• Title/Summary/Keyword: ED$_{}$ 50/

Search Result 431, Processing Time 0.03 seconds

Studies on Digitalis Receptor Desensitization in Rat Ventricle

  • Lee, Shin-Woong-;Jang, Tae-Soo
    • Proceedings of the Korean Society of Applied Pharmacology
    • /
    • 1994.04a
    • /
    • pp.301-301
    • /
    • 1994
  • $^3$H〕Ouabain binding parameters(K$\_$D/ and B$\_$max/,) in homogenates prepared fpom control rat ventricular strip and Langendorff preparations which were not previously exposed to ouabain were compared to those in homogenates from ventricular strip and Langendorff preparations that had been first exposed to a complete ouabain dose-response curve(10$\^$-7/M to 10$\^$-4/ M). In rat ventricular strips and Langendorff perfused rat heart preparations, cumulative dose-response cruves of ouabain revealed biphasic positive inotropic effects, a "low-dose" and a "high-dose" effect with ED$\_$50/ values of 0.5${\mu}$M and 35${\mu}$M ouabain, respectively- The "low-dose" effect in rat ventricular strips disappeared or was diminished significantly when the ouabain dose-response curve wag repeated after the washout of the effects of the first curve, whereas the maximal "high-dose" effect was identical in both exposures to oubain. However, there was no change in the "low-dose" effects in both sets of the Langendorff perfused hearts. The contractile activity of the pre-exposed strips did not indicate the presence of residual ouabain since their basal contractile force was decreased 10% compared to initial control. 〔$^3$H〕Ouabain binding parameters, K$\_$D/ and B$\_$max/, were not changed comparing homogenate of control ventricular strips with that of strips pre-exposed to ouabain. These results suggest that digitalis receptor desensitization in the rat ventricular strip may due to the change of post-receptor events induced by ouabain binding to a high affinity site(${\alpha}$$_2$ isoform).

  • PDF

Purification and Characterization of CDMHK, a Growth Inhibitory Molecule Against Cancer Cell Lines, from Myxobacterium sp. HK1 Isolated from Korean Soil

  • LEE HAN-KI;LEE IN-HYE;YIM JEE-SUN;KIM YONG-HO;LEE SANG-HEE;LEE KISAY;KOO YOON-MO;KIM SANG-JIN;JEONG BYEONG-CHUL
    • Journal of Microbiology and Biotechnology
    • /
    • v.15 no.4
    • /
    • pp.734-739
    • /
    • 2005
  • Myxobacterium sp. HK1, isolated from Korean soil, degrades cellulose, differentiates to fruiting body, and its 16s rDNA has $95\%$ similarity to Polyangium sp. An anticancer molecule, CDMHK, was identified from culture broth of Myxobacterium sp. HK1, and purified by Diaion HP20, Silica gel, Sephadex LH-20 chromatography, and preparative HPLC using an YMC OSD-A C18 column. The molecular structure and formula were determined to be $C_{l2}H_{l9}N_3O_2$ (M.W 237) by MS spectrometry, 300 MHz $^{1}H\;and\;^{13}C$ NMR. The CDMHK was not active against Escherichia coli, Staphylococcus aureus, and Candida albicans. However, this molecule inhibited the growth of various cancer cell lines. The $ED_{50}$ values of CDMHK were determined to be 0.147, 0.086, 0.18, 0.166, and 0.142 $\mu$g/ml against A549, SK-OV-3, SK-MEL-2, VF498, and HCTl5 cancer cell lines, respectively. In addition, the CDMHK was able to induce apoptosis of the CCRF-CEM cancer cell line, evidenced by DNA fragmentation assay and DAPI staining.

Cytotoxic Effects of Some Transition Metals, Nickel(II), Copper(II) and Zinc(II), with 3.6-bis(2'-pyridyl)pyridazines Complexes (몇 가지 전이금속, Ni(II), Cu(II) 및 Zn(II) 3,6-bis(2'-pyridyl)pyridazine 착 화합물들의 세포 독성효과)

