• 제목/요약/키워드: quinolone

검색결과 237건 처리시간 0.032초

Effects of Temperature on the Pharmacokinetics of Ciprofloxacin in the Cultured Black Rockfish (Sebastes schlegeli) and Olive Flounders (Paralichthys olivaceus)

  • Kim Jin Woo;Jo Mira;Jung Sung Hee;Jee Bo Young;Choi Dong Lim;Jo QTae
    • Fisheries and Aquatic Sciences
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    • 제5권3호
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    • pp.200-205
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    • 2002
  • Temperature-dependent pharmacokinetics of ciprofloxacin (CIP) was studied in the cultured olive flounders, Paralichthys olivaceus, and black rockfish, Sebastes schlegeli using high performance liquid chromatography (HPLC) originally developed for quinolone determination from livestock. Pharmacokinetics of CIP was apparently affected by ambient water temperature. In a two-compartment model for flounders after oral dosage of 20 mg/kg, $K_{01},\;at\;13^{\circ}C$ and $23^{\circ}C$ were 4.18 and 1.20/hr, respectively. The $K_{10},\;T_{max}\;and\;C_{max}\;at\;13^{\circ}C$ were 5.574/hr, l4.37${\mu}g/mL\;and\;3.15{\mu}g/mL,$ respectively. The corresponding values at $23^{\circ}C$ were l2.84/hr, 15.39${\mu}g/mL\;and\;6.38{\mu}g/mL$, respectively. The AUC, $T_{1/2} (\alpha)\;and\;T_{1/2}\;(\beta)$ were 278.23 ${\mu}g \cdot hr/mL$, 0.24hr and 47.02hr at $13^{\circ}C$ and 3l7.8l${\mu}g \cdot hr/mL$, 0.30 hrs and 60.78hrs at $23^{\circ}C$ for the flounder, respectively. Similar CIP pharmacokinetics were revealed in the black rockfish after oral dosage of 20 mg/kg under the two water temperature regimes. These pharmacokinetical results have some implication in the optimal usage of recently introduced antibacterials in the farmed fish, which were primarily adapted for poultry and mammalian species.

14년 동안의 편도주위농양의 임상적 양상의 변화 (The Changes in the Clinical Aspects of Peritonsillar Abscess during the Past 14 Years)

  • 박범석;명남숙;이형주;박홍석;한철우;구수권
    • 대한기관식도과학회지
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    • 제15권2호
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    • pp.57-63
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    • 2009
  • Background and Objectives : Peritonsillar abscess is one of the most common illnesses m the ENT field, though its prevalence has been drastically reduced with the development of antibiotics and appropriate early treatment. We analyzed recent clinical characteristics of peritonsillar abscess and compared them with ones of 7 and 14 years ago respectively. Materials and Methods : Sixty-six cases of peritonsillar abscess from 2006 through 2008 were investigated retrospectively and compared with results of 7 and 14 years ago on various clinical factors. Results : Peritonsillar abscess was prevalent in men in their 20s and 30s. Mean period from symptom onset to visit to hospital tended to decrease(5.2 days) but admission days has increased(7.4 days). Body temperature on admission was lower than that of previous studies($36.4^{\circ}C$). Bacteria were isolated in 26 cases(74.2%) out of 35 cases in which culture had been performed. The most common cultured organism was a-hemolytic streptococcus and $\beta$-hemolytic streptococcus that had been most frequently cultured 14 years ago wasn't detected in this study. Conclusion : We found some changes of clinical features in peritonsillar abscess when compared with previous researches. Although there were some differences in cultured organism, antibiotics used commonly-cephalosporin, aminoglycoside, quinolone - were still effective for their eradication.

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Synthesis of 8-Alkoxy-4,5-dihydro-[1,2,4]triazole[4,3-a]quinoline-1-ones and Evaluation of their Anticonvulsant Properties

  • Sun, Xian-Yu;Jin, Yun-Zhe;Li, Fu-Nan;Li, Gao;Chai, Kyu-Yun;Quan, Zhe-Shan
    • Archives of Pharmacal Research
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    • 제29권12호
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    • pp.1080-1085
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    • 2006
  • A series of 8-alkoxy-4,5-dihydro-[1,2,4]triazole[4,3-a]quinoline-1-one derivatives were synthesized using 7-hydroxy-3,4-dihydro-2(1H)-quinolone as the starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES) and the subcutaneous pentylenetetrazole test (sc-PTZ), and their neurotoxicities were measured by the rotarod neurotoxicity test (Tox). The tests demonstrated that 8-hexyloxy-4,5-dihydro-[1.2.4]triazole[4.3-a]quinoline-1-one (4e) and 8-heptyloxy-4,5-dihydro-[1,2,4]triazole[4, 3-a]quinoline-1-one (4f) were the most potent anticonvulsants, with 4e having $ED_{50}$ values of 17.17 mg/kg and 24.55 mg/kg and protective index ($PI=TD_{50}/ED_{50}$) values of 41.9 and 29.3 in the MES and sc-PTZ tests, respectively, and 4f having $ED_{50}$ values of 19.7 mg/kg and 21.2 mg/kg and PI values of 36.5 and 33.9 in the MES and sc-PTZ tests, respectively. The PI values of 4e and 4f were many fold better than that of the marketed drugs phenytoin, carbamazepine, phenobarbital and valproate, which have PI values in the range of 1.6-8.1 in the MES test and <0.22-5.2 in the sc-PTZ test. Structure-activity relationships were also discussed.

