• 제목/요약/키워드: $IC_{50}$ values

검색결과 1,075건 처리시간 0.035초

Production and Characterization of Monoclonal Antibodies to a Generic Hapten for-Class-Specific Determination of Organophosphorus Pesticides

  • Jang, Mi-Soon;Lee, Soo-Jung;Xue, Xiaoping;Kwon, Hyuk-Man;Ra, Choon-Sup;Lee, Yong-Tae;Chung, Tae-Wan
    • Bulletin of the Korean Chemical Society
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    • 제23권8호
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    • pp.1116-1119
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    • 2002
  • Monoclonal antibodies have been generated against a generic hapten, ο,ο-diethyl ο-(5-carboxy-2-fluorophenyl) phosphorothioate, for the determination of organophosphorus (OP) pesticides in a class-specific manner. In an indirect competitive enzyme-linked immunosorbent assay (ELISA) format, employing a heterologous coating antigen, these monoclonal antibodies showed desirable properties for use in the class-specific determination, i.e., broad specificity and high sensitivity. The IC50 values of four commonly used ο,ο-diethyl OP pesticides were fairly uniform ranging from 0.1 to 0.3 ㎛/mL. The IC50 values of three ο,ο-dimethyl derivatives were between 0.3 and 1.4 ㎛/mL. These values, together with the limits of detection (LOD), were better, in terms of the specificity and sensitivity, compared with the values obtained previously with polyclonal antibodies.

쑥갓 스테롤배당체의 아질산염소거작용 및 SOD 유사활성 (Nitrite Scavenging Ability and SOD-like Activity of a Sterol Glucoside form Chrysanthemum coronarium L. var. spatiosum)

  • 조민정;박미정;이흠숙
    • 한국식품과학회지
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    • 제39권1호
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    • pp.77-82
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    • 2007
  • 쑥갓의 항산화 활성을 알아보기 위해 쑥갓 총 메탄올추출물의 아질산염 소거작용과 SOD 유사활성을 측정하였다. 아질산염 소거작용과 SOD 유사활성을 가지고 있는 총 메탄올 추출물로부터 클로로포름, n-부탄올 및 물 분획물을 제조하여 각각의 활성을 측정하였다. pH가 1.5일 때의 클로로포름 분획물의 $IC_{50}$값은 39ppm으로 가장 우수한 아질산염 소거작용을 보였으며, vitamin C와 chlorogenic acid의 $IC_{50}$값이 15ppm과 36ppm일 때 클로로포름 분획물은 양성대조군인 chlorogenic acid와 동등한 소거작용을 보였다. 아질산염 소거작용에 대하여 유의성 있게 높은 활성을 나타낸 클로로포름 분획물을 silica gel 컬럼크로마토그래피와 sephadex LH-20 컬럼크로마토그래피를 이용하여 분획의 활성성분인 compound I을 분리하였다. 분리된 compound를 $^{1}H-NMR$$^{13}C-NMR$ spectral data를 통하여 구조를 동정한 결과 compound I은 ${\beta}-sitosterol-O-{\beta}-D-glucoside$임을 확인하였다. Compound I과 그 aglycone인 ${\beta}-sitosterol$의 아질산염 소거작용과 SOD 유사활성은 다소 차이가 있었다. 양성대조군으로 사용한 vitamin C와 chlorogenic acid의 $IC_{50}$값이 pH 1.5에서 각각 15ppm과 36ppm일때 compound I의 $IC_{50}$값이 335ppm, ${\beta}-sitosterol$$IC_{50}$값이 41ppm으로 가수분해된 aglycone이 아질산염 소거작용이 훨씬 높았다. SOD 유사활성의 경우 vitamin C와 chlorogenic acid의 $EC_{50}$ 값은 38ppm, 449ppm으로 이와 비교시 ${\beta}-sitosterol$과 배당체의 $EC_{50}$ 값은 1,291ppm과 2,000ppm 이상으로 나타났다.

Toxic Effects of Heavy Metals on the Growth and Phosphorus Removal Efficiency of Phosphorus Accumulating Microorganisms (PAOs)

