Massive Bioaccumulation and Self-Assembly of Phenazine Compounds in Live Cells.

ABSTRACT: Clofazimine is an orally administered, FDA-approved drug that massively bioaccumulates in macrophages, forming membrane-bound intracellular structures possessing nanoscale supramolecular features. Here, a library of phenazine compounds derived from clofazimine was synthesized and tested for their ability to accumulate and form ordered molecular aggregates inside cells. Regardless of chemical structure or physicochemical properties, bioaccumulation was consistently greater in macrophages than in epithelial cells. Microscopically, some self-assembled structures exhibited a pronounced, diattenuation anisotropy signal, evident by the differential absorption of linearly polarized light, at the peak absorbance wavelength of the phenazine core. The measured anisotropy was well above the backgroun

SUBMITTER: Min KA 

PROVIDER: S-EPMC4569013 | biostudies-literature | 2015 Aug

REPOSITORIES: biostudies-literature