• Title/Summary/Keyword: Drug Screening

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Screening of Chinese Herbal Medicines with Inhibitory Effect on Aldose Reductase (X) (중국 약용식물 추출물의 알도즈 환원 효소 억제 효능 검색(X))

  • Choi, So-Jin;Kim, Young Sook;Kim, Joo Hwan;Kim, Jin Sook
    • Korean Journal of Pharmacognosy
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    • v.45 no.4
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    • pp.359-365
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    • 2014
  • Aldose reductase (AR) is the key enzyme of the polyol pathway in the development of the diabetic complications. Sixty seven Chinese herbal medicines have been investigated for inhibitory activities on AR. Among them, 7 herbal medicines, Buddleja crispa (twigs and leaves), Taiwania flousiana (twigs and leaves), Sloanea hemsleyana (fruits), Euphorbia nemetocypha (whole plants), Photinia glomerata (twigs and leaves), Vitex yunnanensis (twigs and leaves) exhibited a significant inhibitory activity against AR. Particularly, S. hemsleyana and V. yunnanensis showed 1.2-4.5 times more potent inhibitory activity than the positive control, 3,3-tetramethyleneglutaric acid (TMG).

Drug Screening for the Formulation of Topical Antiblister Preparations (수포독성 처치용 외용제 제제설계를 위한 약물의 검색)

  • 김동욱;박은석;지상철
    • Biomolecules & Therapeutics
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    • v.7 no.2
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    • pp.191-197
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    • 1999
  • The effects of various drugs on the alleviation of the symptoms of chemical bums were evaluated in mice to formulate topical antiblister preparations. After a chemical bum was induced on the mouse dorsal skin with 2-chloroethylethyl sulfide, the drug was applied on the disease site. The effectiveness of the drug was evaluated by determining blister size, necrosis score of skin and appearance of the chemical burns induced. It showed that steroids and aminoglycoside antibiotics had a tendency to protect skin cell, and antihistamines decreased the size of chemical bums. While oleaginous base resulted in deleterious effect, hydrophilic base didn't show a significant difference on the alleviation of the chemical burn symptoms compared to the control.

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A drug screening system: Preparation of cell islets on the hydrophilic surface

  • Gwon, Hyeok-Seong;Bae, Geun-Won;Jeong, Gyeong-Hui;Kim, Ik-Hwan
    • 한국생물공학회:학술대회논문집
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    • 2002.04a
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    • pp.581-584
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    • 2002
  • Individual surface(hydrophilic/hydrophobic) were prepared and mammalian cells were cultured on the hydrophilic region. For drug test, cancer and normal cells were treated with Taxol, as an example. Our system was compared with MTT assay. CHO cells were resistant to Taxol up to 100 nM in both Methods. However, A549 cells was sensitive at 100 nM Taxol in the 2 day-treatment. Cervical carcinoma cell, HeLa, was very sensitive to Taxol. In our system, the cells were not shown from above 20 nM Taxol treatment. Our system was competitive to MTT assay in animal cells for drug test.

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Identification of inhibitors against ROS1 targeting NSCLC by In- Silico approach

  • Bavya, Chandrasekhar
    • Journal of Integrative Natural Science
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    • v.15 no.4
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    • pp.171-177
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    • 2022
  • ROS1 (c-ros oncogene) is one of the gene with mutation in NSCLC (non-small cell lung cancer). The increased expression of ROS1 is leading to the increase proliferation of cell, cell migration and survival. Crizotinib and Entrectinib are the drugs that have been approved by FDA against ROS1 protein, but recently patients started to develop resistance against Crizotinib and there is a need of new drug that could act as an effective drug against ROS1 for NSCLC. In this study, we have performed virtual screening, where compounds are taken from Zinc 15 dataset and molecular docking was performed. The top compounds were taken based upon their binding affinity and their interactions with the residues. The compounds stability and chemical reactivity was also studied through Density Functional theory and their properties. Further study of these compounds could reveal the required information of ROS1-inhibitor complex and in the discovery of potent inhibitors.

