• Archives of Pharmacal Research
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• 제14권2호
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• pp.181-187
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• 1991

The muscarinic antagonist 1-[benzilic 4, 4'-$[^3H]$ QUINUCLIDINYL BENZILATE $([^3H]$ QNB) bound to a single class of muscarinic receptors with high affinity in rabbit ileal membranes. The $K_D\;and\;B_{ max}$ values for $([^3H]$ QNB calculated from analysis of saturation isotherms were 52.5 pM AND 154 fmol/mg, respectively. Chlopheniramine (CHP), histamine $H_1$ blocker, increased $K_D$ vlue for $([^3H]$QNB without affecting the binding site concentrations and Hill coefficient. The $K_i$ value of CHP for inhibition of $([^3H]$QNB binding in ileal membranes was 1.44\mu{M}$ and the pseudo-Hill coefficient for CHP was close to unit. In the functional assay carbachol, muscarinic agonist, increased the contractile force of ileum with $ED_{50}$ value of $0.11\mu{M}$. CHP caused the rightward shift of the dose-response curve to carbachol. The $pA_2$ value of CHP determined from Schild analysis of carbacholinduced contraction was 5.77 and the slope was unity indicating competitive antagonism with carbachol. The dissociation constant $(K_i)$ of CHP obtained in competitive experiments with $([^3H]$ QNB was similar to the $K_A$ value (1.69 \mu{M)}$ of CHP as inhibitor of carbachol induced contraction in rabbit ileum. This result suggest that the binding of $H_i$ blocker. CHP, vs $([^3H]$QNB to muscarinic receptors in ileal membranes represents an interaction with a receptor of physiological relevance.

• 한국식품영양과학회지
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• 제16권2호
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• pp.110-117
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• 1987

재래식(在來式) 적색(赤色)자두(Prunus salicina)로부터 효소(酵素)를 추출(抽出) 정제(精製)하여 그 성질(性質)을 조사(調査)한 결과(結果)는 다음과 같다. 1. 적색(赤色)자두의 PPO는 crude extract보다 $(NH_4)_2SO_4$로 포화(飽和)했을 예 15배(倍), 그리고 Sephadex G-100 column chromatograph를 행하였을 애 64배(倍)로 정제(精製)되었다. 2. 효소반응(酵素反應)의 최적조건(最適條件)은 최적온도(最適溫度) 및 pH가 $35^{\circ}C$ 6.5였으며 주요기질(主要基質) 은 o-diphenol인 catechol로 나타났다. 3. 적색(赤色)자두 PPO의 열안정성(熱安定性)은 $50^{\circ}C$에서 5분간(分間) 처리(處理)하였을 매 초기(初期) PPO의 활성중(活性中) 85%, 30분간(分間) 처리시(處理時)에는 75%의 잔존활성(殘存活性)을 나타내었다. 4. 본(本) 효소(酵素)의 K값은 2.58mM이었다. 5. 저해제(沮害劑)의 효과(效果) 중 L-cysteine, glutathione, ascorbic acid와 potassium cyanide는 1mM 농도(濃度)에서 완전히 효소활성(酵素活性)을 저해(沮害)하였으나 EDTA는 저해효과(沮害效果)가 대단히 약하게 나타났다.

• 한국주조공학회지
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• 제31권6호
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• pp.347-353
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• 2011

There is thixo-extrusion to form high strength aluminum alloy. But, it is a problem that grains become grain coarsening during reheating process because the alloy was exposed at high temperature. In order to solve grain growth during reheating process, calcium was added in Al-Zn-Mg alloys. Primary a grain sizes of semi-solid Al-Zn-Mg-(0, 0.4, 0.6 and 0.9, wt.%)Ca were measured with image analyzer after reheating. Measured primary a grain sizes were applied to LSW(Lifshitz-Slyozov and Wagner) equation to check the effect of Ca on grain coarsening. Coarsening rate constant K values of semi-solid Al-Zn-Mg-(0, 0.4, 0.6 and 0.9, wt.%)Ca alloys were $371\;mm^3s^{-1}$, $247\;mm^3s^{-1}$, $198\;mm^3s^{-1}$ and $166 mm^3s^{-1}$, respectively. As increasing calcium content, K value decreased which means grains are refined. Also, grains of calcium addition were more spherical than that of calcium free.

