• Title/Summary/Keyword: Inhibition constant

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Lubricating Effect of Water-soluble Hexagonal Boron Nitride Nanolubricants on AISI 304 Steel Sliding Pair

  • Gowtham Balasubramaniam;Dae-Hyun Cho
    • Tribology and Lubricants
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    • v.39 no.2
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    • pp.43-48
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    • 2023
  • In this study, we investigate the tribological behavior of AISI 304 stainless steel pairs under deionized water and hexagonal boron nitride (h-BN) water dispersion lubrication. The specimen friction and wear properties are evaluated using a reciprocating ball-on-flat tribometer. The coefficient of friction remains nearly constant throughout the test under both lubricant conditions. The wear depth of the specimens under h-BN lubrication is smaller than that under deionized water lubrication, indicating the inhibition behavior of h-BN nanolubricants on direct metal-metal contacts. Optical micrographs and stylus profilometer measurements are performed to evaluate the severity of damage caused by the sliding motion and to determine the wear morphology of the specimens, respectively. The results show that h-BN nanolubricants does not have a significant effect on the friction behavior but demonstrates reduced wear owing to their trapping effect between the sliding interfaces. Moreover, scanning electron microscopy and energy-dispersive X-ray spectroscopy images of the specimens were acquired to confirm the trapping effect of h-BN between the sliding interfaces. The results also suggest that the trapped lubricants can distribute the contact pressure, reducing the wear damage caused by the metal-metal contact at the interface. In conclusion, h-BN nanolubricants have potential as an anti-wear additive for lubrication applications. Further investigation is needed to provide direct evidence of the trapping effect of h-BN nanoparticles between the sliding interfaces. These findings could lead to the development of more efficient and effective lubricants for various industrial applications.

QSAR on the Inhibition Acticity of Flavopiridol Analogues against Breast Cancer MCF-7 (Flavopiridol 유도체에 의한 유방암 MCF-7 세포의 저해 활성에 관한 구조와 활성과의 관계)

  • Soung, Min-Gyu;Joo, Sung-Mo;Song, Ah-Reum;Sung, Nack-Do
    • Applied Biological Chemistry
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    • v.50 no.3
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    • pp.147-153
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    • 2007
  • To search for a molecular design of a new breast cancerous inhibitory active compound, 2D-QSAR and HQSAR between the substituents of flavopiridol analogues as substrates and their breast cancerous inhibitory activities against MCF-7 cell were analyzed and discussed quantitatively. It was found that the dispersion with molecule and steric hindrance with substituents will have a tremendous impact on the inhibitory activities from the 2D-QSAR model (1). Also, MR constant is better than that of MS constant as animportant factor. The inhibitory activities from 2D-QSAR model (2) were dependent upon the optimum MR constant (MR = 126 $Cm^3/mol$). Optimized HQSAR model (V) exhibited the best predictability of the inhibitory activities based on the cross-validated $r^2_{cv}$($q^2$= 0.583) and non-cross-validated conventional coefficient ($r^2_{ncv}$= 0.982). From the contribution maps, the inhibitory activity by the imino group on $C_9$ atom was higher than that of the hydroxyl group of $C_8$ atom on the A ring in molecule. Therefore, we can confirm that the dispersion by substituents in molecule is the most important factor in inhibitory activities against MCF-7 cell.

KINETIC STUDIES OF LACTIC ACID FERMENTATION(PART 1) EFFECT OF MECHANICAL AGITATION ON FERMENTATION (유산균 발효에 관한 동력학적 연구(제1보) 발효에 미치는 기계적 교반의 영향)

