• 제목/요약/키워드: Antibiotic mechanism

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ANTIBIOTIC RESISTANCE MECHANISM

  • Lee, Yeon-Hee
    • 한국미생물생명공학회:학술대회논문집
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    • 한국미생물생명공학회 2000년도 Proceedings of 2000 KSAM International Symposium and Spring Meeting
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    • pp.26-32
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    • 2000
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Mechanism of Antibiotic Action and Biosynthesis of Centipedin Purified from Scolopendra subspinipes multilans L. Koch (Centipede)

  • Kim, Ki-Tae;Hong, Sa-Weon;Lee, Jong-Ho;Park, Kyung-Bae;Cho, Key-Seung
    • BMB Reports
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    • 제31권4호
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    • pp.328-332
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    • 1998
  • The 8-hydroxyisocoumarin, named Centipedin, which has a significant antibiotic activity, was separated and solubilized with organic solvents, such as diethyl ether from centipede Scolopendra subspinipes multilans L. Koch. The Centipedin was purified by silicic acid column and high S cation exchange chromatography followed by reverse-phase HPLC. It was confirmed that Centipedin has a potent antibiotic effectiveness against Gram-negative Klebsiella pneumoniae ATCC 8308. The results showed that Centipedin blocks both DNA replication and RNA transcription during the growth of this pathogen in vivo. The biosynthesis of antibiotic 8-hydroxyisocoumarin was studied in vivo by feeding $[^{14}C]-labelled$ compound as a precursor to live centipede, in which $[^{14}C]acetate$ was the most efficiently incorporated into the Centipedin within 30 h after injection. Also, in vitro study on the biosynthesis of Centipedin showed that efficient incorporation of $[^{14}C]acetate$ occurred at pH range 5.0-7.0 for 10 h incubation and decreased significantly after then. It is suggested that 8-hydroxyisocoumarin is one of the defense compounds acting on bacterial infection in Scolopendra subspinipes.

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AcrAB-TolC, a major efflux pump in Gram negative bacteria: toward understanding its operation mechanism

  • Soojin Jang
    • BMB Reports
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    • 제56권6호
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    • pp.326-334
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    • 2023
  • Antibiotic resistance (AR) is a silent pandemic that kills millions worldwide. Although the development of new therapeutic agents against antibiotic resistance is in urgent demand, this has presented a great challenge, especially for Gram-negative bacteria that have inherent drug-resistance mediated by impermeable outer membranes and multidrug efflux pumps that actively extrude various drugs from the bacteria. For the last two decades, multidrug efflux pumps, including AcrAB-TolC, the most clinically important efflux pump in Gram-negative bacteria, have drawn great attention as strategic targets for re-sensitizing bacteria to the existing antibiotics. This article aims to provide a concise overview of the AcrAB-TolC operational mechanism, reviewing its architecture and substrate specificity, as well as the recent development of AcrAB-TolC inhibitors.

고추역병과 시들음병을 방제하는 토착길항세균 Pseudomonas fluorescens 4059의 선발과 길항기작 (Selection and Antagonistic Mechanism of Pseudomonas fluorescens 4059 Against Phytophthora Blight Disease)

  • 정희경;김상달
    • 한국미생물·생명공학회지
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    • 제32권4호
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    • pp.312-316
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    • 2004
  • 토양 우점능이 강한 생물학적 방제제 제조를 위해 경북지역 토양에서 길항균주를 분리하고 이들 중 Fusarium oxysporum, Phytophthora capsici 에 강력한 길항능을 보이는 Pseudomonas sp. 4059 를 선발, 동정하였다. Pseudomonas sp. 4059 의 시들음 병균 Fusarium oxysporum, 고추 역병균 Phytophthora capsici 에 대한 길항기작은 내열성 저분자의 항생물질과 철이온을 특이적으로 흡착하는 siderophore의 생산에 의한 것이다. Pseudomonas sp. 4059 는 항진균성 항생물질 Phenazine 생산 유전자를 소유하며 Salkowski test에 양성인 옥신류 생산도 한다는 것을 확인하였다. Pseudomonas sp. 4059 는 bioochemical tests, API test, MicroLogTM system을 통해 Pseudomonas fluorescens (biotype A)으로 98% 상동성을 보였으므로 이를 Pseudomonas fluorescens (biotype A) 4059 로 명명하였다. 선발된 길항균 Pseudomonas fluorescens (biotype A) 4059는 고추를 기주식물로 하였을 때 고추역병균인 Phytophthora capsici가 원인이 되는 고추역병을 in vivo 상에서도 충분히 억제할 수 있는 생물방제능을 나타내었다.

