Synthesis of Potent Inhibitors of β-Ketoacyl-Acyl Carrier Protein Synthase III as Potential Antimicrobial Agents

Liu, Yan; Zhong, Wu; Li, Rui-Juan; Li, Song

doi:10.3390/molecules17054770

Cited by 12 publications

(11 citation statements)

References 14 publications

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“…In addition, this biosensor was also used to analyse E. coli O157:H7 in synthetic samples, and the results were well consistent with the plate count method. Compared with existing techniques for E. coli detection, such as ELISA and other previous reported methods, [6][7][8][9][10][11][12][13][14] our EIA-based biosensing strategy offered improved sensitivity and widened linear range. Moreover, the proposed approach had the advantages of simplicity, time efficiency, easy preparation, and low cost detection with high stability.…”

Section: Discussionmentioning

confidence: 96%

“…Moreover, the use of antibody offers high specicity intrinsic to the immuno-recognition, which also improves binding efficiency and enhances the selectivity of the biosensor. Furthermore, the proposed biosensor overcomes the limitations of previously reported methods, [6][7][8][9][10][11][12][13][14] and provides simple, rapid, and costeffective detection of E. coli O157:H7 with high sensitivity and selectivity. Hence, the developed electrochemical-based immunosensor might provide a useful and practical tool for E. coli O157:H7 determination and related food safety analysis and clinical diagnosis.…”

Section: Introductionmentioning

confidence: 90%

“…However, this procedure is rather timeconsuming to obtain visible colonies that can be identied. Recent efforts in developing novel non-culture based strategies includes enzyme linked immunosorbent assay (ELISA), 6,7 polymerase chain reaction (PCR), 8,9 protein microassays, 10 quartz crystal microbalance (QCM) system, 11 surface plasmon resonance (SPR), 12,13 and ow cytometry 14 -based assay methods. For example, PCR-based assays involve the amplication and subsequent analysis of pathogen-specic nucleic acid by PCR and sequencing, which have the ability of simultaneous analysis of multiple pathogens.…”

Section: Introductionmentioning

confidence: 99%

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Electrochemical immunosensor assay (EIA) for sensitive detection of E. coli O157:H7 with signal amplification on a SG–PEDOT–AuNPs electrode interface

Guo

Wang

Liu

et al. 2015

Analyst

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A novel electrochemical immunosensor assay (EIA) for highly sensitive and specific detection of Escherichia coli O157:H7 has been developed. This immunosensor is constructed by the assembly of capture antibody on SG-PEDOT-AuNPs composites modified glass carbon electrode. In the presence of target E. coli O157:H7, horseradish peroxidase (HRP)-labeled antibody is captured on the electrode surface to form a sandwich-type system via the specific identification. As a result, E. coli O157:H7 detection is realized by outputting a redox current from electro-reduction of hydrogen peroxide reaction catalyzed by HRP. In our assay, the combination of the unique properties of sulfonated graphene (SG) and gold nanoparticles (AuNPs) can not only accelerate electron transfer on electrode interface, but also provide an excellent scaffold for the conjugation of capture antibody that significantly improves the target capture efficiency and enhances the sensitivity of the biosensor. The results reveal the calibration plot obtained for E. coli O157:H7 is approximately linear from 7.8 × 10-7.8 × 10(6) colony-forming unit (cfu) mL(-1) with the limit of detection of 3.4 × 10 cfu mL(-1). In addition, the biosensor has been successfully applied to the quantitative assay of E. coli O157:H7 in synthetic samples (spring water and milk). Hence, the developed electrochemical-based immunosensor might provide a useful and practical tool for E. coli O157:H7 determination and related food safety analysis and clinical diagnosis.

