• Title/Summary/Keyword: Organic IC

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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.
    • Journal of the Korean Chemical Society
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    • v.55 no.5
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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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    • v.33 no.4
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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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    • v.27 no.1
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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.

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

  • Lee, Sun-young;Ju, Jeh-Beak;Sohn, Tae-Won;Cho, Won-Il;Cho, Byung-Won
    • Journal of the Korean Electrochemical Society
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    • v.8 no.1
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    • pp.1-5
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    • 2005
  • Electric double layer capacitors(EDLCS) based on the charge stored at the interface between a hi팀 surface area carbon electrode and an organic electrolyte solution are widely used as a maintenance-free power source for IC memories and microcomputers. The achievement of the excellent performance of the capacitor requires an electrolyte solution which provides high conductivities over a wide temperature range and good electrochemical stabilities to allow the capacitor to be operated at high voltage. The electrochemical capacitor using a carbon material as electrodes and using an organic electrolyte with $1M-LiPF_6$ in PC-GBL-DEC(volume ratio 1:1:2) has specific capacitance of 64F/g.

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

  • Jeong, Gyeong Han;Kim, Tae Hoon
    • Food Science and Preservation
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    • v.23 no.7
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    • pp.989-994
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    • 2016
  • As part of our continuing search for bioactive natural products, the antioxidant and ${\alpha}$-glucosidase inhibitory activities of an 80% methanolic extract and organic solvent soluble-portions of Aruncus dioicus var. kamtschaticus roots were investigated by using a bioassay system. The antioxidant activity of A. dioicus var. kamtschaticus roots extract and organic solvent soluble-portions were assessed by examining with 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) ($ABTS^+$) radical scavenging. In addition, anti-diabetic effects of the A. dioicus var. kamtschaticus root extract and organic solvent soluble-portions were tested via ${\alpha}$-glucosidase inhibition assay. The total phenolic contents of the products were determined by applying UV-VIS spectrophotometry. All tested samples showed dose-dependent radical scavenging and ${\alpha}$-glucosidase inhibitory properties. In particular, the ${\alpha}$-glucosidase inhibitory and radical scavenging effects of the ethyl-acetate (EtOAc)-soluble portion from the roots of A. dioicus var. kamtschaticus were greater than those from other solvent-soluble portions. These results indicate that A. dioicus var. kamtschaticus could be considered a new effective source of natural antioxidants and anti-diabetic materials. More systematic research of the constituents of the roots of this A. dioicus variety will be conducted to further develop its antioxidative and anti-diabetic properties.

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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    • v.35 no.1
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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.

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

  • Park, Yhun Jung;Ku, Chang-Sub;Kim, Min-Jin;Lee, Mi Kyeong;Kim, Ki Ohk;Ryu, Hyung Won;Song, Hyuk-Hwan;Kim, Doo Young;Oh, Sei-Ryang
    • Journal of Applied Biological Chemistry
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    • v.58 no.1
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    • pp.31-38
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    • 2015
  • The rhizomes of Anemarrhena asphodeloide was extracted with 100% ethanol and concentrated subfractions were separated with medium pressure liquid chromatography-based activity profiling. One compound was isolated from the subfraction 10 through the repeated preparative high performance liquid chromatography (prep-HPLC). According to physico-chemical and spectroscopic data including NMR and MS, the chemical structures of the compound was determined as nyasol (1). Nyasol was exhibited potent inhibitory activity for NO ($IC_{50}:12.5{\mu}g/mL$), tyrosinase ($IC_{50}:12.5{\mu}g/mL$), melanin contents ($IC_{50}:12.5{\mu}g/mL$), thymus and activation-regulated chemokine (TARC) production ($IC_{50}:6.25{\mu}g/mL$). As a result, nyasol has an excellent inflammation-dependent anti-whitening and TARC production activity. It could be used to a large range of functional cosmetics.

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

  • Park, Da-Jeong;Ahn, Joon-Young;Shin, Hye-Jung;Bae, Min-Suk
    • Journal of Korean Society for Atmospheric Environment
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    • v.30 no.5
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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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    • v.26 no.1
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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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    • v.36 no.4
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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.