• Title/Summary/Keyword: Derivative values

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Compounds Obtained from Sida acuta with the Potential to Induce Quinone Reductase and to Inhibit 7,12-Dimethylbenz-[a]anthracene-Induced Preneoplastic Lesions in a Mouse Mammary Organ Culture Model

  • Jang, Dae-Sik;Park, Eun-Jung;Kang, Young-Hwa;Su, Bao-Ning;Hawthorne, Michael-E.;Vigo, Jose-Schunke;Graham, James-G.;Cabieses, Fernando;Fong, Harry H.S.;Mehta, Rajendra-G.;Pezzuto, John-M.;Kinghorn, A.-Douglas
    • Archives of Pharmacal Research
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    • v.26 no.8
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    • pp.585-590
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    • 2003
  • Activity-guided fractionation of the EtOAc-soluble extract of the whole plants of Sida acuta using a bioassay based on the induction of quinone reductase (OR) in cultured Hepa 1c1c7 mouse hepatoma cells, led to the isolation of ten active compounds of previously known structure, quindolinone (1), cryptolepinone (2), 11-methoxyquindoline (3), N-trans-feruloyltyramine (4), vomifoliol (5), loliolide (6), 4-ketopinoresinol (7), scopoletin (8), evofolin-A (9), and evofolin-B (10), along with five inactive compounds of known structure, ferulic acid, sinapic acid, syringic acid, ($\pm$)-syringaresinol, and vanillic acid. These isolates were identified by physical and spectral data measurement. A new derivative of quindolinone, 5,10-dimethylquindolin-11-one (1a) was synthesized and characterized spectroscopically. Of the active substances, compounds 1-3 and 1a exhibited the most potent QR activity, with observed CD (concentration required to double induction) values ranging from 0.01 to 0.12 $\mu$ g/mL. Six compounds were then evaluated in a mouse mammary organ culture assay, with cryptolepinone (2), N-trans-feruloyltyramine (4), and 5,10-dimethylquindolin-11-one (1a) found to exhibit 83.3, 75.0, and 66.7% inhibition of 7,12-dimethylbenz[a]anthracene-induced preneoplastic lesions, respectively, at a dose of 10 $\mu\textrm{g}$/mL.

Single Photo Resection Using Cosine Law and Three-dimensional Coordinate Transformation (코사인 법칙과 3차원 좌표 변환을 이용한 단사진의 후방교회법)

  • Hong, Song Pyo;Choi, Han Seung;Kim, Eui Myoung
    • Journal of the Korean Society of Surveying, Geodesy, Photogrammetry and Cartography
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    • v.37 no.3
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    • pp.189-198
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    • 2019
  • In photogrammetry, single photo resection is a method of determining exterior orientation parameters corresponding to a position and an attitude of a camera at the time of taking a photograph using known interior orientation parameters, ground coordinates, and image coordinates. In this study, we proposed a single photo resection algorithm that determines the exterior orientation parameters of the camera using cosine law and linear equation-based three-dimensional coordinate transformation. The proposed algorithm first calculated the scale between the ground coordinates and the corresponding normalized coordinates using the cosine law. Then, the exterior orientation parameters were determined by applying linear equation-based three-dimensional coordinate transformation using normalized coordinates and ground coordinates considering the calculated scale. The proposed algorithm was not sensitive to the initial values by using the method of dividing the longest distance among the combinations of the ground coordinates and dividing each ground coordinates, although the partial derivative was required for the nonlinear equation. In addition, since the exterior orientation parameters can be determined by using three points, there was a stable advantage in the geometrical arrangement of the control points.

