• Title/Summary/Keyword: Drug screening

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PFG NMR Study of Intra-cellular Drug Uptake in Xenopus laevis Oocyte

  • Kwan, soo-Hong;Yeom Gyo-Seon;Kim, Eun-Hee;Lee, Chul-hyun;Lee, Sang-Do;Cheong, chae-joon
    • Journal of the Korean Magnetic Resonance Society
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    • v.9 no.1
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    • pp.29-37
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    • 2005
  • Intra-cellular drug uptake in Xenopus laevis oocyte has been elucidated using localized MR spectroscopy (MRS) and PFG NMR techniques at a 600 $MH_z$(Bruker, 14.1 T) NMR spectrometer. The localized MRS has been done with a homemade probe, and shows the intra-cellular uptake of nicotinamide. The self-diffusion of the molecule in Xenopus oocyte was obtained by PFG NMR technique. The measured data are well fitted with a linear combination of two exponential functions, which shows that there are two types of drug molecules, intra-and extra-cellular molecules. Diffusion coefficients of intra- and extra-cellular drug molecules are 3.7 $\times$ $10^{-11}$ $\m^{2}/s$and 6.4 $\times$ $10^{-10}$ $\m^{2}/s$, respectively. In the weighting factors there is shown that about 5% of drug molecule is inside the cells. These techniques can be used for drug screening in molecule-, cell-, and tissue-based preclinical test.

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Development of Primer Sets for the Detection of Polygonum multiflorum, Cynanchum wilfordii and C. auriculatum (유전자 마커를 이용한 하수오, 백수오 및 이엽우피소 종 판별법 개발)

  • Kim, Kyu-Heon;Kim, Yong-Sang;Kim, Mi-Ra;Lee, Ho-Yeon;Lee, Kyu Ha;Kim, Jong Hwan;Seong, Rack Seon;Kang, Tae Sun;Lee, Jin-Ha;Jang, Young-Mi
    • Journal of Food Hygiene and Safety
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    • v.30 no.3
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    • pp.289-294
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    • 2015
  • The aim of this study was to develop rapid screening method for the identification of Chinese herbal medicine species with similar appearance, Polygonum multiflorum, Cynanchum wilfordii and C. auriculatum, by using genetic markers. As a genetic marker, psbA-trnH gene in chloroplast was selected due to differences in sequence among the three species. Species-specific primers were designed based on the sequences of the marker gene of P. multiflorum, C. wilfordii, and C. auriculatum, and the expected size of PCR products was 160, 147, and 119 bp, respectively. Under the developed conditions, cross-reaction was not detected among these three plant species. To confirm the efficiency of our species-specific primers, the optimized method was applied to a variety of processed products composed of mostly P. multiflorum and C. wilfordii, demonstrating that our method was a rapid and easy screening assay. Our findings suggest this screening method can be utilized to prevent the distribution of economically motivated adulteration food and to improve consumer's right.

Current Methodologies for Membrane Permeability Assessment

  • Shin, Beom-Soo;Youn, Yu-Seok;Jeong, Seong-Hoon;Park, Eun-Seok;Lee, Mann-Hyung;Yoo, Sun-Dong
    • Journal of Pharmaceutical Investigation
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    • v.40 no.spc
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    • pp.19-31
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    • 2010
  • Orally administrated drugs permeate the biological membrane by various transport mechanisms. The oral absorption potential is closely related to the physicochemical properties of the drug and interaction with the physiological factors surrounding the site of absorption. Assessment of the drug membrane permeability is an integral part of the early stage drug developmental process. Appropriate selection of the permeability screening method at the right stage of drug development process is important in achieving successful developmental outcomes. This review aims at introducing currently available in vitro and in vivo screening methods for the membrane permeability assessment.

Isolation and Bioactivity Analysis of Salidroside from Acer tegmentosum using On-line Screening HPLC-ABTS+ Assay (On-line Screening HPLC-ABTS+ Assay을 이용한 산청목으로부터 Salidroside의 분리 및 생물활성 분석)

  • Lee, Kwang Jin;Song, Na-Young;Ma, Jin Yeul
    • KSBB Journal
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    • v.29 no.2
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    • pp.124-130
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    • 2014
  • Acer tegmentosum was a traditional Korean herbal medicine showing various pharmacological activities. In this work, A. tegmentosum were extracted with boiling water and then successively partitioned with dichloromethane, ethyl acetate, n-butyl alcohol (n-BuOH), and water. Salidoside, the target compound, was purified in n-BuOH phase using a chromatography method. For the analysis of salidoside, TLC and LC-MS were used as well as on-line screening $HPLC-ABTS^+$ assay with three different wavelength of 254, 280, and 320 nm. An amount of 1.34 g of salidoside were obtained in n-BuOH phase fromAcer tegmentosum was a traditional Korean herbal medicine showing various pharmacological activities. In this work, A. tegmentosum were extracted with boiling water and then successively partitioned with dichloromethane, ethyl acetate, n-butyl alcohol (n-BuOH), and water. Salidoside, the target compound, was purified in n-BuOH phase using a chromatography method. For the analysis of salidoside, TLC and LC-MS were used as well as online screening $HPLC-ABTS^+$ assay with three different wavelength of 254, 280, and 320 nm. An amount of 1.34 g of salidoside were obtained in n-BuOH phase from 3 kg of dry biomass. The on-line screening $HPLC-ABTS^+$ assay is rapid and efficient tool to search bioactivity from A. tegmentosum. 3 kg of dry biomass. The on-line screening $HPLC-ABTS^+$ assay is rapid and efficient tool to search bioactivity from A. tegmentosum.

