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Synthesis, Characterization and in vitro Anti-Tumoral Evaluation of Erlotinib-PCEC Nanoparticles

  • Barghi, Leila;Asgari, Davoud;Barar, Jaleh;Nakhlband, Aylar;Valizadeh, Hadi
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.23
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    • pp.10281-10287
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    • 2015
  • Background: Development of a nanosized polymeric delivery system for erlotinib was the main objective of this research. Materials and Methods: Poly caprolactone-polyethylene glycol-polycaprolactone (PCEC) copolymers with different compositions were synthesized via ring opening polymerization. Formation of triblock copolymers was confirmed by HNMR as well as FT-IR. Erlotinib loaded nanoparticles were prepared by means of synthesized copolymers with solvent displacement method. Results: Physicochemical properties of obtained polymeric nanoparticles were dependent on composition of used copolymers. Size of particles was decreased with decreasing the PCL/PEG molar ratio in used copolymers. Encapsulation efficiency of prepared formulations was declined by decreasing their particle size. Drug release behavior from the prepared nanoparticles exhibited a sustained pattern without a burst release. From the release profiles, it can be found that erlotinib release rate from polymeric nanoparticles is decreased by increase of CL/PEG molar ratio of prepared block copolymers. Based on MTT assay results, cell growth inhibition of erlotinib has a dose and time dependent pattern. After 72 hours of exposure, the 50% inhibitory concentration (IC50) of erlotinib hydrochloride was appeared to be $14.8{\mu}M$. Conclusions: From the obtained results, it can be concluded that the prepared PCEC nanoparticles in this study might have the potential to be considered as delivery system for erlotinib.

Direct Block of Cloned $K^+$ Channels, Kv1.5 and Kv1.3, by Cyclosporin A, Independent of Calcineurin Inhibition

  • Choi, Bok-Hee;Hahn, Sang-June
    • The Korean Journal of Physiology and Pharmacology
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    • v.9 no.6
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    • pp.353-361
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    • 2005
  • The interaction of cyclosporine A (CsA), an immunosuppressant, with rat brain Kv1.5 (Kv1.5) channels, which were stably expressed in Chinese hamster ovary cells, was investigated using the whole-cell patch-clamp technique. CsA reversibly blocked Kv1.5 currents at +50 mV in a reversible concentrationdependent manner with an apparent $IC_{50}$ of 1.0μM. Other calcineurin inhibitors (cypermethrin, autoinhibitory peptide) had no effect on Kv1.5 and did not prevent the inhibitory effect of CsA. Fast application of CsA led to a rapid and reversible block of Kv1.5, and the onset time constants of the CsA-induced block were decreased in a concentration-dependent manner. The CsA-induced block of Kv1.5 channels was voltage-dependent, with a steep increase over the voltage range of channel opening. However, the block exhibited voltage independence over the voltage range in which channels were fully activated. The rate constants for association and dissociation of CsA were $7.0{\mu}M{-1}s^{-1}$ and $8.1s^{-1}$, respectively. CsA slowed the deactivation time course, resulting in a tail crossover phenomenon. Block of Kv1.5 by CsA was use-dependent. CsA also blocked Kv1.3 currents at +50 mV in a reversible concentration-dependent manner with an apparent $IC_{50}$ of $1.1{\mu}M$. The same effects of CsA on Kv1.3 were also observed in excised inside-out patches when applied to the internal surface of the membrane. The present results suggest that CsA acts directly on Kv1.5 currents as an open-channel blocker, independently of the effects of CsA on calcineurin activity.

Blockade of Kv1.5 channels by the antidepressant drug sertraline

  • Lee, Hyang Mi;Hahn, Sang June;Choi, Bok Hee
    • The Korean Journal of Physiology and Pharmacology
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    • v.20 no.2
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    • pp.193-200
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    • 2016
  • Sertraline, a selective serotonin reuptake inhibitor (SSRI), has been reported to lead to cardiac toxicity even at therapeutic doses including sudden cardiac death and ventricular arrhythmia. And in a SSRI-independent manner, sertraline has been known to inhibit various voltage-dependent channels, which play an important role in regulation of cardiovascular system. In the present study, we investigated the action of sertraline on Kv1.5, which is one of cardiac ion channels. The effect of sertraline on the cloned neuronal rat Kv1.5 channels stably expressed in Chinese hamster ovary cells was investigated using the whole-cell patch-clamp technique. Sertraline reduced Kv1.5 whole-cell currents in a reversible concentration-dependent manner, with an $IC_{50}$ value and a Hill coefficient of $0.71{\mu}M$ and 1.29, respectively. Sertraline accelerated the decay rate of inactivation of Kv1.5 currents without modifying the kinetics of current activation. The inhibition increased steeply between -20 and 0 mV, which corresponded with the voltage range for channel opening. In the voltage range positive to +10 mV, inhibition displayed a weak voltage dependence, consistent with an electrical distance ${\delta}$ of 0.16. Sertraline slowed the deactivation time course, resulting in a tail crossover phenomenon when the tail currents, recorded in the presence and absence of sertraline, were superimposed. Inhibition of Kv1.5 by sertraline was use-dependent. The present results suggest that sertraline acts on Kv1.5 currents as an open-channel blocker.

