• 제목/요약/키워드: IC values

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한약재 13종의 hERG 채널 관련 심장독성 평가 (hERG Channel-Related Cardiotoxicity Assessment of 13 Herbal Medicines)

  • 하혜경;이시온;김동현;서창섭;신현규
    • 대한한의학회지
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    • 제42권3호
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    • pp.44-55
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    • 2021
  • Objectives: As the use of herbal medicinal products (HMPs) increases worldwide, systematic verification of the safety of HMPs is required. The induction of cardiotoxicity is one of the major factors in post-approval withdrawal of medicinal products, and drug-induced cardiotoxicity assessment is emerging as an important step in drug development. In the present study, we evaluated human ether-à-go-go-related gene (hERG) potassium channel-related cardiotoxicity to predict the risk of cardiac arrhythmia in thirteen herbal medicines known to have cardiac toxicity. Methods: We measured the inhibition rate of hERG potassium channel activity of 13 medicinal herbal extracts in hERG-expressing HEK 293 cells using an automated patch-clamping system. Quinidine was used as a positive control for inhibition of hERG activity. Results: Extracts of Evodiae Fructus, Strychni Semen, and Corydalis Tuber potently inhibited the activity of hERG, and IC50 values were 3.158, 19.87, and 41.26 ㎍/mL, respectively. Cnidi Fructus, Ephedra Herba, Lithospermi Radix, Polygoni Multiflori Radix, Visci Ramulus et Folium, Asiasari Radix et Rhizoma, and Scolopendra weakly inhibited hERG activity, and the IC50 value for each herbal medicine was more than 400 ㎍/mL. Aconiti Kusnezoffii Tuber and two types of Aconiti Lateralis Radix Preparata (Po and Yeom) had weak inhibitory activity against hERG, and the IC50 values were more than 700 ㎍/mL. The IC50 value of quinidine against hERG was 1.021 𝜇M. Conclusion: Evodiae Fructus, Strychni Semen, and Corydalis Tuber acted as potent inhibitors against hERG. These herbal medicines may cause cardiac arrhythmia through QT prolongation, so care should be taken when taking them.

Effect of Temperature on the Fracture Toughness of A516 Gr70 Steel

  • Seok, Chang-Sung
    • Journal of Mechanical Science and Technology
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    • 제14권1호
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    • pp.11-18
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    • 2000
  • Fracture toughness JIC and KIC tests were performed on A516 Gr70 carbon steel plate at the temperature ranging from -$160^{\circ}C$ to $600^{\circ}C$, and test results were analyzed according to ASTM E 813 and ASTM E 399. Unloading compliance J-integral tests were performed on 1TCT specimens. The relation between the $J_{IC}$ value and the test temperature was obtained. It was concluded that the temperature ranging from $-15^{\circ}C$ to $600^{\circ}C$ is the upper shelf region of ductile-brittle transition temperature, and in this temperature range, fracture toughness $J_{IC}$ values decreased with increasing temperature. The ductile brittle transition temperature of the material may be around $-30^{\circ}C$. In the region near $-30^{\circ}C$, the tendency of $J_{IC}$ to decrease with decreasing temperature was significant.

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원자력 압력용기강(SA508-3)의 탄소성 파괴인성 평가 (The Evaluation for Elastic-Plastic Fracture Toughness in a Reactor Pressure Vessel Steel(SA508-3))

  • 오세욱;윤한기;임만배
    • 한국해양공학회지
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    • 제7권2호
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    • pp.91-102
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    • 1993
  • The elastic-plastic fracture thoughness J sub(IC) of Nuclear Reactor Vessel Steel(SA 508-3) which has high toughness was discussed at temperatures RT, $-20^{\circ}C$, $200^{\circ}C$ and 1/2/CT specimen was used for this study. Especially the two methods recommended in ASTM and JSME were compared. It was difficult to find J sub(IC) by ASTM R-curve method with the specimen used for this research, while JSME R-curve method yielded good result. The stretched zone width menthod gave slightly larger J sub(IC) values than those by the R-curve method for SA 508-3 steel.