  • Kwon, Byung-Mok;Lee, Chong-Ock;Choi, Sang-Un;Sung, Nack-Do
    • Applied Biological Chemistry
    • /
    • v.49 no.1
    • /
    • pp.21-24
    • /
    • 2006
  • A series of cytotoxic activities $(ED_{50})$ in vitro against six human cancers (lung cancer, uterine cancer, skin cancer, brain cancer, colon cancer and adenocarcinoma) and their seventeen cell lines of 3,6-bis(2'-pyridyl)pyridazine, 1, 3,6-bis-(6'-methyl-2'-pyridyl)pyridazine, 2 and their transition metal, Ni(II), Cu(II) and Zn(II) complexes, $3{\sim}6$ were measured. Particularly, the results revealed that the cytotoxic activities against the brain cancer cell line (SNB-19) and the colon cancer cell line (SW62) of bis- [3,6-bis-(6'-methyl-2'-pyridyl)pyridazine-$k^2N^2,N^3$]chlorocopper(II)perchlorate, 4 were shown to be higher than that of the first generation anticancer agent, Cis-platin.

Basic Oxygen Furnace Slag as a Liming Agent for Paddy and Upland Field Soils (전로슬래그 시용의 토양개량 및 작물의 수량증대 효과)

  • 이충일
    • Resources Recycling
    • /
    • v.7 no.1
    • /
    • pp.50-56
    • /
    • 1998
  • Basic oxygen furnace @OF) slag. a by-pradud of thc iron and steelmaking industry produced in largc quantities in Korea, poszs a subslantial disposal challenge. The BOF slag used in this study was if3 CaCO, in total n e u ~ ~ pnowger and application of 7-8 Mgha' was needed to bring soil pH to 6.5 horn pH 5.0-5.5 m silly clay or clay loam sod wnlained about 10% orgaoic matter. A field assay was conducted to shldg whether BOP slag could bc used as a dolomitic k i n g agent for agricullural soils. Four slag rates (0, 4, 8, 12 Mgha-')were investigated for their effcfect on soil pmperti~, mineral concentralions in leaf tissues of rice and soybean, and yield of the crops. Slag application at 8 Mgha-' rate in paddy field increased pH, Ca Mg, P, Si and Fe wntenl in sail and rice yield by 4.3-14.25 depending an the soil type. h upland field the 8 Mghaf ratc increa3ed pH, Ca and Fe wntent m soil and soybean yield by 36.6%. Thus, BOF slag appears to be a useful liming mate&\ulcornerl for corrzch~gs oil acidity on both paddy and upland ficld soils and for innwing Ca, Mg, P, Si, and Fe wncenhation in plants.

  • PDF

Clinical Features of Acute Acetanilide Herbicide Poisoning (급성 아세트아닐라이드계 제초제 중독의 임상 분석)

  • Park, Cheol-Sang;Lee, Mi-Jin;Park, Seong-Soo;Jeong, Won-Joon;Kim, Hyun-Jin
    • Journal of The Korean Society of Clinical Toxicology
    • /
    • v.9 no.2
    • /
    • pp.49-55
    • /
    • 2011
  • Purpose: Acetanilide has been in widespread use as an amide herbicide compound. However, available data regarding acute human poisoning is scarce. The aim of this study was to analyze the clinical characteristics of acetanilide poisoning in order to identify the risk factors associated with severity. Methods: We conducted a retrospective observational study encompassing the period January 2005 to December 2010, including adult ED patients suffering from acetanilide intoxication. Toxicological history, symptoms observed, clinical signs of toxicity, and laboratory test results were collected for each patient. The patients were classified into two groups for analysis, according their poisoning severity score (PSS). Resulting clinical data and prognostic variables were compared between mild-to-moderate poisoning (PSS 1/2 grades), and severe poisonings and fatalities (PSS 3/4 grades). Results: There were a total of 37 patients, including 26 alachlor, 6 s-metolachlor, 4 mefenacet, and 1 butachlor cases. The majority of patients (81.1%) were assigned PSS 1/2 grades. Changes in mental status and observation of adverse neurologic symptoms were more common in the PSS 3/4 group. The median ingested volume of amide herbicide compound was 250 ml (IQR 200-300 ml) in the PSS 3/4 group, and 80 ml (IQR 50-138 ml) in the PSS 1/2 group. Also, the median GCS observed in the PSS 3/4 group was 13 (IQR 10-14), which was markedly low as compared to a median GCS of 15 in the PSS 1/2 group. Overall mortality rate was 5.4%, and profound cardiogenic shock was observed prior to death in all fatalities. Conclusion: When compared to previous reports, acute acetanilide poisoning resulted in relatively moderate severity. The presence of neurologic manifestations, hypotension, lower GCS score, and larger ingested volumes was associated with more serious effects and mortalities.

