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Ginsengenin derivatives synthesized from 20(R)-panaxotriol: Synthesis, characterization, and antitumor activity targeting HIF-1 pathway

  • Guo, Hong-Yan;Xing, Yue;Sun, Yu-Qiao;Liu, Can;Xu, Qian;Shang, Fan-Fan;Zhang, Run-Hui;Jin, Xue-Jun;Chen, Fener;Lee, Jung Joon;Kang, Dongzhou;Shen, Qing-Kun;Quan, Zhe-Shan
    • Journal of Ginseng Research
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    • v.46 no.6
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    • pp.738-749
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    • 2022
  • Background: Ginseng possesses antitumor effects, and ginsenosides are considered to be one of its main active chemical components. Ginsenosides can further be hydrolyzed to generate secondary saponins, and 20(R)-panaxotriol is an important sapogenin of ginsenosides. We aimed to synthesize a new ginsengenin derivative from 20(R)-panaxotriol and investigate its antitumor activity in vivo and in vitro. Methods: Here, 20(R)-panaxotriol was selected as a precursor and was modified into its derivatives. The new products were characterized by 1H-NMR, 13C-NMR and HR-MS and evaluated by molecular docking, MTT, luciferase reporter assay, western blotting, immunofluorescent staining, colony formation assay, EdU labeling and immunofluorescence, apoptosis assay, cells migration assay, transwell assay and in vivo antitumor activity assay. Results: The derivative with the best antitumor activity was identified as 6,12-dihydroxy-4,4,8,10,14-pentamethyl-17-(2,6,6-trimethyltetrahydro-2H-pyran-2-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl(tert-butoxycarbonyl)glycinate (A11). The focus of this research was on the antitumor activity of the derivatives. The efficacy of the derivative A11 (IC50 < 0.3 µM) was more than 100 times higher than that of 20(R)- panaxotriol (IC50 > 30 µM). In addition, A11 inhibited the protein expression and nuclear accumulation of the hypoxia-inducible factor HIF-1α in HeLa cells under hypoxic conditions in a dose-dependent manner. Moreover, A11 dose-dependently inhibited the proliferation, migration, and invasion of HeLa cells, while promoting their apoptosis. Notably, the inhibition by A11 was more significant than that by 20(R)-panaxotriol (p < 0.01) in vivo. Conclusion: To our knowledge, this is the first study to report the production of derivative A11 from 20(R)-panaxotriol and its superior antitumor activity compared to its precursor. Moreover, derivative A11 can be used to further study and develop novel antitumor drugs.

Distribution Characteristics of Quaternary Geology and Aggregate Resources in Geumsan-gun, Chungcheongnam-do (충청남도 금산군 일대 제4기 지질 및 골재자원 분포 특성)

  • Kim, Jin Cheul;Kim, Ju Yong;Lee, Jin-Young
    • Economic and Environmental Geology
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    • v.54 no.5
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    • pp.595-603
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    • 2021
  • Sand layer distribution, which is the main target of river and land aggregate resources, mainly belongs to alluvial and river sedimentary environments among the Quaternary sedimentary environments. The distribution of aggregate resources in the area of Geumsan-gun, Chungcheongnam-do is characteristically developed around a sedimentation environment in which intrusive meandering river dominate. Although the area around Bonhwangcheon Stream and the area near the confluence of small streams are small, the river floodplain develops and corresponds to the aggregate distribution area. The sedimentary layer formed in the sedimentary environment such as colluvial deposits or alluvial fan deposits has a relatively low distribution rate of aggregate resources. The vertical distribution of the Quaternary sedimentary layers in the Geumsan-gun region ranges from about 5 to 12 m and has an average Quaternary sedimentary thickness of 8 m. The aggregate-bearing section has an average thickness of 3.6 m, and the average grain size is about 21% clay-silt, 67% sand, and 12% gravel. The main characteristics of the aggregate-bearing section are that coarse-grained sand predominates, and gravel is sub-angular or sub-rounded, and the sorting is generally poor and has a massive form of deposits, and the soil colour ranges from dark grey to yellowish-brown. In Geumsan-gun, the most likely distribution area for aggregate development is the alluvial sedimentary and river sedimentary layers distributed along the current and former riverbeds of the main Geumgang River, Bonhwangcheon and small River tributaries.

