• Title/Summary/Keyword: cyclic action

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Relationship Between Tyrosinase Inhibitory Action and Oxidation-Reduction Potential of Cosmetic Whitening Ingredients and Phenol Derivatives

  • Sakuma, Katsuya;Ogawa, Masayuki;Sugibayashi, Kenji;Yamada, Koh-ichi;Yamamoto, Katsumi
    • Archives of Pharmacal Research
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    • v.22 no.4
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    • pp.335-339
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    • 1999
  • The oxidation-reduction potentials of cosmetic raw materials, showing tyrosinase inhibitory action, and phenolic compounds structurally similar to L-tyrosine were determined by cylcic voltammetry. The voltammograms obtained could be classified ito 4 patterns (patterns 1-4). Patterns 1, characterized by oxidation and reduction peaks as a pair, was observed with catechol, hydroquinone or phenol, and pattern 2 exhibiting another oxidation peak in addition to oxidation and reduction peaks as a pair was found with arbutin, kojic acid, resorcinol, methyl p-hydroxybenzoate and L-tyrosine as the substrate of tyrosinase. Pattern 3 with an independent oxidation peak only was expressed by L-ascorbic acid, and pattern 4 with a reduction peak only at high potentials, by hinokitiol. The tyrosinase inhibitory activity of these compounds was also evaluated using the 50% inhibitory concentration ($IC_{50}$) and the inhibition constant (Ki) as parameters. Hinokitiol, classified as patterns 4, showed the highest inhibitory activity (lowest $IC_{50}$ and Ki). Hydroquinone showing the second highest activity belonged to pattern 1, which also included compounds exhibiting pattern 2 was relatively low with Ki values being in the order of 10-4 M. Although there was no consistent relationship between oxidation-reduction potentials and tyrosinase inhibitory action, the voltammetry data can be used as an additional index to establish the relationship between the structure and the tyrosine inhibitory activity.

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Anthraquinones and Sterols from the Korean Marine Echiura Urechis unicintus (한국산 해양 의충동물 개불에서 Anthraquinone 및 Sterol 성분연구)

  • Chang, Sung-keun;Park, Yong-Hyun;Chai, Seuk;Kim, In-Kyu;Seo, Young-Wan;Cho, Ki-woong;Shin, Jong-Heon
    • Journal of the Korean Chemical Society
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    • v.42 no.1
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    • pp.64-68
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    • 1998
  • Three anthraquinones, chrysophanol, physcion and 1-o-methyl-2-methoxychrysophanol which have $Na^+,K^+-ATPase$ and cyclic AMP phosphodiesterase lowering activities related to cardiotonic action were isolated from the Korean marine echiura, Urechis unicintus. Spectroscopic methods, including HMQC, HMBC and NOE studies, were used to establish the structures.

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Experimental studies on steel frame structures of traditional-style buildings

  • Xue, Jianyang;Qi, Liangjie
    • Steel and Composite Structures
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    • v.22 no.2
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    • pp.235-255
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    • 2016
  • This paper experimentally investigated the behavior of steel frame structures of traditional-style buildings subjected to combined constant axial load and reversed lateral cyclic loading conditions. The low cyclic reversed loading test was carried out on a 1/2 model of a traditional-style steel frame. The failure process and failure mode of the structure were observed. The mechanical behaviors of the steel frame, including hysteretic behaviors, order of plastic hinges, load-displacement curve, characteristic loads and corresponding displacements, ductility, energy dissipation capacity, and stiffness degradation were analyzed. Test results showed that the Dou-Gong component (a special construct in traditional-style buildings) in steel frame structures acted as the first seismic line under the action of horizontal loads, the plastic hinges at the beam end developed sufficiently and satisfied the Chinese Seismic Design Principle of "strong columns-weak beams, strong joints-weak members". The pinching phenomenon of hysteretic loops occurred and it changed into Z-shape, indicating shear-slip property. The stiffness degradation of the structure was significant at the early stage of the loading. When failure, the ultimate elastic-plastic interlayer displacement angle was 1/20, which indicated high collapse resistance capacity of the steel frame. Furthermore, the finite element analysis was conducted to simulate the behavior of traditional-style frame structure. Test results agreed well with the results of the finite element analysis.

