• 제목/요약/키워드: Drug screening

검색결과 536건 처리시간 0.024초

사상성 곰팡이 (Monascus sp.) 유래 항암 물질의 탐색 (Screening of Anti-cancer Compounds Originated from Filamentous Fungi (Monascus sp.))

  • 신영민;박혜련;안원근
    • 동의생리병리학회지
    • /
    • 제19권3호
    • /
    • pp.671-676
    • /
    • 2005
  • In this study, we investigated the antioxidant effect of extract from Monascus pillosus, on the human wild-type p53 and p21 expressing A549 lung epithelial cell line and MCF-7 mammary adenocarcinoma cell line stimulated by NO. $P21^{waf/cip1}$ was identified as a gene induced in senescent cells. It is a cyclin-dependent kinase inhibitor and has been shown to cause cell cycle arrest and apoptosis. While p53-regulated stimulation of p21 appears to be central for the permanent growth-arrest, the role of p21 in p53-triggered cell death is unclear. Low dose of sodium nitroprusside (SNP) induced the development of senescence associated with increased expression of p53 and p21 in A549 cells. Inhibition of p21 transactivating activity requires high level correlates with the amount of p53 necessary to cause cell death. Association of p21 and p53 results in inhibition of p21-stimulated transcription. This requires a higher p53 level than is necessary for transcriptional activation of endogenous p53-responsive gene but correlates well with the level of p53 necessary to cause cell death. Exposure to W-1 inhibited oxidative stresses-induced senescence-like arrest, resulting in a significant reduction in p53 and p21 steady state levels. These results suggest that p53 and p21 play a central role in the onset of senescence. Thus, it is important to emphasize control of oxidative balance in tumor prevention and aging.

단미 한약 복용중 발견한 Gilbert's syndrome 2예 임상고찰 (Report on Two Cases of Gilbert's Syndrome Found in the Process of Administering Herbs)

  • 이종덕;김동웅
    • 동의생리병리학회지
    • /
    • 제28권6호
    • /
    • pp.657-661
    • /
    • 2014
  • Gilbert's syndrome is one that shows a benign course with intermittent unconjugate hyperbilirubinemia without any evidence of hepatobiliary tract disease or hemolysis. It is often found in a health examination or blood laboratory test by chance. In particular, patients who are taking drugs, including herbal medicine should be careful for their medication due to the possibility of associations with changes in liver function because of drug metabolism, sometimes they have to quit the use of the medication for a certain period and often they should get an additional test. Two male patients increased serum total bilirubin level without other systemic symptoms in screening test for clinical herb medicine pharmacokinetics study. Therefor they was diagnosed with suspected Gilbert's syndrome. They had been calory deprivation test with 24 hours fasting state. They also performed liver function test and ultrasonogram for evaluation of hepatobiliary tract disease. Total serum bilirubin was markedly increased, especially unconjugate bilirubin level higher over the two times than base line after they had been calory deprivation for 24 hours, They was not found another abnormality all laboratory results and physical examination. This study is a report on two cases of hyperbilirubinemia, diagnosed as Gilbert's syndrome, which were found in the process of a clinical pharmacokinetic study of a decoction of medicinal herbs.

Fusarium 곰팡이독소 T-2 독소와 HT-2 독소의 국.내외 연구동향 (Trends in Researches of Fusarium Mycotoxins, T-2 toxin and HT-2 toxin in Domestic and Foreign Countries)

  • 이수진;김미혜;오상석;전향숙
    • 한국식품위생안전성학회지
    • /
    • 제27권1호
    • /
    • pp.1-17
    • /
    • 2012
  • T-2 toxin and HT-2 toxin, belong to type A trichothecences, are the most toxic mycotoxins among the trichothecene family. These mycotoxins are commonly found in cereals such as maize, wheat, barley, oats and rice, and their occurrence in food can be of concern. This review investigated the current trends of patents and researches on T-2 toxin and HT-2 toxin pertaining to natural occurrence, toxicity, metabolism, risk assessment, analytical and screening methods, and reduction/detoxification techniques. As compared with other $Fusarium$ mycotoxins, there are limited data for natural occurrence and risk assessment, and regulatory limit and official analytical methods on T-2 toxin and HT-2 toxin in domestic and foreign countries. In particular, selective deacetylation at the C3 and/or C4 positions of T-2 toxin by carboxyesterase present in foods was reported to cause the disappearance of T-2 and the extremely high HT-2 recoveries. Currently, regulatory limits for T-2 and HT-2 are under discussion in EU. For enforcement purposes it is essential to have available precise and reliable analytical methods applicable at the regulatory levels for the T-2 toxin and HT-2 toxin and relevant commodities. In addition, a further study on natural occurrence, risk assessment and reduction/detoxification techniques will be recommended.