Effects of Ventilation Systems on Interior Environment of the Growing-finishing Pig House in Korea (육성$\cdot$비육돈사 내에서 환기형태별 환경조사 연구)

  • Song J. I.;Yoo Y. H.;Jeong J. W.;Kim T. I.;Choi H. C.;Kang H. S.;Yang C. B.;Lee Y. Y.
    • Journal of Animal Environmental Science
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    • v.10 no.2
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    • pp.93-100
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    • 2004
  • An experiment was conducted to establish comparison of ventilation efficiency in an enclosed and conventional growing-finishing pig house. The experimental pigs were in winter and summer. The main results of the experiment are as follows : Then the air from planar slot inlet the pig house flow out through the sidewall outlet operated by exhaust fan(Gl). The second structure has an air input through the circular duct inlet are plated side the juncture of the entering wall and the air into the pig house flow out through the chimney and pit outlet are operated by exhaust fan(G2). Through the air into relay fan the pig house flow out through the curtains in sidewall(G3). Similarly, air comes in through the circular duct inlet are placed the air into the pig house flow out through the curtains in sidewall (G4). Air flow rate on the floor level which is the low part of pen and the living area of pigs in the G2 and G4 system during winter was measured at 0.2 to 0.3 m/s at the 0.5 to 0.6 m/s at the maximum ventilation efficiency. As for the results of detrimental gas(ammonia) concentration ratio analysis, while G2 and G4 system sustained of summer 13.3 $\~$ 16.6 ppm, winter 14.0 $\~$ 14.6 ppm level, Gl and G3 system sustained of summer 14.6 $\~$ 20.3 ppm, winter 20.3 $\~$ 25.0 ppm, and the latter one is lower than that of the G1 and G3 system.

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Ultimate behavior of long-span steel arch bridges

  • Cheng, Jin;Jiang, Jian-Jing;Xiao, Ru-Cheng;Xiang, Hai-Fan
    • Structural Engineering and Mechanics
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    • v.14 no.3
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    • pp.331-343
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    • 2002
  • Because of the increasing span of arch bridges, ultimate capacity analysis recently becomes more focused both on design and construction. This paper investigates the static and ultimate behavior of a long-span steel arch bridge up to failure and evaluates the overall safety of the bridge. The example bridge is a long-span steel arch bridge with a 550 m-long central span under construction in Shanghai, China. This will be the longest central span of any arch bridge in the world. Ultimate behavior of the example bridge is investigated using three methods. Comparisons of the accuracy and reliability of the three methods are given. The effects of material nonlinearity of individual bridge element and distribution pattern of live load and initial lateral deflection of main arch ribs as well as yield stresses of material and changes of temperature on the ultimate load-carrying capacity of the bridge have been studied. The results show that the distribution pattern of live load and yield stresses of material have important effects on bridge behavior. The critical load analyses based on the linear buckling method and geometrically nonlinear buckling method considerably overestimate the load-carrying capacity of the bridge. The ultimate load-carrying capacity analysis and overall safety evaluation of a long-span steel arch bridge should be based on the geometrically and materially nonlinear buckling method. Finally, the in-plane failure mechanism of long-span steel arch bridges is explained by tracing the spread of plastic zones.

