• Title/Summary/Keyword: Side-chain effect

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Enzymatic Characteristics of steroid $\Delta^1$-dehydrogenase from Arthrobacter simplex

  • Lee, Mi-Kyung;Bae, Moo
    • Journal of Microbiology and Biotechnology
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    • 제4권2호
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    • pp.119-125
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    • 1994
  • Steroid $\Delta^1$-dehydrogenase purified from hydrocortisone-induced cells of Arthrobacter simplex converted various 3-ketosteroids into their corresponding $\Delta^1$-dehydrogenated products. The transformation efficiencies depend upon the chemical structure of the steroids, especially length of the side chain at 17 position and hydroxyl groups at 11 and 17 positions. The Km values for androstenedione, the most favorable substrate examined, and hydrocortisone were 74 ${\mu}M$ and 294 ${\mu}M$, respectively. The optimum temperature and pH of the enzyme reaction were 35$^{\circ}C$ and pH 9, respectively, and the enzyme was relatively stable at the range from 20 to 35$^{\circ}C$ and from pH 5 to 10 after one hour of incubation. The enzyme activity was markedly inhibited in the presence of $Cu^{2+},\;Fe^{3+},\;Hg^{2+},\;Mo^{6+}$ ions, and somewhat inhibited by $Zn^{2+}$ and $Fe^{2+}$. $\alpha,\alpha'$-Dipyridyl that inhibits 9$\alpha$-hydroxylase and accumulates 1,4-androstadiene-3,17-dione from sterols revealed no inhibitory effect on this enzyme. EGTA showed inhibitory effect. $\beta$-Estradiol competitively inhibited the enzyme activity. Chemical modifications of the enzyme were attempted with several reagents. p-Hydroxymer-curibenzoate showed inhibition of the enzyme activity and protection of the substrate. This suggests that cysteine residue may be involved in the active site of the enzyme.

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Apicularen A, a Macrolide from Chondromyces sp., Inhibits Growth Factor Induced In Vitro Angiogenesis

  • Kwon, Ho-Jeong;Kim, Dong-Hoon;Shim, Joong-Sub;Ahn, Jong-Woong
    • Journal of Microbiology and Biotechnology
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    • 제12권4호
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    • pp.702-705
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    • 2002
  • Apicularen A (Api A) was recently isolated from Chondromyces sp. as a potent antitumor agent. Because of its unique chemical structure, a macrolide with a highly unsaturated amide side chain, and potent growth inhibitory effect in various cancer cell lines, Api A is currently in clinical trial for cancer therapy. In the present study, the effect of Api A on in vitro angiogenesis of bovine aortic endothelial cells (BAECS) was investigated. Api A potently inhibited the proliferation of BAECS in a dose-dependent manner. Treatment of the endothelial cells with up to 10 ng/ml of the compound did not show any cytotoxicity. In addition, it inhibited basic fibroblast growth factor (bFGF)-induced invasion and capillary tube formation of BAECS at concentrations of 2-5 ng/ml. These results, therefore, demonstrate that Apl A is a novel antiangiogenic agent and may suppress the growth of tumors, at least in part, by the inhibition of neovascularization.

프리틸트각의 발생과 전기광학 특성에 있어서의 배향층의 효과 (Effect of alignment layer on pretilt angle generation and EO performance)

  • 박태규;서대식
    • 한국전기전자재료학회:학술대회논문집
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    • 한국전기전자재료학회 1999년도 추계학술대회 논문집
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    • pp.537-540
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    • 1999
  • Effect of alignment layers on pretilt angle generation and electrical characteristics in nematic liquid crystal(NLC) by using photo-alignment techniques on polyimide (PI) surface with side chain were studied. The generated pretilt angle of the NLC on rubbed PI surface with 1-layer is almost the same as that of the 2-layers. However, the generated pretilt angle of the NLC on photo-induced PI surface with 2-layers is larger than that of the 1-layer. Therefore, the pretilt angle of the NLC on photo-induced PI surface is attributed to surface roughness due to photo-depolymerization of the polymer with UV light irradiation on PI surface. Next we observed the same characteristics of voltage-transmittance (V-T) and response time for 1- and 2-layers on PI surface. We also observed the same voltage holding ratio (VHR) characteristics for 1- and 2-layers on photo-aligned PI surface. Consequently, we suggest that the VHR of photo-aligned TN-LCD is higher than that of the rubbing-aligned TN-LCD.

