• Title/Summary/Keyword: Clavulanic acid

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Comparative Activities of Novel $\beta$-Lactamase Inhibitors, 6-Exomethylene Penamsulfones (CH1240, CH2140) in Experimental Mouse Infection Model

  • Park, Kye-Whan;Yim, Chul-Bu;Kim, Ki-Ho
    • Archives of Pharmacal Research
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    • v.21 no.5
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    • pp.527-530
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    • 1998
  • The antibacterial activity of novel ${\beta}$-lactamase inhibitors, 6-exomethylene penamsulfones (CH1240, CH2140), has been compared in vivo with that of sulbactam and clavulanic acid against b-lactamase producing strains. In vivo microbiological assessment was used as experimental mouse infection model by gram negative strains. Against Pseudomonas aeruginosa F0013, cefoperazone/CH 1240 was slightly less active than sulbactam. ampicillin/CH 2140 was less effective than sulbactam against escheriachia coli 3457. Especially against Citrobacter diversus 2046E, amoxicillin/CH 2140 was the most potent and amoxicillin/CH 1240 was slightly more active than clavulanic acid. consequently the difference in efficacy between the drug combinations appers to be related to the degree of protection afforded the animals by the b-lactamasse inhibitors. CH1240 and CH2140 are promising new agents and should undergo further investigations.

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Synthesis and ${\beta}-Lactamase$ Inhibitory Activity of 7-Exomethylene Cephalosporanates (7-엑소메칠렌 세팔로스포라네이트 유도체의 합성과 $\beta$- 락타메이즈 억제작용)

  • 이종민;최수항;이현수;임채욱;임철부
    • YAKHAK HOEJI
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    • v.43 no.6
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    • pp.782-788
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    • 1999
  • 7-Oxocephalosporanate 1 was treated with phosphonium salts 2~4 by Wittig reaction to afford 7-exomethylene cephalosporanates 5~7. They were oxidized to sulfones 8~10 with mCPBA. Deprotecton of benzhydryl 7-exomethylene cephalosporanate with $AlCl_3$ and NaHCO_3$ gave sodium salts of 7-exomethylene cephalosporanates 11~16. The ${\beta}-lactamase$ inhibitory activity of synthesized compounds 11~16 were compared with sulbactam, tazobactam and clavulanic acid against Type I, II, III, IV and TEM-2 $\beta$-lactamase in vitro. Compound 15 showed more potent activity than sulbactam and clavulanic acid against Type III, IV ${\beta}-lactamase$ enzyme.

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Enhancement of Clavulanic Acid by Replicative and Integrative Expression of ccaR and cas2 in Streptomyces clavuligerus NRRL3585

  • Hung, Trinh Viet;Malla, Sailesh;Park, Byoung-Chul;Liou, Kwang-Kyoung;Lee, Hei-Chan;Sohng, Jae-Kyung
    • Journal of Microbiology and Biotechnology
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    • v.17 no.9
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    • pp.1538-1545
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    • 2007
  • Clavulanic acid (CA) is an inhibitor of ${\beta}$-lactamase that is produced from Streptomyces clavuligerus NRRL3585 and is used in combination with other antibiotics in clinical treatments. In order to increase the production of CA, the replicative and integrative expressions of ccaR (encoding for a specific regulator of the CA biosynthetic operon) and cas2 (encoding for the rate-limiting enzyme in the CA biosynthetic pathway) were applied. Six recombinant plasmids were designed for this study. The pIBRHL1, pIBRHL3, and pIBRHL13 were constructed for overexpression, whereas pNQ3, pNQ2, and pNQ1 were constructed for chromosomal integration with ccaR, cas2, and ccaR-cas2, respectively. All of these plasmids were transformed into S. clavuligerus NRRL3585. CA production in transformants resulted in a significantly enhanced amount greater than that of the wild type, a 2.25-fold increase with pIBRHLl, a 9.28-fold increase with pNQ3, a 5.06-fold increase with pIBRHL3, a 2.93-fold increase with pNQ2 integration, a 5.79-fold increase with pIBRHLl3, and a 23.8-fold increase with pNQ1. The integrative pNQl strain has been successfully applied to enhance production.

Profiles of Toxin genes and Antibiotic Susceptibility of Staphylococcus aureus Isolated from Perilla Leaf Cultivation Area (들깻잎 재배단지에서 분리한 Staphylococcus aureus의 독소 유전자와 항생제 감수성 분석)

