Choline uptake in cultured porcine endothelial cells isolated from cer
ebral microvessels was investigated. A large part of the choline that
was taken up was incorporated into phospholipids within 24 h. Phorbol
12-myristate 13-acetate (PMA, 10(-7) M), a protein kinase C activator,
enhanced choline uptake and acetylcholine (ACh) synthesis in endothel
ial cells. The PMA-induced enhancement of choline uptake was neither a
ffected by calphostin C (10(-7) M), an inhibitor of protein kinase C,
nor hemicholinium 3 (10(-5) M) treatment. These results suggest that b
rain endothelial cells have a choline uptake system, which is not iden
tical to the high-affinity choline uptake system located in cholinergi
c neurons, and that the PMA-induced enhancement of choline uptake is i
ndependent of protein kinase C activation. Some of the choline taken u
p from the extracellular space is used for acetylcholine synthesis.