Dextran에 결합된 새로운 Quinolone계 항균제의 개발 (Development of New Quinolone Antibacterials with Dextran-bond)

  • 김선일;나재운
    • 공업화학
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    • 제5권3호
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    • pp.501-508
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    • 1994
  • 방출조절성 약제를 개발하기 위한 방법으로 1-ethyl-6-fluoro-1, 4-dihydro-4-oxo-7-(1-piperazinyl)quitoline-3-carboxylic acid의 $C_3$ 위치를 Vilsmeier reagent로 chlorination하여 이를 dextran과 반응시켜 1-ethyl-6-fluoro-1, 4-dihydro-4-oxo-7-(1-piperazlnyl) quinoline-3-carboxylic acid-dextran 중합체약을 합성하였다. 중합체약에 대한 최소발육저지농도(MICs)로서 Gram 양성세균 Bacillus subtillis ATCC 6633, Staphyloccus aureus ATCC 25923, Mycrobacterium phlei IFO 3158 및 Salmonella typhimurium KCTC 1925에 대해서 각각 $5{\mu}g/ml$의 농도로 균의 발육을 억제하였다. Micrococcus luteus ATCC 9341에 대해서는 $80{\mu}g/ml$로 약한 활성을 보였을 뿐, Gram 양성세균들에 대하여 전반적으로 강한 저항성을 보여주었다. Gram 음성세균인 Escherichia coli KCTC 1039, Escherichia coli ESS, Klebsiella puenmouiae KCTC 1560 및 Psendomonas aeruginosa IFO 13130 균주들에 대해서도 각각 $5{\mu}g/ml$로 대조물질과 유사한 항균성을 보여주었다. 한편, quinolone계 항균제가 진균류에 대하여 감수성을 보이지 않는 것처럼 중합체약도 진균인 Candida albicans ATCC 10231에 대해서는 감수성을 보여주지 않았다.

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수온에 따른 Norfloxacin의 잉어(Cyprinus carpio)와 뱀장어(Anguilla japonica)체내에서 약물동태학적 특성 (Effects of Temperature on the Pharmacokinetics of Norfloxacin inCarp (Cyprinus carpio) and Eel (Anguilla japonica))

  • 김진우;정승희;이주석;최동림;조미라
    • 한국어병학회지
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    • 제15권2호
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    • pp.49-56
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    • 2002
  • Effects of Temperature on the Pharmacokinetics of norfloxecin (NFX) were studied in the cultured carp,Cyprinus carpio, and cel, Anguilla japonica, using high performance liquid chromatography (HPLC) originally developed for quinolone determination in livesrocks. Pharmacokinetics of NFX was apparently affected by ambiem water temperature. In a two-compaament model for carp after oral dosage of 20 mg/K01 at $13^{\circ}C$ and $23^{\circ}C$ and 5.20/hr, respectively. In carp the $K_{\iota\nu}$, $T_{max}$and $C_{max}$ for carp at $13^{\circ}C$ were 13.30/hr, 17.44 ${\mu}g$/$m\ell$ and 7.00 ${\mu}g$/$m\ell$, respectively. The" correspoeding values at $23^{\circ}C$ were 3.93/hr, 15.40 ${\mu}g$/$m\ell$ and 9.44 ${\mu}g$/$m\ell$, respectively. The AUC and T were 355.66 ${\mu}g$ hr/$m\ell$, and 12.70 hr at $13^{\circ}C$ and 417,24 ${\mu}g$ hr/$m\ell$ and 13.86 hrs at $23^{\circ}C$, respectively. Similar trends were revealed in the NFX pharmacokinetics of eel kept under the two water temperature regimes aftee oral NFX dosage of 20 mg/kg. These pharmacokinetkal results have some implication in the optimal usage of recently introduced antibacterials in farmed fish, which were originally adapted for poultry and mammalian species.

