• 제목/요약/키워드: IC values

검색결과 1,217건 처리시간 0.031초

The antioxidant and cytotoxic activities of Sonchus oleraceus L. extracts

  • Yin, Jie;Kwon, Gu-Joong;Wang, Myeong-Hyeon
    • Nutrition Research and Practice
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    • 제1권3호
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    • pp.189-194
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    • 2007
  • This study investigated in vitro antioxidant activity of Sonchus oleraceus L. by extraction solvent, which were examined by reducing power, hydroxyl radical-scavenging activity(HRSA) and 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assays. 70% MeOH extract had the greatest reducing power while EtOH extract had the greatest HRSA. The antioxidant activity of S. oleraceus extracts was concentration dependent and its $IC_{50}$ values ranged from 47.1 to $210.5\;{\mu}g/ml$ and $IC_{50}$ of 70% MeOH, boiling water and 70% EtOH extracts were 47.1, 52.7 and $56.5\;{\mu}g/ml$, respectively. 70% MeOH extract of S. oleraceus contained the greatest amount of both phenolic and flavonoid contents. The extracts tested had greater nitrite scavenging effects at lower pH conditions. The cytotoxic activity showed that EtOH extract had the best activity against the growth of stomach cancer cell. These results suggest that S. oleraceus extract could be used as a potential source of natural antioxidants.

생약으로 산화적 결합 효소인 갑상선 peroxidase의 저해제 검색 (Screening of Inhibitor of Thyroid Peroxidase, an Oxidative Coupling Enzyme from Natural Products)

  • 이현정;장미영;김미리;배기환;석대은
    • 약학회지
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    • 제43권3호
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    • pp.334-341
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    • 1999
  • Thyroid peroxidase is a biochemical target protein for the antithyroid drugs. Ethanol extracts from one hundred and thirty seven natural products were screened for the inhibition of thyroid peroxidase activity. Thyroid peroxidase was purified from porcine thyroids, and the inhibition of peroxidase activity was evaluated using guaiacol oxidation (C-C coupling) assay. Twenty one natural products expressed a remarkable inhibition (>50%) of peroxidase activity at $330{\mu\textrm{g}}$ solid weight/m. The 50% inhibitory concentration ($IC_{50}$) of 70% ethanol extract from six potent natural products ranged from 3.1 to $31.2{\;}{\mu\textrm{g}}$ solid weight/m, in contrast to the range ($0.33~0.54{\;}{\mu\textrm{g}}/ml$) of $IC_{50}$ values fro catechin and epigallocatechin gallate as positive controls. Noteworthy, the extract of Camellia taliensis showed irreversible inhibition of the enzyme. It is suggested that extract from some natural products such as Camellia taliensis, Rheum undulatum or Euphorbia perinensis, exhibiting a potent inhibition of peroxidase activity, may be developed as sources of potent antithyroid agents.

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Cap-Modified Hydroxamate Analogues as Histone Deacetylases Inhibitors and Antitumor Agents

  • Zhang, Qing-Wei;Feng, Juan;Li, Jian-Qi
    • Bulletin of the Korean Chemical Society
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    • 제35권1호
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    • pp.129-134
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    • 2014
  • Two series of SAHA-liked hydroxamate analogues were designed, synthesized and evaluated for their biological activities against nuclear HDACs. Compounds of Series I were found to be very effective inhibitors of cancer cell growth in the PC-3, Hut78, K562 and Jurkat E6-1 cancer cell lines with mean $IC_{50}$ values from $0.54{\mu}M$ (Ic, Jurkat E6-1) to $7.73{\mu}M$ (Ib, K562), indicating that they are cell permeable and the benzimidazolyl-based ligands are flexible enough to occupy the binding site of HDAC.

