• Title/Summary/Keyword: Quinolone antibacterial

검색결과 65건 처리시간 0.037초

연교김패전(連翹金貝煎)의 Escherichia coli에 대한시험관내 항균력 평가 (In Vitro Antibacterial Effects of Yeonkyokeumpae-jeon against Escherichia coli)

  • 한상겸;김동철
    • 대한한방부인과학회지
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    • 제28권1호
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    • pp.29-45
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    • 2015
  • Objectives: The object of this study was to observe the in vitro antibacterial effects of Yeonkyokeumpae-jeon (YKKPJ) have been used for treating various gynecological diseases including mastitis in Korea, and individual six kinds of herbal composition aqueous extracts - Forsythiae Fructus (FF), Millettiae Caulis (MC), Lonicerae Flos (LF), Fritillaria Thunbergii Bulb (FT), Taraxci Herba (TH) and Prunellae Spica (PS) against E. coli. Methods: Antibacterial activities against E. coli of YKKPJ, FF, MC, LF, FT, TH and PS aqueous extracts were detected using standard agar microdilution methods. In addition, the effects on the bacterial growth curve were also monitored at MIC and $MIC{\times}2$ levels. The effects on the intracellular killing and bacterial invasion of individual test materials were also observed using Raw 264.7 and MCF-7. The results were compared with ciprofloxacin, a second generation of quinolone antibiotics in the present study. Results: MIC of YKKPJ, FF, MC, LF, FT, TH, PS aqueous extracts against E. coli were detected as $0.039{\pm}0.013mg/ml$, $0.064{\pm}0.033mg/ml$, $0.108{\pm}0.053mg/ml$, $0.078{\pm}0.027mg/ml$, $16.250{\pm}8.385mg/ml$, $15.625{\pm}9.375mg/ml$, $0.254{\pm}0.131mg/ml$, repectively. YKKPJ, FF, MC, LF, FT, TH, PS aqueous extracts showed antibacterial effects against to E. coli, except for FT and TH, which were showed negligible antibacterial effects, respectively. In addition, ciprofloxacin with YKKPJ, FF, MC, LF and PS aqueous extracts also showed marked dosage-dependent inhibition of bacterial growth, and favorable inhibitory effects on the both bacterial invasion and intracellular killing assays using MCF-7 and Raw 264.7 cells were detected in this experiment. Conclusions: The results obtained in this study suggest that traditional polyherbal formula YKKPJ aqueous extracts showed more favorable antibacterial activities as compared to individual six kinds of herbal composition aqueous extracts. The antibacterial effects of YKKPJ against E. coli considered as results of complicated synergic effects of their six kinds of herbal components rather than simple antibacterial effects of single herbal components. It means, YKKPJ aqueous extracts may show potent anti-infectious effects against E. coil for mastitis.

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.

Leptospermum scoparium 추출물중 케톤체 분획물의 항균력 및 항생제와의 병용효과 (Activities of Ketonic Fraction from Leptospermum scoparium alone and Synergism in Combination with Some Antibiotics Against Various Bacterial Strains and Fungi)

  • 김은희;이계주
    • 약학회지
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    • 제43권6호
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    • pp.716-728
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    • 1999
  • Whole oil and ketonic fraction (KF) of Leptospermum scoparium have been tested for their antimicrobial activity and combination effect with several antibiotics against various bacterial strains and fungi by using microbiological assay methods. Antibacterial activities of KF against a number of test strains were 2-3 fold stronger than those of whole oil. MICs of the KF were $65~125{\;}{\mu\textrm{g}}/ml$ against seven gram positive bacterial strains, $65~250{\;}{\mu\textrm{g}}/ml$ against 19 methicillin resistance Staphylococcus aureus strains, and $65~50{\;}{\mu\textrm{g}}/ml$ against 14 quinolone resistance strains. However, KF showed little or no activity against gram negative bacteria. MICs of the KF were $16~250{\;}{\mu\textrm{g}}/ml$ against more than 50% of the anaerobic bacterial strains tested. KF showed the higher antibacterial activity than bacitracin against 10 strains of Bacteroids thetaiotaomicron, or three strains of Bacteroides ovatus, and the more active than ciprofloxacin against one strain of Bacteroides thetaiotaomicron and three strains of Bacteroids ovatus. The MICs of KF was 63 and $250{\;}{\mu\textrm{g}}/ml$ against Aspergillus niger and Candida albicans, respectively. Antibacterial activities of KF in combination with 19 antibiotics against 14 strains and with four antifungal agents against one fungal strain were determined by paper strip diffusion method. While most of combination showed additivity, KF showed synergism with bacitracin, exfadroxil, cephradin, and meropenem for 29~57% of the strains tested. However, ofloxacin, enoxacin, sparfloxacin showed antagonism with KF for 43~71% of the strains. KF alone and in combination with bacitracin, gentamycin, neomycin, itraconazole, fluconazole, terfinafine and ketoconazole against five bacterial strains or one fungus strain synergistic effect was demonstrated against 33% of strains examined with FIC index value below 0.5 by checkerboard study. Synergistic effect of KF with gentamicin against Staphylococcus epidermidis 329 (QRS) was found by time-kill study.

