• 제목/요약/키워드: compound-K

검색결과 8,269건 처리시간 0.033초

Synthesis and Smooth Muscle-Selective Relaxant Activity of a Piperidine Analogue: 1-(4'-Fluorophenacyl)-4-Hydroxy-4-Phenyl-Piperidinium Chloride

  • Taqvi, Syed Intasar Hussain;Ghayur, Muhammad Nabeel;Gilani, Anwarul Hassan;Saify, Zafar Saeed;Aftab, Mohammad Tariq
    • Archives of Pharmacal Research
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    • 제29권1호
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    • pp.34-39
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    • 2006
  • The antispasmodic and vasodilator activities of a newly synthesized piperidine derivative (1-(4'fluorophenacyl)-4-hydroxy-4-phenyl-piperidinium chloride) were studied in vitro. The test compound exhibited a dose-dependent relaxant effect on the spontaneous and $K^+$ (75 mM)-induced contractions of isolated rabbit jejunum with respective $EC_{50}$ values of 0.01 mM(0.01-0.02, 95% CI) and 0.30 mM (0.17-0.56). The $Ca^{++}$ channel blocking (CCB) activity was confirmed when the test compound (0.1-0.2 mM) shifted the $Ca^{++}$ dose-response curves to the right, similar to that produced by verapamil ($0.1-1.0{\mu}M$), a standard CCB. In the isolated rabbit aorta, the test compound showed a dose-dependent vasodilator effect on $K^+$ (75 mM)-induced contractions with an $EC_{50}$ value of 0.08 mM (0.02-0.26) while also suppressed the norepinephrine ($1{\mu}M$) control peak responses with $EC_{50}$ value of 0.08 mM (0.05-0.13, n=5). When tested in Langendorff perfused rabbit heart preparation, the test compound exhibited a negligible inhibitory effect on the rate or force of atrial and ventricular contractions when tested up to 5 mM. The results show smooth muscle-selective relaxant effect of the test compound on intestinal and vascular preparations mediated possibly via blockade of voltage and receptor-operated $Ca^{++}$ channels.

컴파운더 보우 지레 시스템의 기구학적 해석 (Kinematic Analysis of Levering Systems in Compound Bows)

  • 이용성;김홍석;정성균;최웅재;김영근;박경래;신기훈
    • 대한기계학회논문집A
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    • 제37권1호
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    • pp.55-60
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    • 2013
  • 컴파운더 보우는 리커브 보우와 비교하여 케이블 및 캠 풀리로 구성되는 지레시스템을 사용하여, 궁사가 보우를 최대 위치로 당기기 위해 필요로 하는 힘을 줄이는 동시에 더 많은 에너지를 축적할 수 있도록 해준다. 지금까지 컴파운더 보우의 효율 및 성능을 향상시키기 위해 경험적인 방법에 기초하여 많은 특허가 제안되었지만, 해석적인 방법에 대한 연구는 별로 없었다. 그러므로 본 연구에서는 컴파운더 보우 지레 시스템의 기구학적인 해석을 위한 방법을 제안하여 지레시스템의 캠 형상 및 보우 날개의 재질변화에 따른 효과를 설계자가 쉽게 예측할 수 있도록 하고자 한다.

Antifungal Activity of Magnolol and Honokiol

  • Bang, Kyu-Ho;Kim, Yoon-Kwan;Min, Byung-Sun;Na, Min-Kyun;Rhee, Young-Ha;Lee, Jong-Pill;Bae, Ki-Hwan
    • Archives of Pharmacal Research
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    • 제23권1호
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    • pp.46-49
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    • 2000
  • Two neolignan compound, magnolol $(5,5^{l}-diallyl-2,2^{l}-dihydroxybiphenyl, 1)$ and honokiol $(5,5^{l}-diallyl-2,4^{l}-dihydroxybiphenyl, 2)$ were isolated from the stem bark of Magnolia obovata and evaluated for antifungal activity against various human pathogenic fungi. Compound 1 and 2 showed significant inhibitory activities against Trichophyton mentagrophytes, Microsporium gypseum, Epidermophyton floccosum, Aspergillus niger, Cryptococcus neoformans, and Candida albicans with minimum inhibitory concentrations (MIC) in a range of $25-100{\mu}g/ml$. Therefore, compound 1 and 2 could be used as lead compounds for the development of novel antifungal agents.