HPLC Analysis and Screening of Standard Compound on Cibotii Rhizoma for Standardization of GCSB-5 Preparation (생약복합제 GCSB-5의 품질 표준화를 위한 구척의 지표성분 탐색 및 HPLC 분석)

  • Cha, Bae-Cheon;Lee, Eun-Hee
    • Korean Journal of Pharmacognosy
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    • v.41 no.1
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    • pp.48-53
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    • 2010
  • GCSB-5 preparation is a purified extract from a mixture of 6 medicinal plants(Acanthopanacis Cortex, Achyranthis Radix, Saposhnikoviae Radix, Cibotii Rhizoma, Glycine Semen Nigra, Eucommiae Cortex) that have been widely used for the treatment of various bone disorders. The aim of this study was to investigate HPLC analysis method and screening of standard compound on Cibotii Rhizoma for quality standardization of a medicinal crude drug GCSB-5. Onitin-4-O-$\beta$-D-glucopyranoside was isolated from Cibotii Rhizoma as the standard compound and identified on the basis of spectroscopic data such as NMR. HPLC analysis method for the determination of onitin-4-O-$\beta$-D-glucopyranoside was established for the quality control of the medicinal plants of Cibotii Rhizoma species, GCSB-5 raw material and GCSB-5 preparation. And validation of HPLC analysis methods were conformed for verification of HPLC methods by check to specificity, linearity, intra-day precision, inter-day precision and accuracy following ICH guideline.

Expression and purification of human mPGES-1 in E. coli and identification of inhibitory compounds from a drug-library

  • Kim, Woo-Il;Choi, Kyung-A;Do , Hyun-Soo;Yu, Yeon-Gyu
    • BMB Reports
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    • v.41 no.11
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    • pp.808-813
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    • 2008
  • Human microsomal prostaglandin E synthase-1 (mPGES-1) is a membrane associated protein that catalyzes the conversion of prostaglandin $H_2$ ($PGH_2$) into prostaglandin $E_2$ ($PGE_2$). In this study, the expression of human mPGES-1 in E. coli was significantly enhanced by modifying the utility of specific codons and the recombinant mPGES-1 was efficiently purified to homogeneity. The $K_m$ and $V_{max}$ of the purified enzyme were determined and the trimeric state characterized by chemical cross-linking with glutaraldehyde. The purified mPGES-1 was used for the screening of a chemical library of bioactive or drug compounds to identify novel inhibitors, and oxacillin and dyphylline were identified as moderately inhibiting mPGES-1 with $I_{C50}$ values of 100 and 200 ${\mu}M$, respectively. As these compounds competitively inhibited the catalysis of $PGH_2$, their binding sites appeared to be located near the $PGH_2$ binding pocket.

Development of Soluble Epoxide Hydrolase Inhibitor Screening Methods for Discovery of Drug Candidate in Cardiovascular Diseases (심혈관계 질환 치료제 후보물질 발굴을 위한 Soluble Epoxide Hydrolase 억제평가 방법 개발)

  • Lee, Gwan-Ho;Kim, Bong-Hee;Kim, Sang-Kyum
    • YAKHAK HOEJI
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    • v.56 no.1
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    • pp.42-47
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    • 2012
  • Soluble epoxide hydrolase (sEH) is a metabolic regulator of epoxyeicosatrienoic acids (EETs). EETs have many beneficial effects, vasodilation, anti-diabetes, anti-inflammation, cardiovascular protection, renal protection. Therefore, selective sEH inhibitors have a potential for treating these diseases. In the present study, screening methods for sEH inhibitors using PHOME ((3-phenyl-oxiranyl)-acetic acid cyano-(6-methoxynaphthalen-2-yl)-methyl ester) and 14-15-EET as substrates were established. To determine selectivity, microsomal epoxide hydrolase (mEH) inhibition assay was also developed using styrene oxide as a substrate of microsomal epoxide hydrolase. Our results obtained from 12-[[(tricyclo[3.3.1.13,7]dec-1-ylamino)carbonyl]amino]-dodecanoic acid (AUDA) used as a positive sEH inhibitor and valpromide used as a positive mEH inhibitor showed that these methods are useful for discovery of drug candidates.