  • PDF

Interaction of Antihistaminics with Muscarinic Receptor (III) - Relationship between binding and functional in vitro data -

  • Lee, Shin-Woong;Park, Young-Joo
    • Archives of Pharmacal Research
    • /
    • v.14 no.2
    • /
    • pp.181-187
    • /
    • 1991
  • The muscarinic antagonist 1-[benzilic 4, 4'-$[^3H]$ QUINUCLIDINYL BENZILATE $([^3H]$ QNB) bound to a single class of muscarinic receptors with high affinity in rabbit ileal membranes. The $K_D\;and\;B_{ max}$ values for $([^3H]$ QNB calculated from analysis of saturation isotherms were 52.5 pM AND 154 fmol/mg, respectively. Chlopheniramine (CHP), histamine $H_1$ blocker, increased $K_D$ vlue for $([^3H]$QNB without affecting the binding site concentrations and Hill coefficient. The $K_i$ value of CHP for inhibition of $([^3H]$QNB binding in ileal membranes was 1.44\mu{M}$ and the pseudo-Hill coefficient for CHP was close to unit. In the functional assay carbachol, muscarinic agonist, increased the contractile force of ileum with $ED_{50}$ value of $0.11\mu{M}$. CHP caused the rightward shift of the dose-response curve to carbachol. The $pA_2$ value of CHP determined from Schild analysis of carbacholinduced contraction was 5.77 and the slope was unity indicating competitive antagonism with carbachol. The dissociation constant $(K_i)$ of CHP obtained in competitive experiments with $([^3H]$ QNB was similar to the $K_A$ value (1.69 \mu{M)}$ of CHP as inhibitor of carbachol induced contraction in rabbit ileum. This result suggest that the binding of $H_i$ blocker. CHP, vs $([^3H]$QNB to muscarinic receptors in ileal membranes represents an interaction with a receptor of physiological relevance.

  • PDF

Induction of Growth Hormone Release by Dioscin from Dioscorea batatas DECNE

  • Lee, Ho-Young;Jung, Dae-Young;Ha, Hye-Kyung;Son, Kun-Ho;Jeon, Su-Jin;Kim, Chung-Sook
    • BMB Reports
    • /
    • v.40 no.6
    • /
    • pp.1016-1020
    • /
    • 2007
  • In this study, dioscin was isolated from Dioscoreae Rhizoma (DR), which is the rhizome of Dioscorea batatas DECNE. that inhabits broad areas of Korea and Japan. To determine whether dioscin induced growth hormone (GH) release, we evaluated its induction effects on GH release both in vitro and in vivo. The 70% methanol extract of DR, and its n-hexane and n-BuOH fractions, induced rat GH (rGH) release in rat pituitary cells 10-fold, 8-fold, and 5-fold higher than the control ($0.36{\pm}0.02 nM$), respectively (p < 0.05 each). The dioscin-induced rGH release of the cells was concentration-dependent and its $ED_{50}$ was $1.14{\times}10^{-5} M$. Within 90 minutes after intravenous administration of $10{\mu}g$/kg (p < 0.05 at $t_{max}$), dioscin caused the greatest increase in rGH concentration ($C_{max}$) in the rat plasma ($34.16{\pm}14.10 ng/ml$) (n = 4), which was twice as high as the control group ($12.88{\pm}3.29 ng/ml$) (n = 27).

Efficient Data Management for Hull Condition Assessment

  • Jaramillo, David;Cabos, Christian;Renard, Philippe
    • International Journal of CAD/CAM
    • /
    • v.6 no.1
    • /
    • pp.9-17
    • /
    • 2006
  • Performing inspections for Hull Condition Monitoring and Assessment as stipulated in IACS unified requirements and IMO's Condition Assessment Scheme (CAS) IMO Resolution MEPC.94(46), 2001, Condition Assessment Scheme, IMO Resolution MEPC.111(50), 2003, Amendments to regulation 13G, addition of new regulation 13H involves a huge amount of measurement data to be collected, processed, analysed and maintained. Information to be recorded consists of thickness measurements and visual assessment of coating and cracks. The amount of data and increasing requirements with respect to condition assessment demand efficient computer support. Currently, due to the lack of standardization for this kind of data, the thickness measurements are recorded manually on ship drawings or tables. In this form, handling of the measurements is tedious and error-prone and assessment is difficult. Data reporting and analysis takes a long time, leading to some repairs being performed only at the next docking of the ship or making an additional docking necessary. The recently started ED funded project CAS addresses this topic and develops-as a first step-a data model for Hull Condition Monitoring and Assessment (HCMA) based on XML-technology. The model includes simple geometry representation to facilitate a graphically supported data collection as well as an easy visualisation of the measurement results. In order to ensure compatibility with the current way of working, the content of the data model is strictly confined to the requirements of the measurement process. Appropriate data interfaces to classification software will enable rapid assessment by the classification societies, thus improving the process in terms of time and cost savings. In particular, decision-making can be done while the ship is still in the dock for maintenance.