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Antioxidative Properties of Different Solvent Extracts from Persimmon (Diospyros kaki cv. Fuyu) Flower-Buds

  • You, Dong-Hyun;Lee, Seung-Cheol
    • Preventive Nutrition and Food Science
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    • 제16권4호
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    • pp.328-332
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    • 2011
  • After preparation of acetone, ethanol, methanol, and water extracts (10 g/300 mL) of dried persimmon (Diospyros kaki cv. Fuyu) flower-buds, total phenolic contents (TPC), 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity (RSA), 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) RSA, reducing power (RP), and tyrosinase inhibitory activity of the extracts were evaluated. The methanol extracts produced the highest TPC (113.39 mg gallic acid equivalents/g), DPPH RSA ($IC_{50}=40.25\;{\mu}g/mL$), ABTS RSA ($IC_{50}=58.17\;{\mu}g/mL$) and RP ($IC_{50}=69.43\;{\mu}g/mL$) activities while the water extracts generated the lowest values. The ethanol extract showed the highest tyrosinase inhibitor activity (88.90%) at a concentration of 1 mg/mL. These results indicated that persimmon flower-buds may be a useful source of natural antioxidants.

J-R 곡선에서의 균열길이 감소현상에 관한 연구 (II) (A Study on the Apparent Negative Crack Growth Phenomenon of J-R Curve(II))

  • 석창성;최용식
    • 대한기계학회논문집
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    • 제16권9호
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    • pp.1627-1631
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    • 1992
  • 본 연구에서는 균열길이 감소현상의 처리법에 대하여 고찰하고자 하며, 내용 을 요약하면 다음과 같다. (1) 오프세트(offset)법의 배경 및 오프세트법에 의한 균열길이 감소현상의 처리 방법 을 제안하였다. (2) 실제의 균열길이의 측정과 $J_{IC}$실험해석을 통하여, 수정식과 오프세트법의 타 당성을 검토하였다.

DNA Strand-Nicking Principles of Mucuna birdwoodiana

  • Han, Ah-Reum;Mar, Woong-Chon;Seo, Eun-Kyoung
    • Natural Product Sciences
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    • 제9권2호
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    • pp.105-108
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    • 2003
  • During our research program to find DNA strand-scission agents from higher plants, the MeOH extracts of the stems of Mucuna birdwoodiana Tutcher. (Leguminosae) exhibited the most potent activity with an $IC_{50}$ value of $4.9\;{\mu}g/ml$. Thus, detailed laboratory investigation was performed, and led to the isolation of known compounds, $({\pm})$-catechin (1) and (-)-epicatechin(2) as active principles. Compounds 1 and 2 showed significant activity of DNA strand-scission with $IC_{50}$ values of 10.8 and $7.5\;{\mu}g/ml$, respectively (positive control, bleomycin: $IC_{50}\;3.3\;{\mu}g/ml$.

Synthesis of New 6-(4-Fluorophenyl)-5-(2-substituted pyrimidin-4-yl)imidazo[2,1-b] thiazole Derivatives and their Antiproliferative Activity against Melanoma Cell Line

  • Park, Jin-Hun;Oh, Chang-Hyun
    • Bulletin of the Korean Chemical Society
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    • 제31권10호
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    • pp.2854-2860
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    • 2010
  • Synthesis of a new series of pyrimidinyl-imidazo[2,1-b]thiazole derivatives is described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the pyrimidinyl ring side chain was investigated. The biological results indicated that most of the newly synthesized compounds showed moderate activity against A375, compared with Sorafenib. Among all of these derivatives, the cyclic sulfamide derivatives IIIa, IIIb, and IIIe showed the most potent antiproliferative activity against A375 human melanoma cell line. The IC50 values of compounds IIIa,b were in nanomolar scale. In addition, compound IIIe ($IC_{50}=1.9\;{\mu}M$) also demonstrated more potent antiproliferative activity compared with Sorafenib ($IC_{50}=5.6\;{\mu}M$).

온도변화에 따른 철도차량용 제동디스크의 물성치 변화에 관한 연구 (A Study on the Mechanical Properties of the Braking Disk due to the Change of Temperature)

  • 김재훈;강부병;김형진;석창성
    • 한국철도학회:학술대회논문집
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    • 한국철도학회 2003년도 추계학술대회 논문집(III)
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    • pp.383-388
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    • 2003
  • This study investigates the change of the temperature and mechanical properties of the braking disk for the railway vehicle. The average temperature is measured about $100^{\circ}C$ and the maximum temperature is measured over $200^{\circ}C$ by non-contact sensor from Seoul to Chunan. In the $20^{\circ}C-300^{\circ}C$, the $0.2\%$ offset yield strengths of the disk (GC25-30 material) are a little down to the reference value, but the linear relation of tensile test result is not find from the linear change of temperature. However, $J_{IC}$ values have the inverse proportion to the temperature, and the $J_{IC}$ value at $200^{\circ}C$ decrease $30.55\%$ from the $J_{IC}$. value of the room temperature. This result means that the crack length on the braking disk is rapidly increase at $200^{\circ}C$