  • LEE Keun-Tai;HAN Bong-Ho
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.12 no.3
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    • pp.155-160
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    • 1979
  • Mechanical agitation in fermentation process enhances the fermentation activity of microbes by means of oxygen supply and frequent collision with substrate. However, the fermentation activity of microaerophilic bacteria is inhibited by the excess oxygen resulted from the mechanical agitation. On this account, a a strain of Lactobacillus bulgarius was cultured to know the inhibition effect of the mechanical agitation and determine the optimum conditions for tile process of lactic acid fermentation. The growth rate of L. bulgaricus and the consumption rate of tile substrate revealed an identical pattern in changes. The two rates were constant in the range of the modified Reynolds number of $1\times10^5\;to\;5\times10^5$ while they showed linear increase in the range of the modified Reynolds number of $1\times10^5\;to\;10\times10^5$. Under the conditions of the modified Reynolds number more than $10\times10^5$, the both rates decreased. At the modified Reynolds number of $10\times10^5$, the maximum specific growth rate and the saturation constant of L. bulgaricus were 0.58/hr and 6.74g/l, respectively.

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The Vasodilating Mechanism of Sodium Nitroprusside and Forskolin on Phorbol dibutyrate-Induced Contractions in Rat Aorta (Sodium nitroprusside와 Forskolin의 Phorbol ester 수축에 대한 혈관이완작용의 기전)

  • Ahn, Hee-Yul
    • The Korean Journal of Pharmacology
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    • v.31 no.3
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    • pp.291-297
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    • 1995
  • The objectives of this study is to compare the inhibitory mechanism of sodium nitroprusside and forskolin on the phorbol ester, activator of protein kinase C (PKC), -induced contractions in rat aorta. $0.1\;{\mu}M$ phorbol dibutyrate (PDBu) induced sustained contractions and increased phosphorylations of myosin light chain (MLC) time-dependently. At 30 min, the contractions and phosphorylations of MLC by PDBu were augmented maximally and remained constant. Moreover, $^{45}Ca^{2+}$ uptake was increased 30 min after PDBu stimulation from resting values. Sodium nitroprusside which activates guanylyl cyclase followed by increasing cGMP, inhibited the PDBu-induced contractions concentration-dependently. On the other hand, forskolin which activates adenylyl cyclase followed by increasing cAMP, also inhibited the PDBu-induced contractions concentration-dependently. However, sodium nitroprusside was more potent to inhibition of the PDBu-induced contractions than forskolin. Sodium nitroprusside inhibited $^{45}Ca^{2+}$ uptake by PDBu stimulation. Forskolin also inhibited $^{45}Ca^{2+}$ uptake by PDBu stimulation. Sodium nitroprusside and forskolin inhibited the phosphorylations of MLC by PDBu, respectively. However, sodium nitroprusside was more potent to inhibition of phosphorylations of MLC by PDBu than forskolin. From these results, Sodium nitroprusside via cGMP or forskilin via cAMP may reduce myoplasmic $Ca^{2+}$ followed by suppression of phosphorylations of MLC of PKC-mediated contractions, which results in vasodilation. However, cGMP may play a role more importantly than cAMP on the regulation of protein kinase C-mediated contraction in vascular smooth muscle.

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Binding Profiles of Oxomemazine to the Muscarinic Receptor Subtypes (Oxomemazine의 Muscarinic Receptor Subtypes에 대한 결합성질)

  • Lee, Shin-Woong;Kim, Jeung-Gu
    • The Korean Journal of Pharmacology
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    • v.30 no.1
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    • pp.49-57
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    • 1994
  • The binding properties of oxomemazine to muscarinic receptors using the ability of oxomemazine to inhibit $[^3H]QNB$ binding in membrane fractions of rat cerebrum and guinea pig ventricle and ileum were investigated. $[^3H]QNB$ bound to a single class of muscarinic receptors with a dissociation constant of approximately 60 pM in three tissue preparations. Pirenzepine and oxomemazine inhibited $[^3H]QNB$ binding in cerebrum with a Hill coefficient lower than unity, and the inhibition data were best described by a two-site model. The relative densities of the high $(M_1)\;and\;low\;(M_2)$ affinity sites for pirenzepine were 60 and 40%, with corresponding Ki values of 16 and 431 nM, and those $(O_H\;and\;O_L)$ for oxomemazine 40 and 60%, with corresponding Ki values of 80 and 1350 nM. However, the inhibition data of both drugs vs $[^3H]QNB$ in ventricle and ileum appeared to obey the law of mass-action (Hill coefficient close to 1). The apparent Ki values of pirenzepine were 850 and 250 nM, and those of oxomemazine 1460 and 570 nM in ventricle and ileum, respectively. Thus, oxomemazine like pirenzepine has high affinity for cerebrum, moderate affinity for ileum and low affinity for ventricle. These results suggest that oxomemazine could recognize the muscarinic receptor subtypes with a high affinity for the $M_1$ sites.

