• Title/Summary/Keyword: IC Method

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6-(1-Hydroxy or Acyloxyalkyl)-5,8-Dialkoxy-1,4-Naphthoquinones: Synthesis, Evaluation of Cytotoxic Activity; Antitumor Activity and Inhibitory effect on DNA Topoisomerase-I (6-(1-하이드록시 또는 아실옥시알킬)-5,8-디알콕시-1,4-나프토퀴논 유도체의 합성, DNA Topoisomerase-I에 대한 억제, 세포독성 및 항암활성)

  • Kim, Yong;Choi, Su-La;Myung, Pyung-Keun;Ahn, Byung-Zun
    • YAKHAK HOEJI
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    • v.44 no.2
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    • pp.141-148
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    • 2000
  • A new synthetic method of 6-(1-oxyalkyl)-5,8-dimethoxy-1,4-naphthoquinones was developed, 2-formyl-1,4,5,8-tetramethoxynaphthalene was oxidized to form 6-formyl-5,8-dimethoxy-1,4-naphthoquinone(DMNQ). This was selectively reduced and benzylated to produce 6-formyl-5,8-dimethoxy-1,4-dibenzyloxynaphthalene, to which various alkylmagnesium halide were added, followed by debenzylation and oxidation in sequence, yielding 6-(1-hydroxyalkyl)-DMNQ derivatives. 6-(1-hydroxyalkyl)-5,8-diethoxy-1,4-naphthalene (DENQ) derivatives were synthesized by similar procedure. 1'-OH of the naphthoquinone derivatives was acylated with various alkanoic acids to give 6-(1-acyloxyalkyl)-DMNQ or DENQ derivatives. TOPO-I inhibitory activity and cytotoxicity of DENQs were less potent than that of DMNQs. Among the DMNQ and DENQ analogues, the ones with alkyl group being heptyl were most potent in TOPO-I inhibition $IC_{50}$/; 30.1, 36.4 $\mu$M). DUNQ derivatives with a longer side chain exhibited a weaker cytotoxicity. A correlation between size of the alkyl side chain and cytotoxicity was not observed for DENQ derivatives. Acylation of 1'-hydroxyl group, in general, decreased both TOPO-I inhibitory activity and cytotoxicity T/C (%) values of the DENQ derivatives on S-180 intraperitoneal tumor were larger than those of DMNQ derivatives. Among the compounds synthesized,6-(1-hydroxyheptyl)-DENQ and 6-(1-hex-anoyloxyoctyl)-DMNQ showed the highest T/C values of 183% and 182%, respectively.

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IMPROVING METHOD FOR VERIFYING STEERING ANGLE SIGNAL OF EPS (차량용 EPS의 조향각 신뢰성 향상 제안)

  • Jang, Hyunseop;Kwon, Dowook;Han, Sangwhi
    • Annual Conference of KIPS
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    • 2012.11a
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    • pp.1507-1510
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    • 2012
  • 본 논문은 EPS(전자식 파워 스티어링)에 사용되는 Torque and Angle sensor 의 절대각 신뢰성 보증 방식에 관한 것으로, Inductive 방식의 센서에서 절대각 신호 신뢰성 보증에 대한 효과적인 방법을 제시한다. 전동식 파워 스티어링 시스템의 ECU(전자제어유닛)는 조타각도를 출력하는 2 개의 소자에서 버니어 알고리즘을 통해 360 도 이상의 멀티 조타각을 인식하게 된다. 토크&조향각 센서는 절대 조향각을 계산하는 1 개의 Hall IC 소자 신호와, 상대 조향각을 계산하는 ASIC 소자 신호를 사용하여 멀티 조타각을 인식한다. 인식된 조타각이 추가적인 검증 절차 없이 제어에 사용된다면, 센서의 이상 발생 시에 운전자의 조타감을 불편해질 수 있고, 나아가서는 차량사고의 위험을 발생시킬 수 있다.따라서 차량 거동 시 절대 조향각의 신뢰성 검증은 제어와 동시에 항상 요구되어야 한다. 특히, 유럽/미국 업계의 ISO 26262 표준 도입에 따라 절대 조향각의 높은 신뢰성이 요구된다. 본 논문에서는 이러한 요구사항을 만족하기 위해 측정된 절대각 신호를 기준으로 상대각 신호 2 개를 측정에 사용하고, Driving 시에도 절대각 기준의 신뢰도 향상을 위해 절대각 신호 1 개를 비교기로 사용한다. 최적화된 에러 기준을 근거로 절대 조향각 신호의 신뢰성을 보장하는 방법을 제안한다. 이러한 방법을 적용한다면, 정확하고 안정적으로 조타각을 결정함으로써 EPS 안전성 확보에 도움을 줄 수 있다.