Usability Evaluation for Simple Payment Service Based on Mobile Application -Focused on Shinhan and Samsung- (모바일 간편결제 애플리케이션 사용성 평가 연구 -신한FAN 앱카드와 삼성 앱카드를 중심으로-)

  • Lee, Kyung-Joo;Kim, Seung-In
    • Journal of Digital Convergence
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    • v.16 no.9
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    • pp.421-426
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    • 2018
  • This study is meant to derive what is needed to enhance the convenience and satisfaction of users of mobile credit card applications. For the first step, the current status of simple payment service using application has been identified and in-depth interview by reorganizing Peter Morvile's Honeycomb model into the five usage principle based on the main function of the application card. As a result, it was found that users prefer personalized services that fulfill the purpose and key functions of the app card and take into account their consumption patterns rather than too many additional functions. Based on this study, it is expected that it would help card companies increase their experience with app card users and strengthen their platforms.

A Study on the Fundamental Cause of Stall Stagnation Phenomena in Surges in Compressor Systems

  • Yamaguchi, Nobuyuki
    • International Journal of Fluid Machinery and Systems
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    • v.10 no.2
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    • pp.119-137
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    • 2017
  • Although the stall stagnation phenomena have often been experienced in site and also analytically in numerical experiments in surges in systems of compressors and flow paths, the fundamental causes have not been identified yet. In order to clarify the situations, behaviours of infinitesimal disturbance waves superposed on a main flow were studied in a simplified one-dimensional flow model. A ratio of the amplifying rate of the system instability to the characteristic slope of the compressor element was surveyed as the instability enhancement factor. Numerical calculations have shown the following tendency of the factor. In the situation where both the sectional area ratio and the length ratio of the delivery flow-path to the suction duct are sufficiently large, the enhancement factors are greater in magnitude, which means occurrence of ordinary deep surges. However, in the situation where the area ratio and/or the length ratio is relatively smaller, the enhancement factor tends to lessen significantly, which situation tends to suppress deep surges for the same value of the characteristic slope. It could result in the stall stagnation condition. In the domain of area ratio vs. length ratio of the delivery duct to the suction duct, contour-lines of the enhancement factor behave qualitatively similar to those of the stall stagnation boundaries of a fan analytically obtained, suggesting that a certain range of the enhancement factor values could specify the stagnation occurrence. The significant decreases in the factors are observed to accompany appearances of phase lags and travelling waves in the wave motions, which macroscopically suggests breaking down of the complete surge actions of filling and emptying of the air in the delivery duct. The strength of the action is deeply related with acoustic interferences and is evaluated in terms of the volume-modified reduced resonance frequency proposed by the author. These observations have shown the fundamental cause and the sequence of the stall stagnation in principle.

Mechanism Improvement of the Heat Exchanger for the Thermal Efficiency Increase of Hot Air Heater (온풍난방기의 열효율 증대를 위한 열교환기 구조개선)

  • Kang, Geum-Choon;Kang, Yoen-Ku;Ryou, Young-Sun;Kim, Young-Joong;Lee, Si-Young;Paek, Yee
    • Journal of Biosystems Engineering
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    • v.34 no.5
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    • pp.363-370
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    • 2009
  • Hot air heater with light oil combustion is used as the most common heater for greenhouse heating in the winter season. Hot air heaters of 256,246 units have been supplied as main greenhouse heating equipment until 2008 and greenhouse heating cost has reached to 620 billions won in Korea. In order to improve the thermal efficiency of the hot air heater and to reduce the expenses for greenhouse heating, prototype hot air heater was manufactured and tested in this experiment. The heat exchanger of tested prototype hot air heater was circular and hexagonal pipe type and inline and stagger arrangement type. Capacity of the heating was 43,062 kJ/h and total heat transfer area of the heat exchanger was $10.728\;m^2$. According to the performance test, it could supply heat of 38,240 to 35,100 kJ/h depending on the fan motor speed of 1,740~1,220 rpm, respectively. Thermal efficiency of hot air heater was 87.0% to 80.8% in the same conditions. As a result, thermal efficiency of hot air heater with hexagonal pipe-stagger arrangement heat exchanger developed in this study was higher 10.2% than that of conventional hot air heater and heating energy saving rate of 14.3% increased.