  • Sin, Da Hee;Kim, Deok Hyeon;Kim, Jong In;Lee, Moon-Soon;Chung, Keun-Yook
    • 한국토양비료학회지
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    • 제46권6호
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    • pp.673-680
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    • 2013
  • Phosphorus accumulating microorganisms (PAOs) are influenced by various environmental factors and heavy metals. This study was performed to evaluate the effects of the selected heavy metals on the growth and phosphorus removal capacity of Bacillus sp. 3434 BRRJ, Pseudomonas aerunogisa, and Bacillus Subtilis, well known as PAOs. The heavy metals used in this study included Cu, Cd, As, and Zn. The $IC_{50}$ (median inhibition concentration) values of Bacillus sp. 3434 BRRJ for the Cu, Cd, As, and Zn were 8.07 mg $L^{-1}$, 0.18 mg $L^{-1}$, 73.62 mg $L^{-1}$ and 0.25 mg $L^{-1}$, respectively. The $IC_{50}$ values of Pseudomonas aerunogisa for the Cu, Cd, As, and Zn were 4.45 mg $L^{-1}$, 0.16 mg $L^{-1}$, 18.51 mg $L^{-1}$ and 2.34 mg $L^{-1}$, respectively. The $IC_{50}$ values of Bacillus Subtilis for the Cu, Cd, As, and Zn were 3.81 mg $L^{-1}$, 0.18 mg $L^{-1}$, 11.31 mg $L^{-1}$ and 0.47 mg $L^{-1}$, respectively. The phosphorus removal efficiencies of the three bacteria, Bacillus sp. 3434 BRRJ, Pseudomonas aerunogisa, and Bacillus subtilis were 93.12%, 71.81%, and 65.31%, respectively. Based on the results of the three PAOs obtained from the study, it appears that Bacillus sp. 3434BRRJ may have the best results in terms of their growth rate and P removal efficiencies.

Comparison of on Rat Intestinal Digestive Enzyme Inhibitory Activity and Antioxidant Enzyme Activity of Korean and Chinese Schizandra chinensis

  • Chae Hee-Jun;Hwang Hyun-Ik;Lee In-Soon;Moon Hae-Yeon
    • 대한의생명과학회지
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    • 제11권4호
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    • pp.517-523
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    • 2005
  • The purpose of this study was to determine the effect of rat intestinal a-glucosidase inhibitor; methanol $(80\%)$, ethanol $(80\%)$ and water extract of Schizandra chinensis in Korea (KS: Schizandra chinensis in Korea) and China (CS: Schizandra chinensis in China). When the final concentration was 1 mg/ml for each sample (KS and CS), methanol extract of KS ($IC_{50}$ 1.62 mg/ml) showed $46.8\%$, ethanol extract of KS ($IC_{50}$ 1.48 mg/ml) showed $47.4\%$, water extract of KS ($IC_{50}$ 1.72 mg/ml) showed $46.3\%$ and methanol extract of CS ($IC_{50}$ 8.35 mg/ml) showed $13.3\%$, ethanol extract of CS ($IC_{50}$ 8.05 mg/lml) showed $16\%$, water extract of CS ($IC_{50}$ 8.37 mg/ml) showed $11.54\%$ of inhibitor for p-nitrophenyl $\alpha-D-glucopyranoside$ (pNPG) $\alpha-glcosidase$ activity, respectively. And the contents of total phenol, flavonoid of Schizandra chinensis were measured. When the final concentration was 1mg/ml for each sample (KS and CS), total phenol and flavonoid in KS were higher than CS, respectively. The order superoxide dismutase (SOD) activity $IC_{50}$ values of each solvent extracts of KS were: 2.006 mg/ml methanol extract, 2.304 mg/ml ethanol extract and 2.5 mg/ml water extract, which were higher than that of each solvent extracts CS as: 2.881 mg/ml methanol extract, 3.085 mg/ml ethanol extract and 3.190 mg/ml water extract.

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1,1-Diphenyl-2-picrylhydrazyl Radical Scavenging Compounds of Fraxini Cortex

  • Kim, Hyun-Chul;An, Ren-Bo;Jeong, Gil-Saeng;Oh, Seung-Hwan;Kim, Youn-Chul
    • Natural Product Sciences
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    • 제11권3호
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    • pp.150-154
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    • 2005
  • The radical scavenging effect of the MeOH extract of Fraxini Cortex on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical was examined. The $CH_2Cl_2$-and n-BuOH-soluble fractions of MeOH extract showed the promising DPPH radical scavenging effects, and further purified by silica gel, Sephadex LH-20 column chromatography, and reversed-phase C-18 MPLC to yield five coumarins, esculetin (1), fraxidin (2), fraxetin (3), fraxidin $8-O-{\beta}-D-glucopyranoside$ (fraxin methyl ether) (5), esculin (6), and a secoiridoid oleuropein (4), and a coumarin-secoiridoid escuside (7). Compounds 1, 3, and 4 showed potent DPPH radical scavenging effects, exhibiting $IC_{50}$ values of 14.68, 9.64, and $22.03\;{\mu}M$, respectively. Compounds 6 and 7 also showed moderate effects with $IC_{50}$ values of 147.79 and $72.73\;{\mu}M$, respectively. L-Ascorbic acid was used as a positive control and exhibited the $IC_{50}$ value of $50.31\;{\mu}M$.