Herbal Drug Interactions Due to Alteration of Metabolism

  • Woo, Won-Sick
    • Korean Journal of Pharmacognosy
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    • v.25 no.1
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    • pp.1-10
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    • 1994
  • The screening of 150 Chinese drugs which are most frequently prescribed in Korean traditional medicine showed that at least 30% of the drugs affected barbiturate-induced hypnosis. This effect was mainly attributable to the alteration of drug metabolism. Phytochemical works resulted in the isolation of furanocoumarins, lignans, sesquiterpenes and saponins as drug metabolism modifiers. The structure-activity relationship is discussed.

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A NAT for reliable HCV RNA detection from plasma and plasma-derived medicinal products

  • Yoo, Si-Hyung;Jung, Sa-Rah;Park, Su-Jin;Kim, Sun-Nam;Hong, Choong-Man;Lee, Ki-Hong;Oh, Ho-Jung;Kang, Hye-Na;Shin, In-Soo;Choi, Seoung-Eun;Hong, Sung-Ran;Lee, Seok-Ho;Hong, Seung-Hwa
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.300.2-301
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    • 2002
  • HCV is transmitted via various plasma-derived medicinal products. The transmission of HCV could. however, be prevented by screening plasma pools with NAT and validating HCV viral clearance during the manufacturing of plasma derivatives, Although various screening methods including commercial kits are available. it is yet to develop an analytical method to detect HCV in both plasma and plasma derivatives. The objective of this study was to develop a reliable in house method for reliable for the HCV RNA detection from plasma and plasma derivatives. (omitted)

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Protective Effects of the Ethanol Extract of Viola tianshanica Maxim against Acute Lung Injury Induced by Lipopolysaccharides in Mice

  • Wang, Xue;Yang, Qiao-Li;Shi, Yu-Zhu;Hou, Bi-Yu;Yang, Sheng-Qian;Huang, Hua;Zhang, Li;Du, Guan-Hua
    • Journal of Microbiology and Biotechnology
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    • v.27 no.9
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    • pp.1628-1638
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    • 2017
  • Viola tianshanica Maxim, belonging to the Violaceae plant family, is traditionally used in Uighur medicine for treating pneumonia, headache, and fever. There is, however, a lack of basic understanding of its pharmacological activities. This study was designed to observe the effects of the ethanol extract (TSM) from Viola tianshanica Maxim on the inflammation response in acute lung injury (ALI) induced by LPS and the possible underlying mechanisms. We found that TSM (200 and 500 mg/kg) significantly decreased inflammatory cytokine production and the number of inflammatory cells, including macrophages and neutrophils, in bronchoalveolar lavage fluid. TSM also markedly inhibited the lung wet-to-dry ratio and alleviated pathological changes in lung tissues. In vitro, after TSM ($12.5-100{\mu}g/ml$) treatment to RAW 264.7 cells for 1 h, LPS ($1{\mu}g/ml$) was added and the cells were further incubated for 24 h. TSM dose-dependently inhibited the levels of proinflammatory cytokines, such as NO, $PGE_2$, $TNF-{\alpha}$, IL-6, and $IL-1{\beta}$, and remarkably decreased the protein and mRNA expression of $TNF-{\alpha}$ and IL-6 in LPS-stimulated RAW 264.7 cells. TSM also suppressed protein expression of $p-I{\kappa}Ba$ and p-ERK1/2 and blocked nuclear translocation of $NF-{\kappa}B$ p65. The results indicate that TSM exerts anti-inflammatory effects related with inhibition on $NF-{\kappa}B$ and MAPK (p-ERK1/2) signaling pathways. In conclusion, our data demonstrate that TSM might be a potential agent for the treatment of ALI.