In vitro and in vivo Antibacterial Activities of the New Quinolone, DWQ-013 (새로운 퀴놀론계 항균제 DWQ-013의 항균작용)

  • Yu, Young-Hyo;Park, Nam-Jun;Kim, Byung-O;Choi, Moon-Jung;Shim, Jeom-Soon;Kang, Tae-Chung;Lee, Jae-Wook;Kim, Dae-Young
    • YAKHAK HOEJI
    • /
    • v.38 no.3
    • /
    • pp.265-273
    • /
    • 1994
  • ln vitro and in vivo antibacterial activities of DWQ-013(1-cyclopropyl-6,8-difluoro-7-(3-methylthiomethylpyrrolidinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid), a new fluoroquinolone antibacterial agent, were compared with those of ciprofloxacin, sparfloxacin and ofloxacin against aerobic and anaerobic standard strains and clinical isolates. DWQ-013 had a broad spectrum and potent antibacterial activity against Gram-positive and Gram-negative bacteria. The antibacterial activity of DWQ-013 against Staphylococcus aureus was equal to that of sparfloxacin(SPFX) and superior to those of ciprofloxacin(CPFX). The antibacterial activity against Gram-negative bacteria was slightly lower than those of ciprofloxacin and sparfloxacin. MIC of DWQ-013 against Pseudomonas aeruginosa$(0.781{\sim}1.563\;{\mu}g/ml)$ was usually equal to that of sparfloxacin$(0.781\;{\mu}g/ml)$ and was inferior to that of ciprofloxacin$(0.098\;{\mu}g/ml)$. The number of viable cells was decreased rapidly after addition of DWQ-013 at concentration of $1{\sim}2$ folds of MIC.

  • PDF

Preventive Effects on Porcine Epidemic Diarrhea(pED) Using by PEDV Antiserum I. Serological Results, RT-PCR for Fecal and Small Intestin, FA Test (함혈청 투여에 따른 돼지 유행성 설사병 예방효과 I. 혈청학적 결과, RT-PCR 검사, 형광항체검사)

  • Chi, Yong-Zhe;Han, Jeong-Hee;Kwon, Hyuk-Moo;Hahn, Tae-Wook;Jeong, Hyun-Kyu;Park, Bong-Kyun;
    • Korean Journal of Veterinary Pathology
    • /
    • v.6 no.1
    • /
    • pp.19-26
    • /
    • 2002
  • The purpose of this study was to investigate to potective effects against porcine epidemic diarrhea virus (PEDV) infection in piglets by administration of the PEDV antiserum orally at 2 hrs, 24hrs and 36hrs after birth. six piglets administered the antiserum were experimentally infected with PEDV at five-day-old. Control group were four piglets infected with PEDV only. Serum antibody titers against PEDV were examined by serum neutralization (SN) test, dectection for PEDV or PEDV antigen from feces and small intestines was tested by reverse transcription-polymerase chain reaction (RT-PCR) and indirect immunoflurescence (IFA). The results obtained were as follows; 1. The piglets administered the PEDV antiserum showed higher antibody titers than those of control group and sustained during the experimental period. 2. The detection rate of PEDV in feces and small intestines by RT-PCR were 26.2% and 16.7% in PEDV antiserum treated group and 48.1 % and 75.0% in control group, respectively. 3. The detection rate of PEDV antigen in the small intestine by IFA were 0% in PEDV antiserum treated group and 50.0% in control group, respectively. It was concluded that oral administration of antiserum against PEDV to piglets was effective in preventing PEDV infection.

  • PDF