• 제목/요약/키워드: Organic IC

검색결과 152건 처리시간 0.036초

Design, Synthesis and Biological Evaluation of Novel Analogs of Bortezomib

  • Rao, R. Janaki Rama;Rao, A.K.S. Bhujanga;Swapna, K.;Rani, B. Baby;Kumar, S. Prasanna;Awantika, S.;Murthy, Y.L.N.
    • 대한화학회지
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    • 제55권5호
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    • pp.765-775
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    • 2011
  • Novel analogs of bortezomib were designed, synthesized and in vitro biological evaluation was carried out using human tumor cell lines A549 and PC3. Docking studies of these analogs of bortezomib was discussed. According to biological investigations, the inhibitors 4, 6, and 8 were found to be more potent than reference drug candidate bortezomib. A549 cell line showed significant sensitivity towards 4, 6, and 8 with $IC_{50}$ values 14.03, 18.5, and 12.4 nM, respectively, and PC3 cell line showed IC50 values 26.1, 37.0, and 21.2 nM, respectively. The $IC_{50}$ values of bortezomib in these cell lines are 27.3 nM and 42.0 nM.

Studies on Benzofuran-7-carboxamides as Poly(ADP-ribose) Polymerase-1 (PARP-1) Inhibitors

  • Lee, Sun-Kyung;Yi, Kyu-Yang;Lee, Byung-Ho;Oh, Kwang-Seok
    • Bulletin of the Korean Chemical Society
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    • 제33권4호
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    • pp.1147-1153
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    • 2012
  • Benzofuran-7-carboxamide was identified as a novel scaffold of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor. A series of compounds with various 2-substituents including (tertiary amino)methyl moieties substituted with aryl ring and aryl groups containing tertiary amines, were synthesized and biologically evaluated to elucidate the structure-activity relationships and optimize the potency. 2-[4-(Pyrrolidin-1-ylmethyl)phenyl]-benzofuran-7-carboxamide (42) was the most potent as an IC50 value of 40 nM among those.

Macasiamenene V, a New Stilbenoid from the Leaves of Macaranga inermis

  • Aldin, Muhammad Fajar;Tjahjandarie, Tjitjik Srie;Saputri, Ratih Dewi;Tanjung, Mulyadi
    • Natural Product Sciences
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    • 제27권1호
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    • pp.45-48
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    • 2021
  • One new compound, macasiamenene V (1), and two known stilbenes (2-3) were isolated from Macaranga inermis Pax & K.Hoffm leaves. The structure of 1 was fully assigned based on the information on high-resolution MS and (1D, 2D) NMR spectra. The cytotoxic of compounds 1-3 was evaluated against 4T1 and HeLa cells. Compounds 2-3 showed high activity against HeLa cells with an IC50 value of 1.09 and 0.88 ㎍/mL, respectively.

유기용매전해질에 따른 전기이중층캐패시터의 전기화학적 특성 (Electrochemical Characteristics of EDLCs with Selectivity Factors for the Organic Electrolyte)

  • 이선영;주재백;손태원;조병원;조원일
    • 전기화학회지
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    • 제8권1호
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    • pp.1-5
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    • 2005
  • 높은 비표면적을 갖는 carbon과 유기용매 전해질 사이의 계면에서 생기는 전기이중층용량을 기본으로 작동하는 전기이중층 캐패시터는 IC memories, microcomputer 등으로 폭 넓게 사용되며 maintenance-free의 영구적인 back-up용 전원으로 넓게 사용되고 있다 EDLC에 사용되는 전해질은 이온 전도도가 높아야 하고 사용되는 온도 범위가 넓어야 한다. 그리고 고전압을 인가했을 때 전해질이 전기화학적으로 안정해야 한다. 본 실험에서는 고전압에서 안정적인 액상 유기계 전해질을 사용하여 전기이중층캐패시터의 전기화학적 특성을 확인하였다. Paste rolling법으로 제조된 탄소전극과 $1M-LiPF_6$ in PC-GBL-DEC (volume ratio 1:1:2)의 유기용매전해질을 사용한 전기이중층캐패시터가 64F/g의 우수한 비축전용량을 발현하였다

재배 삼나물 뿌리 추출물의 자유 라디칼소거 및 α-glucosidase 저해활성 (Free radical scavenging and α-glucosidase inhibitory effects of a roots extract of Aruncus dioicus var. kamtschaticus)

