• 제목/요약/키워드: mimetic

검색결과 178건 처리시간 0.02초

The Inhibitory Effect of Apigenin on the Agonist-Induced Regulation of Vascular Contractility via Calcium Desensitization-Related Pathways

  • Je, Hyun Dong;Kim, Hyeong-Dong;La, Hyen-Oh
    • Biomolecules & Therapeutics
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    • 제22권2호
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    • pp.100-105
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    • 2014
  • Apigenin, a natural flavonoid found in a variety of vegetables and fruits, has been shown to possess many biological functions. The present study was undertaken to investigate the influence of apigenin on vascular smooth muscle contractility and to determine the mechanism involved. Denuded aortic rings from male rats were used and isometric contractions were recorded and combined with molecular experiments. Apigenin significantly relaxed fluoride-, thromboxane $A_2$ mimetic- or phorbol ester-induced vascular contraction, which suggests that apigenin could be an anti-hypertensive that reduces agonist-induced vascular contraction regardless of endothelial nitric oxide synthesis. Furthermore, apigenin significantly inhibited fluoride-induced increases in pMYPT1 levels and phorbol ester-induced increases in pERK1/2 levels, which suggests the mechanism involving the inhibition of Rho-kinase and MEK activity and the subsequent phosphorylation of MYPT1 and ERK1/2. This study provides evidence regarding the mechanism underlying the relaxation effect of apigenin on agonist-induced vascular contraction regardless of endothelial function.

Sequence to Structure Approach of Estrogen Receptor Alpha and Ligand Interactions

  • Chamkasem, Aekkapot;Toniti, Waraphan
    • Asian Pacific Journal of Cancer Prevention
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    • 제16권6호
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    • pp.2161-2166
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    • 2015
  • Estrogen receptors (ERs) are steroid receptors located in the cytoplasm and on the nuclear membrane. The sequence similarities of human $ER{\alpha}$, mouse $ER{\alpha}$, rat $ER{\alpha}$, dog $ER{\alpha}$, and cat $ER{\alpha}$ are above 90%, but structures of $ER{\alpha}$ may different among species. Estrogen can be agonist and antagonist depending on its target organs. This hormone play roles in several diseases including breast cancer. There are variety of the relative binding affinity (RBA) of ER and estrogen species in comparison to $17{\beta}-estradiol$ (E2), which is a natural ligand of both $ER{\alpha}$ and $ER{\beta}$. The RBA of the estrogen species are as following: diethyl stilbestrol (DES) > hexestrol > dienestrol > $17{\beta}-estradiol$ (E2) > 17- estradiol > moxestrol > estriol (E3) >4-OH estradiol > estrone-3-sulfate. Estrogen mimetic drugs, selective estrogen receptor modulators (SERMs), have been used as hormonal therapy for ER positive breast cancer and postmenopausal osteoporosis. In the postgenomic era, in silico models have become effective tools for modern drug discovery. These provide three dimensional structures of many transmembrane receptors and enzymes, which are important targets of de novo drug development. The estimated inhibition constants (Ki) from computational model have been used as a screening procedure before in vitro and in vivo studies.

리포솜 지질막의 성질에 미치는 지질 조성의 영향 (Effects of Lipid Composition on the Properties of Phospholipid Liposomal Membranes)

  • 김민;한석규;김종국
    • 약학회지
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    • 제38권2호
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    • pp.131-139
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    • 1994
  • Calcein-encapsulated small unilamellar vesicles of various lipid composition were prepared using the sonication technique, and their stabilities at $20^{\circ}C$ were examined by measuring calcein leakage from the liposomes. The fluidity of these liposomal bilayers was also investigated by measuring the fluorescence polarization of DPH labelled into the liposomes. The results showed that liposomes made of PC mixtures with different acyl chain length were very stable, which may be due to the formation of interdigitated bilayer structure. The addition of cholesterol further stabilized these PC liposomes. However, addition of cholesterol reduced the encapsulation efficiences of liposomes. The fluidity of the liposomes was significantly decreased by cholesterol in the liquid crystalline state, but not changed in the gel state. These results suggest that the enhanced stability of PC mixture liposomes may be ascribed to the formation of stable interdigitated bilayer structure. In membrane-mimetic and drug-delivery studies, vesicles made of mixtures of various phospholipids are recommended instead of addition of cholesterol to the phospholipid.