랫드에서 fluoroquinolone 항균제 DW-116의 단회 경구투여에 의한 태반통과와 약물동태연구 (Placental Transfer and Pharmacokinetics of a Single Oral Dose of the Fluoroquinolone Antibacterial DW-116 in Rats)

  • 김종춘;신호철;허정두;이종화;정문구;윤효인
    • Biomolecules & Therapeutics
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    • 제10권1호
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    • pp.43-49
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    • 2002
  • The present study was conducted to investigate the placental transfer and pharmacokinetics of the flu-oroquinolone antibacterial DW-116 in pregnant rats. The placental transfer and pharmacokinetics of DW-116 were examined after a single oral dose of 500 mg $^{14}C$ DW-116/kg on gestational day 18. Maternal and fetal tissues were collected at 0.17 0.5,1,2,4,8, and 24 h after dosing. Maximum radioactivity was detected in maternal plasma, placenta, and whole fetus at 1 h, and in amniotic plasma at 4 h after dosing. Thereafter, radioactivity gradually disappeared from these tissues and was 16~28% of maximum levels at 24 h after dosing. Radioactivity in whole fetus were higher than those in the maternal plasma and placenta. The $T_{1/2,abs}$, $T_{1/2,{\beta}},$ AUC, $T_{max},$ and $C_{max}$ in the maternal plasma were approximately 6 min, 13.3 h, 1620 $ug^*hr/ml,$ 0.5 h, and 136 ug/ml, respectively. Those in the placenta were approximately 20 min, 12.3 h, 2150 $ug^*h/$m\ell$,$ 1.0 h, and 172 ug/ml, respectively. Those in the whole fetus were 13 min, 12.8 h,2549 $ug^*h/$m\ell$,$ 1 h, and 191 ug/ml, respectively. In the amniotic fluid of maternal uterus, the 4T_1/2,abs}$, $T1/2,{\beta},$ AUC, $T_{max},$ and $C_{max}$ were approximately 1.3 h,9.3 h,2508 $ug^*h/$m\ell$,$ 4.4 h, and 135 ug/ml, respectively. While DW-116 disappeared biphasically from maternal plasma, whole fetus and placenta, it was eliminated monophasically from amniotic fluid. In conclusion, this study demonstrated that the absorption and distribution of DW-116 in maternal plasma and placenta were extensively rapid, and that the test chemical well passed the blood-placenta barrier and was transferred to the fetus.

Viridicatol from Marine-derived Fungal Strain Penicillium sp. SF-5295 Exerts Anti-inflammatory Effects through Inhibiting NF-κB Signaling Pathway on Lipopolysaccharide-induced RAW264.7 and BV2 Cells

  • Ko, Wonmin;Sohn, Jae Hak;Kim, Youn-Chul;Oh, Hyuncheol
    • Natural Product Sciences
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    • 제21권4호
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    • pp.240-247
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    • 2015
  • Viridicatol (1) has previously been isolated from the extract of the marine-derived fungus Penicillium sp. SF-5295. In the course of further biological evaluation of this quinolone alkaloid, anti-inflammatory effect of 1 in RAW264.7 and BV2 cells stimulated with lipopolysaccharide (LPS) was observed. In this study, our data indicated that 1 suppressed the expression of well-known pro-inflammatory mediators such as inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2, and consequently inhibited the production of iNOS-derived nitric oxide (NO) and COX-2-derived prostaglandin E2 ($PGE_2$) in LPS stimulated RAW264.7 and BV2 cells. Compound 1 also reduced mRNA expression of pro-inflammatory cytokines such as $interleukin-1{\beta}$ ($IL-1{\beta}$), interleukin-6 (IL-6), and tumor necrosis $factor-{\alpha}$ ($TNF-{\alpha}$). In the further evaluation of the mechanisms of these anti-inflammatory effects, 1 was shown to inhibit nuclear factor-kappa B ($NF-{\kappa}B$) pathway in LPS-stimulated RAW264.7 and BV2 cells. Compound 1 blocked the phosphorylation and degradation of inhibitor kappa B $(I{\kappa}B)-{\alpha}$ in the cytoplasm, and suppressed the translocation of $NF-{\kappa}B$ p65 and p50 heterodimer in nucleus. In addition, viridicatol (1) attenuated the DNA-binding activity of $NF-{\kappa}B$ in LPS-stimulated RAW264.7 and BV2 cells.