High Throughput 프로세스에서 품질혁신의 성능평가를 위한 Z-Factor의 적용방안 (Implementation of Z-Factor Statistics for Performance Evaluation of Quality Innovation in the High Throughput Process)

  • 최성운
    • 대한안전경영과학회지
    • /
    • 제15권1호
    • /
    • pp.293-301
    • /
    • 2013
  • The purpose of this study is to introduce the limit of previously used six sigma quality process evaluation metrics, $Z_{st}$ and $P_{pk}$, and a solution to overcome this drawback by using a metric based on performance evaluation of Z-factor quality innovation. Case analysis on projects from national six sigma contest from 2011 to 2012 is performed and literature review on new drug development HTS (High Throughput Screening) is used to propose innovative performance evaluation metrics. This research shows that experimental study on six sigma evaluation metric, $Z_{st}$ and $P_{pk}$, have no significance difference between industrial type (Manufacturing, Semi-Public Institute, Public Institute) and CTQ type (Product Technology Type CTQ, Process Technology Type CTQ). Following discovery characterize this quality improvement as fixed target type project. As newly developed moving target type of quality innovation performance metric Z-Factor is used for evaluating experimental study, hypothetical analysis suggests that $Z_{st}$ and $P_{pk}$ share different relationship or even show reciprocal relationship. Constraints of the study are relatively small sample size of only 37 projects from past 2 years and conflict on having interview and communication with six sigma quality practitioner for qualitative experimental study. Both moving target type six sigma innovation project and fixed target type improvement project or quality circle enables efficient ways for a better understanding and quality practitioner use by applying quality innovation performance metric. Downside of fixed target type quality performance evaluation metric, $Z_{st}$ and $P_{pk}$, is presented through experimental study. In contrast, advantage of this study is that high throughput requiring product technology, process technology and quantum leap typed innovation effect is evaluated based on precision and accuracy and Z-Factor that enables relative comparison between enterprises is proposed and implemented.

생약복합제 Pulmuone Healthy Aloe Gel의 위장질환 개선 효과 (Antigastritic and Antiulcerative Effect of Pulmuone Healthy Aloe Gel)

  • 강민희;조소연;김현수;김동현;정춘식
    • 약학회지
    • /
    • 제49권3호
    • /
    • pp.237-243
    • /
    • 2005
  • Present study was performed for the development of a new supplementary product with gastroprotective effect. The preliminary screening were conducted for the effects of HCl-ethanol-induced gastric lesions in rats. Samples were aloe gel, active hexose correlated compound (AHCC) mentioned that have GI protective property and pulmuone healthy aloe gel (PHAG) that mixture of natural products from Pulmuone company. Aloe gel significantly inhibited HCl-ethanol-induced gastric lesions at the oral dose of 5 ml/kg. AHCC showed the strongest effectiveness at the oral dose of 1,200 mg/kg. PHAG also showed the significant effects at the oral dose of 10, 20 g/kg. In pylorus ligated rats, the treatments of aloe gel, AHCC and PHAG showed decrease in the volume of gastric secretion and acid output. And aloe gel, AHCC and PHAG significantly suppressed the aspirin-induced ulcer and chronic ulcer in pylorus ligated rats. The treatments of aloe gel and PHAG significantly reduced acetic acid-induced ulcer at the oral dose of 5 ml/kg and 10 g/kg for 12 days. In this study; we have found that PHAG had significant improvement in acute gastritis and ulcer at the dose of 20 g/kg and in chronic gastritis and ulcer at the dose of 10 g/kg. Also we evaluated the anti-bacterial activity against H. pylori treated with aloe gel, AHCC and PHAG. PHAG had a equivalent anti bacterial activity with ampicillin against H. pylori at the dose of 1 g/kg.

