Central nervous system depressant action of flavonoid glycosides.
The pharmacological effects on the central nervous system (CNS) of a range of available flavonoid glycosides were explored and compared to those of the glycosides 2S-hesperidin and linarin, recently isolated from valeriana. The glycosides 2S-neohesperidin, 2S-naringin, diosmin, gossipyn and rutin exerted a depressant action on the CNS of mice following i.p. injection, similar to that found with 2S-hesperidin and linarin. We demonstrate in this work that these behavioural actions, as measured in the hole board, thiopental induced sleeping time and locomotor activity tests, are unlikely to involve a direct action on gamma-aminobutyric acid type A (GABA(A)) receptors. The corresponding aglycones were inactive, pointing to the importance of the sugar moieties in the glycosides in their CNS depressant action following systemic administration. The pharmacological properties of the flavonoid glycosides studied here, in addition to our previous results with hesperidin and linarin, opens a promising new avenue of research in the field.
Fernández
Sebastián P
SP
Instituto de Química y Fisicoquímica Biológicas, Facultad de Farmacia y Bioquímica, Buenos Aires, Argentina.
Wasowski
Cristina
C
Loscalzo
Leonardo M
LM
Granger
Renee E
RE
Johnston
Graham A R
GA
Paladini
Alejandro C
AC
Marder
Mariel
M
D000818:Animals; D002492:Central Nervous System Depressants / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology*; D006027:Glycosides / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects / Q000502:physiology; D010936:Plant Extracts; D011485:Protein Binding / Q000187:drug effects / Q000502:physiology; D051381:Rats; D017208:Rats, Wistar; D012890:Sleep / Q000187:drug effects / Q000502:physiology
D002492:Central Nervous System Depressants; D005419:Flavonoids; D006027:Glycosides; D010936:Plant Extracts