• Title/Summary/Keyword: Effective half life

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Inhibition of HIV-1 Replication by the Water-soluble Extract Mixture of Ricini Semen and Coptidis Rhizoma

  • Kim, Kyong-Tai;Park, Se-Young;Hong, Eun-Kyung;Han, Yong-Bok;Kim, Jong-Bae
    • Biomolecules & Therapeutics
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    • v.3 no.3
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    • pp.210-216
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    • 1995
  • Partially purified water-soluble extract mixture from Ricini and Coptidis (named as RIC) showed to be a potent inhibitor of human immunodeficiency virus-1 (HIV-1) replication. RIC was evaluated for in vitro anti-HIV activity using SupTl and H9 cells infected by a recombinant virus (pSVCAT) containing chloramphenicol acetyltransferase (CAT) gene substituted for nef gene in the HIV-1 genome. RIC inhibited syncytiaformation of SupTl cells with a half maximal effective concentration, $IC_{50}$/, of 2.5 $\mu\textrm{g}$/mι and showed marked inhibition of CAT activity in the infected H9 cells and also suppressed reverse transcriptase (RT) activity in the supernatant of the infected H9 culture. However, RIC did not inhibit the activity of reverse transcriptase directly when it was mixed with the enzyme or with viral particles. Berberine, one of components of RIC, also showed similar anti-HIV activity as RIC did. The data suggest that there are active ingredients which mediate anti-HIV activity in RIC.

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Binding Mode Studies of Indenoisoquinoline Analogues into Human Topoisomerase I-DNA Complex Using Flexible Docking (Human Topoisomerase I-DNA 절개가능 복합체에 대한 Indenoisoquinoline 유도체들의 결합양상 연구)

  • Park, In-Seon;Kim, Bo-Yeon;Kim, Choon-Mi;Choi, Sun
    • YAKHAK HOEJI
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    • v.53 no.4
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    • pp.228-234
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    • 2009
  • Topoisomerase I (Topo I) participates in the DNA replication, transcription, and repair. Binding of Topo I inhibitor to the Topo I-DNA cleavage complex forms stabilized ternary complex which blocks DNA religation and ultimately causes cell death. Camptothecin (CPT) and its derivatives have been among the most effective anticancer drugs by inhibition of topo I. However, efforts to synthesize non-CPT drugs have been actively going on because the CPT derivatives have several limitations such as poor solubility, short half-life, and side effects. As an indenoisoquinoline, NSC314622 is not as potent as CPT, but its chemical stability and slower reversibility of the cleavage complex made it a good lead compound. Recently, a series of indenoisoquinoline analogues were synthesized with substituted dimethoxy or methylenedioxy on the aromatic ring and alkylamino on the lactam nitrogen. Some of them showed quite good Topo I inhibitory activity. Using the computer docking program, Surflex-Dock, indenoisoquinoline analogues were docked into the human Topo I-DNA cleavable complex. The docking results showed that the compounds with activity better than NSC314622 intercalated between the -1 and +1 base pairs at the cleavage site, but those with little or no activities did not appear to intercalate. These results could be useful to design new Topo I inhibitors improved than CPT.

Polymer Effects on Appetite Suppression by Lipoic Acid Nanoparticles (리포익산 나노 입자의 식욕 억제에 대한 고분자의 영향)

  • Choi, Hye-Min;Park, Chul-Ho;Lee, Ki-Up;Park, Joong-Yeol;Koh, Eun-Hee;Kim, Hyoun-Sik;Lee, Jong-Hwi
    • Journal of Pharmaceutical Investigation
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    • v.37 no.6
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    • pp.349-354
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    • 2007
  • For decades, the various virtues of ${\alpha}-lipoic$ acid (ALA), a natural material synthesized in most cells, have been intensively studied and proved. Recently it was reported that ALA caused significant bodyweight reduction via appetite suppression. Unfortunately, the efficacy requires an administration over 50 mg/kg. The low bioavailability and the short plasma half life of ALA lead us to explore novel pharmaceutical dosage forms using nanoparticles. In this study, the effect of polymeric stabilizers on the bioavailability improvement of ALA nanoparticles was investigated. The reduction of particle size via nano-comminution technology was successful resulting in volume average particle sizes of 320 - 340 nm. The in vitro release rate of ALA did not reflect the decrease of particle size, possibly because of the self polymerization of ALA during nano-comminution. The type of polymeric stabilizers could not affect the release rate either. However, the in vivo food intake results of ALA showed that nano-suspensions were more effective than microparticles or a salt form. The nano-suspension containing polyvinyl pyrrolidone as the primary stabilizer and polyacrylic acid as the secondary stabilizer showed more improved efficacy for 2 hours.

