Reserpine Is the New Addition into the Repertoire of AcrB Efflux Pump Inhibitors

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Standard

Reserpine Is the New Addition into the Repertoire of AcrB Efflux Pump Inhibitors. / Shaheen, A; Afridi, W A; Mahboob, S; Sana, M; Zeeshan, N; Ismat, F; Mirza, O; Iqbal, M; Rahman, M.

I: Molecular Biology, Bind 53, Nr. 4, 10.08.2019, s. 674-684.

Publikation: Bidrag til tidsskriftTidsskriftartikelfagfællebedømt

Harvard

Shaheen, A, Afridi, WA, Mahboob, S, Sana, M, Zeeshan, N, Ismat, F, Mirza, O, Iqbal, M & Rahman, M 2019, 'Reserpine Is the New Addition into the Repertoire of AcrB Efflux Pump Inhibitors', Molecular Biology, bind 53, nr. 4, s. 674-684. https://doi.org/10.1134/S0026893319040113

APA

Shaheen, A., Afridi, W. A., Mahboob, S., Sana, M., Zeeshan, N., Ismat, F., Mirza, O., Iqbal, M., & Rahman, M. (2019). Reserpine Is the New Addition into the Repertoire of AcrB Efflux Pump Inhibitors. Molecular Biology, 53(4), 674-684. https://doi.org/10.1134/S0026893319040113

Vancouver

Shaheen A, Afridi WA, Mahboob S, Sana M, Zeeshan N, Ismat F o.a. Reserpine Is the New Addition into the Repertoire of AcrB Efflux Pump Inhibitors. Molecular Biology. 2019 aug. 10;53(4):674-684. https://doi.org/10.1134/S0026893319040113

Author

Shaheen, A ; Afridi, W A ; Mahboob, S ; Sana, M ; Zeeshan, N ; Ismat, F ; Mirza, O ; Iqbal, M ; Rahman, M. / Reserpine Is the New Addition into the Repertoire of AcrB Efflux Pump Inhibitors. I: Molecular Biology. 2019 ; Bind 53, Nr. 4. s. 674-684.

Bibtex

@article{e412d29240c146d89ae95c6bab5876cd,
title = "Reserpine Is the New Addition into the Repertoire of AcrB Efflux Pump Inhibitors",
abstract = "Acriflavine resistance protein B (AcrB) serves as prototype for multidrug resistance (MDR) efflux transporters of resistance nodulation division (RND) superfamily. AcrB has been proven as potential drug target with many synthetic and natural inhibitors have been identified such as those belonging to pyranopyridine, naphthamide and pimozide classes. The plant derived alkaloid inhibitors represented by reserpine has been found to inhibit both ATP binding cassette and major facilitator efflux transporters. In this study we report the reserpine induced inhibition of RND transporter AcrB. The preliminary docking analysis hints that reserpine shares its binding site with ciprofloxacin, a known substrate of AcrB and could possibly act as competitive inhibitor. For in vitro validation, AcrB from Salmonella typhi was cloned under the control of tac promoter and resulting vector was introduced into E. coli C41(DE3). Under autoinduced conditions, cells overexpressing AcrB transporter were subjected to combined dose of ciprofloxacin and reserpine. The combined exposure resulted in enhanced ciprofloxacin-induced growth inhibition of cells expressing AcrB transporter as compared to control cells transformed with vector of backbone sequence. Time kill analysis further confirmed these findings. To the best of our knowledge, this is first study to show that exposure to reserpine induces inhibition of AcrB. The assay developed in this study allows simple and reproducible detection of substrate/inhibitor effects upon AcrB and related efflux transporters.",
author = "A Shaheen and Afridi, {W A} and S Mahboob and M Sana and N Zeeshan and F Ismat and O Mirza and M Iqbal and M Rahman",
note = "Erratum: 10.1134/S0026893319090012",
year = "2019",
month = aug,
day = "10",
doi = "10.1134/S0026893319040113",
language = "English",
volume = "53",
pages = "674--684",
journal = "Molekulyarnaya Biologiya",
issn = "0026-8933",
publisher = "M A I K Nauka - Interperiodica",
number = "4",

}

RIS

TY - JOUR

T1 - Reserpine Is the New Addition into the Repertoire of AcrB Efflux Pump Inhibitors

AU - Shaheen, A

AU - Afridi, W A

AU - Mahboob, S

AU - Sana, M

AU - Zeeshan, N

AU - Ismat, F

AU - Mirza, O

AU - Iqbal, M

AU - Rahman, M

N1 - Erratum: 10.1134/S0026893319090012

PY - 2019/8/10

Y1 - 2019/8/10

N2 - Acriflavine resistance protein B (AcrB) serves as prototype for multidrug resistance (MDR) efflux transporters of resistance nodulation division (RND) superfamily. AcrB has been proven as potential drug target with many synthetic and natural inhibitors have been identified such as those belonging to pyranopyridine, naphthamide and pimozide classes. The plant derived alkaloid inhibitors represented by reserpine has been found to inhibit both ATP binding cassette and major facilitator efflux transporters. In this study we report the reserpine induced inhibition of RND transporter AcrB. The preliminary docking analysis hints that reserpine shares its binding site with ciprofloxacin, a known substrate of AcrB and could possibly act as competitive inhibitor. For in vitro validation, AcrB from Salmonella typhi was cloned under the control of tac promoter and resulting vector was introduced into E. coli C41(DE3). Under autoinduced conditions, cells overexpressing AcrB transporter were subjected to combined dose of ciprofloxacin and reserpine. The combined exposure resulted in enhanced ciprofloxacin-induced growth inhibition of cells expressing AcrB transporter as compared to control cells transformed with vector of backbone sequence. Time kill analysis further confirmed these findings. To the best of our knowledge, this is first study to show that exposure to reserpine induces inhibition of AcrB. The assay developed in this study allows simple and reproducible detection of substrate/inhibitor effects upon AcrB and related efflux transporters.

AB - Acriflavine resistance protein B (AcrB) serves as prototype for multidrug resistance (MDR) efflux transporters of resistance nodulation division (RND) superfamily. AcrB has been proven as potential drug target with many synthetic and natural inhibitors have been identified such as those belonging to pyranopyridine, naphthamide and pimozide classes. The plant derived alkaloid inhibitors represented by reserpine has been found to inhibit both ATP binding cassette and major facilitator efflux transporters. In this study we report the reserpine induced inhibition of RND transporter AcrB. The preliminary docking analysis hints that reserpine shares its binding site with ciprofloxacin, a known substrate of AcrB and could possibly act as competitive inhibitor. For in vitro validation, AcrB from Salmonella typhi was cloned under the control of tac promoter and resulting vector was introduced into E. coli C41(DE3). Under autoinduced conditions, cells overexpressing AcrB transporter were subjected to combined dose of ciprofloxacin and reserpine. The combined exposure resulted in enhanced ciprofloxacin-induced growth inhibition of cells expressing AcrB transporter as compared to control cells transformed with vector of backbone sequence. Time kill analysis further confirmed these findings. To the best of our knowledge, this is first study to show that exposure to reserpine induces inhibition of AcrB. The assay developed in this study allows simple and reproducible detection of substrate/inhibitor effects upon AcrB and related efflux transporters.

U2 - 10.1134/S0026893319040113

DO - 10.1134/S0026893319040113

M3 - Journal article

C2 - 31397441

VL - 53

SP - 674

EP - 684

JO - Molekulyarnaya Biologiya

JF - Molekulyarnaya Biologiya

SN - 0026-8933

IS - 4

ER -

ID: 225692428