• Bulletin of the Korean Chemical Society
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• 제35권8호
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• pp.2438-2442
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• 2014

A kinetic study is reported for $S_NAr$ reaction of 1-fluoro-2,4-dinitrobenzene (5a) and 1-chloro-2,4-dinitrobenzene (5b) with alkali-metal ethoxides (EtOM, M = Li, Na, K and 18-crown-6-ether complexed K) in anhydrous ethanol. The second-order rate constant increases in the order $k_{EtOLi}$ < $k_{EtO^-}$ < $k_{EtONa}$ < $k_{EtOK}$ < $k_{EtOK/18C6}$ for the reaction of 5a and $k_{EtOLi}$ < $k_{EtONa}$ < $k_{EtO^-$ < $k_{EtOK}$ < $k_{EtOK/18C6}$ for that of 5b. This indicates that $M^+$ ion behaves as a catalyst or an inhibitor depending on the size of $M^+$ ion and the nature of the leaving group ($F^-$ vs. $Cl^-$). Substrate 5a is more reactive than 5b, although the $F^-$ in 5a is ca. $10pK_a$ units more basic than the $Cl^-$ in 5b, indicating that the reaction proceeds through a Meisenheimer complex in which expulsion of the leaving group occurs after the rate-determining step (RDS). $M^+$ ion would catalyze the reaction by increasing either the nucleofugality of the leaving group through a four-membered cyclic transition state or the electrophilicity of the reaction center through a ${\pi}$-complex. However, the enhanced nucleofugality would be ineffective for the current reaction, since expulsion of the leaving group occurs after the RDS. Thus, it has been concluded that $M^+$ ion catalyzes the reaction by increasing the electrophilicity of the reaction center through a ${\pi}$-complex between $M^+$ ion and the ${\pi}$-electrons in the benzene ring.

• Archives of Pharmacal Research
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• 제24권1호
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• pp.55-63
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• 2001

Aucubin, an irdoid g1ucoside, was investigated to determine whether it has a stimulating effect on $\alpha$-amanitin excretion in $\alpha$-amanitin intoxicated rats, and whether there is binding activity to calf thymus DNA. High-performance liquid chromatography (HPLC) analysis of $\alpha$-amanitin in rat urine allowed quantitative measurement of the $\alpha$-amanitin concentration with a detection limit of 50${mu}g/ml$. In this system, a group treated with both $\alpha$-amanitin and aucubin showed that o(-amanitin was excreted about 1.4 times faster than in the $\alpha$-amanitin only treated group. Our previous results showed that the toxicity of $\alpha$-amanitin is due to specific inhibition of RNA polymerase activity and the resultant blockage of the synthesis of certain RNA species in the nucleus. However, no significant activity change on RNA polymerase from Hep G2 cells was observed when aucubin was treated with $\alpha$-amanitin at any concentration tested. Nevertheless, aucubigenin inhibited both DNA polymerase (IC50, 80.5${mu}g/ml$) and RNA polymerase (IC50, 135.0${mu}g/ml$) from the Hep G2 cells. The potential of both $\alpha$-amanitin and aucubin to interact with DNA were examined by spectrophotometric analysis. $\alpha$-Amanitin showed no significant binding capacity to calf thymus DNA, but aucubin was found to interact with DNA, and the apparent binding constant ($K_{app}$) and apparent number of binding sites per D7A phosphate ($B_{app}$) were 0.45$0.45{\times}$$10^4$ $M^{-1}$ and 1.25, respectively.

• Biomolecules & Therapeutics
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• 제1권1호
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• pp.1-8
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• 1993

It has been known that calcium antagonists also inhibit the radioligand binding to muscarinic and $\alpha$-adrenergic receptors and, in case of verapamil, these inhibitions may play a role in the effects of verapamil on the heart. In this study, the effects of nicardipine, nifedipine, nimodipine, diltiazem and verapamil on the binding of [$^3H$]dihydroalprenolol (DHA) to dog cardiac ${\beta}$-adrenergic receptors were examined. A single uniform [$^3H$]DHA binding site ($K_D/= 5nM\;and\;B_{max}=2600$ fmol/mg protein) was identified in dog cardiac sarcolemma. [$^3H$]DHA binding was not affected by the usual therapeutic concentrations of these calcium antagonists (nanomolar range) but in the "nonspecific"concentration ranges ($28-180{\mu}m$) these drugs inhibited [$^3H$]DHA binding to $\beta$-adrenergic receptors. Nicardipine, nifedipine, nimodipine and diltiazem competed for [$^3H$]DHA binding to ${\beta}$-adrenergic receptors with dissociation constants ($K_i$) of $28{\mu}m,\' 74{\mu}m, 39{\mu}m \;and \;35{\mu}m,$ respectively. Verapamil ($K_i=176.5 {\mu}m$) was less potent inhibitor than other drugs and this inhibition was noncompetitive; the maximal binding capacity ($B_{max}$) $300 {\mu}m$ verapamil without change in the apparent dissociation constant (4K_D$) for DHA. These results indicate that the inhibitory action of calcium antagonists at high concentrations on ${\beta}$-adrenergic receptors is not involved in the therapeutic effects of these drugs by the calcium channel blocking action.