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Potent Inhibition of Monoamine Oxidase B by a Piloquinone from Marine-Derived Streptomyces sp. CNQ-027

  • Lee, Hyun Woo;Choi, Hansol;Nam, Sang-Jip;Fenical, William;Kim, Hoon
    • Journal of Microbiology and Biotechnology
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    • 제27권4호
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    • pp.785-790
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    • 2017
  • Two piloquinone derivatives isolated from Streptomyces sp. CNQ-027 were tested for the inhibitory activities of two isoforms of monoamine oxidase (MAO), which catalyzes monoamine neurotransmitters. The piloquinone 4,7-dihydroxy-3-methyl-2-(4-methyl-1-oxopentyl)-6H-dibenzo[b,d]pyran-6-one (1) was found to be a highly potent inhibitor of human MAO-B, with an $IC_{50}$ value of $1.21{\mu}M$; in addition, it was found to be highly effective against MAO-A, with an $IC_{50}$ value of $6.47{\mu}M$. Compound 1 was selective, but not extremely so, for MAO-B compared with MAO-A, with a selectivity index value of 5.35. Compound 1,8-dihydroxy-2-methyl-3-(4-methyl-1-oxopentyl)-9,10-phenanthrenedione (2) was moderately effective for the inhibition of MAO-B ($IC_{50}=14.50{\mu}M$) but not for MAO-A ($IC_{50}$ > $80{\mu}M$). There was no time-dependency in inhibition of MAO-A or -B by compound 1, and the MAO-A and -B activities were almost completely recovered in the dilution experiments with an excess amount of compound 1. Compound 1 showed competitive inhibition for MAO-A and -B, with $K_i$ values of 0.573 and $0.248{\mu}M$, respectively. These results suggest that piloquinones from a microbial source could be potent reversible MAO inhibitors and may be useful lead compounds for developing MAO enzyme inhibitors to treat related disorders, such as depression, Parkinson's disease, and Alzheimer's disease.

황벽나무 열매 추출물로부터 신규 화합물의 분리 및 구조분석 (A New Compound Isolation and Structure Analysis from Phellodendron Amurense Fruit Extract)

  • 김영희;최정은;홍진영;조창욱;이정민;김수지
    • Journal of the Korean Wood Science and Technology
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    • 제41권4호
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    • pp.269-275
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    • 2013
  • 본 연구는 유기질 문화재 보존을 위해 한국 전통 약용식물을 대상으로 항균 및 살충활성을 검증한 결과 황벽나무 열매 추출물이 우수한 활성을 나타냄을 확인하였다. 황벽나무 열매 추출물을 비극성 용매로 분획하여 그 중 가장 활성이 우수한 ethylacetate 분획물을 대상으로 실리카젤 및 Sephadex LH-20 컬럼 크로마토그래피를 실시하고 Prep-TLC를 이용하여 화합물을 순수 분리하였다. 화합물은 UV spectrum 분석 결과 260 nm 파장에서 최대흡수피크가 관찰되었고, $^1H$, $^{13}C$, HMQC, HMBC NMR과 ESI mass spectrum을 이용하여 화학구조를 분석한 결과 (4'-ethyl-2'-methylfuranyl)-6-methoxy-7-methylnona-2E,4E,6Z,8E-tetraenoic acid의 새로운 화합물임을 알 수 있었다.

저탄소강의 질화침탄과 산화처리시 분위기 변화에 따른 조직 및 부식특성에 관한 연구 (A Study on the Corrosion Properties and Microstructure of the Nitrocarburized and Oxidized Low Carbon Steel according to the Treatment Atmospheres)

  • 신평우;이구현;남기석;박율민;조형준
    • 열처리공학회지
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    • 제17권2호
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    • pp.87-93
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    • 2004
  • Nitrocarburizing was carried out with various $CH_4$ gas composition with 4 torr gas pressure at $570^{\circ}C$ for 3 hours and post oxidation was carried out with 100% $O_2$ gas atmosphere with 4 torr at different temperatures for various time. In the case of plasma nitrocarburizing, It is that the ratio of ${\varepsilon}-Fe_{2-3}$(N, C) and ${\gamma}^{\prime}-Fe_4$(C, N), which comprise the compound layer phase, depend on concentrations of $N_2$ gas and $CH_4$ such that when the concentration of $N_2$ and $CH_4$ increased, the ratio of ${\gamma}^{\prime}-Fe_4$(C, N) decreased, but the ratio of ${\varepsilon}-Fe_{2-3}$(N, C) increased. The thickness of compound layer consistently increased as gas concentration increased regardless of $N_2$ and $CH_4$ expect when the concentration of $CH_4$ was 3.5 volume%, it decreased insignificantly. When oxidizing for 15min in the temperature range of $460{\sim}570{^\circ}C$, the study found small amount of $Fe_3O_4$ at the temperature of $460{^\circ}C$ and also found that amounts of $Fe_2O_3$. and $Fe_3O_4$ on the surface and amount of ${\gamma}^{\prime}-Fe_4$(C, N) in the compound layer increased as the increased over $460^{\circ}C$, but the thickness of the compound layer decreased. Corrosion resistance was influenced by oxidation times and temperature.

황금으로부터 항산화 활성 성분의 분리 (Isolation of Antioxidative Compound from Scutellaria baicalensis G.)