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Antioxidative and Neuroprotective Effects of Enzymatic Extracts from Leaves of Perilla frutescens var.japonica

  • Kim, Eun-Kyung;Lee, Seung-Jae;Lim, Beong-Ou;Jeon, You-Jin;Song, Min-Dong;Park, Tae-Kyu;Lee, Kwang-Ho;Kim, Bo-Kyung;Lee, Sang-Rak;Moon, Sang-Ho;Jeon, Byong-Tae;Park, Pyo-Jam
    • Food Science and Biotechnology
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    • 제17권2호
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    • pp.279-286
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    • 2008
  • The antioxidative activity of various enzymatic extracts from leaves of Perilla frutescens var. japonica was evaluated by measuring 1,1-diphenyl-2-picrylhydrazyl (DPPH), hydroxyl, and alkyl radical scavenging activity using an electron spin resonance (ESR) spectrometer. For this study, the leaves were enzymatically hydrolyzed by 8 carbohydrases (Dextrozyme, AMG, Promozyme, Maltogenase, Termamyl, Viscozyme, Celluclast, and BAN) and 9 proteases [Flavourzyme, Neutrase, Protamex, Alcalase, PP-trypsin (trypsin from porcine pancreas), papain, pepsin, $\alpha$-chymotrypsin, and BP-trypsin (trypsin from bovine pancreas)]. The DPPH radical scavenging activities of Promozyme and Alcalase extracts were the highest, and the $IC_{50}$ values were 77.25 and $109.66\;{\mu}g/mL$, respectively. All enzymatic extracts of the leaves scavenged hydroxyl radical, and the $IC_{50}$ values of Celluclast and pepsin extracts which were the highest activity were 243.34 and $241.86\;{\mu}g/mL$, respectively. The BAN and $\alpha$-chymotrypsin extracts showed the highest scavenging activities, and the $IC_{50}$ values were 21.13 and $33.23\;{\mu}g/mL$, respectively. The pepsin extracts from the leaves showed protective effect on $H_2O_2$-induced DNA damage. In addition, the pepsin extracts decreased cell death in PC-12 cells against $H_2O_2$-induced oxidative damage. The findings of the present study suggest that enzymatic extracts of the leaves possess antioxidative activity.

Antioxidant Constituents from the Leaves of Cedrela sinensis A. Juss

  • Lee, Ik-Soo;Wei, Chun-Hua;Thoung, Phuong Thien;Song, Kyung-Sik;Seong, Yeon-Hee;Bae, Ki-Hwan
    • 한국약용작물학회지
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    • 제14권5호
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    • pp.267-272
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    • 2006
  • Phytochemical study on the EtOAc fraction from the MeOH extract of the leaves of Cedrela sinensis led to the isolation of five known phenolic compounds (1-5), whose structures were identified as (+)-catechin (1), $kaempferol-3-0-{\alpha}- L-rhamnopyranoside$ (2), quercetin (3), $quercetin-3-O-{\alpha}-L-rhamnopyranoside$ (4), and $quercetin-3-O-{\beta}-D-glucopyranoside$ (5), respectively, by comparing their spectral $(uv,\;JR,\;IH\;and\;^{13}C-NMR,\;and\;ESI-MS)$ and physicochemical data with those reported in the literature. Among the isolated compounds (1-5), compounds 1 and 3-5 exhibited significant DPPH radical scavenging effects with $IC{_50}$ values ranging from $21.3{\pm}1.4\;to\;38.1{\pm}3.2 {\mu}M$ as well as superoxide anion radical scavenging effects with $IC{_50}$ values ranging from $9.4{\pm}0.7\;to\;21.2{\pm}3.6 {\mu}M$. Furthermore, compounds 1 and 3-5 also exhibited considerable inhibitory effects on LDL peroxidation induced by either $CU^{2+}$ or AAPH with $IC{_50}$ values ranging from $1.4{\pm}0.4\;to\;11.9{\pm}1.4\;{\mu}M$. These results indicated that flavonoids are the major constituents of C. sinensis and considered to be antioxidant principles of this plant.