bc5b00463_si_001.pdf (1.02 MB)
Taming Amphotericin B
journal contribution
posted on 2015-10-21, 00:00 authored by Vaclav Janout, Wiley
A. Schell, Damien Thévenin, Yuming Yu, John R. Perfect, Steven L. RegenA strategy
is introduced for enhancing the cellular selectivity
of Amphotericin B (AmB) and other classes of membrane-disrupting agents.
This strategy involves attaching the agent to a molecular umbrella
to minimize the disruptive power of aggregated forms. Based on this
approach, AmB has been coupled to a molecular umbrella derived from
one spermidine and two cholic acid molecules and found to have antifungal
activities approaching that of the native drug. However, in sharp
contrast to AmB, the hemolytic activity and the cytotoxcity of this
conjugate toward HEK293 T cells have been dramatically reduced.