  • 김석창;안건석;박채규;전병선;이종태;박원종
    • 한국약용작물학회지
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    • 제14권4호
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    • pp.212-216
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    • 2006
  • 황금 (Scutellaria baicalensis Gergi)에 함유된 항산화 억제활성 물질을 분리하고 항산화 효과에 대하여 조사한 결과는 다음과 같다. 1. 황금 500g을 100% MeOH로 추출하여 150g의 수율을 얻었으며, 다시 분획하여 Ethyl ether 13.2g과 n-BuOH 10.3g, Water 126.5g을 얻었다. 2. Ethyl ether 분획을 Column chromatography, TLC 및 HPLC를 이용하여 xanthine oxidase 억제활성을 가진 compound I을 분리하였다. 3. $^1H-NMR,\;^{13}C-NMR$, MS spectrometer 등 분광학적 방법을 이용하여 Compound I의 구조를 규명한 결과, flavonoid 물질로서 compound I은 구조식이 3,5,7-trihydroxy-2'-methoxy-flavanone로 확인되었다.

Resveratrol Anglog 3,5,2',4'-Tetramethoxy-trans-stilbene, Potentiates the Inhibotion of Cell Growth and Induces Apoptosis in Human Cancer Cells

  • Nam, Kyung-Ae;Kim, Sang-hee;Heo, Yeon-Hoi;Lee, Sang-Kook
    • Archives of Pharmacal Research
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    • 제24권5호
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    • pp.441-445
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    • 2001
  • Resveratrol, a trihydroxystilbene found in grapes and several plants, has been shown to be active in inhibiting multistage carcinogenic process. Using resveratrol as the prototype, we synthesized several analogs and evaluated their growth inhibitory effect using cultured human cancer cells. In the present report we show that one of the resveratrol analogs, 3, 5,2',4'-tetramethoxy-trans-stilbene, potentiated the inhibition of cancer cell growth. Prompted by the strong growth Inhibitory activity of the compound ($IC_{50}$; $0.8{\mu}$ g/ml) compared to resveratrol ($IC_{50}$; $18{\mu}$ug/ml) in cultured human colon cancer cells (Col2), we performed an action mechanism study using the compound. The compound induced the accumulation of cellular DNA contents in the sub-CO phase DNA contents of the cell cycle by in a time-dependent manner. The morphological changes were also consistent with an apoptotic process. This result indicated that the compound induced apoptosis of cancer cells, and may be a candidate for use in the development of potential cancer chemotherapeutic or cancer chemopreventive agents.

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레이저웰딩기술을 이용한 고속 광통신용 송신모듈 제작 및 특성 연구 (Characteristics of High Speed Optical Transmitter Module Fabricated by Using Laser welding Technique)

  • 강승구;송민규;장동훈;편광의
    • 대한전기학회:학술대회논문집
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    • 대한전기학회 1995년도 추계학술대회 논문집 학회본부
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    • pp.552-554
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    • 1995
  • In long-haul high speed optical communications, the distance between a transmitter and a receiver depends on the amount of light coupled to a single mode optical fiber from the laser diode(LD) as well as the LD characteristic itself. And the transmitter module must have long lifetime. high reliability, and even simple structure. Such points have induced laser welding technique to be a first choice in opto-electronic module packaging because it can provide strong weld joint in a short time with very small coupling loss. In this paper, packaging considerations and characteristics for high speed LD modules are discussed. They include optical path design factors for larger aligning tolerance, and novel laser welding processes for component assembly. For low coupling loss after laser welding processes, the optical path for optimum coupling of a single mode optical fiber into the LD chip was designed with the GRIN lens system providing sufficiently large aligning tolerance both in the radial and axial directions. The measured sensitivity of the LD module was better than -33.7dBm(back to back) at a BER of $10^{-10}$ with a 2.5Gbps NRZ $2^{23}-1$ PRBS.

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A Novel Bromoindole Alkaloid from a Korean Colonial Tunicate Didemnum sp.

  • Hahn, Dongyup;Kim, Geum Jin;Choi, Hyukjae;Kang, Heonjoong
    • Natural Product Sciences
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    • 제21권4호
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    • pp.278-281
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    • 2015
  • Chemical investigation on a colonial marine tunicate, Didemnum sp. led to the isolation of a series of indole alkaloids including a new (1) and two known metabolites (2-3). Based on the spectroscopic analysis including 1D and 2D NMR along with MS spectra, the structure of 1 (16-epi-18-acetyl herdmanine D) was elucidated as a new amino acid derivative. The absolute configuration of 1 was determined by comparison of specific rotation with the known compound. The structures of compounds 2 and 3 were also identified as bromoindole containing compounds N-(6-bromo-1H-indole-3-carbonyl)-L-arginine and (6-bromo-^1H-indol-3-yl) oxoacetamide, respectively, based on $^1H$ and $^{13}C$ NMR data, MS data and specific rotation value. Their pharmacological potentials as antibacterial agents and FXR antagonists were investigated, but no significant activity was found. However, the structural similarity of compound 1 to compound 4 suggested the anti-inflammatory potential of compound 1.