Distinct Regional and Cellular Localization of Hyperpolarization-activated Cyclic Nucleotide-gated Channel 1 in Cerebellar Cortex of Rat

  • Kwon, Young-Joon;Kim, Tae-Sung
    • Journal of Korean Neurosurgical Society
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    • v.42 no.3
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    • pp.205-210
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    • 2007
  • Objective : Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels mediate the hyperpolarization-activated currents (Ih) that participate in regulating neuronal membrane potential and contribute critically to pacemaker activity, promoting synchronization of neuronal networks. However, distinct regional and cellular localization of HCN channels in the brain have not been precisely defined. Aim of this study was to verify the precise cellular location of HCN1 channels in rat cerebellum to better understand the physiological role these channels play in synaptic transmission between CNS neurons. Methods : HCN1 expression in rat brain was analyzed using immunohistochemistry and electron-microscopic observations. Postsynaptic density-95 (PSD-95), otherwise known as locating and clustering protein, was also examined to clarify its role in the subcellular location of HCN1 channels. In addition, to presume the binding of HCN1 channels with PSD-95, putative binding motifs in these channels were investigated using software-searching method. Results : HCN1 channels were locally distributed at the presynaptic terminal of basket cell and exactly corresponded with the location of PSD-95. Moreover, nine putative SH3 domain of PSD-95 binding motifs were discovered in HCN1 channels from motif analysis. Conclusion : Distinct localization of HCN1 channels in rat cerebellum is possible, especially when analyzed in conjunction with the SH3 domain of PSD-95. Considering that HCN1 channels contribute to spontaneous rhythmic action potentials, it is suggested that HCN1 channels located at the presynaptic terminal of neurons may play an important role in synaptic plasticity.

Effect of bond and bidirectional bolting on hysteretic performance of through bolt CFST connections

  • Ajith, M.S.;Beena, K.P.;Sheela, S.
    • Earthquakes and Structures
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    • v.19 no.5
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    • pp.315-329
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    • 2020
  • Through bolt connections in Concrete Filled Steel Tubes (CFSTs) has been proved to be good in terms of seismic performance and constructability. Stiffened extended end plate connection with full through type bolt helps to avoid field weld altogether, and hence to improve the quality of joints. An experimental study was conducted on the hysteretic performance of square interior beam-column connections using flat extended end plates with through bolt. The study focuses on the effect of the bond between the tie rod and the core concrete on the cyclic performance of the joint. The study also quantifies how much the interior joint is getting strengthened due to the confinement effect induced by bi-directional bolting, which is widely used in 3D moment resisting frames. For a better understanding of the mechanism and for the prediction of shear capacity of the panel zone, a mathematical model was generated. The various parameters included in the model are the influence of axial load, amount of prestress induced by bolt tightening, anchorage, and the concrete strut action. The study investigates the strength, stiffness, ductility, and energy dissipation characteristics. The results indicate that the seismic resistance is at par with American Institute of Steel Construction (AISC) seismic recommendations. The bidirectional bolting and bond effect have got remarkable influence on the performance of joints.

Experimental Study on the Stability of Dredged Soil Bed under Cyclic Wave Actions (파랑작용에 의한 준설토 지반의 안정성에 관한 실험적 연구)