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호텔의 건축적 속성이 운영 수익에 주는 영향에 관한 연구 - 서울지역 관광호텔을 중심으로 - (A Study on the Influence of Hotel's Architectural Attributes on Operating Revenue - Focused on Tourist Hotel in Seoul -)

  • 김현광;황희준
    • 대한건축학회논문집:계획계
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    • 제34권8호
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    • pp.43-50
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    • 2018
  • The purpose of this study is to analyze the effect of architectural attributes on operating revenue by concentrating on the facility side and to investigate how much individual architectural factors can affect operating revenue. The time range of this study is limited to 2015, and the spatial range is limited to a tourist hotel in Seoul that can be easily surveyed and verified. The analysis method is to confirm the significance and influence of each attribute through regression analysis. According to the results, The room part such as number of rooms or area showed a relatively low correlation with "revenue per available room (Rev.PAR)" than "average daily rate (ADR)", but showed a high correlation with non - architectural attributes such as auxiliary facilities and chain. This shows that factors that influence the operating profit of hotel are not the part of the room but the other factors such as the auxiliary facilities work more. In addition, the presence of spa and the number of auxiliary facilities in the hotel have a positive effect on the operating profit of the hotel due to the non - architectural attributes. This is expected to provide a new direction for future research in studying hotel facilities.

Cytotoxic Effects on HL-60 Cells of Myosin Light Chain Kinase Inhibitor ML-7 Alone and in Combination with Flavonoids

  • Lee, Joong-Won;Kim, Yang-Jee;Choi, Young-Joo;Woo, Hae-Dong;Kim, Gye-Eun;Ha, Tae-Kyung;Lee, Young-Hyun;Chung, Hai-Won
    • Toxicological Research
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    • 제25권4호
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    • pp.181-188
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    • 2009
  • Uncontrolled cell growth and increased cell proliferation are major features of cancer that are dependent on the stable structure and dynamics of the cytoskeleton. Since stable cytoskeleton structure and dynamics are partly regulated by myosin light chain kinase (MLCK), many current studies focused on MLCK inhibition as a chemotherapeutic target. As a potent and selective MLCK inhibitor, ML-7 [1-(5-iodonaphthalene-1-sulfonyl)-1 H-hexahydro-1,4-diazapine hydrochloride] is a promising candidate for an anticancer agent, which would induce apoptosis as well as prevents invasion and metastasis in certain types of cancer cells. This study assessed cytotoxic effects of ML-7 against HL-60 cells and therapeutic efficacy of ML-7 as a potential antileukemia agent. Trypan-blue exclusion assays showed dose- and time- dependent decreases in ML-7 treated HL-60 cells (p<0.05). Comet assays revealed a significant increase in DNA damage in HL-60 cells after treatment with $40{\mu}M$ ML-7 for 2h. Sub-G1 fractions, analyzed by flow cytometry increased in a dose-dependent manner, suggesting that ML-7 can induce apoptotic cell death in HL-60 cells. ML-7 was selectively cytotoxic towards HL-60 cells; not affecting normal human lymphocytes. That selective effect makes it a promising potential anti-leukemia agent. In addition, anticancer efficacy of ML-7 in combination with flavonoids (genistein or quercetin) or anticancer drugs (cisplatin or Ara-C) against HL-60 cells was assessed. Combination of ML-7 with flavonoids increased the anti-cancer effect of ML-7 to a greater extent than combination with the anticancer drugs. This implies that ML-7 in combination with flavonoids could increase the efficacy of anticancer treatment, while avoiding side effects cansed by conventional anticancer drug-containing combination chemotherapy.