The Effects of Alpinia katsumadai Extract on Anti-inflammation and Melanogenesis

  • Lee, Jae-Soeb;Jeong, See-Hwa;Ko, Kang-Il;Kim, Ki-Ho;Chong, Chom-Kyu;Park, Soo-Nam
    • 대한화장품학회지
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    • 제25권1호
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    • pp.69-88
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    • 1999
  • Several solvent extracts from Alpinia katsumudai were prepared and their various anti-inflammatory activities were evaluated. Alpinia katsumadai extract showed high various anti-inflammatory effects among the 8 medicinal plant extracts, Butanol extract from Alpinia katsumndai showed a potent anti-oxidative and free radical scavenging activities, Free radical scavenging effect of butanol fraction of Alpinia katsumadai($IC_{50}$/ : 50$\mu$g/m$\ell$) was higher than butylated hydroxytoluene($IC_{50}$/ : 50$\mu$g/m$\ell$) and ascorbic acid($IC_{50}$/ : 22$\mu$g/m$\ell$). Alpinia katsumadai butanol fraction exhibited relatively high antioxidative activity($IC_{50}$/ : 335$\mu$g/m$\ell$) compared to ascorbic acid. The inhibitory effect of Alpinia katsumadal ethanol extract on elastase exhibited 10 to 78% at 100 to 1000$\mu$g/m$\ell$ concentration , tile $IC_{50}$/ values with 465.7$\mu$g/m$\ell$ for porcine pancreatic elastase(PPE) and 481.9$\mu$g/m$\ell$ for human leukocyte elastase(HLE), respectively The Alpinta katsumadai extract inhibited effectively hyaluronidase activity($IC_{50}$/ 335$\mu$g/m$\ell$), and showed inhibition in vitro on delayed hypersensitivity when it was topically applied. These results suggest that Alpinia katsumadai extract may reduce inflammatory skin trouble. The Alpinia katsumadai extract also showed higher Inhibitory effect of melanin biosynthesis on cultured melanoma cell compared to arbutin and kojic acid.

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1-Methyl Substituent and Stereochemical Effects of 2-Phenylcyclopropylamines on the Inhibition of Rat Brain Mitochondrial Monoamine Oxidase A and B

  • Kang, Gun-Il;Hong, Suk-Kil;Choi, Hee-Kyung
    • Archives of Pharmacal Research
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    • 제10권1호
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    • pp.50-59
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    • 1987
  • (E)-2-Phenylcyclopropylamine ((E)-TCP), (Z)-2-Phenylacyclopropylamine ((Z)-TCP), (E)-1-methyl-2-phenylcyclopropylamine ((E)-MTCP), and (Z)-1-methyl-2-phenylcyclopropylamine ((Z)-MTCP) were synthesized and used to determine to what extent 1-methylsubstitution and stereochemistry of 2-phenycyclopropylamines affect inhibition of monoamine oxidase (MAO). Inhibition of rat brain mitochondrial MAO-A and B by the compounds were measured using serotonin and benzylamine as the substrate, respectively and $IC_{50}$ values obtianed with 95% confidence limits by the method of computation. For the inhibition of MAO-A, (E)-MTPC ($IC_{50}$ = 6.2 * $10^{-8}$M) was found to be 37 times more potent than (Z)-MTCP ($IC_{50}$ = 7.8 * $10^{-8}$M), was 7 times more potent than (Z)-MTCP($IC_{50}$= 4.7 * $10^{-7}$M) and (E)-TCP($IC_{50}$ =7.8 * $10^{-8}$M),0.6 times as potent as (Z)- TCP ($IC_{50}$ = 4.4 * $10^{-8}$M). The results suggested that while without 1-methyl group, potency of a (Z)-isomer was comparable to that of (E)-isomer, the methyl group in its (Z)-position was very unfavorable to the inhibition of MAO and that in its (E)-position, the methyl group contributed positively to the potency as found by the fact that (E)-MTCP was 1-5 times more potent than (E)-TCP. In view of the selective inhibition of MAO-A- or B over MAO-A and 1-methyl substitution as well as the stereochemical factors did not significantly influence the selectivity.