Evaluation of Phototoxicity for Cosmetics and Alternative Method (화장품 광독성 평가와 동물대체시험법)

  • Lee, Jong-Kwon;Sin, Ji-Soon;Kim, Jin-Ho;Eom, Jun-Ho;Kim, Hyung-Soo;Park, Kui-Lea
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.31 no.3 s.52
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    • pp.245-251
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    • 2005
  • Safety is one of the key issue in the regulation of cosmetics. Cosmetic Act deals with it in Korea. The guidance for the testing cosmetic ingredients and their safety evaluation are prepared by Korea Food and Drug Administration. Ultraviolet radiation could Induce skin damage, edema, erythema, photoaging, immune dysfunction and skin cancer. Ultraviolet radiation is classified as Group 2A(probably carcinogenic to humans) by International Agenry for Reaserch on Cancer(IARC). The in vitro methodologies for evaluating the toxic potential of ingredients reported in the literature have not yet been sufficiently validated for use in areas other than the study for mutagenicity/genotoxicity, for pre-screening for severe irritancy, for screening of phototoxicity and for evaluating the percutaneous absorption. The 3T3 neutral red uptake photoxicity test (3T3 NRU PT) was accepted as OECD toxicity guideline in 2002. The 3T3 NRU PT is an in vitro method based on a comparison of the cytotoxicitv of a chemical when tested in the presence and in the absence of exposure to a non-cytotoxic dose of UVA/visible light.

Development of Rapid Analysis Method for Pesticide Residues by GC-MS/MS (GC-MS/MS를 이용한 잔류농약 신속검사법 개발)

  • Choi, Yong-Hoon;Nam, Hye-Seon;Hong, Hye-Mi;Lee, Jin-Ha;Chae, Kab-Ryong;Lee, Jong-Ok;Kim, Hee-Yun;Yoon, Sang-Hyeon
    • The Korean Journal of Pesticide Science
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    • v.9 no.4
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    • pp.292-302
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    • 2005
  • Condition of Ion-Trap gas chromatography-mass spectrometry (GC-MS) for rapid screening of 206-pesticides residues in agricultural foodstuffs was optimized. As applying a wide-bore column (10 m${\times}$0.53 mm, DF 0.25 um) connected with a fused silica restrictor (0.6 m${\times}$0.1 mm), a significant retention time reduction was obtained. Additionally, the shape of peaks was sharper and higher than classical GC's and GC-MS's, which allowed lower detection limits. To easily manage many spectral data, both of Electron Ionization(EI) and Chemical Ionization(CI) techniques were adopted in screening procedure. At the following steps, MS-MS technique were used to confirm screened analytes in complicated matrices.

Recruitment and Selection of Police Officials in the United States -the System and it's Implications- (미국 경찰관 모집·선발제도의 특징 및 함의)

  • Park, Dong-Kyun
    • The Journal of the Korea Contents Association
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    • v.11 no.5
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    • pp.384-392
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    • 2011
  • Recruitment and selection are separate but mutually reinforcing processes. The goal of recruitment is to attract the largest number of applicants possible to apply to the agency, and selection is the process of weeding out unqualified candidates and identifying qualified candidates. In this context, the recruitment and selection system of police officials is an important issue because it affects their future performance as police officers on the job, especially their policing skills, perception of society, occupational ethics. This study suggested the characteristics of U. S. recruitment and selection system of police officials. In the U. S, each police agency sets up its own recruitment and selection standards and procedures. However, recruitment and selection process follows a certain sequence : receiving application, psychological examination, background check, polygraph test, drug screening, interview, physical agility, and medical test. Special characteristic of American police system regarding recruitment and selection is that many law enforcement agencies use a polygraph test to ensure the integrity of the candidates. Another interesting screening process is a drug test because many Americans abuse illegal drugs. A candidate officer must submit urine or a hair sample for screening test. Police human resources specialists should continually identify the most innovative tests and approaches recruit and select police officers. Recruitment and selection strategies should increasingly attract and retain those officers who have the attributes to work in a community-oriented policing environment.