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Alkali Metal Ion Catalysis and Inhibition in Nucleophilic Substitution Reactions of 3,4-Dinitrophenyl Diphenylphosphinothioate with Alkali Metal Ethoxides in Anhydrous Ethanol: Effect of Changing Electrophilic Center from P=O to P=S

  • An, Jun-Sung;NamKoong, Gil;Kang, Ji-Sun;Um, Ik-Hwan
    • Bulletin of the Korean Chemical Society
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    • v.32 no.7
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    • pp.2423-2427
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    • 2011
  • Pseudo-first-order rate constants ($k_{obsd}$) have been measured spectrophotometrically for nucleophilic substitution reactions of 3,4-dinitrophenyl diphenylphosphinothioate 9 with alkali metal ethoxides (EtOM, M = Li, Na, K) in anhydrous ethanol at $25.0{\pm}0.1^{\circ}C$. The plot of $k_{obsd}$ vs. [EtOM] is linear for the reaction of 9 with EtOK. However, the plot curves downwardly for those with EtOLi and EtONa while it curves upwardly for the one with EtOK in the presence of 18-crown-6-ether (18C6). Dissection of $k_{obsd}$ into $k_{EtO^-}$ and $k_{EtOM}$ (i.e., the second-order rate constant for the reaction with dissociated $EtO^-$ and ion-paired EtOM, respectively) has revealed that the reactivity increases in the order $k_{EtOLi}$ < $k_{EtONa}$ < $k_{EtO^-}$ ${\approx}$ $k_{EtOK}$ < $k_{EtOK/18C6}$, indicating that the reaction is inhibited by $Li^+$ and $Na^+$ ions but is catalyzed by 18C6-crowned $K^+$ ion. The reactivity order found for the reactions of 9 contrasts to that reported previously for the corresponding reactions of 1, i.e., $k_{EtOLi}$ > $k_{EtONa}$ > $E_{EtOK}$ > $k_{EtO^-}$ ${\approx}$ $k_{EtOK/18C6}$, indicating that the effect of changing the electrophilic center from P=O to P=S on the role of $M^+$ ions is significant. A four-membered cyclic transition-state has been proposed to account for the $M^+$ ion effects found in this study, e.g., the polarizable sulfur atom of the P=S bond in 9 interacts strongly with the soft 18C6-crowned $K^+$ ion while it interacts weakly with the hard $Li^+$ and $Na^+$ ions.

rvH1N1 Neuraminidase Inhibitory Activities of Phenolics from Perilla frutescens (L.) and Their Contents in Cultivars and Germplasm