A Case Study on the Intensive Semester Operation of Online-based Project Learning Using Python : Focusing on S Women's University (파이썬을 활용한 온라인 기반 프로젝트의 집중학기제 운영사례 : S 여대를 중심으로)

  • Kyun, Suna;Jang, Jiyoung
    • Journal of Engineering Education Research
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    • v.24 no.5
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    • pp.3-14
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    • 2021
  • This study deals with the case of online-based project learning, which was designed for the purpose of university educational innovation and enhancing learners' competencies required by society, operated during the COVID-19 pandemic. The course was applied Python programming language, team-based project learning, and intensive course system, which is required by our society and companies in the era of the 4th industrial revolution. Also it was operated as a non-face-to-face online class, which would have been operated in an offline class if it had not been for Covid 19 pandemic, to explore the possibilities and educational effects of online learning. To do this, 32 university students participated in online-based project learning during 8 weeks, and then conducted a survey. The survey results were analyzed in terms of i) non-face-to-face online learning, ii) team-based project learning, and iii) application of the intensive course system. Results say that most of the learners were satisfied with the online learning, team-based project learning, and the intensive semester system applied in this course at a high level, and also they clearly presented the reasons. Thereby, it has been confirmed that the learners were already well aware of the pros and cons of each learning method. Based on these results, the implications were discussed.

Whitening Activity of Abeliophyllum distichum Nakai Leaves According to the Ratio of Prethanol A in the Extracts

  • Jang, Tae-Won;Choi, Ji-Soo;Kim, Hoi-Ki;Lee, Eun-Ja;Han, Man-Wook;Lee, Ki-Beom;Kim, Do-Wan;Park, Jae-Ho
    • Korean Journal of Plant Resources
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    • v.31 no.6
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    • pp.667-674
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    • 2018
  • In this study, we evaluated the whitening activity of prethanol A and water extracts from Abeliophyllum distichum Nakai. The extracts were prepared using 0, 50, 70, and 100% prethanol A at $121^{\circ}C$, 1.2 atm for 15 minutes. To confirm effective extraction, the acteoside content of each extract was analyzed with the HPLC-PDA method. The antioxidant activity was evaluated using DPPH and ABTS scavenging activity assays, and the whitening activity was evaluated based on inhibitory activities on the protein and mRNA expression of tyrosinase, tyrosinase-related protein 1 (TRP-1), tyrosinase-related protein 2 (TRP-2), and microphthalmia-associated transcription factor (MITF) in B16 F10 cells. Each extract showed strong antioxidant and whitening activity. $IC_{50}$ values of antioxidant activity from each extract were in order of 100%, 70%, 50%, and 0%. In addition, whitening activity inhibited the protein and mRNA expression of melanin synthesis factor, following the same pattern as antioxidant activity. In conclusion, water and prethanol A extracts of A. distichum showed effective antioxidant and whitening activity and are thus considered to be valuable materials for whitening cosmetics. The results of this study will also provide basic data for the safe and efficient production of A. distichum as a cosmetic material.