  • Kang, Yoon-Koo
    • Journal of Ocean Engineering and Technology
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    • v.20 no.4 s.71
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    • pp.43-49
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    • 2006
  • Detailed investigations were carried out on the stability of the dredged soil bed against wave actions, aimedat establishing the design method of artificial tidal flats using dredged soil. The soil was dredged at Nagoya port, Japan, and has a mean grain size of 0.013mm. Basic features of artificial dredged soil bed against wave actions were explained from a series of model experiments in a wave flume. The two types of section shapes were employed; one is a horizontal bed and the other is a sloped one. Changes of the bed profile, shear strength, grain size distribution and water content, according to the wave actions, were measured in detail. The cumulative effect of the wave actions, over about one week, was investigated. A dredged soil bed moves withthe wave actions with relatively small wave height. It should be especially. noted that the clay component is dissolved and flown out, away from the surface layer, and consequently the surface layer hardens, as if it is covered with sand. Wren the wave height is gradually increased, the bed is not liquefied and the shear strength of the dredged bed is increased by a wave-induced dissipation of pore pressures in the bed and a decrease of clay component by the wave-induced leakage.

Antiallergic Action of Magnolia Officinalis on Immediate Hypersensitivity Reaction

  • Shin, Tae-Yong;Kim, Dae-Keun;Chae, Byeung-Suk;Lee, Eon-Jeong
    • Archives of Pharmacal Research
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    • v.24 no.3
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    • pp.249-255
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    • 2001
  • We studied the effect of aqueous extract of Magnolia officinalis bark (Magnoliaceae) (MOAE) on the immediate hypersensitivity reaction. MOAE (0.01 to 1g/kg) dose-dependently inhibited compound 48/80 induced systemic anaphylaxis in rats. MOAE (0.1 and 1g/kg) also significantly inhibited local immunoglobulin E (lgE)-mediated passive cutaneous anaphylactic reaction. When MOAE was pretreated at concentrations ranging from 0.01 to 1g/kg, the levels of plasma histamine were reduced in a dose-dependent manner. MOAE (0.001 to 1 mg/ml) dose-dependently inhibited the histamine release from rat peritoneal mast cells (RPMC) activated by compound 48/80 or anti-dinitrophenyl (DNP) Igl. The level of cyclic AMP (CAMP) in RPMC, when MOAE was added, significantly increased compared with that of the normal control. Moreover, MOAE (0.01 to 1 mg/ml) had a significant inhibitory effect on anti-DNP Igl-induced tumor necrosis factor-$\alpha$ production from RPMC. These results indicate that MOAE inhibits immediate hypersensitivity reaction in vivo and in vitro.

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Experimental tests and global modeling of masonry infilled frames

  • Bergami, Alessandro Vittorio;Nuti, Camillo
    • Earthquakes and Structures
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    • v.9 no.2
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    • pp.281-303
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    • 2015
  • The effects of infill panels on the response of r.c. frames subjected to seismic action are widely recognized. Numerous experimental investigations were effected and several analytical models were developed on this subject. This work, which is part of a larger project dealing with specific materials and structures commonly used in Italy, discusses experimental tests on masonry and samples of bare and infilled portals. The experimental activity includes tests on elemental materials, and 12 wall samples. Finally, three one-bay one-story reinforced concrete frames, designed according to the outdated Italian technical code D.M. 1996 without seismic details, were tested (bare and infilled) under constant vertical and cyclic lateral load. The first cracks observed on the framed walls occurred at a drift of about 0.3%, reaching its maximum capacity at a drift of 0.5% while retaining its capacity up to a drift of 0.6%. Infill contributed to both the stiffness and strength of the bare reinforced concrete frame at small drifts thus improving overall system behavior. In addition to the experimental activities, previously mentioned, the recalibration of a model proposed by Comberscue (1996) was evaluated. The accuracy of an OpenSees non linear fiber based model of the prototype tested, including a strut element was verified through a comparison with the final experimental results. This work has been partially supported by research grant DPC-ReLUIS 2014.