Effective Half-life of I-131 in Patients with Differentiated Thyroid Cancer Treated by Radioactive I-131 (I-131 치료를 받은 분화갑상선암 환자에서 I-131의 유효반감기)

  • Park, Seok-Gun
    • Nuclear Medicine and Molecular Imaging
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    • v.42 no.6
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    • pp.464-468
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    • 2008
  • Purpose: Effective half life of I-131 ($T_{eff}$) in patients with differentiated thyroid cancer treated by I-131 is must-know value for dose calculation and determination of release time from isolation room. There has been no report about $T_{eff}$ in Koreans. Thus, author tried to measure dose rate without radiation exposure to faculty members and calculated $T_{eff}$. Methods: Probe of radiation survey meter was fixed at the wall of isolation room, and body of survey meter was placed outside the room. With this simple arrangement, author could measure radiation frequently without radiation exposure to faculty members in 68 patient (F=55, M=13, age=$47{\pm}13.7$) treated by I-131 ($3.7{\sim}7.4\;GBq$) for differentiated thyroid cancer from Jan 2006 to Dec 2006. From this data, $T_{eff}$, 48 hr retention rate, and the time necessary to whole body retention of I-131 become less than 1.1 GBq were calculated. Serum creatinine levels were measured before and after thyroid hormone withdrawal. Results: $T_{eff}$ was $15.4{\pm}4.3\;hr$ ($9.4{\sim}32.5\;hr$). There was a loose correlation between $T_{eff}$ and serum creatinine concentration (r=0.45). 48hr retention was $4.9{\pm}4.2%$ ($1{\sim}23%$). Time necessary to whole body retention of I-131 become less than 1.1 GBq was calculated as $47.1{\pm}13.2\;hr$ for 9.25 GBq, $42.1{\pm}11.9\;hr$ for 7.4 GBq, $35.7{\pm}10.0\;hr$ for 5.55 GBq, and $26.7{\pm}7.5\;hr$ for 3.7 GBq dose of I-131. Conclusion: Author successfully measured radiation dose rates in isolated patients treated by high dose of I-131 without radiation exposure to the faculty members with simple arrangement of survey meter probe. Using those data, $T_{eff}$ and some other indices were calculated.

The Awareness of Secondary Teachers and Students toward Animal Dissection in Biology Class (동물 해부실험에 대한 중학교 교사와 학생들의 인식)

  • Lee, Sun-Kyung;Lee, Jae-Young;Kim, In-Ho
    • Journal of The Korean Association For Science Education
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    • v.16 no.4
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    • pp.451-460
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    • 1996
  • The ethical issue is one of the most important themes in both science and environmental education. Especially related to the right of other species, animal dissection has been brought about two contradictory attitudes. In spring 1996, a survey was conducted to assess the status of animal dissection in secondary schools and the awareness of 94 biology teachers and 422 secondary students toward animal dissection. And the meaning of animal dissection in biology class was discussed in terms of environmental education. The findings were as follows: First, most of students(96.6%) had participated once or twice to animal dissection experiments(eg. fish, frog, shellfish, cuttlefish and chicken). And about half of teachers (57.4$\sim$64.9%) and some students(41.9%) felt ethical conflict in animal dissection. Second, many teachers(81.0%) and students(87.1%) thought that animal dissection was effective method to achieve the goal of biology education, but they needed more consideration on the respect for life in animal dissection experiment. Third, many teachers(88.3%) had students, who objected to animal dissection, participate obligatorily or passively. Fourth, teachers and students thought that audio-visual media such as video(teachers 63.5%, students 39.7%), computer simulations(teachers 31.7%, students 28.1%) and models(teachers 22.2%, students 24.1%) could be effective as alternatives. These findings suggest that animal dissection experiment, although it is needed to achieve the goal of biology education, requires careful consideration on the rights of animal and the respect for life, and alternatives for students who object to animal dissection in biology class.