Antiproliferative Effects of Free and Encapsulated Hypericum Perforatum L. Extract and Its Potential Interaction with Doxorubicin for Esophageal Squamous Cell Carcinoma

  • Amjadi, Issa;Mohajeri, Mohammad;Borisov, Andrei;Hosseini, Motahare-Sadat
    • Journal of Pharmacopuncture
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    • v.22 no.2
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    • pp.102-108
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    • 2019
  • Objectives: Esophageal squamous cell carcinoma (ESCC) is considered as a deadly medical condition that affects a growing number of people worldwide. Targeted therapy of ESCC has been suggested recently and required extensive research. With cyclin D1 as a therapeutic target, the present study aimed at evaluating the anticancer effects of doxorubicin (Dox) or Hypericum perforatum L. (HP) extract encapsulated in poly(lactic-co-glycolic acid) (PLGA) nanoparticles on the ESCC cell line KYSE30. Methods: Nanoparticles were prepared using double emulsion method. Cytotoxicity assay was carried out to measure the anti-proliferation activity of Dox-loaded (Dox NPs) and HP-loaded nanoparticles (HP NPs) against both cancer and normal cell lines. The mRNA gene expression of cyclin D1 was evaluated to validate the cytotoxicity studies at molecular level. Results: Free drugs and nanoparticles significantly inhibited KYSE30 cells by 55-73% and slightly affected normal cells up to 29%. The IC50 of Dox NPs and HP NPs was ~ 0.04-0.06 mg/mL and ~ 0.6-0.7 mg/mL, respectively. Significant decrease occurred in cyclin D1 expression by Dox NPs and HP NPs (P < 0.05). Exposure of KYSE-30 cells to combined treatments including both Dox and HP extract significantly increased the level of cyclin D1 expression as compared to those with individual treatments (P < 0.05). Conclusion: Dox NPs and HP NPs can successfully and specifically target ESCC cells through downregulation of cyclin D1. The simultaneous use of Dox and HP extract should be avoided for the treatment of ESCC.

Docetaxel-loaded PLGA nanoparticles to increase pharmacological sensitivity in MDA-MB-231 and MCF-7 breast cancer cells

  • Tran, Phuong;Nguyen, Thu Nhan;Lee, Yeseul;Tran, Phan Nhan;Park, Jeong-Sook
    • The Korean Journal of Physiology and Pharmacology
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    • v.25 no.5
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    • pp.479-488
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    • 2021
  • This study aimed to develop docetaxel (DTX) loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (DTX-NPs) and to evaluate the different pharmacological sensitivity of NPs to MCF-7 and MDA-MB-231 breast cancer cells. NPs containing DTX or coumarin-6 were prepared by the nanoprecipitation method using PLGA as a polymer and d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) as a surfactant. The physicochemical properties of NPs were characterized. In vitro anticancer effect and cellular uptake were evaluated in breast cancer cells. The particle size and zeta potential of the DTX-NPs were 160.5 ± 3.0 nm and -26.7 ± 0.46 mV, respectively. The encapsulation efficiency and drug loading were 81.3 ± 1.85% and 10.6 ± 0.24%, respectively. The in vitro release of DTX from the DTX-NPs was sustained at pH 7.4 containing 0.5% Tween 80. The viability of MDA-MB-231 and MCF-7 cells with DTX-NPs was 37.5 ± 0.5% and 30.3 ± 1.13%, respectively. The IC50 values of DTX-NPs were 3.92- and 6.75-fold lower than that of DTX for MDA-MB-231 cells and MCF-7 cells, respectively. The cellular uptake of coumarin-6-loaded PLGA-NPs in MCF-7 cells was significantly higher than that in MDA-MB-231 cells. The pharmacological sensitivity in breast cancer cells was higher on MCF-7 cells than on MDA-MB-231 cells. In conclusion, we successfully developed DTX-NPs that showed a great potential for the controlled release of DTX. DTX-NPs are an effective formulation for improving anticancer effect in breast cancer cells.