Anti-oxidative Capacity Analysis of Water-Soluble Substances According to Varieties and Maturity Stages in Mulberry Leaves and Fruits (뽕나무 품종별.시기별 뽕잎과 오디의 항산화능 분석)

  • Kim Hyun-Bok
    • Journal of Sericultural and Entomological Science
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    • v.47 no.2
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    • pp.62-67
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    • 2005
  • Much attention has been focused on the activity of the natural antioxidants present in fruits and vegetables, because potentially these components may reduce the level of oxidative stress. Especially, mulberry leaves containing many natural components are considerable resource far natural antioxidants. The antioxidant capacity of mulberry leaves was investigated with minilum L-100 device and ARAW-KIT (anti-radical ability of water-soluble substance), in comparison to the ascorbic acid. The appropriate conditions for pre-treatments of mulberry leaves were 80% MeOH, 30 sec. vortex mixing. The antioxidant capacity of 16 varieties was 3303.4 nmol (ascorbic acid equivalents) at opening stage of five leaves in spring. The highest stage of antioxidant capacity (3708.0 nmol) and yield rate was just before the coloration stare with anthocyanin in fruits, whereas the lowest stage was middle of June (2231.6 nmol) and about two months growing stage after summer pruning (2064.6 nmol). But after summer pruning, the antioxidant capacity of mulberry.

The characteristics of types and annual trends of pop-up fashion stores - Focused on domestic cases - (패션 팝업 스토어의 연도별 변화 추이 및 유형 특성 - 국내 사례를 중심으로 -)

  • Yu, Jihun;Choi, Doree
    • The Research Journal of the Costume Culture
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    • v.23 no.5
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    • pp.822-834
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    • 2015
  • Contemporary fashion companies have been planning marketing strategies that can promote brands and products more effectively for satisfying consumers' increasingly diversified needs. For this reason, retail spaces have continued to evolve and the modern concept of pop-up stores appeared through this process. Therefore, the object of this study was to research domestic pop-up fashion store cases by collecting article data. These data are from Internet fashion-specialty sites and analyze the types and characteristics of pop-up fashion stores by providing basic information that will be useful in the pop-up fashion stores of companies when they establish their marketing strategies. This study utilized the content analysis method and derived the results by using SPSS Statistics. As a result of this study, the type of "pop-up fashion stores opening in distribution enterprises" comprised the highest percentage of the whole store types and the pop-up fashion stores' management purposes were focused on product introduction, promotion, and market testing. As time passed, not only did pop-up fashion stores' growth rate increased, but also the types of pop-up fashion stores have become more diverse. In other words, contemporary fashion companies are utilizing more pop-up fashion stores as a marketing strategy than before. However, due to the short history of domestic pop-up fashion stores, the variety of research is still insufficient, so more extensive research on pop-up fashion stores is required.

A Study on the Flow Characteristics of Groundwater and Grout in Jointed Rock (절리암반내 지하수 및 주입재의 유동특성에 관한 연구)

  • 문현구;송명규
    • Journal of the Korean Geotechnical Society
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    • v.15 no.5
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    • pp.229-240
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    • 1999
  • The groundwater flow and grout flow in individual rock joint and jointed rock mass are studied using various methods of analysis such as (i) the finite difference method, (ii) channel network analysis and (iii) joint network analysis. The flow behaviour is investigated in two distinguishable scales of observation: one for a rough joint of a laboratory scale having variable aperture, and the other for field- scale rock masses having three sets of intermittent joints. In the former case, the aperture-dependent channel flow is identified for both water and grout flows. The comparison of the flow rate in a rough joint is made between the finite difference analysis and existing analytical solution. In the latter case, the effects of increasing number of joints on the groundwater inflow into a circular opening of various diameters are analyzed using both the joint network method and Goodman's analytic solution. Comparisons are made between the two methods. The boundary effects in the joint network method are discussed. The inhomogeneity of joint network and its impacts on the groundwater inflow are also discussed.