Rapid determination and quantification of hair-growth compounds in adulterated products by ultra HPLC coupled to quadrupole-orbitrap MS

  • Lee, Ji Hyun;Park, Han Na;Kang, Gihaeng;Kim, Nam Sook;Park, Seongsoo;Lee, Jongkook;Kang, Hoil
    • Analytical Science and Technology
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    • v.32 no.2
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    • pp.56-64
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    • 2019
  • Recently, a number of adulterated products, which are advertised as hair-growth enhancer have been emerged among those who suffer hair loss disease. For continuous control of illegal products, in this study, a rapid and sensitive method for simultaneous screening of 12 compounds that enhance hair-growth was established to protect public health by ultrahigh-performance liquid chromatography coupled to quadrupole-orbitrap mass spectrometry (UHPLC-Q-Orbitrap-MS). Fragmentation pathways of them were proposed based on $MS^2$ spectral data obtained using the established method. In this analysis, the LODs and LOQs ranged from 0.05 to 50 ng/mL and from 0.17 to 167 ng/mL, respectively. The square of the linear correlation coefficient ($R^2$) was determined as more than 0.995. The intra- and inter-assay accuracies were respective 88-112 % and 88-115 %. Their precision values were measured within 5 % (intra-day) and 10 % (inter-day). Mean recoveries of target compounds in adulterated products ranged from 84 to 115%. The relative standard deviation of stability was less than 12 % at $4^{\circ}C$ for 48 h. The method was employed to screen 14 dietary supplements advertised to be effective for the treatment of hair loss. Some of the products (~21 %) were proven to contain synthetic drugs that promote hair growth such as triaminodil, minoxidil, and finasteride.

Cytotoxicity of Two Novel Cisplatin Analogues, $(CPA)_2Pt[DOLYM]$ and (DACH)Pt[DOLYM], to Human Cancer Cells In Vitro

  • Choi, Sang-Un;Kim, Kwang-Hee;Choi, Eun-Jung;Park, Sung-Hee;Kim, Kwan-Mook;Shon, Youn-Soo;Lee, Chong-Ock
    • Archives of Pharmacal Research
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    • v.22 no.2
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    • pp.151-156
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    • 1999
  • Despite the impressive antitumor activity of cisplatin, two major limitations of the drug, that is severe side effects and drug-resistance of cancer cells, make its use difficult of r cancer therapy. These limitations have resulted in a greate deal of effort having been expended into structural modifications of cisplatin. In this study, we tested two novel cisplatin analogues, (CPA)2 Pt[DOLYM] (COMP-I) and (DACH)Pt[DOLYM] (CoMP-II), for the mode of cytotoxic action against human tumor cells comparing with cisplatin and carboplatin in vitro. These two novel analogues had considerable cytotoxic activities against five kinds of human solid tumor cells, and especially COMP-II was more effective on HCT15 colon cancer cells than other compounds. In addition, COMP-II had cytostatic activity at low concentrations (10~0.3${\mu}g/ml$), but other compounds revealed little effect on tumor growth at the low concentration.

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A Study on Sick Role Behavior of Some Hypertensive Workers (일부 근로자들의 고혈압치료형태에 관한 연구)

  • Lee, Eun-Il;Kim, Soon-Duck;Cha, Chul-Whan
    • Journal of Preventive Medicine and Public Health
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    • v.19 no.2 s.20
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    • pp.203-212
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    • 1986
  • Hypertension is one of the most well known risk factors for cerebrovascular or coronary heart disease and is a major public health problem. Early detection and treatment of hypertension are essential, but the compliance of treatment on hypertension is not easy to achive. Hypertensive workers are being detected by the annual screening under the Labour Standard Law in Korea but the solidified control system for them is not existing. This study about workers 'Motive-Belief-Action in non-drug and drug treatment of their hypertension would be worthwhile to interpret how the workers actually behave in coping with hypertension, and also would be advisable to construct the follow-up program in Korea. In the field research process two criteria were used to select sample group. The first criterion included the workers who were screened to be hypertensive with their blood pressure above 160/95 in this survey. The second one was used to classify study-group respondents who had known their hypertension by successive annual screening. From such criteria a total of 156 male workers were sampled in 21 industries, the author interviewed them using the structured questionnaire which consisted of Belief-Motive-Action items about non-drug and drug treatment for hypertension with open-ended question on symptom of hypertension. The summary is as follows: 1) Sixty-one percent of respondents had ever checked their blood pressure somewhere besides the annual screening. 2) Most respondents(97.2%) complained no symptoms of hypertension at all. 3) Belief level of non-drug treatment was relatively high (82.1%-64.7%), but motive(55.1%-28.2%) and action(38.5%-16.7%) levels were low. 4) Belief level of drug treatment was relatively lower than that of non-drug treatment, blue collar workers showed higher artier level of drug treatment than white collar workers, and correlation coefficient between belief and motive on drug treatment was lower in group of not-recognizing their family history of hypertension than recognized group. Such findings indicated that belief on drug treatment of hypertensive workers would be problematic. 5) White collar workers showed significant lower correlation coefficients between Motive and Action of salt restriction, restriction of fatty diet and relaxation than blue collar workers. 6) Mild hypertension group showed low levels of Motive and Action of non-drug treatment(salt restriction, restriction of fatty diet and relaxation) and also showed low correlation coefficient between Belief and Motive of above non-drug treatment.

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