• Title/Summary/Keyword: Q-method

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Measurement of Human Cytochrome P450 Enzyme Induction Based on Mesalazine and Mosapride Citrate Treatments Using a Luminescent Assay

  • Kim, Young-Hoon;Bae, Young-Ji;Kim, Hyung Soo;Cha, Hey-Jin;Yun, Jae-Suk;Shin, Ji-Soon;Seong, Won-Keun;Lee, Yong-Moon;Han, Kyoung-Moon
    • Biomolecules & Therapeutics
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    • v.23 no.5
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    • pp.486-492
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    • 2015
  • Drug metabolism mostly occurs in the liver. Cytochrome P450 (CYP) is a drug-metabolizing enzyme that is responsible for many important drug metabolism reactions. Recently, the US FDA and EU EMA have suggested that CYP enzyme induction can be measured by both enzymatic activity and mRNA expression. However, these experiments are time-consuming and their interassay variability can lead to misinterpretations of the results. To resolve these problems and establish a more powerful method to measure CYP induction, we determined CYP induction by using luminescent assay. Luminescent CYP assays link CYP enzyme activity to firefly luciferase luminescence technology. In this study, we measured the induction of CYP isozymes (1A2, 2B6, 2C9, and 3A4) in cryopreserved human hepatocytes (HMC424, 478, and 493) using a luminometer. We then examined the potential induction abilities (unknown so far) of mesalazine, a drug for colitis, and mosapride citrate, which is used as an antispasmodic drug. The results showed that mesalazine promotes CYP2B6 and 3A4 activities, while mosapride citrate promotes CYP1A2, 2B6, and 3A4 activities. Luminescent CYP assays offer rapid and safe advantages over LC-MS/MS and qRT-PCR methods. Furthermore, luminescent CYP assays decrease the interference between the optical properties of the test compound and the CYP substrates. Therefore, luminescent CYP assays are less labor intensive, rapid, and can be used as robust tools for high-throughput CYP screening during early drug discovery.

A Study on the Risk of Pesticide Exposure by Food Intake (식이섭취를 통한 농약폭로의 위해도에 관한 연구)

  • 전옥경;이용욱
    • Journal of Food Hygiene and Safety
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    • v.14 no.2
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    • pp.201-215
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    • 1999
  • Limited information is available on the acceptability of Korean MRLs(maximum residue limits) and the health risk based on the pesticide exposure by food intake. The aim of this study was to evaluate TMDI(theoretical maximum daily intake) and EDI(estimated daily intake) for Korean by using MRLs, food intake, residue data, and correction factors, and compare with ADI(acceptable daily intake) in order to estimate the health risk based on the pesticide exposure. The study was performed in three steps. In the frist step, the residual pesticides in each category of food were investigated using the pesticide residue analytical data(1995-96) from officially approved organizations and the analytical data for poultry was adopted from Korean food code method. In the second step, TMDI was estimated from MRLs and food factors, and was compared with ADI. In the third step, the effectiveness of each culinary treatment (washing, peeling, steaming, boiling, and salting) was evaluated and EDI was calculated using pesticide residue data, food factor, and correction factor by treatment. TMDI obtained from MRLs and food intake, and food intake was summed as 1,100.99 g, which was 79.1% of total consumption. The percent ratio of TMDI to ADI for 156 pesticides was mostly below 80% and only 30 pesticides exceeded the ADI. In particular, non-treated EDI from pesticide residue data and food intake was summed up to about 43 $\mu\textrm{g}$/day/capita, and the rank was procymidone(8.6 $\mu\textrm{g}$) > maleic hydrazide(8.2 $\mu\textrm{g}$) > EPN(3.7 $\mu\textrm{g}$) > deltamethrin(3.5 $\mu\textrm{g}$) > cypermethrin(3.0 $\mu\textrm{g}$). The treated EDI calculated from pesticide residue data, food intake, and correction factor by culinary treatment was summed up to 13.7 $\mu\textrm{g}$/day/captia. The percentage of ADI was TMDI(79.74%) > non-treated EDI (0.17%) > treated EDI (0.04%), and the exposure level of Korean population to whole pesticides was below the level to produce health risk. Oncogenic risk of five pesticides used in Korea whose oncogenic potency(Q*) was known were assessed from TMDI and treated EDI. Dietary oncogenic risk for Korean was estimated to be 2.0$\times$10-3 on the basis of TMDI, 8.3$\times$10-7 on the basis of treated EDI. The oncogenic risk from TMDI exceeded the risk level(1$\times$10-6) of EPA, whereas the oncogenic risk from treated EDI and real exposure level lower than that of EPA.

