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Antituberculosis Drug Interactions with Membranes: A Biophysical Approach Applied to Bedaquiline

LAQV, REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, 4050-313 Porto, Portugal
Institute of Inorganic Chemistry, Graz University of Technology, Stremayergasse 6/V, 8010 Graz, Austria
Author to whom correspondence should be addressed.
Membranes 2019, 9(11), 141;
Received: 10 October 2019 / Revised: 24 October 2019 / Accepted: 27 October 2019 / Published: 30 October 2019
(This article belongs to the Section Membrane Preparation and Characterization)
This work focuses on the interaction of the novel and representative antituberculosis (anti-TB) drug bedaquiline (BDQ) with different membrane models of eukaryotic and prokaryotic cells. The effect of BDQ on eukaryotic cell membrane models was assessed using liposomes, namely, multilamellar vesicles (MLVs) made of 1,2-dimyristoyl-rac-glycero-3-phosphocholine (DMPC) and also a mixture of DMPC and cholesterol (CHOL) (8:2 molar ratio). To mimic the prokaryotic cell membrane, 1,2-dimyristoyl-sn-glycero-3-phospho-rac-(1-glycerol) (DMPG) and 1,1′2,2′-tetra-oleoyl-cardiolipin (TOCL) were chosen. Powerful biophysical techniques were employed, including small-angle X-ray scattering (SAXS) and wide-angle X-ray scattering (WAXS), to understand the effect of BDQ on the nanostructure of the membrane models. The results showed that BDQ demonstrated a pronounced disordering effect in the bacterial cell membrane models, especially in the membrane model with cardiolipin (CL), while the human cell membrane model with large fractions of neutral phospholipids remained less affected. The membrane models and techniques provide detailed information about different aspects of the drug–membrane interaction, thus offering valuable information to better understand the effect of BDQ on their target membrane-associated enzyme as well as its side effects on the cardiovascular system. View Full-Text
Keywords: antibiotic; liposomes; membrane models; WAXS; SAXS; tuberculosis antibiotic; liposomes; membrane models; WAXS; SAXS; tuberculosis
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MDPI and ACS Style

Pinheiro, M.; Amenitsch, H.; Reis, S. Antituberculosis Drug Interactions with Membranes: A Biophysical Approach Applied to Bedaquiline. Membranes 2019, 9, 141.

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