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Section: Discussionmentioning

confidence: 96%

Section: Introductionmentioning

confidence: 90%

Section: Introductionmentioning

confidence: 99%

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Electrochemical immunosensor assay (EIA) for sensitive detection of E. coli O157:H7 with signal amplification on a SG–PEDOT–AuNPs electrode interface

Guo

Wang

Liu

et al. 2015

Analyst

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“…Mtb fabH has no homologous proteins in humans. The six alkaloids (vasicoline, vasicolinone, vasicinone, vasicine, adhatodine, and anisotine, Figure 1(b)) extracted from the leaves of Justicia adhatoda and the selected synthetic small molecule compounds were found to have moderate activity against fabH [16,17].…”

Section: β-Ketoacyl-acylmentioning

confidence: 99%

Advances in Key Drug Target Identification and New Drug Development for Tuberculosis

Gong

2022

BioMed Research International

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Tuberculosis (TB) is a severe infectious disease worldwide. The increasing emergence of drug-resistant Mycobacterium tuberculosis (Mtb) has markedly hampered TB control. Therefore, there is an urgent need to develop new anti-TB drugs to treat drug-resistant TB and shorten the standard therapy. The discovery of targets of drug action will lay a theoretical foundation for new drug development. With the development of molecular biology and the success of Mtb genome sequencing, great progress has been made in the discovery of new targets and their relevant inhibitors. In this review, we summarized 45 important drug targets and 15 new drugs that are currently being tested in clinical stages and several prospective molecules that are still at the level of preclinical studies. A comprehensive understanding of the drug targets of Mtb can provide extensive insights into the development of safer and more efficient drugs and may contribute new ideas for TB control and treatment.

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“…β-ketoacyl-acyl carrier protein synthase III of M. tuberculosis (mtKASIII) links the fatty acid synthase I and II systems, catalyzing the condensation of fatty acid synthase I–derived acyl-coenzyme (Co)A with malonyl-acyl-carrier protein [ 23 , 24 , 25 ]. It is also a key condensing enzyme responsible for the initiation of type II fatty acid biosynthesis and is a potential target for novel anti-TB agents [ 26 ]. We previously reported on synthetic lead and natural compounds with broad-spectrum anti-bacterial activity as inhibitors of KAS III protein [ 27 , 28 ].…”

Section: Introductionmentioning

confidence: 99%

Phloretin Exerts Anti-Tuberculosis Activity and Suppresses Lung Inflammation

et al. 2017

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An increase in the prevalence of the drug-resistant Mycobacteria tuberculosis necessitates developing new types of anti-tuberculosis drugs. Here, we found that phloretin, a naturally-occurring flavonoid, has anti-mycobacterial effects on H37Rv, multi-drug-, and extensively drug-resistant clinical isolates, with minimum inhibitory concentrations of 182 and 364 μM, respectively. Since Mycobacteria cause lung inflammation that contributes to tuberculosis pathogenesis, anti-inflammatory effects of phloretin in interferon-γ-stimulated MRC-5 human lung fibroblasts and lipopolysaccharide (LPS)-stimulated dendritic cells were investigated. The release of interleukin (IL)-1β, IL-12, and tumor necrosis factor (TNF)-α was inhibited by phloretin. The mRNA levels of IL-1β, IL-6, IL-12, TNF-α, and matrix metalloproteinase-1, as well as p38 mitogen-activated protein kinase and extracellular signal-regulated kinase phosphorylation, were suppressed. A mouse in vivo study of LPS-stimulated lung inflammation showed that phloretin effectively suppressed the levels of TNF-α, IL-1β, and IL-6 in lung tissue with low cytotoxicity. Phloretin was found to bind M. tuberculosis β-ketoacyl acyl carrier protein synthase III (mtKASIII) with high affinity (7.221 × 107 M−1); a binding model showed hydrogen bonding of A-ring 2′-hydroxy and B-ring 4-hydroxy groups of phloretin with Asn261 and Cys122 of mtKASIII, implying that mtKASIII can be a potential target protein. Therefore, phloretin can be a useful dietary natural product with anti-tuberculosis benefits.

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Synthesis of Potent Inhibitors of β-Ketoacyl-Acyl Carrier Protein Synthase III as Potential Antimicrobial Agents

Cited by 12 publications

References 14 publications

Electrochemical immunosensor assay (EIA) for sensitive detection of E. coli O157:H7 with signal amplification on a SG–PEDOT–AuNPs electrode interface

Electrochemical immunosensor assay (EIA) for sensitive detection of E. coli O157:H7 with signal amplification on a SG–PEDOT–AuNPs electrode interface

Advances in Key Drug Target Identification and New Drug Development for Tuberculosis

Phloretin Exerts Anti-Tuberculosis Activity and Suppresses Lung Inflammation

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