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Oak Forests of the Daegok-cheon Petroglyphs Area in Ulsan, South Korea (울산 대곡천 암각화 유적지 일대의 참나무림 다양성과 분포 특성)

  • Lee, Gyeong-Yeon;Kim, Jong-Won
    • Korean Journal of Ecology and Environment
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    • v.50 no.1
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    • pp.126-136
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    • 2017
  • We describe characteristics of diversity and distribution of oak forests on the Daegok-cheon gorge of the Southeastern Korean Peninsula, the oldest prehistoric site, in view of a sort of food resources of acorns. The $Z{\ddot{u}}rich$-Montpellier School's method was adopted for field investigation on the oak dominant stands. A total of 20 phytosociological $relev\acute{e}s$ composed of 193 taxa were analyzed by syntaxonomy and ecological flora. The Daegok-cheon's oak forests occupied 36.9% ($513,374m^2$) of the surveyed area, and its 99% ($507,677m^2$) was Quercus variabilis and Q. serrata stands. Oak forests of the Daegok-cheon gorge are a kind of regional vegetation type characterizing by the high relative net contribution degree (r-NCD) of Platycarya strobilacea and Sapium japonicum, which are an edaphic type of the xerophilous and thermophilic oak forests. The region of the Daegok-cheon petroglyphs is defined as an ecoregion with rich acorn supply and abundant water resources, and the warmer environment, which attracts prehistoric man.

Antioxidative, Antimutagenic, and Cytotoxic Activities of Ethanol Extracts from Cornus officianalis (산수유(Cornus officianalis) 에탄올 추출물의 항산화, 항돌연변이 활성 및 암세포 성장 억제 효과)

  • Jeon, Yeon-Hee;Kim, Mi-Hyun;Kim, Mee-Ra
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.37 no.1
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    • pp.1-7
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    • 2008
  • The antioxidative, antimutagenic and cytotoxic activities of ethanol extract from Cornus officianalis have been studied. The antioxidant activity of the ethanol extract was measured by 1,1-diphenyl-2-picrylhydrazyl (DPPH) method. The inhibition effects on the mutagenicity in Salmonella Typhimurium TA100 were evaluated by Ames test and cancer cell inhibitory effects in Hep3B cell and HeLa cell were tested by MTT assay. Cornus officianalis had an important free radical-scavenging activity towards the DPPH radical. At a concentration of 500 ppm, the DPPH radical-scavenging activity of Cornus officianalis was similar to that of L-ascorbic acid. None of the extracts produced a mutagenic effect on S. Typhimurium TA100. The ethanol extract from Cornus officianalis showed about 77% of inhibition at 500 ppm on the mutagenicity induced by 4-nitroquinoline-1-oxide. The extract from Cornus officianalis showed strong cytotoxicity against Hep3B and HeLa cells, with inhibition of 83 and 78% at a dose of $700{\mu}g$/plate, respectively. Moreover, the ethanol extracts had 34.33 mg H.E/g of polyphenols and 5.67 mg Q.E/g of flavonoids, respectively. Therefore, the present study showed antioxidative, antimutagenic and anticancer potential of the ethanol extract from Cornus officianalis.

Design of An Open-Ended Coaxial Cavity Resonator (한쪽 면이 열린 동축 공동 공진기의 설계에 대한 연구)

  • Lee, Yun-Min;Kim, Jin-Kook;Hur, Jung
    • The Journal of the Institute of Internet, Broadcasting and Communication
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    • v.13 no.4
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    • pp.201-208
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    • 2013
  • This paper is a study of an empirical design of an open-ended coaxial cavity resonator. It can be done by using the radius of the inner conductor, the inner radius and the length of the resonator. However, the basic coaxial transmission -line theory can be seen that the characteristics of the resonant frequency and the Q value are varied by the change of length, regardless of the value of radius of the inner conductor and inner radius of the resonator. We find out the impact of radius of the inner conductor, inner radius of the resonator and the length of the resonator parameter and propose the optimized empirical resonator design method by reducing the error between the theoretical value and the design value. Based on the simulation, several resonators are fabricated by the size of 14 mm for the radius of inner conductor, 2 mm, 5 mm, 10 mm respectively for the inner radius of resonator, and 8.5 mm for the length of the resonator. The resonant frequencies of the produced resonators were measured at 6.1, 5.7, 6.5 GHz respectively. According to the result of simulation and measurement, we know that we can design the relatively exact open-ended coaxial cavity resonator by applying the basic coaxial transmission-line theory directly when the length of the resonator is less than 10 mm, and adding the correction factor of 0.5 GHz to the calculated resonant frequency in case of more than 10 mm of the length of the resonator.