  • Kim, Se-Ri;Cha, Min-Hee;Chung, Duck-Hwa;Shim, Won-Bo
    • Journal of Food Hygiene and Safety
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    • v.30 no.1
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    • pp.51-58
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    • 2015
  • Thirty one of Staphylococcus aureus isolated from perilla leaf cultivation areas in Miryang were investigated on the characteristics, such as enterotoxin genes and antibiotic susceptibility. Five toxin genes (sea, seb, sec, sed, and see) were examined by PCR method. Disc diffusion method was used to examine the antibiotic susceptibility of S. aureus by using 18 types of antibiotic discs with different concentrations. Among enterotoxin-encoding genes, sea and sed genes were co-detected from 4 isolates (12.9%), sed gene was founded in 9 isolates (29.0%), and see gene was founded in 1 isolate (3.2%). However seb and sec and tsst were not detected in any isolates. As a result of antibiotic susceptibility test, 7 isolates (22.6%) were resistant to 12 antibiotics (penicillin, ampicillin, oxacillin, amoxicillin-clavulanic acid, cefazolin, cephalothin, imipenem, gentamicin, tetracycline, ofloxacin, norfloxacin, and erythromycin). 2 isolates (6.5%) were resistant to 5 antibiotics (penicillin, ampicillin, amoxicillin-clavulanic acid, gentamycin, and telithromycin). MRSA (Methicilline Resistant Staphylococcus aureus) was founded in packing vinyl, hands, and perilla leaves.

Antibiotic Resistance and Assessment of the Food-borne Pathogenic Microorganisms in Ready to Eat Meals (식사대용 식품(Ready-to-eat meals) 중 병원성 세균의 분포와 항생제 감수성 양상)

  • Hong, Eun-Kyung;Kim, Yun-A;Lee, Do-Kyung;Kang, Byung-Yong;Ha, Nam-Joo
    • Korean Journal of Microbiology
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    • v.42 no.4
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    • pp.265-270
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    • 2006
  • This study was performed in order to measure the level of food-borne pathogenic bacteria and antibiotic resistance pattern of found ready to eat meals such as Him-bap, Cho-bap, Hamburger, Sandwich and packed lunch boxes. A total of 497 samples were collected from supermarket and department of Seoul, Kyung-ki, Inctleon, Kang-won, Chung-Cheong from November, 2005 to March, 2006. The contaminated microorganisms were in most cases tract relative strain like E. coli and S. aureus. Result have shown E. coli was detected 4 strains and S. aureus was detected 22 strains. 26 strains were also tested the antibiotic resistance pattern. 26 strains were shown to be relatively susceptible to synercid, vancomycin, teicoplanin, ciprofloxacin, gentamycin, lincomycn, cefotaxime, meropenem, cephalosporin, amoxicillin-clavulanic acid by the MIC dilution method, but E. coli 1 strain was resistant to amoxicillin-clavulanic acid.

Antimicrobial effects of β-lactamase inhibitor/β-lactam antibiotics on staphylococcal mastitis (Staphylococcus aureus에 의한 유방염에 대한 β-lactamase 저해제/β-lactam계 항균제 치료 효과)

  • Lim, Suk-Kyung;Lim, Jae-Hhyang;Joo, Yi-Seok;Moon, Jin-San;Lee, Ae-Ri;Koh, Hong-Bum
    • Korean Journal of Veterinary Research
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    • v.43 no.1
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    • pp.113-120
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    • 2003
  • The antimicrobial effect of ${\beta}$-lactam antibiotics, which had ${\beta}$-lactamase inhibitor activity, on Staphylococcus aureus isolated from mastitis was investigated in this study. Out of 166 isolates, 99 isolates (59.6%) produced ${\beta}$-lactamase, and 98 isolates of 99 were ${\beta}$-lactamase positive in above $12.5{\mu}g/m{\ell}$ MIC of penicillin. In the providence distribution, ${\beta}$-lactamase production rate of 4 providence, Gangwon, Gyeonggi, Chungcheong, and Jeolla was 100%, 65.7%, 58.8%, and 50.0%, respectively. Antibiotic activities of ${\beta}$-lactam antibiotics against lactamase positive isolates also were investigated. Antimicrobial effects of ampicillin/sulbactam or amoxicillin/clavulanic acid treated group were better than ampicillin or amoxicillin treated group. In antimicrobial effects on intracellular S aureus, there was no difference 1 hour and 4 hour treatment in control, ampicillin, and amoxicillin group, but in 18 hours treatment, ampicillin/sulbactam or amoxicillin/clavulanic acid had a better effect than ampicillin or amoxicillin (p<0.05).

Comparison of the efficacy of amoxicillin-clavulanic acid with metronidazole to azithromycin with metronidazole after surgical removal of impacted lower third molar to prevent infection

  • Sayd, Shermil;Vyloppilli, Suresh;Kumar, Krishna;Subash, Pramod;Kumar, Nithin;Raseel, Sarfras
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • v.44 no.3
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    • pp.103-106
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    • 2018
  • Objectives: The goal of the study was to investigate the clinical effects of amoxicillin-clavulanic acid (500+125 mg) with metronidazole 400 mg administered three times daily (Group I) versus azithromycin 500 mg administered once daily and with metronidazole 400 mg three times daily (Group II) for the prevention of postoperative infection following mandibular third molar surgical removal. Materials and Methods: The study design was a single-center prospective study. Patients who reported to the Department of Oral and Maxillofacial Surgery between February 2015 and January 2017 for removal of mandibular third molar were screened, and 108 patients were chosen. One surgeon carried out all procedures. Patients were prescribed antibiotics until the two groups contained a similar number of cases. Results: Our data showed that Group II had fewer incidences of surgical site infection, but with no statistical significance. Conclusion: Although both treatments are used routinely after removal of the mandibular third molar, neither is significantly better than the other.