에센셜 오일이 항균 활성에 미치는 효과 (The Effect of Essential Oils on Antimicrobial Activity)

  • 박상남;강윤정
    • 융합정보논문지
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    • 제10권4호
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    • pp.104-114
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    • 2020
  • 본 연구는 식물에서 항생제로 알려진 11 가지 에센셜 오일(피톤치드)을 선별 한 후 혼합한 정유를 사용하여 최고의 항생제를 조사하였다. 최소억제농도 (MIC)와 최소사멸농도 (MBC) 측정 결과 Essential Oil B와 E가 목적 균의 억제효과가 높았다. 이 실험에 사용 된 S. aureus를 함유하는 모든 그람 양성 박테리아는 높은 항생제 활성을 나타냈다. 그리고 그람 양성 박테리아에서 A. baumanii와 곰팡이에서 C. albicans만이 높은 항생제 활동을 보였다. 우리의 실험에 사용 된 에센셜 오일은 항생제 활성이 뛰어난 천연 항생제 및 자연 의학의 에센셜 오일을 사용한 주요 연구와 비교할 때 더 우수한 항생제 활성을 보였다. 시험에 사용한 공시물질인 Essential Oil이 어떤 항균활성의 기전을 가지는지 알 수 없으나 다른 선행 연구결과와 비교해 볼 때 세포벽의 합성저해기전으로 해석하고 있다. 이러한 결과로부터, 항생제 활성을 갖는 일부 물질 또는 기능성 제품이 개발 될 것으로 예상된다.

Structural Insights for β-Lactam Antibiotics

  • Dogyeoung, Kim;Sumin, Kim;Yongdae, Kwon;Yeseul, Kim;Hyunjae, Park;Kiwoong, Kwak;Hyeonmin, Lee;Jung Hun, Lee;Kyung-Min, Jang;Donghak, Kim;Sang Hee, Lee;Lin-Woo, Kang
    • Biomolecules & Therapeutics
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    • 제31권2호
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    • pp.141-147
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    • 2023
  • Antibiotic resistance has emerged as a global threat to modern healthcare systems and has nullified many commonly used antibiotics. β-Lactam antibiotics are among the most successful and occupy approximately two-thirds of the prescription antibiotic market. They inhibit the synthesis of the peptidoglycan layer in the bacterial cell wall by mimicking the D-Ala-D-Ala in the pentapeptide crosslinking neighboring glycan chains. To date, various β-lactam antibiotics have been developed to increase the spectrum of activity and evade drug resistance. This review emphasizes the three-dimensional structural characteristics of β-lactam antibiotics regarding the overall scaffold, working mechanism, chemical diversity, and hydrolysis mechanism by β-lactamases. The structural insight into various β-lactams will provide an in-depth understanding of the antibacterial efficacy and susceptibility to drug resistance in multidrug-resistant bacteria and help to develop better β-lactam antibiotics and inhibitors.