돼지 및 닭에서 분리된 균에 대한 봉독의 최소억제농도(MIC) (The minimum inhibitory concentration (MIC) of bee venom against bacteria isolated from pigs and chickens)

  • 김순태;황지영;성명숙;제소양;배동록;한상미;이성해
    • 한국동물위생학회지
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    • 제29권1호
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    • pp.19-26
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    • 2006
  • Bee venom is synthesized in the venom gland's of worker and queen bees and stored in their venom sacs. Bee venom is a rich source of enzymes, peptides and biogenic amines. there are at least 18 active components in the venom which have some pharmaceutical properties. This study was performed to evaluate minimum inhibitory concentration(MIC) of bee venom against bacteria isolated from pjgs and chickens with disease. In case of reference strains, the MIC $({\mu}g/m{\ell})$ of Staphylococcus aureus ATCC 6538, Streptococcus mutans ATCC 25175, and Salmonella typhimurium ATCC 6538 were 64, 64 and 32, respectively. In case of bacteria isolated from pig and chicken, the MIC of Staphylococcus aureus, Staphylococcus hyicus and Staphylococcus chromogenes were 8, 128 and 128, and that of 11 strains of Escherichia coli were 8 to >512 and that of 8 strains of Salmonella sup were >512. Antibacterial resistance test of 22 strains isolated from pig and chicken and 3 reference strains were performed by agar gel diffusion method, using 17 antibacterial drugs including penicillin, cefazolin, tetracycline and quinolone group. The multiple drug resistant patterns were found in most strains isolated from pig and chicken.

은교산(銀翹散)과 Rufloxacin의 병용투여(倂用投與)가 Klebsiella pneumoniae 호흡기감염(呼吸器感染)에 미치는 영향 (Effects of in vivo Synergism of Eunkyo-san, a Poly-Herbal Formula and Rufloxacin against Klebsiella pneumoniae Respiratory Infections)

  • 하연귀;박미연;최해윤;김종대;송광규
    • 동의생리병리학회지
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    • 제19권3호
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    • pp.753-759
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    • 2005
  • In order to evaluate the in vivo synergic effect of Eunkyo-san with quinolone antibiotics, rufloxacin (RUFX), the viable bacterial numbers and histopathological changes were monitored after experimental respiratory infection with Klebsiella peumoniae NCTC 9632. The obtained results were as follows : In RUFX group, the viable bacterial numbers were significantly decreased compared to those of control group and these were more dramatically decreased compared to those of single treatment with RUFX, respectively in concomitant treated groups with Eunkyo-san. In control group, severe infiltration of inflammatory cells, hemorrhage and hypertrophy of alveolar linings were demonstrated at microscopical levels. However, these abnormal histopathological changes were significantly decreased compared to those of control group in RUFX group, and these were more dramatically decreased compared to those of single treatment with RUFX, respectively in concomitant treated groups with Eunkyo-san. In RUFX group, the LSA% (luminal surface of alveolar%) were significantly increased compared to those of control group and these were more dramatically decreased compared to those of single treatment with RUFX, respectively in concomitant treated groups with Eunkyo-san. According to these results, it is considered that in vivo antibacterial activity of RUFX group was dramatically increased by concomitant use of Eunkyo-san against K. pneumoniae NCTC 9632 infection of respiratory tract.

마황윤폐탕(麻黃潤肺湯)과 Ciprofloxacin의 병용(倂用)이 호기성 Gram(-) 세균주(細菌株)에 대한 시험관내(試驗管內) 항균력(抗菌力)에 미치는 영향 (Synergic Effect of Mahwangyounpae-tang and Ciprofloxacin on 5 Strains of Aerobic Gram-negative Bacteria)

  • 유한상;박미연;최해윤;구덕모;김종대;송광규
    • 동의생리병리학회지
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    • 제19권3호
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    • pp.684-689
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    • 2005
  • In order to evaluate the in vitro synergic effect of Mahwangyounpae-tang which was a traditional poly-herbal formula has been used in the treatment of respiratory diseases in oriental medicine, and quinolone antibiotics, ciprofloxacin (CPFX), the minimal inhibitory concentration (MIC), $MIC_{50}$ and MIC90 of single use of quinolones and concomitant treatment with Mahwangyounpae-tang against 5 strains of aerobic gram negative bacteria, Escherichia coli, Klebsiella peumoniae, Hemophilus influenzae, Citrobacter freundii and Pseudomonas aeruginosae. The obtained results were as follows : In the case of aerobic gram negative bacteria, the MIC, $MIC_{50}$ and $MIC_{90}$ against Klebsiella peumoniae and Pseudomonas aeruginosae was significantly decreased in concomitant treated groups with Mahwangyounpae-tang compared to those of single treated groups of CPFX, respectively. However, no significant changes were demonstrated against Echerichia coli, Hemophilus influenzae and Citrobacter freundii. According to these results, it is considered as the in vitro antibacterial activity of CPFX was dramatically increased by concomitant use of Mahwangyounpae-tang against some strains of aerobic gram negative bacteria and the increase and selectivity of antibacterial activities against strains were chosen by the selectivity of Mahwangyounpae-tang not CPFX activity.