The Antimelanogenic Effects of Compounds Extracted from Bamboo Inner Film (죽황(竹黃)으로부터 분리한 미백활성 성분의 멜라닌생성 억제효과)

  • Lee, Ki-Moo;Lee, Eun-Chang;Cho, Soon-Chang;Moon, Surk-Sik
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.34 no.4
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    • pp.287-301
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    • 2008
  • In order to develop a new depigmenting agent, extracts were obtained from 60 native plants and their antimelanogenic activities were screened by evaluating the inhibitory effect on tyrosinase which is a major enzyme responsibles for the melanin synthesis. The extracts of Trichosanthes kirilowii fruits, Phyllostachys bambusoides inner films (BIF), Clerodendrum trichotomum leaves, and Acer okamotoanum leaves showed relatively high inhibitory effect on tyrosinase and their $IC_{50}$ values were $50{\sim}100{\mu}g/mL$. The extract of BIF inhibited melanin synthesis of B16F10 melanoma cells by 52%, which was the highest among those of various extracts. Furthermore, the effect of BIF extract is 10% higher than that of arbutin (42%), a popular depigmenting agent in Korea. Ten compounds having antimelanogenic activity were isolated from the BIF extract by solvent extraction and chromatography. These compounds were identified as phenolic derivatives: SM701, SM702, SM703, and BPR211 were hydroquinone derivatives; SM707 a gallic acid derivative; SM704, SM705, SM706, SM708 and SM709 ferulic acid derivatives. The free radical scavenging activities of these compounds were measured and compared to those of hydroquinone and vitamin C. The $SC_{50}$ values scavenging 50% DPPH of SM702 and SM709 were $60{\sim}70{\mu}M$ similar to that of hydroquinone and those of SM701 and SM708 were $30{\sim}40{\mu}M$ slightly lower than that of vitamin C. These results suggest the presence of components having high antioxidant activity in the BIF extract. The SM709, identified as 1,2-O-diferulylglycerol, inhibited the activities of tyrosine hydroxylase and dopa oxidase by 18 and 60%, respectively. The SM709 also inhibited the melanin synthesis of B16F10 melanoma cells by 62% and this was the highest antimelanogenic activity among those obtained from the various purified compounds. Therefore, antimelanogenic activity of the BIF extract was concluded to be due to both inhibition of DOPA oxidase and antioxidant activity.

Rough Set Analysis for Stock Market Timing (러프집합분석을 이용한 매매시점 결정)

  • Huh, Jin-Nyung;Kim, Kyoung-Jae;Han, In-Goo
    • Journal of Intelligence and Information Systems
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    • v.16 no.3
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    • pp.77-97
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    • 2010
  • Market timing is an investment strategy which is used for obtaining excessive return from financial market. In general, detection of market timing means determining when to buy and sell to get excess return from trading. In many market timing systems, trading rules have been used as an engine to generate signals for trade. On the other hand, some researchers proposed the rough set analysis as a proper tool for market timing because it does not generate a signal for trade when the pattern of the market is uncertain by using the control function. The data for the rough set analysis should be discretized of numeric value because the rough set only accepts categorical data for analysis. Discretization searches for proper "cuts" for numeric data that determine intervals. All values that lie within each interval are transformed into same value. In general, there are four methods for data discretization in rough set analysis including equal frequency scaling, expert's knowledge-based discretization, minimum entropy scaling, and na$\ddot{i}$ve and Boolean reasoning-based discretization. Equal frequency scaling fixes a number of intervals and examines the histogram of each variable, then determines cuts so that approximately the same number of samples fall into each of the intervals. Expert's knowledge-based discretization determines cuts according to knowledge of domain experts through literature review or interview with experts. Minimum entropy scaling implements the algorithm based on recursively partitioning the value set of each variable so that a local measure of entropy is optimized. Na$\ddot{i}$ve and Booleanreasoning-based discretization searches categorical values by using Na$\ddot{i}$ve scaling the data, then finds the optimized dicretization thresholds through Boolean reasoning. Although the rough set analysis is promising for market timing, there is little research on the impact of the various data discretization methods on performance from trading using the rough set analysis. In this study, we compare stock market timing models using rough set analysis with various data discretization methods. The research data used in this study are the KOSPI 200 from May 1996 to October 1998. KOSPI 200 is the underlying index of the KOSPI 200 futures which is the first derivative instrument in the Korean stock market. The KOSPI 200 is a market value weighted index which consists of 200 stocks selected by criteria on liquidity and their status in corresponding industry including manufacturing, construction, communication, electricity and gas, distribution and services, and financing. The total number of samples is 660 trading days. In addition, this study uses popular technical indicators as independent variables. The experimental results show that the most profitable method for the training sample is the na$\ddot{i}$ve and Boolean reasoning but the expert's knowledge-based discretization is the most profitable method for the validation sample. In addition, the expert's knowledge-based discretization produced robust performance for both of training and validation sample. We also compared rough set analysis and decision tree. This study experimented C4.5 for the comparison purpose. The results show that rough set analysis with expert's knowledge-based discretization produced more profitable rules than C4.5.