A Curcuminoid and Two Sesquiterpenoids from Curcuma zedoaria as Inhibitors of Nitric Oxide Synthesis in Activated Macrophages

  • Jang, Mi-Kyung;Lee, Hwa-Jin;Kim, Ji-Sun;Ryu , Jae-Ha
    • Archives of Pharmacal Research
    • /
    • 제27권12호
    • /
    • pp.1220-1225
    • /
    • 2004
  • The overproduction of nitric oxide (NO) by inducible nitric oxide synthase (iNOS) is known to be responsible for vasodilation and hypotension observed in septic shock and inflammation. Inhibitors of iNOS, thus, may be useful candidates for the treatment of inflammatory diseases accompanied by overproduction of NO. In the course of screening oriental anti-inflammatory herbs for the inhibitory activity of NO synthesis, a crude methanolic extract of Curcuma zedoaria exhibited significant activity. The activity-guided fractionation and repetitive chromatographic procedures with the EtOAc soluble fraction allowed us to isolate three active compounds. They were identified as 1,7-bis (4-hydroxyphenyl)-1,4,6-heptatrien-3-one (1), procurcumenol (2) and epiprocurcumenol (3) by spectral data analyses. Their concentrations for the 50% inhibition of NO production $(IC_{50})$ in lipopolysaccharide (LPS)-activated macrophages were 8, 75, 77 ${\mu}M$, respectively. Compound 1 showed the most potent inhibitory activity for NO production in LPS-activated macrophages, while the epimeric isomers, compound 2 and 3 showed weak and similar potency. Inhibition of NO synthesis by compound 1 was very weak when activated macrophages were treated with 1 after iNOS induction. In the immunoblot analysis, compound 1 suppressed the expression of iNOS in a dose-dependent manner. In summary, 1,7-bis (4-hydroxyphenyl)-1,4,6-heptatrien-3-one from Curcuma zedoaria inhibited NO production in LPS-activated macrophages through suppression of iNOS expression. These results imply that the traditional use of C. zedoaria rhizome as anti-inflammatory drug may be explained at least in part, by inhibition of NO production.

요양병원 입원 노인의 자아존중감에 따른 건강상태와 간이영양상태 비교 (Comparison of Health Status and Mini Nutritional Assessment according to Self-esteem of Elderly in Care Hospital)

  • 김은미;권진
    • 동아시아식생활학회지
    • /
    • 제25권4호
    • /
    • pp.631-642
    • /
    • 2015
  • The purpose of the study was to examine health status and mini nutritional assessment (MNA) according to self-esteem status of elderly in care hospital. The survey was carried out from $13^{th}$ to $31^{st}$ of September, 2014 in five care hospitals. Analysis was performed for 226 subjects. Evaluation criteria included demographics, clinical status, MNA, health-related quality of life (EQ-5D) and self-esteem. The SE I, SE II and SE III groups were divided by self-esteem scores. Data were analyzed one-way ANOVA, Duncan' multiple range test and Pearson's correlation using SPSS 15.0. Education level, religion, dental condition and medical endurance type were significantly different in all groups. Many elderly people were normal BMI ($20.94{\sim}21.67kg/m^2$). Self-esteem significantly increased in order of SE I, SE II and SE III. Mobility, usual activity and anxiety or depression were significantly different in all groups, and EQ-5D of SE II and SE III groups were significantly higher than that of SE I group. Comparison of MNA screening score in elderly patients was as follows : Score for food intake, psychological stress or acute disease, neuropsychological problems, pressure scores or skin ulcer, protein intake, mode of feeding, nutritional status and health status in SE I group were significantly lower than those of SE II and SE III groups. Mobility and drug intake of SE I group were significantly lower than those of SE III groups. Fruit and vegetable intake SE I group were significantly higher than those of SE II and SE III groups. MIS (Malnutrition Indicator Score) was significantly different among the SE I, SE II and SE III groups. We conclude that self-esteem score is positively correlated with protein intake, nutrition status, health status and MIS in elderly care hospital. To improve nutritional status of elderly in care hospitals, systematic nutrition management and self-esteem education program should be implemented.