  • Ha, Tae Joung;Lee, Myoung-Hee;Park, Chang-Hwan;Kim, Jung-In;Oh, Eunyoung;Pae, Suk-Bok;Park, Jae Eun;Kim, Sung-Up;Kwak, Do-Yeon
    • Plant Breeding and Biotechnology
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    • v.6 no.4
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    • pp.404-412
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    • 2018
  • The influenza neuraminidase (NA, E.C. 3.2.1.18), an antiviral, has been the target of high pharmaceutical companies due to its essential role in viral replication cycle. Perilla frutescens (P. frutescens) is used in traditional Chinese medicine for various diseases, such as cold due to wind-cold, headache and cough. In this context, four major polyphenolic compounds including rosmarinic acid-3-O-glucoside (1), rosmarinic acid (2), luteolin (3), and apigenin (4) isolated from P. frutescens were evaluated for their inhibitory effect on recombinant virus H1N1 neuraminidase (rvH1N1 NA). Among the test compounds, rosmarinic acid and luteolin inhibited the rvH1N1 NA with an $IC_{50}$ of 46.7 and $8.4{\mu}M$, respectively. The inhibition kinetics analyzed by the Dixon plots indicated that rosmarinic acid and luteolin were noncompetitive inhibitors and that the inhibition constant, $K_I$, was established as 43.9 and $14.3{\mu}M$, respectively. In addition, 578 genetically diverse accessions and 39 cultivars of P. frutescens were analyzed using HPLC to characterize the diversity of polyphenolic composition and concentration. The individual and total compositions exhibited significant difference (P < 0.05), especially rosmarinic acid which was detected as the predominant metabolite in all accessions (58.8%) and cultivars (62.8%). Yeupsil and Sangback cultivars exhibited the highest rosmarinic acid ($3,393.5{\mu}g/g$) and luteolin ($383.3{\mu}g/g$) content respectively. YCPL177-2 with the high concentration ($889.8{\mu}g/g$) of luteolin may be used as a genetic resource for breeding elite cultivars.

Effects of Acai Berry Ethanolic Extracts on Production of Nitric Oxide and Activity of Angiotensin Converting Enzyme Related to Blood Circulation (혈액순환과 관련하여 nitric oxide 생성과 angiotensin converting enzyme 활성에 미치는 Acai berry 에탄올 추출물의 영향)

  • Nam, Hyang;Lee, Su-Gyeong;Kim, Deok Won;Kim, Joo Wan;Kim, Ki Young;Kim, Sung Goo;Kim, Moon-Moo;Chung, Kyung Tae
    • Journal of Life Science
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    • v.23 no.6
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    • pp.743-750
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    • 2013
  • The aim of this study is to develop a supplementary therapeutic agent capable of promoting vascular circulation. The effects of Acai berry ethanolic extracts (ABEE) on activity of angiotensin converting enzyme from rabbit lung, production of nitro oxide in both murine macrophage cells and vascular endothelial cells as well as antioxidant effects were investigated in this study. First of all, it was observed the direct effects of ABEE on reducing power and antioxidant effect lipid peroxidation. In addition, ABEE showed a protective effect on DNA oxidation induced by hydroxyl radical. Furthermore, ABEE at 0.01% exerted approximately 50% inhibition on activity of angiotensin converting enzyme. ABEE increased the production of nitric oxide in endothelial cells, but decreased the induction of nitric oxide stimulated by lipopolysaccharide in microphage. The expression levels of superoxide dismutase (SOD)-2 and -3 were enhanced by ABEE treatment, however, the expression level of SOD-1 remained constant. Moreover, the expression level of nitric oxide synthases-1 (NOS-1), a constitutive enzyme, was increased by ABEE, but that of NOS-2, a inducible enzyme, was constant. It was also found that the level of Nrf-2, a transcription factor of SOD, was increased by ABEE. Therefore, these results demonstrate that ABEE could promote blood circulation via above actions, suggesting that may be helpful for health of blood vessel.

