Title:Choline-Containing Phospholipids: Structure-Activity Relationships Versus Therapeutic Applications
Volume: 22
Issue: 38
Author(s): S.K. Tayebati, G. Marucci, C. Santinelli, M. Buccioni and F. Amenta
Affiliation:
关键词:
含胆碱磷脂、脑血管病、甘磷酸胆碱，胞二磷胆碱，胆碱衍生物的合成。
摘要: Choline is a quaternary ammonium salt, and being an essential component of
different membrane phospholipids (PLs) contributes to the structural integrity of cell
membranes. Choline-containing phospholipids (CCPLs) include phosphatidylcholine
(PC), sphingomyelin (SM), and choline alphoscerate (GPC). PC is the major phospholipid
in most eukaryotic cells. It is involved in SM synthesis, choline/choline metabolite
re-generation, and fatty acid/GPC formation. This paper has reviewed chemical, biological
and therapeutic features of CCPLs by analyzing: a) effects of exogenous CCPLs, b)
influence of GPC treatment on brain cholinergic neurotransmission, and c) neuroprotective
effects of GPC alone or in association with acetylcholinesterase inhibitors in animal models of brain
vascular injury, d) synthesis of the choline analogs, containing a short alkyl chain instead of a methyl
group. Cytidine-diphosphocholine and GPC, protect cell membranes and could be helpful in the sequelae
of cerebrovascular accident treatment. Moreover, cellular membrane breakdown is suggested as a feature of
neurodegeneration both in acute (stroke) and in chronic (Alzheimer and vascular dementia) brain disorders.
Published data were focused to a larger extent on the biosynthesis, relevant role in cell life, and crucial
involvement of CCPLs in cholinergic neurotransmission. The possibility of their use in the treatment of
cerebrovascular and neurodegenerative disorders is suggested by published clinical studies. In line
with these potential practical applications in pharmacotherapy, the need of further research in the field of the
synthesis of new choline derivatives with possible activity in nervous system diseases characterized by cholinergic
impairment is discussed.