Effect of lower extremity resistance exercise on gait performance in a patient with systemic lupus erythematosus with cerebral infarction and lower extremity vasculitis: a case study

  • Oh, Yongseop;Woo, Youngkeun
    • Physical Therapy Rehabilitation Science
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    • 제5권2호
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    • pp.106-112
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    • 2016
  • Objective: This study was conducted to investigate the effects of resistant exercise on the gait performance of a patient with systemic lupus erythematosus (SLE) patient. Design: A case study. Methods: A 30-year-old male adult who had been diagnosed with systemic lupus erythmatosus (SLE) in April 2013, right middle cerebral artery infarction, and with left hemiplegia agreed to participate in this case study. Patient was unable to walk due to being affected with adynamia. Due to developing necrotizing vasculitis on the left lower extremity, patient underwent a myotomy on the left thigh. The patient was trained with a progressive resistant exercise program for 8 weeks. An intensity of 15 RM was used for the resistant exercises and the resistance level was increased progressively in order to improve the muscle power of the patient. Methods used to increase resistance included changing positions, providing mechanical resistance instead of manual resistance, transitioning from open kinetic chain to closed kinetic chain exercises, and changing the colors of the theraband to those with increase level of resistance. Outcome measures included the 5-repetition sit-to- stand test (5RSST), Timed Up & Go (TUG), and 10-meter walk test (10MWT). In addition, the GAITRite was used to assess the spatio-temporal gait variables, including gait speed, cadence, stride length of the left side, and double limb support pre and post-intervention. Results: The patient was able to perform sit-to- stand after two weeks of performing the resistant exercises. The patient was able to walk after 4 weeks, and the patient's overall gait performance had improved after 8 weeks. All of the variables had improved after each week. Conclusions: The results of this case study may be used to enhance future efforts to objectively evaluate resistant exercises during gait performance in persons affected by SLE.

방향족 액정동족체 및 Epoxy형 측쇄 액정고분자의 합성 및 성질 I. 저분자 액정 동족체 (Synthesis and Properties of Liquid Crystal Compounds and Epoxy Resin Based Side Chain Liquid Crystal Polymers I. Low Molecular Weight Liquid Crystal Compounds)

  • 박세광;안원술;금창대;박이순
    • 공업화학
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    • 제9권1호
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    • pp.66-70
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    • 1998
  • 정보전자 기기의 디스플레이용 재료로 사용되는 액정/고분자 복합재료의 매트릭스로 사용하기 위한 새로운 선형 및 가교형 측쇄 액정고분자를 제조하기 위하여 필요한 저분자 액정 중간체들을 합성하고 이들의 액정 특성을 살펴보았다. Alkyl spacer의 길이가 다르고 연결기로서 azo기를 그리고 말단기로서 cyano를 공통적으로 가지고 다른 한 말단기로서 bromoalkyl(AZO(n)), azidoalkyl(AZI(n)) 및 amonoalkyl(ALC(n))기를 가지는 저분자 액정 들의 합성을 하였으며 IR, NMR 및 원소분석을 통하여 이를 확인할 수 있었다. 또한 DSC thermogram 및 편광현미경 관찰로부터 이들 저분자 액정들은 모두 일정한 온도 영역에서 네마틱 상의 액정성을 발현하는 것을 알았다. 또한, 저분자 액정 분자들이 spacer 길이, 즉 $-(CH_2)n-$의 n이 짝수 및 홀수로 변화함에 따라 분자 내의 conformation 변화에 따른 $T_{KN}$$T_{NI}$의 값이 전형적인 even-odd 변화 현상을 나타내었다.

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Investigation of the effect of Erythrosine B on a β-amyloid (1-40) peptide using molecular modeling method

  • Lee, Juho;Kwon, Inchan;Cho, Art E.;Jang, Seung Soon
    • EDISON SW 활용 경진대회 논문집
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    • 제4회(2015년)
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    • pp.14-23
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    • 2015
  • Alzheimer's disease is one of the most common types of degenerative dementia. As a considerable cause of Alzheimer's disease, neurotoxic plaques composed of 39 to 42 residue-long amyloid beta($A{\beta}$) fibrils have been found in the patient's brain in large quantity. A previous study found that erythrosine B (ER), a red color food dye approved by FDA, inhibits the formation of amyloid beta fibril structures. Here, in an attempt to elucidate the inhibition mechanism, we performed molecular dynamics simulations to demonstrate the conformational change of $A{\beta}40$ induced by 2 ERs in atomistic detail. During the simulation, the ERs bound to the surfaces of both N-terminus and C-terminus regions of $A{\beta}40$ rapidly. The observed stacking of the ERs and the aromatic side chains near the N-terminus region suggests a possible inhibition mechanism in which disturbing the inter-chain stacking of PHEs destabilizes beta-sheet enriched in amyloid beta fibrils. The bound ERs block water molecules and thereby help stabilizing alpha helical structure at the main chain of C-terminus and interrupt the formation of the salt-bridge ASP23-LYS28 at the same time. Our findings can help better understanding of the current and upcoming treatment studies for Alzheimer's disease by suggesting inhibition mechanism of ER on the conformational transition of $A{\beta}40$ at the molecular level.

