.84 and $0.79{\times}10^{11}/M$, respectively. When radioimmunoassay was performed with the anti-gastrin serum, it was confirmed that the mean concentration of gastrin immunoreactivity in plasma was increased by feeding in humans and rats, and also increased by bombesin administration in rats. The results indicate that the anti-gastrin serum produced in the present investigation is suitable for radioimmunological determination of gastrin in physiological concentration.

  • PDF

Functions of a-Tropomyosin Are Mainly Dependent upon the Local Structures of the Amino Terminus (a-Tropomyosin의 아미노 말단 구조가 기능에 미치는 영향)

  • Cho, Young-Joon
    • Journal of Life Science
    • /
    • v.14 no.5
    • /
    • pp.770-777
    • /
    • 2004
  • It has been previously reported that unacetylated a-tropomyosin(TM) produced in E. coli failed to bind to actin while acetylated muscle TM and Ala-Ser dipeptide fusion TM (AS-TM) bound well to actin. In order to determine the structural requirement of the amino terminus for high actin affinity, a recombinant tropomyosin (Ala-TM) that a single Ala residue was added to the amino terminus of Ala-TM was constructed, overexpressed, and purified from E. coli. Actin affinity of Ala-TM was 2.3$\times$$10^{6}$$M^{-1}$, whereas that of unacetylated TM was considerably lower than 0.1$\times$$10^{-6}$$M^{-1}$ indicating that addition of a single Ala residue to the amino terminus drastically increased, at least twenty times, actin affinity of TM. Ala-TM, however, bound to actin about three times weaker than acetylated TM and AS- TM, implying that the addition of an Ala residue was insufficient for complete restoration of high actin affinity. While Ala-TM, AS-TM, and muscle TM showed inhibition and activation of actomyosin Sl ATPase activity depending on myosin Sl concentration, the degree of inhibition and activation was different from each other. AS-TM exhibited the greatest inhibition of the ATPase at low Sl concentration, whereas the greatest activation of the ATPase was observed with muscle TM. These results, together with previous findings, strongly suggested that local structure of the amino terminus is the crucial functional determinant of TM.