  • 정경한;김태훈
    • 한국식품저장유통학회지
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    • 제23권7호
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    • pp.989-994
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    • 2016
  • 삼나물 뿌리를 80% 메탄올로 침지 추출하여 얻어진 추출물에 대해 n-hexane, EtOAc 및 n-BuOH의 유기용매를 활용하여 순차 분획을 실시하였고, 얻어진 결과물에 대하여 DPPH, $ABTS^+$ 라디칼 소거능 및 ${\alpha}$-glucosidase 저해활성을 평가하였다. DPPH 라디칼 소거능은 총 페놀성 화합물의 함량이 상대적으로 높은 EtOAc 층에서 $IC_{50}$값이 $32.3{\pm}2.3{\mu}g/mL$으로 가장 우수한 DPPH 라디칼 소거능을 확인하였고, 삼나물 뿌리 의 EtOAc 가용부에 다량 존재하는 페놀성 화합물과 라디칼 소거능과의 연관성을 시사하였다. 또한 $ABTS^+$ 라디칼 소거능은 EtOAc 층의 $IC_{50}$값이 $18.9{\pm}2.1{\mu}g/mL$의 우수한 라디칼 소거활성이 확인 하였고, 우수한 라디칼 소거 활성물질의 존재가 시사되었다. 또한, ${\alpha}$-glucosidase 저해활성을 평가한 결과, 우수한 라디칼 소거능을 나타낸 EtOAc 층의 $IC_{50}$$57.8{\pm}7.8{\mu}g/mL$의 저해활성을 나타내었으며, 이는 positive control인 acarbose의 $IC_{50}$값인 $501.1{\pm}17.5{\mu}g/mL$과 비교하여 우수한 활성이었으며, 추출물 상태의 시료를 단일물질로 정제할 경우 더욱 강한 효능의 화합물이 존재할 가능성을 시사하였다. 향후 이들 활성물질 동정을 통한 활성 기작에 대한 연구가 필요하며 본 연구결과는 보다 우수한 라디칼 소거능 및 ${\alpha}$-glucosidase 저해능을 가지는 새로운 기능성 소재 발굴을 위한 기초자료로 활용 가능할 것으로 사료된다.

Evaluation of sensitivity of soil respiration to temperature in different forest types and developmental stages of maturity using the incubation method

  • Lee, Eun-Hye;Suh, Sang-Uk;Lee, Chang-Seok;Lee, Jae-Seok
    • Journal of Ecology and Environment
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    • 제35권1호
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    • pp.1-7
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    • 2012
  • To calculate and predict soil carbon budget and cycle, it is important to understand the complex interrelationships involved in soil respiration rate (Rs). We attempted to reveal relationships between Rs and key environmental factors, such as soil temperature, using a laboratory incubation method. Soil samples were collected from mature deciduous (MD), mature coniferous (MC), immature deciduous (ID), and immature coniferous (IC) forests. Prior to measure, soils were pre-incubated for 3 days at $25^{\circ}C$ and 60% of maximum water holding capacity (WHC). Samples of gasses were collected with 0, 2, and 4 h interval after the beginning of the measurement at soil temperatures of 5, 15, 25, and $35^{\circ}C$ (at 60% WHC). Air samples were collected using a syringe attached to the cap of closed bottles that contained the soil samples. The $CO_2$ concentration of each gas sample was measured by gas chromatography. Rs was strongly correlated with soil temperature (r, 0.93 to 0.96; P < 0.001). For MD, MC, ID, and IC soils taken from 0-5 cm below the surface, exponential functions explained 90%, 82%, 92%, and 86% of the respective data plots. The temperature and Rs data for soil taken from 5-10 cm beneath the surface at MD, MC, ID, and IC sites also closely fit exponential functions, with 83%, 95%, 87%, and 89% of the data points, respectively, fitting an exponential curve. The soil organic content in mature forests was significantly higher than in soils from immature forests (P < 0.001 at 0-5 cm and P < 0.005 at 5-10 cm) and surface layer (P = 0.04 at 0-5 cm and P = 0.12). High soil organic matter content is clearly associated with high Rs, especially in the surface layer. We determined that the incubation method used in this study have the possibility for comprehending complex characteristic of Rs.