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Carrier-Mediated Tissue Distribution and Blood-Brain Barrier Transport of New Quinolones

  • Tsuji, Akira
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1997년도 춘계학술대회
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    • pp.57-63
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    • 1997
  • Animal and clinical investigations have shown that fluoroquinolones, new quinolone antibacterial agents (NQs), are well absorbed across the intestinal tract, with a bioavailability of 60-90% after oral administration. Although some types of carrier-mediated intestinal transport mechanisms have been reported for enoxacin (ENX), ofloxacin (OFLX) and sparfloxacin (SPFX), recent results using a human intestinal epithelial cell line, Caco-2, indicated a passive or nonsaturable transport of SPFX, one of the most hydrophobic NQs. The mechanism underlying the intestinal absorption of NQs is still largely unknown. The distribution of NQs into peripheral tissues including erythrocytes is very rapid and their tissue-to-plasma concentration ratios (Kp) are considerably larger than those of inulin (an extracellular fluid space marker), in spite of almost complete ionization of NQs at the physiological pH. Our findings suggest that OFLX and lomefloxacin (LFLX) are taken up by rat erythrocytes via a transport system common to that of a water-soluble vitamin, nicotinic acid.

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3,4-디클로로아세토페논에 대한 C-아실화와 O-아실화의 경쟁적 반응에 관한 연구 (A Study of the Competitive Reaction of C-Acylation Versus O-Acylation on the 3,4-Dichloroacetophenone)

  • 김유승;마혜덕;김형석
    • 대한화학회지
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    • 제35권5호
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    • pp.580-585
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    • 1991
  • 본 연구는 퀴놀론 중간체 합성을 위한 모델 연구로서 3,4-디클로로아세토페논의 C-, O-아실화의 경쟁반응에 대해 조사하였다. 3,4-디클로로아세토페논의 C-, O-아실화 비율에 대한 염기, 용매, 아실화물의 이탈기 효과에 대해 논하였으며, 이 때 아실화물로는 클로로포름산에틸, 에틸페닐탄산, 그리고 디에틸탄산을 사용하였다. 비극성 용매에서, 사용된 염기의 금속이온 크기가 작으면 작을수록 C-아실화 반응이 지배적으로 일어났다. 이탈기 영향에 있어서는 아실화물의 이탈기 능력이 감소할수록 C-아실화 생성물이 증가함을 볼 수 있었다. 또한 용매의 극성이 감소할수록 C/O-아실화 비율이 증가함을 관찰하였다.

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은교산과 Ciprofloxacin의 병용투여가 Streptococcus pneumoniae 호흡기감염에 미치는 영향 (Investigation Synergism of Eunkyo-san, a Poly-herbal Formula and Ciprofloxacin against Streptococcus pneumoniae Respiratory Infection)

