Oxysterols, oxygenated derivatives of cholesterol selected for their cytost
atic activity and their inhibitory effect on cholesterol synthesis, have be
en investigated for their anti-human immunodeficiency virus (HIV) activity
in vitro. The three oxysterols tested, 7 beta-hydroxycholesterol (7 beta-OH
C), 25-hydroxycholesterol (25-OHC) and 7 beta,25-dihydroxycholesterol (7,25
-OHC), inhibit viral replication at micromolar concentrations. The selectiv
ity indexes for 7 beta-OHC and 25-OHC are quite modest (2 to 8) but reprodu
cible; the dihydroxycholesterol 7,25-OHC exhibited antiviral properties at
concentrations 13- to 25-fold lower than the highest concentration tested a
t which no toxicity was measurable. Oxysterols are naturally occurring comp
ounds, and we speculate on their physiological relevance in HIV-infected in
dividuals.