Article

Anticonvulsant activity of artificial sweeteners: a structural link between sweet-taste receptor T1R3 and brain glutamate receptors.

Medicinal Chemistry, Department of Biological Sciences, Faculty of Exact Sciences, National University of La Plata (UNLP), 47 & 115, La Plata B1900AJI, Buenos Aires, Argentina.
Bioorganic & medicinal chemistry letters (impact factor: 2.65). 04/2012; 22(12):4072-4. DOI:10.1016/j.bmcl.2012.04.076 pp.4072-4
Source: PubMed

ABSTRACT A virtual screening campaign based on application of a topological discriminant function capable of identifying novel anticonvulsant agents indicated several widely-used artificial sweeteners as potential anticonvulsant candidates. Acesulfame potassium, cyclamate and saccharin were tested in the Maximal Electroshock Seizure model (mice, ip), showing moderate anticonvulsant activity. We hypothesized a probable structural link between the receptor responsible of sweet taste and anticonvulsant molecular targets. Bioinformatic tools confirmed a highly significant sequence-similarity between taste-related protein T1R3 and several metabotropic glutamate receptors from different species, including glutamate receptors upregulated in epileptogenesis and certain types of epilepsy.

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Keywords

Acesulfame potassium
 
anticonvulsant molecular targets
 
certain types
 
different species
 
glutamate receptors upregulated
 
Maximal Electroshock Seizure model
 
metabotropic glutamate receptors
 
moderate anticonvulsant activity
 
novel anticonvulsant agents
 
potential anticonvulsant candidates
 
significant sequence-similarity
 
topological discriminant function capable
 
virtual screening campaign
 
widely-used artificial sweeteners