Antifungal activities of coumarins isolated from Angelica gigas and Angelica dahurica against Plant pathogenic fungi (당귀와 백지로부터 분리한 Coumarin계 물질들의 식물병원균에 대한 항균활성)

  • Ryu, Shi-Yong;Kim, Young-Sup;Kim, Heung-Tae;Kim, Seong-Ki;Choi, Gyung-Ja;Kim, Jeoung-Seob;Lee, Seon-Woo;Heor, Jung-Hee;Cho, Kwang-Yun;Kim, Jin-Cheol
    • The Korean Journal of Pesticide Science
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    • v.5 no.3
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    • pp.26-35
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    • 2001
  • In order to search potent antifungal substances from domestic plants, 40 plants cultivated in Korea were collected. After extracting with methanol (MeOH) and concentrating to dryness, the MeOH extracts were screened for in vivo antifungal activity against six plant diseases at a concentration of $2000{\mu}g/mL$. Fourteen extracts showed disease-controlling activity more than 90% against at least one of the 6 plant diseases tested; eight, seven, and three extracts controlled more than 90% the development of rice blast, tomato late blight, and wheat leaf rust, respectively. However, none of the extracts exhibited in vivo antifungal activity more than 90% against rice sheath blight, tomato gray mold, and barley powdery mildew. From the MeOH extracts of Angelica gigas and A. dahurica showing potent controlling activity against rice blast, 1 and 2 antifungal substances, respectively, were isolated by solvent partitioning and column chromatography. The three compounds were identified to be coumarins, namely, decursin, imperatorin, and isoimperatorin, by mass spectrometry and NMR spectroscopy. They were examined for in vitro and in vivo antifungal activities together with umbelliferone (7-bydroxycournarin) and scopoletin (6-methoxy-7-hydroxycoumarin) containing a free hydroxyl group at position 7 to investigate the structure-activity relationship. In vitro, most of 50% growth inhibitory concentrations ($IC_{50}$) were over $200{\mu}g/mL$, indicating that they have relatively weak antifungal activity. The antifungal activity of decursin and scopoletin, containing cyclic alkoxy groups instead of free hydroxyl group at position 7, was stronger than umbelliferone and scopoletin. Especially, decursin and imperatorin showed potent antifungal activities against Pythium ultimum and Magnaporthe grisea, respectively, with $IC_{50}$ values less than $25{\mu}g/mL$. In vivo, decursin and imperatorin showed potent antifungal activity against rice blast, whereas other coumarins hardly controlled the development of 6 plant diseases tested. These results suggest that the antifungal activity of 7-hydroxycoumarin derivative is substantially increased when the hydroxyl group at position 7 is protected by a stable cyclic alkoxy grouping.

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Estimation of Genetic Parameters and Genetic Trends for Major Economic Traits in Swine (종돈의 주요 경제형질에 대한 유전모수 및 유전적 변화 추세 추정에 대한 연구)