Spectroelectrochemical Study for Thin Film of Gold Nanoparticles (금 나노입자 박막의 분광전기화학적 연구)

  • Seo, Seong S.;Chambers, James Q.
    • Journal of the Korean Chemical Society
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    • v.50 no.1
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    • pp.32-36
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    • 2006
  • films of gold nanoparticles were formed on indium tin oxide (ITO) by an electrodeposition method from an aminosilicate stabilized gold colloid solution. The thin films were examined by cyclic voltammetry (CV), scanning electron microscopy (SEM), UV-visible, and energy dispersive X-ray spectroscopy (EDXS). The surface coverage of gold nanoparticles on the thin film was estimated to 1.2 nanomole/cm2. An anthraquinone-2, 6-disulfonic acid, disodium salt (AQDS) self-assembled layer was generated by immersing gold thin film into 1mM of AQDS in 0.1M HClO4 solution for over 20 hours. As a result, a new absorbance peak from the multi-layers (AQDS/thin film of gold /ITO) was obtained about at 690 nm. Also, the surface plasmon absorption of multi-layers was measured by UV-Visible spectrometer along with chronoamperometry by applying the various potentials from +0.5V to -0.5V. The maximum surface plasmon absorption band at 550 nm was decreased by applying negative potentials. The change of absorbance was correlated with the surface coverage of the AQDS indicating the pseudo-capacity surface state of the AQDS layer was coupled to the energy level of the plasmonband by applied negative potentials.

The Effect of the Phytoncide in Decreasing the Mouth Odor (피톤치드의 입냄새 제거효과)

  • Park, Jae-Bong;Auh, Q-Schick;Chun, Yang-Hyun;Lee, Jin-Yong;Hong, Jung-Pyo
    • Journal of Oral Medicine and Pain
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    • v.32 no.2
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    • pp.151-156
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    • 2007
  • Antimicrobial action of phytoncide in the mouth decrease odor-producing microorganisms. Also phytoncide has malodor effect by reaction with volatile sulfur compounds. Phytoncide has excellent malodor effect in microbiologically and chemically. This study prove the malodor effect of phytoncide by use ferrous sulfate. So I try to make new treatment method for halitosis. I get the results as follows. 1. The difference of mean value of absorbancy was 0.849 between the mean absorbancy of deposition by add phytoncide to saliva and the saliva only. 2. The difference of mean value of absorbancy was 0.701 between the mean absorbancy of deposition by add phytoncide to distilled water and the distilled water only. 3. The difference of mean value(0.849) in saliva by existence of phytoncide was larger than in double distilled water(0.701) by existence of phytoncide. Therefore, phytoncide make more deposition in saliva than double distilled water by reaction with sulfur compounds. As the results, phytoncide reaction with sulfur compounds in saliva. It take malodor action in liquid state effectively. It is thought, only the toothpaste it knows from in the limit which does not have a side effect by the human body it adds in the oral cavity of the mouth rinse and with the fact that it will be able to use positively in clinic.

Vegetation Structure of Mountain Ridge from Miwangjae to Cheonwhangbong in Weolchulsan National Park (월출산국립공원 미왕재-천황봉 구간의 능선부 식생구조)

  • Choo Gab-Cheul;Kim Gab-Tae;Cho Hyun-Seo
    • Korean Journal of Environment and Ecology
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    • v.20 no.2
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    • pp.114-121
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    • 2006
  • To investigate the vegetation structure of mountain ridge from Miwangjae to Cheonwhangbong, 11 plots($2000m^2$) set up with random sampling method were surveyed. Three groups of Quercus mongolica community, Quercus mongolica-Styrax japonica community, Q. mongolica-Pinus densiflora community were classified by cluster analysis. Quercus mongolica was a major woody plant species in the ridge area from Miwangjae to Cheonwhangbong, and Styrax japonica and Pinus densiflora was partly occupied. High positive correlations was proved between Prunus sargentii and Euonymus alatus for. ciliato-dentatus; Quercus serrata and Euonymus alatus; Sorbus alnifolia and Euonymus alatus, Magnolia sieboldii; Acer pseudo-sieboldianum and Euonymus alatus for. ciliato-dentatus; Rhododendron schlippenbachii and Euonymus alatus for. ciliato-dentatandus; Euonymus alatus and Lindera obtusiloba, Castanea crenata, Lindera erythrocarpa; Lespedeza bicolor and Rhododendron schlippenbachii; Castanea crenata and Magnolia sieboldii; Magnolia sieboldii and Lindera erythrocarpa, and relatively high negative correlations was proved between Rhododendron schlippenbachii and Euonymus alatus; Lespedeza bicolor and Castanea crenata; Stephanandra incisa and Magnolia sieboldii; Rhododendron yedoense var. poukhanense and Lindera erythrocarpa; Euonymus alatus for. ciliato-dentatus and Magnolia sieboldii; Fraxinus sieboldiana and Sapium japonicum; Prunus sargentii and Lespedeza maximowiczii; Lespedeza maximowiczii and Lindera erythrocarpa. Species diversity(H') of investigated groups was ranged $2.3225{\sim}2.7721$, and it was relatively low value compared to that of mountain ridge area of other national parks.