Antibiotic susceptibility of Clostridium perfringens type D isolated from feces of goats

  • Kim, Jun-Ho;Kim, Jeong-Hwa;Kim, Young-Hoan;Cho, Kwang-Hyun;Nam, Sang Yoon;Lee, Hu-Jang;Lee, Beom Jun
    • Journal of Preventive Veterinary Medicine
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    • v.42 no.4
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    • pp.148-156
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    • 2018
  • Clostridium perfringens (C. perfringens) may cause diarrhea and enterotoxemia in adult and young livestock, leading to problems in the production and management of farms. Four hundred fecal samples were collected from 25 goat farms located in Gyeongsangbuk-do Province in the Republic of Korea. Sixteen C. perfringens strains were isolates from fecal samples, and the isolates were identified as type A (n=11) and type D (n=5). Additionally, ${\alpha}$- and ${\varepsilon}$-toxin genes were detected in 16 and 5 strains by PCR, respectively, and the enterotoxin gene was presented in 2 strains. The antibiotic susceptibility test was performed using the disk diffusion method and E-test method. In the disk diffusion method, ampicillin (n=16) and chloramphenicol (n=15) were highly susceptible to 16 C. perfringens isolates. In the E-test method, ampicillin, amoxicillin, amoxicillin/clavulanic acid and meropenem were susceptible to more than 14 of 16 C. perfringens isolates. This study indicates that administration of antibiotics such as ampicillin, amoxicillin/clavulanic acid and meropenem can prevent and treat C. perfringens infections in goats.

E. faecalis and E. faecium Isolated in Dried Marine Products (시판 건해산물에서 분리한 Enterococcus faecalis와 E. faecium의 미생물학적 특성)

  • Ham, Hee-Jin
    • Journal of Food Hygiene and Safety
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    • v.22 no.4
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    • pp.294-299
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    • 2007
  • Eighty seven strains were isolated from 164 dried marine products(dried squid and dried alaska pollack etc) in Seoul Garak wholesale market. Among 87 isolates, twenty four E. faecalis and 4 E. faecium were identified by API strep kit. Twenty eight strains of E. faecalis, and E. faecium were resistant in streptomycin (95.6%), kanamycin (84.5%), gentamycin (66.7%), cephaloxin (97.8%), ampicillin/sulbactam (88.9%), ticarcillin(66.7%), amikacin (97.8%), sulfonamides (97.8%), ceftriaxone (75.6%), nalidixic acid (100.0%), and cefoxitin (100.0%), and were susceptible in amoxicillin/clavulanic acid(97.8%), chloramphenicol(95.6%), sulfamethoxazole/trimethoprim (97.8%), and tetracycline (71.1%). Also, ten strains of E. faecalis was resistant in $S-K-GM-CF-SAM-TIC-An-S_3-CRO-NA-FOX$ drugs simultaneously. Conclusively, E. faecalis strains from dried marine products were resistant on antibiotic drugs residue.

Antimicrobial Susceptibility of Vibrio parahaemolyticus and Vibrio alginolyticus from Fish Farms on the Southern Coast of Korea (남해안 어류양식장에서 분리된 Vibrio parahaemolyticus와 Vibrio aiginolyticus의 항균제 감수성)

  • SON Kwang-Tae;OH Eun-Gyoung;LEE Tae-Seek;LEE Hee-Jung;Kim Poong-Ho;KIM Ji-Hoe
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.38 no.6
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    • pp.365-371
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    • 2005
  • The antimicrobial resistance patterns to the 10 antimicrobial agents of potential pathogenic vibrios isolated from seawater and a variety of farmed fishes, including oliver flounder (Payalichthys olivaceus), black rock fish (Sebastes schlegeli), red sea bream (Pagyus major) and sea bass (Lateolabyax japonicus), were investigated from May to October, 2004. A total of 314 strains of the genus vibrios were isolated from 126 collected samples, and the number of isolated strains of Vibrio payahaemolyticus and Vibrio alginolyticus were 194 and 120, respectively. Apparently $98.5\%$ of V. parahaemolyticus and $100\%$ of V. alginolyticus isolates demonstrated antimicrobial resistance against at least one antimicrobial agent. The resistance of V. parahaernolyticus isolates to ampicillin ($97.9\%$) was highest, followed by oxolinic acid ($26.8\%$), amikacin ($19.1\%$) and tetracycline and amoxicillin/clavulanic acid ($6.7\%$). V. alginolyticus isolates were resistant to ampicillin ($100\%$), solfamethoxazoleit,imethopenem ($25\%$), amikacln ($21.7\%$), amoxicillin/clavulanic acid ($15.8\%$), ciprofloxacin ($13.3\%$), and tetracycline and doxycycline ($11.7\%$). The rate of multiple antimicrobial resistance to at least four antimicrobials was higher in the V. alginolyticus isolates ($20.8\%$) than in the V. parahaemolyticus ($6.7\%$).