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Physiological Activities of Thiacremonone Produced in High Temperature and High Pressure Treated Garlic

  • Woo, Koan Sik;Hwang, In Guk;Kim, Hyun Young;Lee, Sang Hoon;Jeong, Heon Sang
    • Preventive Nutrition and Food Science
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    • 제21권1호
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    • pp.68-72
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    • 2016
  • To examine the possibility of using thiacremonone isolated from high-temperature-high-pressure treated garlic, this study investigated the physiological activities properties. The $IC_{50}$ values of hydroxyl, superoxide, hydrogen peroxide, and nitric oxide radical scavenging activities of thiacremonone were 92.50, 65.05, 12.60, and $81.53{\mu}g/mL$, respectively. On the other hand, the activities of vitamin C were 104.93, 99.43, 42.42, and $122.64{\mu}g/mL$, and the activities of butylated hydroxyanisole were 37.22, 68.45, 22.47, and $40.54{\mu}g/mL$, respectively. The $IC_{50}$ value of ACE inhibition activities of thiacremonone and captoprill were 0.265 and $0.036{\mu}g/mL$, respectively. The $IC_{50}$ value of xanthine oxidase inhibition activities of thiacremonone and allopurinol were 39.430 and $9.346{\mu}g/mL$, respectively. The $IC_{50}$ value of tyrosinase inhibition activities of thiacremonone and kojic acid were 101.931 and $65.648{\mu}g/mL$, respectively.

황금찰수수(Sorghum bicolor L. cv. Hwanggeumchalsusu) 유래 에탄올 추출물 및 폴리페놀계 화합물의 항산화 활성 및 뉴라미니데이즈 억제 효과 (Antioxidative Effect and Neuraminidase Inhibitory Activity of Polyphenols Isolated from a New Korean Red Waxy Sorghum (Sorghum bicolor L. cv. Hwanggeumchalsusu))

  • 나지은;서경혜;고지연;이미자;강현중;김선림;정일민;서우덕
    • 생명과학회지
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    • 제25권7호
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    • pp.786-794
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    • 2015
  • 본 연구는 황금찰수수의 에탄올 추출물을 이용하여 항산화 활성 및 뉴라니미데이즈 억제 효과를 조사하였다. 헥산, 에틸아세테이트, 메탄올과 70% 에탄올 조추출물에서 항산화력의 IC50값을 비교한 결과 70% 에탄올 추출물이 DPPH 라디칼 소거능, ABTS 라디칼 소거능에서 각각 83.2±2.7, 85.6±2.4 μg/ml으로 가장 높았고, 뉴라니미데이즈 억제활성 IC50값을 비교한 결과 메탄올 추출물에서 1.8±0.1 μg/ml로 나타났다. 또한 황금찰수수 추출물에서 컬럼크로마토그래피와 UPLC-PDA-MS/MS 분광기 분석을 통해, Gallic acid (1), Protocatecuic acid (2), p-Hydroxy benzoic acid (3), Vanillic acid (4), Caffeic acid (5), Ferulic acid (6), Luteolinidin (7), Apigeninidin (8), Luteolin (9), 총 9종의 폴리페놀 화합물을 확인하였다. 또한 각각의 화합물에 대한 항산화력의 IC50값을 비교한 결과 Luteolinidin이 DPPH 라디칼 소거능, ABTS 라디칼 소거능에서 각각 10.9±0.5, 8.6±3.0 μM로 가장 우수 하였고, 뉴라니미데이즈 억제활성은 Luteolin이 12.9±3.8의 IC50값과 비경쟁적 저해모델을 보였다. 결과적으로 황금찰수수는 높은 항산화 효과와 뉴라미니데이즈 억제활성을 보여 식품, 사료 등의 새로운 기능성소재로 다양하게 활용될 수 있음을 시사한다.

Design and Synthesis of an Anticancer Diarylurea Derivative with Multiple-Kinase Inhibitory Effect

  • El-Gamal, Mohammed I.;Oh, Chang-Hyun
    • Bulletin of the Korean Chemical Society
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    • 제33권5호
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    • pp.1571-1576
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    • 2012
  • A diarylurea compound 1 possessing pyrrolo[3,2-$c$]pyridine nucleus was designed and synthesized with structure similarity to Sorafenib. Compound 1 was tested over 60-cancer cell line panel at a single dose concentration of 10 ${\mu}M$ and showed high activity. It was further tested in a five-dose mode to determine its $IC_{50}$, TGI, and $LC_{50}$ values over the 60 cell lines. Compound 1 showed high potency and good efficacy, and was accordingly tested at a single dose concentration of 10 ${\mu}M$ over a panel of 40 kinases. At this concentration, it completely inhibited the enzymatic activities of a number of oncogenic kinases, including ABL, ALK, c-RAF, FLT3, KDR, and TrkB. The target compound was subsequently tested over these 6 kinases in 10-dose testing mode in order to determine its $IC_{50}$ values.