Chemical transformation and target preparation of saponins in stems and leaves of Panax notoginseng

  • Wang, Ru-Feng;Li, Juan;Hu, Hai-Jun;Li, Jia;Yang, Ying-Bo;Yang, Li;Wang, Zheng-Tao
    • Journal of Ginseng Research
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    • v.42 no.3
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    • pp.270-276
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    • 2018
  • Background: Notoginsenoside Ft1 is a promising potential candidate for cardiovascular and cancer disease therapy owing to its positive pharmacological activities. However, the yield of Ft1 is ultralow utilizing reported methods. Herein, an acid hydrolyzing strategy was implemented in the acquirement of rare notoginsenoside Ft1. Methods: Chemical profiles were identified by ultraperformance liquid chromatography coupled with quadruple-time-of-flight and electrospray ionization mass spectrometry (UPLC-Q/TOF-ESI-MS). The acid hydrolyzing dynamic changes of chemical compositions and the possible transformation pathways of saponins were monitored by ultrahigh-performance LC coupled with tandem MS (UHPLC-MS/ MS). Results and conclusion: Notoginsenoside Ft1 was epimerized from notoginsenoside ST4, which was generated through cleaving the carbohydrate side chains at C-20 of notoginsenosides Fa and Fc, and vinaginsenoside R7, and further converted to other compounds via hydroxylation at C-25 or hydrolysis of the carbohydrate side chains at C-3 under the acid conditions. High temperature contributed to the hydroxylation reaction at C-25 and 25% acetic acid concentration was conducive to the preparation of notoginsenoside Ft1. C-20 epimers of notoginsenoside Ft1 and ST4 were successfully separated utilizing solvent method of acetic acid solution. The theoretical preparation yield rate of notoginsenoside Ft1 was about 1.8%, which would be beneficial to further study on its bioactivities and clinical application.

Comparison between the Subjective Evaluation and the Objective Evaluation of the Effect of Pain Control in the Masticatory Muscle Pain

  • Kim, Dong-Keun;Ahn, Chi-Hyuk;Hwang, Mi-Jin;Lee, Yeon-Hee;Kang, Soo-Kyung;Auh, Q-Schick;Hong, Jung-Pyo;Chun, Yang-Hyun
    • Journal of Oral Medicine and Pain
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    • v.41 no.2
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    • pp.61-71
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    • 2016
  • Purpose: This study was designed to evaluate the comparison between the subjective and the objective evaluation of pain control effect in masticatory muscle pain depending on time and dose change. Methods: The patients were recruited to this study and diagnosed according to the Research Diagnostic Criteria for Temporomandibular Disorders (RDC/TMD). Experimental group were divided into three groups; saline injection group (n=10), morphine 1.5 mg injection group (n=10), and morphine 3.0 mg injection group (n=10). Evaluation list was the subjective pain evaluation (visual analogue scale, McGill pain questionnaire) and the objective pain evaluation (pressure pain threshold [PPT], pressure pain tolerance [PTO]). The subjective and the objective pain evaluation were performed at the times of just before injection, 10 minutes, 30 minutes, 1 hour, 24 hours, and 48 hours after injection. Then, data were statistically analyzed. Results: The results were as follows: 1) There is no statistically significant difference between the results of the subjective and the objective pain evaluation with regard to the short-term (within 1 hour) analgesic effect of morphine sulfate. 2) However, after 1 hour of injection, while the subjective pain evaluation score still decreased, the objective pain evaluation didn't show significant changes in PPT and PTO (1 hour, p<0.05; 24 hours, p<0.01; 48 hours, p<0.001). 3) In comparison to changes in the dose, the McGill pain questionnaire was the most statistically effective method among the subjective pain evaluations (1.5 mg, p<0.05; 3 mg, p<0.01). Conclusions: Therefore, it was revealed that the subjective pain evaluation was more effective to evaluate long-term pain control, and that the McGill pain questionnaire could be an effective way to evaluate pain control depending on dose changes. It requires further investigations with time and dose extension.