Study on the Change of Antioxidant Activity by Enzymatic Hydrolysis in Sophora japonica Linne, Houttuynia cordata Thunberg, Leonurus japonicus Houttuyn (괴화, 어성초, 익모초에서 효소 분해에 의한 항산화 활성 변화 연구)

  • Cha, Bae Cheon
    • Journal of Korean Medicine for Obesity Research
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    • v.21 no.1
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    • pp.1-9
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    • 2021
  • Objectives: The enzymatic hydrolysis is one of the processing methods that improve its effectiveness on medicinal herbs. In this research, changes in ingredients and activity by enzymatic hydrolysis were studied. Methods: For this study, a carbohydrate hydrolase such as viscozyme, which converts glycosides to aglycone, was applied to induce constituent changes in Sophora japonica Linne, Houttuynia cordata Thunberg and Leonurus japonicus Houttuyn. Changes in antioxidant activity were measured using the 1,1-diphenyl-2-picrylhydrazl (DPPH) method, and changes in ingredients were analyzed by high performance liquid chromatography. Results: As a result of enzymatic hydrolysis, the content of quercetin was increased from 1.26 mg/g to 29.66 mg/g in Sophora japonica Linne, from 0 mg/g to 0.66 mg/g in Houttuynia cordata Thunberg and from 0.43 mg/g to 0.71 mg/g in Leonurus japonicus Houttuyn. As a result of the antioxidant experimentation, the IC50 of Sophora japonica Linne decreased from 5 ug/ml (MeOH extract) and 9.1 ug/ml (EtOAc fraction) to 3.0 ug/ml, Houttuynia cordata Thunberg decreased from 15.6 ug/ml (MeOH extract) and 13.6 ug/ml (EtOAc fraction) to 11.2 ug/ml, and Leonurus japonicus Houttuyn decreased from 14.4 ug/ml (MeOH extract) and 12.6 ug/ml (EtOAc fraction) to 10.2 ug/ml. Conclusion: In conclusion, it was confirmed that glycoside rutin contained in the three medicinal herbs was changed to quercetin which is the aglycone, by the enzymatic hydrolysis using viscozyme. In terms of antioxidant activity, Sophora japonica Linne showed a significant antioxidant activity value that closes to the control group butylated hydroxyanisole. Houttuynia cordata Thunberg and Leonurus japonicus Houttuyn showed a minor increase in antioxidant activity.

The Effects of Chronic Ankle Instability on Postural Control during Forward Jump Landing (전방 점프 착지 시 만성 발목 불안정성이 자세 조절에 미치는 영향)

  • Kim, Kew-wan;Jeon, Kyoungkyu;Park, Seokwoo;Ahn, Seji
    • Korean Journal of Applied Biomechanics
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    • v.32 no.1
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    • pp.9-16
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    • 2022
  • Objective: The purpose of this study was to investigate how the chronic ankle instability affects postural control during forward jump landing. Method: 20 women with chronic ankle instability (age: 21.7 ± 1.6 yrs, height: 162.1 ± 3.7 cm, weight: 52.2 ± 5.8 kg) and 20 healthy adult women (age: 21.8 ± 1.6 yrs, height: 161.9 ± 4.4 cm, weight: 52.9 ± 7.2 kg) participated in this study. For the forward jump participants were instructed to stand on two legs at a distance of 40% of their body height from the center of force plate. Participants were jump forward over a 15 cm hurdle to the force plate and land on their non-dominant or affected leg. Kinetic and kinematic data were obtained using 8 motion capture cameras and 1 force plates and joint angle, vertical ground reaction force and center of pressure. All statistical analyses were using SPSS 25.0 program. The differences in variables between the two groups were compared through an independent sample t-test, and the significance level was to p < .05. Results: In the hip and knee joint angle, the CAI group showed a smaller flexion angle than the control group, and the knee joint valgus angle was significantly larger. In the case of ankle joint, the CAI group showed a large inversion angle at all events. In the kinetic variables, the vGRF was significantly greater in the CAI group than control group at IC and mGRF. In COP Y, the CAI group showed a lateral shifted center of pressure. Conclusion: Our results indicated that chronic ankle instability decreases the flexion angle of the hip and knee joint, increases the valgus angle of the knee joint, and increases the inversion angle of the ankle joint during landing. In addition, an increase in the maximum vertical ground reaction force and a lateral shifted center of pressure were observed. This suggests that chronic ankle instability increases the risk of non-contact knee injury as well as the risk of lateral ankle sprain during forward jump landing.