Controlling robot by image-based visual servoing with stereo cameras

  • Fan, Jun-Min;Won, Sang-Chul
    • Proceedings of the Korea Society of Information Technology Applications Conference
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    • 2005.11a
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    • pp.229-232
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    • 2005
  • In this paper, an image-based "approach-align -grasp" visual servo control design is proposed for the problem of object grasping, which is based on the binocular stand-alone system. The basic idea consists of considering a vision system as a specific sensor dedicated a task and included in a control servo loop, and we perform automatic grasping follows the classical approach of splitting the task into preparation and execution stages. During the execution stage, once the image-based control modeling is established, the control task can be performed automatically. The proposed visual servoing control scheme ensures the convergence of the image-features to desired trajectories by using the Jacobian matrix, which is proved by the Lyapunov stability theory. And we also stress the importance of projective invariant object/gripper alignment. The alignment between two solids in 3-D projective space can be represented with view-invariant, more precisely; it can be easily mapped into an image set-point without any knowledge about the camera parameters. The main feature of this method is that the accuracy associated with the task to be performed is not affected by discrepancies between the Euclidean setups at preparation and at task execution stages. Then according to the projective alignment, the set point can be computed. The robot gripper will move to the desired position with the image-based control law. In this paper we adopt a constant Jacobian online. Such method describe herein integrate vision system, robotics and automatic control to achieve its goal, it overcomes disadvantages of discrepancies between the different Euclidean setups and proposes control law in binocular-stand vision case. The experimental simulation shows that such image-based approach is effective in performing the precise alignment between the robot end-effector and the object.

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A Design of Heat-Sink and DMX512 Communication Control for High-Power LEDs (고출력 LED 방열 및 DMX512 통신 제어 설계)

  • Kim, Ki-Yun;Ham, Kwang-Keun
    • The Journal of Korean Institute of Communications and Information Sciences
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    • v.38C no.8
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    • pp.725-732
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    • 2013
  • Recently, various applications for LED lightings are growing continuously due to their better performances such as low power consumption, longer life time, operation speed, controllability, high quality color rendering, and sustainability. However, in developing the high-powered LEDs illumination system, heat-sink problem is one of the important obstacle. In this paper, a heat-sink design with multi-layered structure for high-powered LEDs is proposed, which is composed of metal core PCB, heat-pipes, heat-sink plates, and fans. And also, in this paper, a design for LED controls using DMX512 protocols through RS-485 communications is proposed, which is considered as de facto international standard in LEDs illumination control and is widely used in landscape lighting and stage lighting. In this paper, LED control and its application techniques are introduced and the method of wireless remote control for main controller is proposed.

Smoke Control According to the Ventilation Capacity in Subway Tunnel Fire: I. FDS Simulation (지하철 터널 화재시 환기시설의 용량에 따른 제연효과 I. FDS 시뮬레이션)

  • Park, Kyung-Jun;Lee, Ki-Jun;Hadi, Bettar El;Lee, Jai-Hyo;Shin, Dong-Il
    • Journal of the Korean Institute of Gas
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    • v.15 no.3
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    • pp.31-38
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    • 2011
  • In this study, we investigate simulation studies to confirm the removal of smoke through ventilation when the subway car is on fire and stopped in an underground subway tunnel, by using Fire Dynamics Simulator (FDS) which is being upgraded by NIST. The structure of subway tunnel and train for simulation modeling are based actual data from Seoul metropolitan subway. The main purpose of this study is to assure the removal efficiency of the ventilation when changing the ventilation capacity between 2.0 m/s and 3.0 m/s. The results of the study shows that carbon monoxide (CO) and carbon dioxide ($CO_2$) are reduced by about 35% as the ventilation capacity is increased by 0.5 m/s. This study also performs the grid sensitivity verification of FDS for improved accuracy of the results. To find the effective size of the grid, three cases are simulated and the results are compared.