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Interactions of N'-acetyl-rifabutin and N'-butanoyl-rifabutin With Lipid Bilayers: A Synchrotron X-ray Study

Interactions of N'-acetyl-rifabutin and N'-butanoyl-rifabutin With Lipid Bilayers: A Synchrotron X-ray Study

Marina Pinheiro, Cláudia Nunes, João M Caio, Cristina Moiteiro, Gerald Brezesinski, Salette Reis

Int J Pharm. 2013 Sep 10;453(2):560-8.

PMID: 23796838

Abstract:

This work focuses on the interaction of N'-acetyl-rifabutin (RFB2) and N'-butanoyl-rifabutin (RFB3) with human and bacterial cell membrane models under physiological conditions. The effect of RFB2 and RFB3 on human cell membrane models was assessed using multilamellar vesicles (MLVs) composed of 1,2-dimyristoyl-rac-glycero-3-phosphocholine (DMPC). In order to mimic the bacterial cell membrane, MLVs of 1,2-dimyristoyl-sn-glycero-3-phospho-rac-(1-glycerol) (DMPG) and a mixture of 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (DPPE) and 1,2-dipalmitoyl-sn-glycero-3-phospho-rac-(1-glycerol) (DPPG) (8:2 molar ratio) were chosen. Small and wide-angle X-ray scattering (SAXS and WAXS) were used to study the effect of these antimycobacterial compounds on the structure formed in aqueous lipid dispersions. This study contributes to understanding the molecular mechanisms of the drugs delivery through the human and bacterial cells and the effect of these antimycobacterial compounds on the membrane lipids organization, which is related with their antibiotic efficacy and toxic effects.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP18656387	1,2-Dimyristoyl-rac-glycero-3-phosphocholine		18656-38-7	Price

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