Inhibitory Activity of Advanced Glycation Endproducts (AGEs) Formation and Antioxidant Activity of Processed Korean Medicines (포제한약재의 최종당화산물 생성 억제 활성 및 항산화 효과)

  • Lee, AhReum;Kwon, OJun;Choi, JoonYoung;Roh, Seong-Soo
    • The Korea Journal of Herbology
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    • v.32 no.3
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    • pp.63-69
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    • 2017
  • Objectives : Advanced glycation end product (AGEs) is combine formation of glucose and protein. AGEs and reactive oxygen species are potential therapeutic targets for the various disease such as diabetic complications, renal injury, skin damage. The aim of this study was investigated the AGEs inhibitory activity and antioxidant activity of water extracts from 40 Korean medicines and 5 heating-processed Korean medicines. Methods: AGEs formation inhibitory activities of Korean medicines measured using bovine serum albumin (BSA), glucose, and fructose. Then, five effective Korean medicines were selected and heated with 30% ethanol. The AGEs inhibitory activities of heated Korean medicine were measured compared with not-heated Korean medicines. The antioxidant activities were evaluated through radical scavenging assays using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radicals. Furthermore, we examined total phenol and flavonoids contents. Results: Scutellariae Radix, Corni Fructus, Persimmon Fruit, Paeoniae Radix, Mori Folium respectively reduced AGEs production. Morever, heating-processed Scutellariae Radix has AGEs inhibitory activities better than not-processed Scutellariae Radix. Heating- processed Scutellariae Radix scavenged DPPH and ABTS effectively and $IC_{50}$ of DPPH and ABTS radical scavenging activity of Heat processed Scutellariae Radix were $15.47{\pm}0.26{\mu}g/m{\ell}$ and $12.07{\pm}1.23{\mu}g/m{\ell}$. It caused heat processing methods of Scutellariae Radix up regulated total phenol and flavonoids contents ($26.68{\pm}0.01$ to $46.15{\pm}0.10$, $20.30{\pm}0.38$ to $64.20{\pm}0.52$). Conclusion: It has AGEs inhibitory activities that 20 kind of medicinal plants of 40 medicinal plants. Especially, heat processed Scutellariae Radix has excellent AGEs inhibitory activities and antioxidant effect.

A Study on Improvement of Maritime Traffic Analysis Using Shape Format Data for Maritime Autonomous Surface Ships (자율운항선박 도입을 위한 수치해도 데이터 활용 해상교통분석 개선방안)

  • Hwang, Taewoong;Hwang, Taemin;Youn, Ik-Hyun
    • Journal of the Korean Society of Marine Environment & Safety
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    • v.28 no.6
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    • pp.992-1001
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    • 2022
  • The maritime traffic analysis has been conducted in various ways to solve problems arising from the complex marine environment. However, recent trends in the maritime industry, such as the development of the maritime autonomous surface ships (MASS), suggest that maritime traf ic analysis needs change. Accordingly, based on the studies conducted over the past decade for improvements, automatic identification system (AIS) data is mainly used for maritime traffic analysis. Moreover, the use of geographic information that directly af ects ship operation is relatively insufficient. Therefore, this study presented a method of using a combination of shape format data and AIS data to enhance maritime traffic analysis in preparation for the commercialization of autonomous ships. Consequently, extractable marine traffic characteristics were presented when shape format data were used for marine traffic analysis. This is expected to be used for marine traffic analysis for the introduction of autonomous ships in the future.