It has been recently demonstrated in the laboratory that the cytoskeletal i
nhibitor cytochalasin E has an indirect inhibitory effect on the function o
f the intestinal Na+-sugar cotransporter (SGLT1). The present work confirms
that cytochalasin E inhibits SGLT1 activity through cytoskeleton disruptio
n, showing that in anaerobic conditions (N-2 bubbling), which implies low c
ytosolic ATP levels, the inhibition is not observed. As it occurs in sugar
transport, the Na+-dependent intestinal transport of phenylalanine decrease
s if cytochalasin E is present in the incubation medium. However, the activ
ity of the brush border enzymes sucrase, amino peptidase N and gamma-glutam
yl transferase is not affected by the inhibitor. These enzymes only have on
e transmembrane domain and the active center is projected to the intestinal
lumen. Therefore, cytoskeleton changes that could modify the transmembrane
enzyme segment do not alter the activity of these enzymes. Examination of
the intestine morphology after 30 min incubation with cytochalasin E shows
only light modifications which do not seem to explain the inhibitory effect
s of the toxin on Na+-sugar or Na+-phenylalanine cotransporters function. O
n the whole, these results indicate that the inhibition of cytochalasin E o
n galactose and phenylalanine intestinal transport is secondary to its acti
on on cytoskeleton through protein structure modifications.