Calcium Current and Background Current Activation in L-triiodothyronine Loaded Ventricular Myocytes of the Rabbit

  • Han, Jin;Kim, Eui-Yong;Han, Jae-Hee;Park, Choon-Ok;Hong, Seong-Geun;Leem, Chae-Hun;So, In-Suk;Ho, Won-Kyung;Earm, Yung-E;Sung, Ho-Kyung
    • The Korean Journal of Physiology
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    • v.26 no.2
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    • pp.99-111
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    • 1992
  • Permissive action of thyroid hormone at the level of Ca channel and responsible mechanisms underlying thyroid hormone-induced change in myocardial contractile state and $T_3-induced$ arrhythmias were investigated in rabbit ventricular or atrial myocytes using whole cell patch clamp technique. Single cells were isolated by Langendorff perfusion with collagenase. Cardiac myocytes were incubated in $low-Cl^-,$, $high-K^+$ medium containing $1_{\mu}M\;L-triiodothyronine\;(T_3)$ at $4^{\circ}C$ for 2.10 hours. The calcium currrent $(I_{Ca})$ was increased in $T_3$ loaded cells, however, the shape of current voltage curve and reverse potential did not altered. Cyclic AMP, cyclic GMP, isoprenaline and 3-isobutyl-1-methyl-xanthine increased $I_{Ca}$ in euthyroid and hyperthyroid conditions, and acetylcholine blocked the increase of $I_{Ca}\;in\;T_3$ loaded cells. The amplitude of $I_{Ca}$ was much larger after perfusing cGMP than cGMP in both conditions, whereas the degree of increase of $I_{Ca}$ was greater after perfusing cAMP than cGMP in $T_3$ loaded cells. The degree of increase of $I_{Ca}$ after perfusing isoprenaline or IBMX also was greater in $T_3$ loaded cells than in control cells. Background current induced by isoprenaline also increased in $T_3$ loaded cells. The Ca release dependent inward current was increased in amplitude but its activation and inactivation time course was not changed in $T_3$ loaded cells. Activation of Na pump current was not changed in $T_3$ loaded cells. From the above results it is suggested that thyroid hormone induced increase in the contractile state of cardiac myocytes are accompanied by augmented $I_{Ca}$ and the increase of Ca release from sarcoplasmic reticulum and the permissive action of thyroid hormone to catecholamines could induce arrhythmias through the increase of $I_{Ca}$ and background current.

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Regulation of Insulin-Sensitive Cyclic Nucleotide Phosphodiesterase in Adipocytes of Streptozotocin-Induced Diabetic Rats (Streptozotocin으로 당뇨병을 유발시킨 흰쥐의 지방세포에서 일어나는 Insulin-Sensitive Phosphodiesterase의 조절에 관한 연구)

  • Park, Kyung-Sun;Lee, Myung-Soon;Kim, Kyung-Hwan
    • The Korean Journal of Pharmacology
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    • v.29 no.2
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    • pp.253-261
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    • 1993
  • Possible changes in the role of insulin-sensitive cyclic nucleotide phosphodiesterase(PDE) in mediating the antilipolytic action of insulin were investigated in adipocytes from streptozotocin-induced diabetic rats. Isolated adipocytes prepared from epididymal adipose tissue were incubated, with or without insulin, at $37^{\circ}C$ for 15 min following pretreatment with various drugs or toxins, and three (plasma membranes, microsomal membranes, and cytosol) fractions prepared by differential centrifugation were then assayed for cAMP phosphodiesterase activity. The PDE activities only in the crude microsomal (P2) fractions were activated by insulin both in diabetic and control rats. The basal PDE activities in P2 fractions of adipocytes from diabetic rats were higher than those from control rats, although the maximal effects observed at 2 nM of insulin, $100\;{\mu}M$ of isoproterenol or the combination of both were not significantly different from each other. The insulin-stimulated PDE activities in P2 fractions of adipocytes from diabetic rats were not changed by PIA, a $A_{1}$ adenosine receptor agonist, whereas they were decreased to the basal PDE activities in those from control rats. In addition, the adipocytes from diabetic rats showed an increased sensitivity to pertussis toxin compared to those from controls. There were no differences between diabetic and control rats in the sensitivity of adipocytes to cholera toxin. These data indicate that the impaired signalling through inhibitory receptors such as adenosine receptors in adipocytes from streptozotocin-induced diabetes relates to the loss or the decreased function of $G_i$ proteins, and leads to the increased activity of the insulin-dependent PDE at the basal states.

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