  • 이상준;전귀옥;송광규;최해윤;김종대
    • 동의생리병리학회지
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    • 제19권4호
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    • pp.1039-1045
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    • 2005
  • In order to evaluate the in vivo synergic effect of Eunkyo-san which was a traditional poly-herbal formula has been used in the treatment of respiratory diseases in Korea, with quinolone antibiotics, ciprofloxacin (CPFX), the viable bacterial number and histopathological changes were monitored after experimental respiratory infection with S. pneumoniae ATCC 6303. The obtained results were as follows: In CPFX groups, the viable bacterial numbers were significantly decreased compared to that of control group and these were more dramatically decreased compared to that of single treatment with CPFX, 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 that of control group in CPFX groups, and these were more dramatically decreased compared to that of single treatment with CPFX, respectively in concomitant treated groups with Eunkyo-san. In CPFX groups, the LSA (luminal surface of alveoli $\%$) were significantly increased compared to that of control group and these were more dramatically decreased compared to that of single treatment with CPFX, respectively in concomitant treated groups with Eunkyo-san. According to these results, it is considered as the in vivo antibacterial activity of CPFX was dramatically increased by concomitant use of Eunkyo-san against S. pneumoniae ATCC 6303 infection of respiratory tract.

은교산(銀翹散)과 Quinolone계 항생제의 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 Effects of Eunkyo-san and Quinolones on 5 Strains of Aerobic Gram-negative Bacteria)

  • 전귀옥;서영호;권은희;조동희;박미연;최해윤;김종대;송광규
    • 대한한방내과학회지
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    • 제26권3호
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    • pp.521-532
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    • 2005
  • Objectives & Methods : In order to evaluate the in vitro synergic effects or Eunkyo-san which is a traditional poly-herbal formula that has been used in the treatment of respiratory diseases in oriental medicine, and quinolone antibiotics, rufloxacin (RUFX) and iprofloxacin(CPFX), experimentation was designed to determine minimal inhibitory concentration(MIC), $MIC_{50}\;and\;MIC_{90}$ of single use of quinolones and concomitant treatment with Eunkyo-san against 5 strains of aerobic gram negative bacteria, Escherichia coli, Klebsiella peumoniae, Hemophilus influenzae, Citrobacter freundii and Pseudomonas aeruginosae. Result : In the case of aerobic gram negative bacteria, the MIC, $MIC_{50}\;and\;MIC_{90}$ against Klebsiella peumoniae and Citrobacter freundii significantly decreased in concomitant-treated groups with Eunkyo-san compared to those of single-treated groups of RUFX and CPFX, respectively. However, no significant changes were demonstrated against Echerichia coli, Hemophilus influenzae and Pseudomonas aeruginosae. Conclusion : According to these results, concomitant use of Eunkyo-san against some strains of aerobic gram-negative bacteria dramatically increases in vitro antibacterial activity of RUFX and CPFX, and the increase and selectivity of antibacterial activities against these strains is attributable to Eunkyo-san, and not RUFX or CPFX activity.

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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.

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.

세팔로스포린 3'-퀴놀론의 합성 및 항균작용 (Synthesis and Antibacterial Activity of Cephalosporin 3'-Quinolone Dithiocarbamate)

  • 나성범;정명희;김완주;지웅길
    • 약학회지
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    • 제37권2호
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    • pp.136-142
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    • 1993
  • To a suspension of 1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-{3,7-diazabicyclo[3.3.0]oct-1(5)-en-3-yl}-4-oxo-3-quinoline carboxylic acid(C1) in sodium hydroxide solution and water is added dropwise with stirring carbon disulfide. [6R-[6$\alpha$, 7$\beta$(Z)]]-7-[[[2-Amino-4-thiazoly)methoxyimino]-acetyl]amino]-3-[[[[7-( 3-carboxy-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-7-guinolonyl)-3,7-diazabicyclo[3.3.0]oct-1(5)-en-3-yl]thioxomethyl]thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-2-carboxylic acid (DACD) was synthesized from 1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-[7-(mercapto) thioxomethyl-[3,7-dia zabicyclo[3.3.0]oct-1(5)-en-3-yl}]-4-oxo-3-quinoline carboxylic acid disodium salt(C2) and cefotaxime. The invitro activity of novel dual-action cephalosporin, DACD, was compared with the in vitro activities of CENO(cefotaxime 3'-norfloxacin dithiocarbamate), cefotaxime, and norfloxacin against a variety of bacterial species. In vitro activity of DACD was superior to that of norfloxacin against Streptococcus pyogenes. Against Gram-positive and Gram-negative bacteria, its activity was almost equal to that of CENO.

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