Centipede Scolopendra subspinipes multilans L. KOCH로부터 정제된 항균 물질 Centipedin의 항균 Spectrum 및 작용 Mechanism 연구 (Antibiotic Spectrum and Mechanism of Centipedin)

  • 김기태;홍사원;원호식;김효준;박경배;조기승
    • 미생물학회지
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    • 제34권1_2호
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    • pp.31-36
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    • 1998
  • 지네 Scolopendra subspinipes multilans L. Koch로부터 정제한 Centipedin의 gram-negative, gram-positive bacteria 및 fungi에 대한 광범위 항균 spectrum을 조사하였으며 액체배지를 사용하여 각 균주에 대한 minimal inhibitory concentrations(MICs)값을 측정하였다. 인체의 기관중 주로 폐에 감염되는 gram-negative bacteria인 Klebsiella pneumoniae ATCC 8308 균주에 대한 MIC값이 $2{\mu}g/ml$로서 가장 강한 항균력을 나타내었고 화농균인 Proteus vulgaris NRRL B-123 균주에 대해서도 MIC값이 $16{\mu}g/ml$로 비교적 높은 항균력을 나타내었으며 항균제로서의 작용 mechanism을 시험한 결과 prokaryotic RNA transcription을 억제함을 알 수 있었다. Human blood leukemia(HL-60)와 mouse B lymphocyte myeloma cell 등의 동물세포에 대한 Centipedin의 cytotoxicity는 없는 것으로 확인되었다.

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Phenazine 1-carboxylic acid resistance in phenazine 1-carboxylic acid producing Bacillus sp. B-6

  • Kim, Kyoung-Ja
    • BMB Reports
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    • 제33권4호
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    • pp.332-336
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    • 2000
  • Phenazine 1-carboxylic acid (PCA) is an antifungal antibiotic isolated from a culture filtrate of Bacillus sp. B-6 producing an acyl CoA synthetase inhibitor. This antibiotic is reported as an inhibitor of an acyl CoA synthetase from Pseudomonas sp.. Bacillus sp. B-6 was resistant to PCA up to 350 ${\mu}g/ml$. We investigated the mechanism of the resistance of Bacillus sp. B-6 to PCA. The rate of growth in a medium containing up to 100 ${\mu}g/ml$ was as rapid as the PCA-free medium. At a PCA concentration of 300 ${\mu}g/ml$, the growth rate was more than half that of the control. In this work, we purified acyl CoA synthetase from Bacillus sp. B-6 and found that this acyl CoA synthetase was much less sensitive to PCA than the acyl CoA synthetase from other source. These findings suggested that the insensitivity of Bacillus sp. B-6 acyl CoA synthetase plays an important role in the PCA resistance of this bacterium.

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Antimicrobial Peptides (AMPs): Peptide Structure and Mode of Action

  • Park, Yoon-Kyung;Hahm, Kyung-Soo
    • BMB Reports
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    • 제38권5호
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    • pp.507-516
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    • 2005
  • Antimicrobial peptides (AMPs) have been isolated and characterized from tissues and organisms representing virtually every kingdom and phylum. Their amino acid composition, amphipathicity, cationic charge, and size allow them to attach to and insert into membrane bilayers to form pores by 'barrel-stave', 'carpet' or 'toroidal-pore' mechanisms. Although these models are helpful for defining mechanisms of AMP activity, their relevance to resolving how peptides damage and kill microorganisms still needs to be clarified. Moreover, many AMPs employ sophisticated and dynamic mechanisms of action to carry out their likely roles in antimicrobial host defense. Recently, it has been speculated that transmembrane pore formation is not the only mechanism of microbial killing by AMPs. In fact, several observations suggest that translocated AMPs can alter cytoplasmic membrane septum formation, reduce cell-wall, nucleic acid, and protein synthesis, and inhibit enzymatic activity. In this review, we present the structures of several AMPs as well as models of how AMPs induce pore formation. AMPs have received special attention as a possible alternative way to combat antibiotic-resistant bacterial strains. It may be possible to design synthetic AMPs with enhanced activity for microbial cells, especially those with antibiotic resistance, as well as synergistic effects with conventional antibiotic agents that lack cytotoxic or hemolytic activity.