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Establishment of the High-Throughput Hair Roots' DNA Isolation System and Verification of Its Appicability for Hanwoo Traceability Using the 11 Microsatellite Makes (대량 모근 시료 DNA 분리 체계 확립과 11 microsatellite maker를 사용하는 한우 생산이력제로의 적용가능성 검증)

  • Lim, Hyun-Tae;Lee, Sang-Ho;Yoo, Chae-Kyoung;Sun, Du-Won;Cho, In-Cheol;Yoon, Du-Hak;Yang, Dae-Young;Cheong, Il-Cheong;Lee, Jung-Gyu;Jeon, Jin-Tae
    • Journal of agriculture & life science
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    • v.44 no.6
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    • pp.91-99
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    • 2010
  • We used a multiplex PCR primer set composed of 11 microsatellite (MS) markers and two sexing markers for gender detection. Genomic DNA extracted from hair roots of 3,510 Hanwoo were genotyped. Based on the 11MS markers, no animals had identical genotypes(TGLA227, BM2113, TGLA53, ETF10, SPS115, TGLA122, ETH3, ETH225, BM1824 and INRA23). The expected probability of identity among genotypes of random individuals (PI), the probability of identity among genotypes from random half-sibs ($PI_{half-sibs}$) and among genotypes of random individuals, and the probability of identity among genotypes from random sibs ($PI_{sibs}$) were estimated as $1.31{\times}10^{-23}$, $2.52{\times}10^{-16}$and $1.09{\times}10^{-6}$, respectively using the API-CALC program, version 1.0. We successfully completed the genotype analysis of 3,510 Hanwoo with a 3.93% genotyping failure rate. It was revealed that extracting DNA from the hair root was a time-efficient and cost-effective method to collect specimens for DNA isolation from live animals. This method also minimized stress for the animals during specimen collection. Among the hair roots from the back, belly, upper tail and lower tail, 5~13 hair roots of the lower tail led to the best genotype analysis results. Finally, we established a 96-well-format method of DNA preparation applicable for high- throughput genotype analysis.

Photodegradation of some Organophosphorous Pesticides (일부 유기인계 농약의 광분해성)

  • 민경진;차춘근
    • Journal of Food Hygiene and Safety
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    • v.14 no.4
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    • pp.339-345
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    • 1999
  • The present study was performed to investigate photodegradation rate constants and degradation products of dichlorvos and methidathion by the USEPA method. The two pesticides were very stable in sunlight for 16 days from September 2 to 18, 1998 and humic acid had no sensitizing effect on the photolysis of each pesticide in sunlight. The photolysis rate was fast-est for methidathion, followed by dichlorvos in the presence of UV irradiation. Photodegradation rate constant and half-life of dichlorvos were 0.0208 and 33.3 min, respectively. Photodegradation rate constant and half-life of methidathion were 0.6789 and 1.0min, respectively. The two pesticides were degraded completely in the presence of UV irradiation and UV irradiation with TiO$_2$in about 3 hours. Therefore, it is suggested that UV treatment will be effective for the degradation of pesticides in the process of drinking water purification. In case of dichlorvos and methidathion, UV irradiation with TiO$_2$was more effective for degradation than W irradiation. In order to identify photolysis products, the extracts of degradation products were analyzed by GC/ MS. The mass spectrum of photolysis products of dichlorvos was at m/z 153, those of the photolysis of methidathion were at m/z 198 and 214, respectively. Photolysis products of dichlorvos was Ο, Ο-dimethyl phosphate(DMP), those of methidathion were Ο, Ο-dimethyl phosphorothioate(DMTP) and Ο, Ο-dimethyl phosphorodithioate (DMDTP).

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Removal of Diclofenac, Ibuprofen and Naproxen using Oxidation Processes (산화공정에서의 Diclofenac, Ibuprofen 및 Naproxen의 제거특성 평가)