지모의 뿌리줄기로부터 분리된 nyasol의 미용효과 (Cosmetic Activities of Nyasol from the Rhizomes of Anemarrhena asphodeloide)

  • 박윤정;구창섭;김민진;이미경;김기옥;류형원;송혁환;김두영;오세량
    • Journal of Applied Biological Chemistry
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    • 제58권1호
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    • pp.31-38
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    • 2015
  • 지모 뿌리를 100% EtOH로 추출, 농축하여 medium pressure liquid chromatography 기반의 NO 분획물 활성 검정법을 이용하여 활성을 검정하였다. preparative high performance liquid chromatography를 반복적인 칼럼크로마토그래피를 수행하여 1개의 단일성분을 분리하였다. NMR, MS 등을 포함한 이화학 및 분광학적 자료에 근거하여 분리된 물질을 구조 분석한 결과 (-)-nyasol로 구조동정 하였다. 분리된 활성물질 nyasol은 NO 생성 억제, melanin과 tyrosinase를 억제하는 미백효과, thymus and activation-regulated chemokine 생성을 억제하는 활성에서 $6.25-12.5{\mu}g/mL$$IC_{50}$ 값을 가지는 강한 저해 활성을 나타냈다. 특히 nyasol은 염증에 의한 항아토피 및 항미백활성에 있어 뛰어난 효능을 나타내었다. 이 결과로 보아 nyasol은 천연 기능성 화장품으로써 이용 가능성을 넓힐 수 있을 것으로 사료된다.

PILS-TOC 및 GC/MS-TD를 이용한 서울시 대기 중 초미세먼지(PM2.5) 유기탄소의 특성 분석 (Characteristics of PM2.5 Carbonaceous Aerosol using PILS-TOC and GC/MS-TD in Seoul)

  • 박다정;안준영;신혜정;배민석
    • 한국대기환경학회지
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    • 제30권5호
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    • pp.461-476
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    • 2014
  • Continuous Water-Soluble Organic Carbons (WSOC) by the Particle Into Liquid Sampler - Total Organic Carbon (PILS-TOC) analyzer were measured at the Seoul intensive monitoring site from June 17 through July 5 in 2014. In addition, the 24 hour integrated PM2.5 collected by Teflon and Quartz filters were analyzed for water soluble ions by Ion chromatography (IC), WSOC by TOC from water extracts, organic carbon (OC), elemental carbon (EC) by carbon analyzer using the thermal optical transmittance (TOT) method, and mass fragment ions (m/z) related to alkanes and PAHs (Poly Aromatic Hydrocarbons) by Gas Chromatography-Mass Spectrometer-Thermal Desorption (GC/MS-TD). Based on the statistical analysis, four different Carbonaceous Thermal Distributions (CTDs) from OCEC thermal-gram were identified. This study discusses the primary and secondary sources of WSOC based on the Classified CTD, organic mass fragments, and diurnal patterns of WSOC. The results provide knowledge regarding the origins of WSOC and their behaviors.

A New Cinnamyl Acid Derivative from the Roots of Willughbeia coriacea Wall.

  • Tanjung, Mulyadi;Tjahjandarie, Tjitjik Sri;Saputri, Ratih Dewi;Harsono, Andre;Aldin, Muhammad Fajar
    • Natural Product Sciences
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    • 제26권1호
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    • pp.79-82
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    • 2020
  • A new cinnamyl acid derivative, willughbein A (1) along with pinoresinol (2), alyterinate A (3), and scopoletin (4), were isolated from the roots of Willughbeia coriacea Wall. The structure of 1 has been determined based on HRESIMS, 1D, and 2D NMR spectral data. All of the isolates were evaluated for their cytotoxicity against three human cancer cells (HeLa, T47D, MCF-7, and P-388). Compound 3 showed moderate activity against P-388 cells with an IC50 value of 3.04 ㎍/mL.

Interaction Characteristics of Nucleoside Analogues with Human Organic Anion Transporter 1 and 3

  • Choi, Jun-Shik;Cheon, Eun-Pa;Han, Hyo-Kyung
    • Journal of Pharmaceutical Investigation
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    • 제36권4호
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    • pp.283-286
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    • 2006
  • The present study aimed to investigate the interaction of nucleoside analogs with human organic anion transporter 1 and 3(hOAT1 and hOAT3) that play a primary role in the tubular uptake of endogenous and exogenous organic anions in the kidney. The interactions of ddC, ara-C, ara-A and ara-U with hOAT1 and hOAT3 were examined using MDCK cells stably overexpressing hOAT1 or hOAT3. Among the tested drugs, ddC showed the highest affinity to hOAT1 with $IC_{50}$ values of 5.2 mM, while ara-A, ara-C and ara-U weakly inhibited the cellular uptake of $[^3H]-PAH$ in MDCK-hOAT1 cells at 1 mM. In contrast, all the tested drugs did not have any inhibition effect on the cellular uptake of $[^3H]-estrone$ sulfate in MDCK-hOAT3 cells over the drug concentration of 0.01-2 mM, implying that they might not interact with hOAT3. Taken all together, the present study suggests that hOAT1 could weakly interact with nucleoside analogues such as ddC, ara-C, ara-A and ara-U but the interaction with hOAT3 during the urinary excretion of these nucleoside analogues may be negligible in the kidney.