Molecular umbrella-amphotericin B conjugates.

Journal Article

A tetrawalled and an octawalled molecular umbrella conjugate of amphotericin B (AmB) have been synthesized. Both conjugates exhibit high water solubility, a low tendency to aggregate, negligible hemolytic activity at 100 μM, and an ability to release a derivative of AmB under reducing conditions that exhibits high antifungal activity. Whereas the larger, octawalled conjugate shows slight adsorption to liposomal membranes and an ability to cross them by passive transport, the tetrawalled analogue shows significant adsorption and much lower bilayer transport activity. The potential of molecular umbrella-AmB conjugates as therapeutic agents is briefly discussed.

Full Text

Duke Authors

Cited Authors

  • Janout, V; Bienvenu, C; Schell, W; Perfect, JR; Regen, SL

Published Date

  • August 2014

Published In

Volume / Issue

  • 25 / 8

Start / End Page

  • 1408 - 1411

PubMed ID

  • 25068916

Electronic International Standard Serial Number (EISSN)

  • 1520-4812

International Standard Serial Number (ISSN)

  • 1043-1802

Digital Object Identifier (DOI)

  • 10.1021/bc500277v

Language

  • eng