• 한국미생물·생명공학회지
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• 제9권3호
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• pp.165-171
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• 1981

E. coil ATCC 9637의 균체를 젤라틴과 DEAE-cellulose의 혼합 성형 후 글루트알데히드 가교법으로 제조론 고정화 penicillin amidase의 differential column reactor에서의 반응속도를 논의하였다. 이러한 반응조의 최적 조작조건은 효소충진량 1g, 기질농도30mM(0.1M 인산완충액, pH8.0), 유출속도 4 $m\ell$/min, 온도 4$0^{\circ}C$이었다. 이 최적조건에서 고정화효소의 일반적인 성질을 조사하였다. Km 상수는 4.8mM 이었고 specific activity 308 units/g 고정화 효소이 었다. 또한 고정화효소에서는 기질에 의한 효소반응 저해효과가 보이지 않았다. 이러한 differential column reactor에서는 column내에서의 pH 감소효과 및 외부 화산효과가 없어지기 때문에 이러한 외부적 영향을 받지 않는 고정화효소의 반응 속도론적 연구에 적합함을 알았다.

• 한국지하수토양환경학회지:지하수토양환경
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• 제10권3호
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• pp.9-15
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• 2005

토양/대수층 처리(Soil Aquifer Treatment, SAT)는 하수처리장으로부터의 2차 또는 3차 처리수를 대수층으로 침투시켜, 토양 매질에서 일어나는 물리적/생화학적 반응에 의해 재처리하는 용수 재이용 기술이다. SAT에서의 주요 관심 대상은 유기물과 질소화합물의 제거와 이송에 있다. 본 연구에서는 암모늄의 질산화 반응, 질소산회물의 탈질 반응, 그리고 유기물의 산화반응을 고려하여 SAT에서 일어나는 반응 메커니즘을 규명하고 이를 지하수 흐름과 이송 모렐 에 접목시킴으로써 SAT 모델링 시스템을 구현하고자 하였다. 실험실 일차원 불포화 토양 컬럼 실험을 통한 모델 검증에서 암모늄, 질산성 질소, DOC, 용존산소 모두 일정한 농도 범위 안에서 일치하였다. 모델 변수에 대한 민감도 분석에서, 암모늄 분배계수는 유출부의 암모늄 농도에, 용존산소 저해상수는 유출부의 유기물 농도에, 그리고 미생물 감쇄계수는 유출부의 용존산소 농도에 영향을 주었다.

• Biomolecules & Therapeutics
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• 제19권1호
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• pp.70-76
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• 2011

Bone remodeling is a dynamic process involving a constant balance between osteoclast-induced bone resorption and osteoblast-induced bone formation. Osteoclasts play a crucial homeostatic role in skeletal modeling and remodeling, and destroy bone in many pathological conditions. Previously, we reported that the hexane soluble fraction of Ficus carica inhibited osteoclast differentiation. Poly unsaturated fatty acids, such as ethyl docosahexaenoate (E-DHA), docosahexaenoic acid (DHA), cis-11,14-eicosadienoic acid (EDA) and eicosapentaenoic acid (EPA), were identified from the hexane soluble fraction of Ficus carica. Among them, E-DHA most potently inhibited osteoclastogenesis in RAW264.7 cells. E-DHA reduced the activities of JNK and NF-$\kappa}B$. E-DHA suppressed the expression of c-Fos and nuclear factor of activated T cells c1 (NFATc1). Interestingly, DHA increased the activity of alkaline phosphatase and expression of bone morphogenetic protein 2 (BMP2) more than E-DHA in MC3T3-E1 cells, suggesting that DHA may induce osteoblast differentiation. The data suggests that a combination of E-DHA and DHA has potential use in the treatment of diseases involving abnormal bone lysis, such as osteoporosis, rheumatoid arthritis and periodontal bone erosion.

• 멤브레인
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• 제22권6호
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• pp.441-449
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• 2012

정수처리용 알루미나 정밀여과 및 광촉매의 혼성공정에서 주기적 질소 역세척 시 휴믹산 농도의 영향을 알아보고, 막오염에 의한 저항 ($R_f$) 및 투과선속 (J), 총여과부피 ($V_T$) 측면에서 정밀여과의 물 역세척 또는 한외여과의 질소 역세척한 기존 결과와 비교 고찰하였다. 그 결과, 휴믹산 농도의 영향으로 막오염이 진행되는 경향은 질소 또는 물 역세척에 따라, 동일한 재질이라도 한외여과 또는 정밀여과에 따라 차이를 보였다. 또한 동일한 재질의 분리막의 경우 한외여과 보다 정밀여과에서 질소 역세척이 막오염 억제에 효과적이고, 동일한 정밀여과인 경우 물 역세척보다 질소 역세척이 효과적이었다. 탁도 처리효율은 휴믹산 농도와 무관하게 거의 일정하였으나, 휴믹산 처리효율은 휴믹산 10 mg/L에서 최대였다. 이러한 결과로부터 정밀여과막의 질소 역세척시 휴믹산의 농도가 증가할수록 처리수의 휴믹산 농도도 높아지지만, 휴믹산 농도 10 mg/L에서 광촉매 구의 흡착과 광산화로 휴믹산이 최대 효율로 제거된다는 것을 알 수 있었다.