흰쥐의 배양 간세포를 이용한 세포독성시험에 있어서 뉴트랄레드 및 젖산 탈수소효소법의 비교 (Comparison of the Two in Vitro Cytotoxicity Assays in Primary Cultured Rat Hepatocytes - the Neutral Red (NR) and Lactate Dehydrogenase (LDH) Tests)

  • 이경태;서성훈
    • Journal of Pharmaceutical Investigation
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    • 제25권4호
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    • pp.365-369
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    • 1995
  • The acute cytotoxicities of chloroquine sulfate, propranolol, ascorbic acid, acetylsalicylic acid and acrylamide on cultured adult rat hepatocytes were evaluated by the use of LDH leakage and NR uptake test. On the basis of $IC_{50}$ values, the rank order of cytotoxicities of these drugs in both tests was chloroquine sulfate > propranolol > acetylsalicylic acid > ascorbic acid. The $IC_{50}$ of LDH test was very similar to that of NR uptake test. Thus, we concluded that both tests are reliable and sensitive methods in detecting toxicity in adult cultured rat hepatocytes.

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마 점질물의 중금속 제거능과 ACE저해 효과 (Removal of Heavy Metal and ACE Inhibition of Yam Mucilage)

  • 하영득;이삼빈;곽연길
    • 한국식품영양과학회지
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    • 제27권4호
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    • pp.751-755
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    • 1998
  • Functional properties of yam mucilage were investigated by physicochemical analysis. Yam mucilage was extracted from the root of yam and then separated into two fractions by its selective aggregation with isopropanol concentration. Each mucilge fraction showed the excellent binding properties with heavy metal ions Co, Cr and Cu. Cr showed the higher affinity with mucilage than Co and Cu at pH 6.3. In ACE inhibition, IC50 values of mucilage fraction 1 and 2 showed 8.99$\mu\textrm{g}$/${mu}ell$ and 7.1$\mu\textrm{g}$/${mu}ell$, respectively.

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Dimming형 IC를 이용한 형광램프용 전자식 안정기의 회로상수 결정 (Determination of the circuit parameters of an electronic ballast for a fluorescent lamp using a dimming ballast controller)

  • 송상빈;김선;곽재영;여인선
    • 한국조명전기설비학회:학술대회논문집
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    • 한국조명전기설비학회 1998년도 학술발표회논문집
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    • pp.156-161
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    • 1998
  • The purpose of this paper is to determine circuit parameters in the inverter part of the electronic dimming ballast for fluorescent lamps, that is adequate to use with the prevailing dimming controller IC. Firstly, the operating frequency characteristics are investigated by varying circuit parameters of electronic ballasts and are matched with the output characteristics of dimming ballast controller. Secondly, circuit parameter values are determined by using PSpice simulation and operating frequency characteristics. Finally its validity is verified from the electrical and light output characteristics on the prototype of the electronic dimming ballast.

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IC 실현에 적합한 정현파 능동 발진기의 회로 및 특성에 관한 연구(II) (Characteristics of the Sinusoidal Active Oscillator Circuit for Integrated Circuit Realization(II))

  • 박종연;이원건;손태호
    • 산업기술연구
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    • 제11권
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    • pp.43-53
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    • 1991
  • Two kinds of simple active oscillators are proposed and analyzed assuming that operational amplifier has two-poles frequency characteristics. The first circuit is composed of one operational amplifier, one resistor and one grounded capacitor. The second oscillator is realized with one operational amplifier and three resitors. Proposed oscillators have the low sensitivity of the oscillation frequency for little variations of the passive element values. By the experimental results obtained with Op-Amp. ${\mu}A741$, the simple oscillators can be useful for the frequency range $1.25 KHz{\leq}f_{01}{\leq}40KHz$ for the active-RC type or $45.45 KHz{\leq}f_{02}{\leq}400KHz$ for the active-R oscillator, and it is shown to transform the active-R oscillator circuit into the voltage controlled type. Therefore, two kinds of oscillator circuit are attractive for the IC realization, because they have one operational amplifier, one resistor and one grounded capacitor, or three resistors.

