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Article

Antimicrobial and Efflux Pump Inhibitory Activity of Carvotacetones from Sphaeranthus africanus Against Mycobacteria

1
Institute of Pharmaceutical Sciences, Department of Pharmacognosy, University of Graz, Universitaetsplatz 4, 8010 Graz, Austria
2
School of Medicine, Vietnam National University—HCMC, Quarter 6, Linh Trung Ward, Thu Duc District, HCM City 700000, Vietnam
3
Institute of Structural and Molecular Biology, Department of Biological Sciences, Birkbeck, University of London, Malet Street, London WC1E 7HX, UK
4
Institute of Pharmaceutical Sciences, Department of Pharmaceutical Chemistry, University of Graz, Schubertstraße 1, 8010 Graz, Austria
5
Department of Pharmacognosy, School of Medicine and Pharmacy, Da Nang University, 41 Le Duan Street, Hai Chau District, Da Nang City 550000, Vietnam
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Antibiotics 2020, 9(7), 390; https://doi.org/10.3390/antibiotics9070390
Received: 15 May 2020 / Revised: 30 June 2020 / Accepted: 6 July 2020 / Published: 8 July 2020
Carvotacetones (1–7) isolated from Sphaeranthus africanus were screened for their antimycobacterial and efflux pump (EP) inhibitory potential against the mycobacterial model strains Mycobacterium smegmatis mc2 155, Mycobacterium aurum ATCC 23366, and Mycobacterium bovis BCG ATCC 35734. The minimum inhibitory concentrations (MICs) of the carvotacetones were detected through high-throughput spot culture growth inhibition (HT-SPOTi) and microbroth dilution assays. In order to assess the potential of the compounds 1 and 6 to accumulate ethidium bromide (EtBr) in M. smegmatis and M. aurum, a microtiter plate-based fluorometric assay was used to determine efflux activity. Compounds 1 and 6 were analyzed for their modulating effects on the MIC of EtBr and the antibiotic rifampicin (RIF) against M. smegmatis. Carvotacetones 1 and 6 had potent antibacterial effects on M. aurum and M. bovis BCG (MIC ≤ 31.25 mg/L) and could successfully enhance EtBr activity against M. smegmatis. Compound 1 appeared as the most efficient agent for impairing the efflux mechanism in M. smegmatis. Both compounds 1 and 6 were highly effective against M. aurum and M. bovis BCG. In particular, compound 1 was identified as a valuable candidate for inhibiting mycobacterial efflux mechanisms and as a promising adjuvant in the therapy of tuberculosis or other non-tubercular mycobacterial infections. View Full-Text
Keywords: Sphaeranthus africanus L.; Compositae; carvotacetones; mycobacteria; ethidium bromide accumulation; efflux pumps; efflux pump inhibitors Sphaeranthus africanus L.; Compositae; carvotacetones; mycobacteria; ethidium bromide accumulation; efflux pumps; efflux pump inhibitors
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MDPI and ACS Style

Tran, H.T.; Solnier, J.; Pferschy-Wenzig, E.-M.; Kunert, O.; Martin, L.; Bhakta, S.; Huynh, L.; Le, T.M.; Bauer, R.; Bucar, F. Antimicrobial and Efflux Pump Inhibitory Activity of Carvotacetones from Sphaeranthus africanus Against Mycobacteria. Antibiotics 2020, 9, 390. https://doi.org/10.3390/antibiotics9070390

AMA Style

Tran HT, Solnier J, Pferschy-Wenzig E-M, Kunert O, Martin L, Bhakta S, Huynh L, Le TM, Bauer R, Bucar F. Antimicrobial and Efflux Pump Inhibitory Activity of Carvotacetones from Sphaeranthus africanus Against Mycobacteria. Antibiotics. 2020; 9(7):390. https://doi.org/10.3390/antibiotics9070390

Chicago/Turabian Style

Tran, Huyen Thi, Julia Solnier, Eva-Maria Pferschy-Wenzig, Olaf Kunert, Liam Martin, Sanjib Bhakta, Loi Huynh, Tri Minh Le, Rudolf Bauer, and Franz Bucar. 2020. "Antimicrobial and Efflux Pump Inhibitory Activity of Carvotacetones from Sphaeranthus africanus Against Mycobacteria" Antibiotics 9, no. 7: 390. https://doi.org/10.3390/antibiotics9070390

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