Sintering of Surface-Modified PMN-PT-BT Powder with MgO Sol and Its Dielectric Properties (MgO 졸로 표면개질된 PMN-PT-BT 분말의 소결 및 유전특성)

  • Han, Kyoung-Ran;Kim, Chang-Sam
    • Journal of the Korean Ceramic Society
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    • v.41 no.12 s.271
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    • pp.929-932
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    • 2004
  • It is known that small amount of MgO in excess is often added to develop pure perovskite single phase of PMN-based composite, however, extra MgO precipitates in grains and inhibits densification of PMN. In this study PMN-PT-BT (PBT) powder was prepared by a conventional mixed oxide method using $(MgCO_3)_4{\cdot}Mg(OH)_2{\cdot}5H_{2}O$ instead of MgO. The precursor was heated at $500^{\circ}C/1h$ and its surface was modified with MgO sol. This effect was investigated in the aspects of sintering and dielectric properties. Small amount of added MgO sol ($0.5{\sim}1.0wt\%$) enhanced sintering substantially below $1000^{\circ}C$. The PBT with $0.5wt\%$ MgO sol sintered at $900^{\circ}C/2h$ had density of $7.62\;g/cm^3$, room temperature dielectric constant of 14800, loss of dielectric constant of $1.1\%$, which were comparable to those of the PBT sintered at $1000^{\circ}C/2h$. It was noticeable that the extra MgO precipitated mostly on triple points and grain boundaries and resulted in inhibition of grain growth.

The Study on $Na^+-Ca^{++}$ Exchange in Heart Mitochondria (심근 Mitochondria의 $Na^+-Ca^{++}$교환에 관한 연구)

  • Shin, Sang-Goo;Kim, Myung-Suk;Lim, Jung-Kyoo
    • The Korean Journal of Pharmacology
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    • v.18 no.2
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    • pp.89-102
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    • 1982
  • The $Na^+-and\;K^+-induced\;Ca^{++}$ release was measured isotopically by millipore filter technique in pig heart mitochondria. With EGTA-quenching technique, the characteristics of mitochondrial $Ca^{++}-pool$ and the sources of $Ca^{++}$ released from mitochondria by $Na^+\;or\;K^+$ were analyzed. The mitochondrial $Ca^{++}-pool$ could be distinctly divided into two components: internal and external ones which were represented either by uptake through inner membrane, or by energy independent passive binding to external surface of mitochondria, respectively. In energized mitochondria, a large portion of $Ca^{++}$was transported into internal pool with little external binding, while in de-enerigzed state, a large portion of transported $Ca^{++}$ existed in the external pool with limited amount of $Ca^{++}$ in the internal pool which was possibly transported through the $Ca^{++}-carrier$ present in the inner membrane. $Na^+$ induced the $Ca^{++}$ release from both internal pool and external pool and external binding pool of mitochondria. In contrast, $K^+$ did not affect $Ca^{++}$ of the internal pool, but, displaced $Ca^{++}$ bound to external surface of the mitochondria. When the $Ca^{++}-reuptake$ was blocked by EGTA, the $Ca^{++}$ release from the internal pool by $Na^+$ was rapid; the rate of $Ca^{++}-efflux$ appeared to be a function of $[Na^+]^2$ and about 8mM $Na^+$ was required to elicit half-maximal velocity of $Ca^{++}-efflux$. So it was revealed that $Ca^{++}-efflux$ velocity was particulary sensitive to small changes of the $Na^+$ concentration in physiological range. Energy independent $Ca^{++}-binding$ sites of mitochondrial external surface showed unique characteristics. The total number of external $Ca^{++}-binding$ sites of pig heart mitochondria was 29 nmoles per mg protein and the dissociation constant(Kd) was $34{\mu}M$. The $Ca^{++}-binding$ to the external sites seemed to be competitively inhibited by $Na^+\;and\;K^+$; the inhibition constant(Ki) were 9.7 mM and 7.1 mM respectively. Considering the intracellular ion concentrations and large proportion of $Ca^{++}$ uptake in energized mitochondria, the external $Ca^{++}-binding$ pool of the mitochondria did not seem to play a significant role on the regulation of intracellular free $Ca^{++}$ concentration. From this experiment, it was suggested that a small change of intracellular free $Na^+$ concentration might play a role on regulation of free $Ca^{++}$ concentration in cardiac cell by influencing $Ca^{++}-efflux$ from the internal pool of mitochondria.

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