  • Kang, Hyun-Sung;Nam, Ki-Chang;Li, Yunxiao;Kim, Kyung-Tai;Lee, Myeong-Seop;Yoon, Jong-Taek;Seo, Kang-Seok
    • Journal of Animal Science and Technology
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    • v.54 no.2
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    • pp.89-94
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    • 2012
  • The objective of this study was to estimate the genetic parameters and breeding value of swine using their economic traits. The traits considered were age at 90 kilograms body weight (D90 kg), backfat thickness (BF) and eye muscle area (EMA). Estimation of genetic parameters and breeding value from 18,668 heads considering the economic traits were based on farm performance data from May 2007 to April 2011. Estimation of genetic parameters based on economic traits revealed that the single best model was fitted after finding source of variance on fixed and random effects and estimated by a multiple trait model using DF-REML (Derivative-FREE Restricted Maximum Likelihood). In this study, the estimated heritabilities of Duroc, Berkshire, Landrace and Yorkshire were about 0.22-0.59 for the D90 kg, 0.47-0.62 for the BF and 0.23-0.37 for the EMA. Genetic correlation of D90 kg with BF and EMA of the four breeds were -0.01-0.24 and -0.35--0.23, respectively. Moreover, the genetic correlation of BF with EMA was -0.68--0.17. On the other hand, the phenotypic correlation of D90 kg with BF and EMA of the four breeds were about 0.01-0.11 and -0.37--0.21, respectively, while the phenotypic correlation of BF with EMA was -0.68--0.17. Results showed that the genetic trends of breeding value every year were decreasing for D90 kg, increasing for BF while for EMA inconsistent values were obtained.

Clinical Efficacy of Erdosteine in Patients with Acute or Chronic Bronchitis -A Randomized, Double Blind, Comparative Study vs. Ambroxol- (급.만성 기관지염 환자에서 엘도스$^{(R)}$(Erdosteine)의 임상효과 -염산 암브록솔과의 무작위 이중맹검 비교시험-)

  • Kim, Seok-Chan;Lee, Sang-Hoak;Song, So-Hyang;Kim, Young-Kyoon;Moon, Hwa-Sik;Song, Jeong-Sup;Park, Sung-Hak
    • Tuberculosis and Respiratory Diseases
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    • v.44 no.6
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    • pp.1296-1307
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    • 1997
  • Background : Erdosteine is a thiol derivative developed for the treatement of chronic obstructive bronchitis, including acute infective exacerbation of chronic bronchitis. Erdosteine has mucomodulating and antioxidant properties and especially exhibits excellent gastrointestinal tolerability. Methods : The study was conducted as a prospective evaluation, with 2 comparative groups orally treated with erdosteine 300mg (bid.) or ambroxol 30mg (b.i.d.) for 7 days and the design of trial was double-blind. The treatments have been assigned randomly to patients (n=80) with acute or chronic bronchitis. The primary end-point used to determine efficacy in this study was subjective symptoms including expectorating frequence, expectoration volume, expectorating difficulty, expectoration viscosity, cough intensity and dyspnea. The secondary end-points of efficacy was the result of arterial blood gas analysis and pulmonary function test. Safety was evaluated with adverse drug reactions and laboratory tests monitoring. 61 patients was included in the efficacy analysis, due to the fact that 19 patients drop-out for different reasons. The obtained values have been analyzed with paired Hest., ANOVA test., multivariate $t^2$-test, repeated measures analysis of covariance, two sample t-test, loglinear-logit model analysis, Fisher's exact test. Results : 1) There was no significant difference on demographic data and vital signs between erdosteine and ambroxol treated groups. 2) The comparison between erdosteine and ambroxol treated groups showed no significant difference in improvement of each symptom in spite of the more favorable efficacy obtained with erdosteine. No difference on the contrary was observed for arterial blood gas analysis and pulmonary function test. 3) As safety is concerned, no clinical significant changes in laboratory test and symptom were induced in erdosteine and ambroxol treated group and two patients in ambroxol treated group drop-out for adverse reactions in symptom. 4) In the evaluation of final clinical efficacy, erdosteine improved more effectively patient's overall symptoms {very good effect (11/31), good effect (12/31), moderate effect (6/31), no effect (2/31), aggravation (0/31)} than ambroxol {very good effect (6/30), good effect (14/30), moderate effect (5/30), no effect (4/30), aggravation (2/30)}. And the probability of symptomatic improvement by erdosteine compared to ambroxol was 2.5 times. (p<0.05). Conclusion : This study showed that erdosteine was clinically effective and safe drug for treatment of acute and chronic bronchitis.

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