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온라인 게임의 치팅 프로그램에 나타난 플레이어의 욕망 - 슈팅 장르를 중심으로 (A Study on Players' Desire in Cheating Programs of Online Game - Focused on Shooter Games)

  • 안진경
    • 한국게임학회 논문지
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    • 제20권4호
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    • pp.89-100
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    • 2020
  • 본 연구는 온라인 게임의 치팅 프로그램에 나타난 플레이어의 욕망을 르네 지라르의 모방 욕망 이론을 통해 규명하는 데 목적을 둔다. 치팅 프로그램은 게임에 참여하는 플레이어들이 갖춰야 할 유희적 태도를 부정하며 게임의 매직 서클을 교란한다. 분석 결과, 치팅 플레이어들의 욕망은 게임의 규칙이 상정한 가상의 '모델 플레이어'를 통해 매개된다. 둘은 내적 매개의 관계를 이루기에, 치팅 플레이어가 이상적 플레이를 모방하는 과정은 끊임없는 대립과 갈등을 야기한다. 기술의 도움을 통해 향상된 플레이어로서의 자신을 꿈꾸지만 게임이 지닌 실패의 미학을 무너뜨린다는 점에서 치팅 플레이어들의 욕망은 트랜스휴먼을 향한 그릇된 욕망으로 정의된다.

2000년대 패션에 표현된 미메시스 연구 (A Study of the Aesthetics of Mimesis in 2000s Fashion)

  • 양수미;권미정
    • 복식
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    • 제59권10호
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    • pp.38-50
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    • 2009
  • Since Homeros in Greece, Mimesis was thought to be an art to imitate the nature, and it means an imitation of the nature classically. Mimetic theories were set to be a kind of art work in the era of Renaissance, and the terminology of mimesis was widely used to replace it with an originality in the 15th century. The purpose of this study is to understand the aesthetics of mimesis expressed in 2000s fashion. For this purpose, I investigated the theories of the mimesis, categorized the definition, then applied those categories for 2000s fashion. Documentary studies were conducted through aesthetics, fashion books and demonstrative studies were processed by analyzing photos from collection fashion magazines and fashion site of internet. In the history of aesthetics, the mimesis could be defined into three categories; the similarity and the representation mimesis, the symbol mimesis and the abstraction mimesis. In fashion, the representation mimesis included a natural and a folk, a period that of 1900s and ancient representation mimesis. The symbol mimesis included psychology and fear symbol mimesis. The abstraction mimesis included hard color, a geometric simplification and distortion mimesis. Analysis on the mimesis expressed in 2000s modern fashion may provide an excellent method for understanding human aesthetic in costume.

SMA를 이용한 캡슐 내시경의 이동메커니즘 설계 및 제작 (Design and fabrication of the Locomotive Mechanism for Capsule Endoscopes Using Shape Memory Alloys (SMA))

  • 이승학;김병규;박종현;박종오
    • 대한기계학회논문집A
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    • 제27권11호
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    • pp.1849-1855
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    • 2003
  • Newly commercialized wireless capsule endoscope has many advantages compared to conventional push-type endoscopes. However, it is moved by the peristaltic waves. Therefore, it can not diagnose desired zones actively. In this paper, a locomotive mechanism for wireless capsule endoscope is proposed to increase the efficiency of endoscopy. We designed and fabricated a prototype using SMA springs and bio-mimetic clamping device. The hollow space in the prototype is allocated for further system integration of a camera module, a RF module and a battery. And the sequential control scheme is employed to improve the efficiency of its locomotion. To validate the performance of the locomotive mechanism, experiments on a silicone rubber pad and in vitro tests are carried out. The results of the experiments indicate that proposed mechanism is effective in harsh environments such as digestive organs of a human.

Dieckol Suppresses CoCl2-induced Angiogenesis in Endothelial Cells

  • Jung, Seung Hyun;Jang, In Seung;Jeon, You-Jin;Kim, Young-Mog;Park, Sun Joo
    • Fisheries and Aquatic Sciences
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    • 제17권3호
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    • pp.305-311
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    • 2014
  • Dieckol is a polyphenol compound isolated from brown algae that has anti-oxidant, anti-inflammatory, and anti-tumor activity. We examined the anti-angiogenic effects of dieckol in endothelial cells under hypoxic conditions. Treatment with $CoCl_2$, a hypoxic mimetic agent, increased proliferation, adhesion, migration, and tube formation in HUVECs, as well as vessel sprouting in rat aortic rings, which correlated well with increased expression of hypoxia-inducible factor 1-alpha ($HIF1{\alpha}$) and ${\beta}1$-integrin. Dieckol suppressed $CoCl_2$-induced adhesion, migration, and tube formation in HUVECs and vessel sprouting in rat aortic rings. Dieckol treatment decreased $CoCl_2$-induced overexpression of $HIF1{\alpha}$ and its downstream signaling molecules, including ${\beta}1$-integrin/Fak, Akt/eNOS, and p38 MAPK. These results suggest that dieckol is a novel angiogenesis inhibitor and a potential treatment for angiogenesis-dependent diseases in humans, such as malignant tumors.