  • Son, Hee-Jong;Yoo, Soo-Jeon;Hwang, Young-Do;Roh, Jae-Soon;Yoo, Pyung-Jong
    • Journal of Korean Society of Environmental Engineers
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    • v.31 no.10
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    • pp.831-838
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    • 2009
  • In order to evaluate a removal characteristic of diclofenac, ibuprofen and naproxen by oxidizing agents, $Cl_2,\;O_3$ and $O_3/H_2O_2$ are used as oxidants in this study. In case of that $Cl_2$ is used for oxidizing pharmaceuticals, ibuprofen is not removed entirely at $Cl_2$ dose range of 0.5~5.0 mg/L for 60 minutes, however, removal tendency of diclofenac and naproxen are so obviously at $Cl_2$ dose higher than 0.5 mg/L. In addition, as $Cl_2$ dose and contact time are increased, the removal rate of diclofenac and naproxen is enhanced. When $O_3$ is used as oxidizing agent, ibuprofen is not eliminated at $O_3$ dose range of 0.2~5.0 mg/L. On the contrary, 72~100% of diclofenac and 49~100% of naproxen are removed at $O_3$ dose of 0.2~5.0 mg/L. From experiments using $O_3/H_2O_2$ as an oxidant, we can find that $O_3/H_2O_2$ is much more effective than $O_3$ only for removal of diclofenac and naproxen. Moreover, the efficiency is raised according to increase of $H_2O_2$ dose, however, experiments using $O_3/H_2O_2$ show that oxidation of pharmaceuticals is less effective as $H_2O_2$ to $O_3$ ratio increased to above approximately 1.0. On reaction rate constant and half-life of diclofenac, ibuprofen and naproxen depending on $Cl_2$, $O_3$ and $O_3/H_2O_2$ dose, an oxidation of pharmaceuticals by $Cl_2$ and $O_3$ particularly has a comparatively high reaction rate constant and short half-life comparing $O_3/H_2O_2$. From above results, we can fine that diclofenac and naproxen can be easily eliminated in oxidation processes.

A Case of Spindle Cell Hemangioendothelioma Involving the Lung, Mediastinum and Brain (폐, 종격동 및 뇌를 침범한 방추세포형 혈관내피종 1예)

  • Kim, Hwan-Tae;Kim, In-Ho;Lee, Bong-Choon;Kang, Chang-Il;Yoon, Hye-Kyoung
    • Tuberculosis and Respiratory Diseases
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    • v.40 no.3
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    • pp.301-307
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    • 1993
  • Intravascular bronchioloalveolar tumor is now recognized as a pulmonary form of hemangioendothelioma(HE). HE is an unusual tumor of adult life which is characterized by proliferation of an "epithelioid" or "spindle" endothelial cell. In the lung it usually presents as multiple bilateral slowly growing nodules less than 2 cm in diameter. The aetiology and pathogenesis of this disease are unknown. Spindle cell HE occurs at any age, but approximately one half of patient are 25 years of age or younger and males are affected twice more frequently than females. On light microscopic examination, the tumor show mild cellular atypia, nearly absent mitoses and electron-microscopic studies reveal evidence of endothelial cell differentiation. Intracytoplasmic localization of Factor VIII-related antigen is demonstrated on immunohistochemical study, which confirmed the endothelial origin of the tumor. No effective therapy is yet known for HE, but survival of this tumor can be quite long. However, one half of the patient have died, usually of progressive pulmonary insufficiency. This 19-yr-old male complained of Rt. chest pain and intermittent hemoptysis. Simple chest film and chest CT scan showed the Rt. pleural effusion, variable sized bilateral pulmonary nodules, irregular large heterogenous tumor with well enhancement and extensive necrosis in the anterior mediastinum. The mediastinal mass was biopsied and diagnosed as spindle cell HE by light microscopic finding and immunohistochemical studies.

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Effect of Temperatures on the Development and Fecundity of Liriomyze chinensis (Diptera: Agromyzidae) (파굴파리의 발육과 산란에 미치는 온도의 영향)

  • 황창연;문형철
    • Korean journal of applied entomology
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    • v.34 no.1
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    • pp.65-69
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    • 1995
  • This study was carried out to investigate the development and fecundity of Liriomyze chinensis under different temperatures. Egg periods were 4.5, 2.9 and 1.9 days, larval periods 12.7, 5.8, 4.5, days, pupal periods 20.1, 16.3 and 13.0 days, and total development periods from egg to adult emergence were 32.5, 25.0 and 19.4 days under 20, 25, $30^{\circ}C$ of constant temperatures, respectively. Based on this results, developmental threshold temperatures were calculated as 13.0, 11.0 and $7.2^{\circ}C$ and total effective temperatures as 33.0, 86.1 and 293.6 degree-days for egg, larva and pupa, respectively. seventy-eight% of the tested files emerged within four hours and a half after lighting, and none was emerged after eight hours and a half. The longevities of male and female were 5.0 and 8.5 days and the female fly laid 165.8 eggs with her life and punctured 983.8 stipples at $25^{\circ}C$.

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