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Phytochemicals as Inhibitors of Bacterial Cell Division Protein FtsZ: Coumarins Are Promising Candidates
Rakesh Pandeet Nankar,
Published in Humana Press Inc.
2014
PMID: 25062781
Volume: 174
   
Issue: 1
Pages: 283 - 296
Abstract
Naturally occurring phytochemicals with reported antibacterial activity were screened for their ability to inhibit the bacterial cell division protein Escherichia coli FtsZ. Among the representative compounds, coumarins inhibit the GTPase and polymerization activities of this protein effectively. Further screening with ten coumarin analogs we identified two promising candidates, scopoletin and daphnetin. The former is found to inhibit the GTPase activity of the protein in a noncompetitive manner. Docking of these coumarins with the modeled protein indicate that they bind to T7 loop, which is different from the GTP-binding site (active site), thereby supporting the experimental data. Lowest binding energy is obtained with scopoletin. 3D QSAR indicates the need for groups such as hydroxyl, diethyl, or dimethyl amino in the 7th carbon for enhanced activity. None of the coumarins exhibited cytotoxicity against NIH/3T3 and human embryonic kidney cell lines. The length of Bacillus subtilis increases in the presence of these compounds probably due to the lack of septum formation. Results of this study indicate the role of coumarins in halting the first step of bacterial cell division process. © 2014, Springer Science+Business Media New York.
About the journal
JournalApplied Biochemistry and Biotechnology
PublisherHumana Press Inc.
ISSN02732289
Open AccessNo
Concepts (90)
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    Bacteriology
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    Binding energy
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    Bins
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    Carbon
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    Cell culture
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    Cell proliferation
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    Cells
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    Cytology
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    Escherichia coli
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    Polymerization
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    COUMARIN
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    Ftsz
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    Gtpase activity
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    Phytochemicals
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    Protofilaments
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    T7 LOOP
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    Proteins
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    2,3 DIMETHOXYBENZOIC ACID
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    2,5 DIMETHOXYBENZOIC ACID
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    4 HYDOXY 3 METHOXYBENZYLAMINE
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    4 HYDROXYLCOUMARIN
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    4 hydroxyphenylacetic acid
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    6 METHYLCOUMARIN
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    7 DIETHYLAMINO 4 METHYLCOUMARIN
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    7 DIMETHYL 4 METHYLCOUMARIN
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    ANISIC ACID
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    ARECOLINE
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    Benzoic acid derivative
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    COUMARIN
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    Coumarin derivative
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    DAPHNETIN
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    ESCULETIN
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    ETHYL GROUP
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    Ftsz protein
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    Functional group
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    Guanosine triphosphatase
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    Hydroxyl group
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    HYDROXYLCOUMARIN
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    HYMECROMONE
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    Methyl group
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    METHYLEUGENOL
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    ORTHO ANISIC ACID
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    PLANT MEDICINAL PRODUCT
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    Quercetin
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    SCOPOLETIN
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    SYRINGOL
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    Umbelliferone
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    Unclassified drug
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    Bacterial protein
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    Cytoskeleton protein
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    DAPHNETIN
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    Ftsz protein, bacteria
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    SCOPOLETIN
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    Umbelliferone derivative
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    3t3 cell line
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    Article
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    Bacillus subtilis
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    Bacterial cell
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    Cell division
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    Circular dichroism
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    Controlled study
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    Crystal structure
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    Cytotoxicity
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    Drug screening
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    Embryo
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    Enzyme inhibition
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    Hek293 cell line
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    Human
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    Human cell
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    IC50
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    METHANOCALDOCOCCUS JANNASCHII
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    Molecular docking
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    Nonhuman
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    Photon correlation spectroscopy
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    Quantitative structure activity relation
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    Transmission electron microscopy
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    Animal
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    Antagonists and inhibitors
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    Chemistry
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    Drug effects
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    Growth, development and aging
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    Mouse
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    Animals
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    Bacterial proteins
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    Cytoskeletal proteins
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    Humans
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    Mice
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    Nih 3t3 cells
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    SCOPOLETIN
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    Umbelliferones