The influence of one week treatment with the
choline-containing
phospholipids cytidine-5'-diphosphocholine (
CDP-choline) and
choline alphoscerate (L-alpha-glyceryl-
phosphorylcholine) at
choline-equivalent doses (
CDP-choline: 325 mg/kg/day;
choline alphoscerate: 150 mg/kg/day) on
vesicular acetylcholine transporter (VAChT), on
choline transporter (CHT) and on
acetylcholine (ACh) concentrations was investigated in rat frontal cortex, striatum and cerebellum. ACh was assayed by HPLC with electrochemical detection, VAChT by Western blot, ELISA and immunohistochemistry, CHT by Western blot and immunohistochemistry. After
CDP-treatment, ACh levels were slightly increased in the frontal cortex, not substantially different in the striatum, and reduced significantly in the cerebellum compared to controls.
Choline alphoscerate stimulated significantly the
neurotransmitter concentration in the frontal cortex, however, the levels were similar to the controls in both the striatum and cerebellum. In comparison to the controls, VAChT expression following either
CDP-choline or
choline alphoscerate treatment, was enhanced greatly in the striatum and cerebellum. Also, ELISA measurements for VAChT showed significant increases in all
choline alphoscerate treated brain areas. In contrast, in the
CDP-choline treated rats the vesicular transporter amount was greater than the control only in the striatum. The
cholinergic presynaptic transporters VAChT and CHT play a relevant role in sustaining new ACh synthesis and release. To sum up,
CDP-choline and
choline alphoscerate stimulated to a different extent the expression of VAChT and CHT primarily in a cognitive area such as frontal cortex. In the lack of novel therapeutic strategies, safe compounds developed since a long time such as the
choline-containing
phospholipids investigated would merit to be further investigated by new and adequate clinical studies. This for assessing their place if any in
pharmacotherapy of
dementia disorders characterized by diminished
cholinergic tone.