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A Study on Fatigue Crack Propagation Behavior with Pure-Ti Plate (순수 티타늄 판재의 피로균열 전파거동에 관한 연구)

  • 오세욱;김태형;김득진;임만배
    • Journal of Ocean Engineering and Technology
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    • v.9 no.1
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    • pp.92-100
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    • 1995
  • The effect of different anisotropy and stress ratio on fatigue crack propagation behavior was investigated under various stress ratio(R=-0.4, -0.2, 0.2, 0.2, 0.4) using pure titanium sheet used in aerospace, chemical and food industry. The rack closure behavior under constant load amplitude fatigue crack propagation test was examined. Fatigue crack propagation rate da/dN was estimated in terms of effective stress intensity factor range, $\Delta$K$_{eff}$, regardless of various stress ratio but was influenced by anisotropy. Also, it was found that the effect of anisotropy was considerably decreased but still not negligible when he da/dN was evaluated by a conventional parameter, $\Delta$$K_{eff}$/E and when the modified da/dN.$\sqrt{\varepsilon}_f$ was evaluated by $\Delta$$K_{eff}$/E. On the other hand, da/dN could be evaluated uniquely by effective new parameter, $\Delta$K$_{eff}$/$sigma_{ys}$, regardless of anisotropy, as int he following equation da/dN=C''[\frac{{\Delta}K_{eff}}{{\sigma}_{ys}}]^{n''}. And effective stress intensity factor range ratio, U was estimated by the following equation with respect to the ratio of reversed plastic zone size, $\Delta r_{p}$ to monotonic plastic zone size, $r_p$ regardless of stress ratio and anisotropy. U=-4.45$(\Delta r_{p}/r_{p})^{2}$+4.1$(\Delta r_{p}/r_{p})$+0.245_{p})$+0.245

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Smoke Control in a Subway Station Platform with Screen Doors - Based on Busan Subway Line 3 - (스크린도어 설치에 따른 지하승강장 제연의 문제점과 대책 - 부산 지하철 3호선을 중심으로 -)

  • Park, Woe-Chul
    • Fire Science and Engineering
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    • v.20 no.1 s.61
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    • pp.50-54
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    • 2006
  • A fire in a subway station platform, completely isolated by screen doors, was numerically simulated to investigate problems in smoke control and find their countermeasures. A part of the platform, $40m{\times}5m$ floor and 3 m high, and a fire of 1 MW were considered, and the smoke extraction system was assumed to start operation at the onset of the fire. For three different values of the exhaust air flow rate, 0.1, 2, and $4m^3/min-m^2$, the distributions of temperature, concentrations of soot and carbon monoxide, and those of visibility were compared. The time-variations of the number of randomly distributed particles in the space were also investigated for the air flow rates to see the efficiency in smoke control. It was shown that smoke control takes time by lack of air supply. It was also confirmed that air supply from the railway to the platform at emergency is needed so that smoke is able to be controlled efficiently, and that opening the doors at the both ends of the platform is desirable until the fire is completely extinguished.

Research on the phenomenon of sick house syndrome and how to remove harmful gases (새집증후군 현상 및 유해가스 제거방안 연구)

  • Choe, Yoowha
    • The Journal of the Convergence on Culture Technology
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    • v.6 no.3
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    • pp.449-456
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    • 2020
  • When you move to a new home, or when you change the wallpaper or flooring of your home, office, etc., you can enjoy the joy of opening your new home with the sick house syndrome, such as the stinging smell and stinging eyes that may appear after the interior work. It is only a moment. Volatile organic compounds from building materials, adhesives, wallpaper, and paints used in new buildings or new furniture cause residents' health and discomfort in indoor life. These volatile organic compounds include benzene, toluene, acetone, and styrene, as well as the representative formaldehyde, and these substances are slowly released over a long period of time, causing acute or chronic diseases to residents. As a method for removing organic volatile substances, physical methods using adsorption, chemical methods for converting volatile substances to other substances, or a mixture of the two are mainly used. In this paper, a sustained release chlorine dioxide gel pack obtained by a method for controlling the reaction rate of a reactant and the release of a product is mixed with a zeolite adsorbent having an optimized hole diameter to adsorb and decompose and remove formaldehyde suspended in the air. I would suggest an effective method.

Effect of AgNO3 Pretreatment on Reducing SO2 Injury in Forsythia koreana Nakai (AgNO3 처리(處理)가 개나리의 SO2 가스 피해(被害) 경감(輕減)에 미치는 영향(影響))

  • Ku, Ja Hyeong
    • Korean Journal of Agricultural Science
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    • v.9 no.2
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    • pp.453-460
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    • 1982
  • In order to investigate the effect of $AgNO_3$ pretreatment on reducing $SO_2$ injury in leaves of Forsythia koreana, changes of pH, chlorophyll content, peroxidase activity, sulfur content, and stomatal behaviour in leaves were examined. 1. $AgNO_3$ sprayed at 200 ppm or above increased black spot development in lower epidermis of leaves. But pretreatment with 100 ppm $AgNO_3$ significantly reduced de foliation and visible injury rate of leaves exposed to $SO_2$. 2. $AgNO_3$ pretreatment prevented lowering pH and decreasing chlorophyll content induced by $SO_2$ injury in leaves. But both $AgNO_3$ pretreatment and $SO_2$ exposure increased peroxidase activity in leaves. 3. $AgNO_3$ pretreatment did not affect reducing $SO_2$ absorption and stomatal opening in leaves exposed to $SO_2$.

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