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지용성 Benz[cd]indole 엽산길항제의 합성 및 In Vitro 항암활성 (Synthesis of Lipophilic Benz[cd]indole Antifolates and Their Antitumor Activity In Vitro)

  • 백두종
    • 약학회지
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    • 제49권1호
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    • pp.60-67
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    • 2005
  • Nonclassical aminobenz[cd]indole antifolates 4, 5 and 6, in which the glutamic acid moiety of the classical antifolates is substituted by 2-phenylglycinamide or 3-aminobenzamide, were synthesized and their in vitro antitumor activity was evaluated. The purpose of this substitution is that the lipophilicity is enhanced due to the aromatic ring of the target compounds for the passive transport through lipid membrane of cells while the hydrogen bonding of the amide is retained in the active site of the enzyme, thymidylate synthase, where the glutamate is originally present. The target compounds were highly cytotoxic against tumor cell lines of murine and human origin with micromolar to nanomolar $IC_{50}$ values. Most effective was compound 4 ($N^6-methyl-N^6$-[4-[(${\alpha}$(S)-aminocarbonylbenzyl) aminocarbonyl]benzyl]-2,6-diaminobenz[cd]indole)with $IC_{50}$ of 2 nM against SW480, human colon adenocarcinoma cell line, which is 650-fold more potent than the reference compound 3.

Cytotoxic C-Benzylated Chalcone and Other Constituents of Ellipeiopsis cherrevensis

  • Wirasathien, Lalita;Pengsuparp, Thitima;Moriyasu, Masataka;Kawanishi, Kazuko;Suttisri, Rutt
    • Archives of Pharmacal Research
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    • 제29권6호
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    • pp.497-502
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    • 2006
  • A new natural C-benzylated chalcone, $2',4'-dihydroxy-3'-(2-hydroxybenzyl)-6{\c}-methoxychalcone$ (2), along with two other flavonoids, tiliroside and kaempferol 3-O-rutinoside, and an oxoaporphine alkaloid, lanuginosine were isolated from the aerial parts of Ellipeiopsis cherrevensis (Annonaceae). Two known polyoxygenated cyclohexene derivatives, ferrudiol and zeylenol, and a new analog, ellipeiopsol D, were also isolated. The chalcone 2 exhibited cytotoxic activity against human small-cell lung-cancer (NCl-H187), epidermoid carcinoma (KB) and breast cancer (BC) cell lines with $IC_{50}$ values of 1.40, 5.31 and $13.92\;{\mu}g/mL$, respectively. This compound also showed antimalarial activity against Plasmodium falciparum with an $IC_{50}$ value of $7.1\;{\mu}g/mL$ as well as antimicrobacterial activity against Mycobacterium tuberculosis with a MIC of 25 mg/mL.

대구의 간 단백질의 효소적 가수분해물로부터 안지오텐신 I 전환효소 저해 펩타이드의 분리.정제 및 특성 (Purification and Characterization of Angiotensin I Converting Enzyme lnhibitory Peptides from Enzymatic Hydrolysate of Cod Liver Protein)

  • 최영일;박표잠;최정호;변희국;정인철;문성훈;김세권
    • 생명과학회지
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    • 제10권2호
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    • pp.140-149
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    • 2000
  • In order to utilize marine processing waste which would normally be discarded, cod liver protein was hydrolysed by ${\alpha}$-chymotrysin, and the hydrolysate was investigated for the new angiotensin I converting enzyme (ACE) inhibitor. Thy hydrolysate was separated into three major types, with molecular weight cut-off (MWCO) values less than 10 kDa, 5 kDa and 1 kDa of ultrafiltration membranes, respectively. ACE inhibitory peptides were isolated from the fractions passed through MWCO 1 kDa membrane, and purified by using ion-exchange chromatography on a SP-Sephadex C-25 column, gel filtration on a Sephadex G-15 column, and HPLC on an ODS column. The purity was identified with capillary electrophoresis. The amino acid sequences of two peptides were Met-Ile-Pro-Pro-Tyr-Tyr (IC50=10.9 ${\mu}$M) and Gly-Leu-Arg-Asn-Gly-Ile (IC50=35.0 ${\mu}$M)

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