Pharmacophore Design for Anti-inflammatory Agent Targeting Interleukin-2 Inducible Tyrosine Kinase (Itk)

  • Chandrasekaran, Meganathan;Sakkiah, Sugunadevi;Thangapandian, Sundarapandian;Namadevan, Sundaraganesan;Kim, Hyong-Ha;Kim, Yong-Seong;Lee, Keun-Woo
    • Bulletin of the Korean Chemical Society
    • /
    • 제31권11호
    • /
    • pp.3333-3340
    • /
    • 2010
  • A three dimensional pharmacophore model was generated for the molecules which are responsible for anti-inflammatory activities targeting Interleukin-2 inducible tyrosine kinase (Itk). 16 structurally diverse molecules were selected as training set to generate the hypotheses using Discovery Studio v2.1. The best hypothesis, Hypo1, comprises two hydrogen bond acceptor (HBA), one hydrophobic aromatic (HA), one ring aromatic (RA) and shows high cost difference (63.71), high correlation coefficient (0.97) as well as low RMS deviation (0.81). Hypo1 has been further validated toward a test set, decoy set and Fischer's randomization method. Furthermore, Hypo1 was used to screen NCI and Maybridge databases. Finally, 2 hit molecules were identified as potential leads against Itk, which may be useful for future drug development.

Fission Yeast-based Screening to Identify Putative HDAC Inhibitors Using a Telomeric Reporter Strain

  • Chung, Kyung-Sook;Ahn, Jiwon;Choi, Chung-Hae;Yim, Nam Hui;Kang, Chang-Mo;Kim, Chun-Ho;Lee, Kyeong;Park, Hee-Moon;Song, Kyung-Bin;Won, Misun
    • Molecules and Cells
    • /
    • 제26권1호
    • /
    • pp.93-99
    • /
    • 2008
  • Transcriptional silencing is regulated by promoter methylation and histone modifications such as methylation and acetylation. We constructed a Schizosaccaromyces pombe reporter strain, KCT120a, to identify modifiers of transcriptional silencing, by inserting the $ura4^+$ gene into a heterochromatic telomere region. Two compounds inhibited the activity of histone deacetylases, induced acetylation of histone H3 and caused apoptotic cell death in HeLa cells. Expression of gelsolin and $p21^{waf1/cip1}$ also increased, as it does in response to HDAC inhibitors such as TSA. Therefore, these compounds appear to be potent inhibitors of HDACs, and hence potential anti-cancer drugs. Our observations suggest that a yeast cell-based assay system for transcriptional silencing may be useful for identifying histone deacetylase inhibitors and other agents affecting chromatin remodeling.

한방병원에 입원한 환자군에서 간기능 검사 이상자의 빈도 조사 (Incidence of Liver Function Test Abnormality among Patients Hospitalized in an Oriental Hospital)

  • 한창우;김수영;민관식;이진혁;이상호;윤유석
    • 대한한의학회지
    • /
    • 제31권2호
    • /
    • pp.109-113
    • /
    • 2010
  • Objectives: Liver function tests are used as screening tests for liver injuries, but their inaccuracy on positive predictive values can result in numerous false positive results. We investigated the incidence of liver function test abnormalities of patients who came to an oriental medicine hospital, in order to present a practical way to rule out false positive results for other studies designed to investigate the safety of Korean herb medicine. Methods: We analyzed the medical records and liver function test results proceeded at admission of all in-patients admitted to Jaseng Oriental Medicine Hospital, from July 2008 to June 2009. Results: Among 1,117 inpatients, 941 executed liver function tests on admission, and 40 were excluded due to their diagnosed liver disease. 747 (82.9%) of 901 enrolled patients were within the normal range of all liver function tests, and 140 (15.5%) and 14 (1.6%) were classified as "abnormalities of liver tests" and "liver injury" respectively, according to the CIOMS (Council for International Organizations of Medical Sciences) criteria. Conclusions: According to the results, among the outcomes of liver function tests proceeded among the patients admitted to the oriental medicine hospital, excluding who were diagnosed with liver disease, 17.1% showed abnormality. This means simple liver function test results are not sufficient in determining liver toxicity of Korean herb medicine (KHM).