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Comparison of Saccharina japonica-Undaria pinnatifida Mixture and Minoxidil on Hair Growth Promoting Effect in Mice

  • Park, Ki Soo;Park, Dae Hwan
    • Archives of Plastic Surgery
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    • 제43권6호
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    • pp.498-505
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    • 2016
  • Background Algae have traditionally been used for promotion of hair growth. Use of hair regrowth drugs, such as minoxidil, is limited due to side effects. The aim of this study was to examine a mixture of Saccharina japonica and Undaria pinnatifida (L-U mixture) on hair growth and to compare the promoting effect of hair growth by a 3% minoxidil and a L-U mixture. Methods To evaluate the hair growth-promoting activity, saline, 50% ethanol, 3% minoxidil, and the L-U mixture were applied 2 times a day for a total of 14 days on the dorsal skin of C57BL/6 mice after depilation. Analysis was determined by using a high-resolution hair analysis system, real-time polymerase chain reaction, and H&E staining. Results On day 14, the hair growth effect of the L-U mixture was the same as that of the 3% minoxidil treatment. The L-U mixture significantly (P<0.05) stimulated hair growth-promoting genes, as vascular endothelial growth factor (VEGF) and insulin-like growth factor -1. Increase of VEGF was observed in the L-U mixture group compared with minoxidil and the negative control. In contrast, the L-U mixture suppressed the expression of transforming growth factor-${\beta}1$, which is the hair loss-related gene. In histological examination in the L-U mixture and minoxidil groups, the induction of an anagen stage of hair follicles was faster than that of control groups. Conclusions This study provides evidence that the L-U mixture can promote hair growth in mice, similar to the effect from minoxidil, and suggests that there is potential application for hair loss treatments.

Inhibitor Design for Human Heat Shock Protein 70 ATPase Domain by Pharmacophore-based in silico Screening

  • Lee, Jee-Young;Jung, Ki-Woong;Kim, Yang-Mee
    • Bulletin of the Korean Chemical Society
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    • 제29권9호
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    • pp.1717-1722
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    • 2008
  • The 70 kDa heat-shock protein (Hsp70) involved in various cellular functions, such as protein folding, translocation and degradation, regulates apoptosis in cancer cells. Recently, it has been reported that the green tea flavonoid (−)-epigallocatechin 3-gallate (EGCG) induces apoptosis in numerous cancer cell lines and could inhibit the anti-apoptotic effect of human Hsp70 ATPase domain (hATPase). In the present study, docking model between EGCG and hATPase was determined using automated docking study. Epi-gallo moiety in EGCG participated in hydrogen bonds with side chain of K71 and T204, and has metal chelating interaction with hATPase. Hydroxyl group of catechin moiety also participated in metal chelating hydrogen bond. Gallate moiety had two hydrogen bondings with side chains of E268 and K271, and hydrophobic interaction with Y15. Based on this docking model, we determined two pharmacophore maps consisted of six or seven features, including three or four hydrogen bonding acceptors, two hydrogen bonding donors, and one lipophilic. We searched a flavonoid database including 23 naturally occurring flavonoids and 10 polyphenolic flavonoids with two maps, and myricetin and GC were hit by map I. Three hydroxyl groups of B-ring in myricetin and gallo moiety of GC formed important hydrogen bonds with hATPase. 7-OH of A-ring in myricetin and OH group of catechin moiety in GC are hydrogen bond donors similar to gallate moiety in EGCG. From these results, it can be proposed that myricetin and GC can be potent inhibitors of hATPase. This study will be helpful to understand the mechanism of inhibition of hATPase by EGCG and give insights to develop potent inhibitors of hATPase.