Effects of Synthetic Pseudoceramides on Sphingosine Kinase Activity in F9-12 Cells

  • Jin, You-Xun;Shin, Kyong-Oh;Park, Myung-Yong;Lee, Shin-Hee;Park, Byeong-Deog;Oh, Sei-Kwan;Yoo, Hwan-Soo;Lee, Yong-Moon
    • Biomolecules & Therapeutics
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    • 제19권1호
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    • pp.134-139
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    • 2011
  • Sphingosine kinase (SPHK) has a central role to control cell death and cell proliferation, which is suggested as a sphingolipid rheostat by regulating the levels between ceramide and sphingosine 1-phosphate (S1P). Therefore, physiological regulators of SPHK will be a good candidate to develop a new targeted drug. For this purpose, a series of synthetic pseudoceramides were tested by SPHK assay either cell-based or cell-free system. K10PC-5 strongly inhibited SPHK, while K6PC-5 activated SPHK in cell-free system. Specifically, K6PC-5 activated SPHK under the co-treatment with $50\;{\mu}M$ dimethylsphingosine (DMS), a SPHK inhibitor. Collectively, we developed a simple SPHK assay system to find SPHK regulatory pseudoceramide compounds, K10PC-5 and K6PC-5 which may be useful to cancer treatment or immune regulation like FTY720, a synthetic sphingolipid mimetic compound.

Structure-Function of the TNF Receptor-like Cysteine-rich Domain of Osteoprotegerin

  • Shin, Joon;Kim, Young-Mee;Li, Song-Zhe;Lim, Sung-Kil;Lee, Weontae
    • Molecules and Cells
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    • 제25권3호
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    • pp.352-357
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    • 2008
  • Osteoprotegerin (OPG) is a soluble decoy receptor that inhibits osteoclastogenesis and is closely associated with bone resorption processes. We have designed and determined the solution structures of potent OPG analogue peptides, derived from sequences of the cysteine-rich domain of OPG. The inhibitory effects of the peptides on osteoclastogenesis are dose-dependent ($10^{-6}M-10^{-4}M$), and the activity of the linear peptide at $10^{-4}M$ is ten-fold higher than that of the cyclic OPG peptide. Both linear and cyclic peptides have a ${\beta}$-turn-like conformation and the cyclic peptide has a rigid conformation, suggesting that structural flexibility is an important factor for receptor binding. Based on structural and biochemical information about RANKL and the OPG peptides, we suggest that complex formation between the peptide and RANKL is mediated by both hydrophobic and hydrogen bonding interactions. These results provide structural insights that should aid in the design of peptidyl-mimetic inhibitors for treating metabolic bone diseases caused by abnormal osteoclast recruitment.

Expression and Purification of a Cathelicidin-Derived Antimicrobial Peptide, CRAMP

  • Park Eu-Jin;Chae Young-Kee;Lee Jee-Young;Lee Byoung-Jae;Kim Yang-Mee
    • Journal of Microbiology and Biotechnology
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    • 제16권9호
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    • pp.1429-1433
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    • 2006
  • Application of recombinant protein production and particularly their isotopic enrichment has stimulated development of a range of novel multidimensional heteronuclear NMR techniques. Peptides in most cases are amenable to assignment and structure determination without the need for isotopic labeling. However, there are many cases where the availability of $^{15}N$ and/or $^{13}C$ labeled peptides is useful to study the structure of peptides with more than 30 residues and the interaction between peptides and membrane. CRAMP (Cathelicidin-Related AntiMicrobial Peptide) was identified from a cDNA clone derived from mouse femoral marrow cells as a member of cathelicidin-derived antimicrobial peptides. CRAMP was successfully expressed as a GST-fused form in E. coli and purified using affinity chromatography and reverse-phase chromatography. The yield of the CRAMP was 1.5 mg/l 1. According to CD spectra, CRAMP adopted ${\alpha}$-helical conformation in membrane-mimetic environments. Isotope labeling of CRAMP is expected to make it possible to study the structure and dynamic properties of CRAMP in various membrane systems.