Metabolite profile and in vitro activities of Phagnalon saxatile (L.) Cass. relevant to treatment of Alzheimer's disease.
The present study describes for the first time the in vitro properties (inhibition of NO production and anticholinesterase) of Phagnalon saxatile (L.) Cass. (Asteraceae). The methanolic extract showed antioxidant activity that was measured by DPPH assay and beta-carotene bleaching test. The same extract inhibited NO production in the murine monocytic macrophage cell line RAW 264.7. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition was assessed by modifications of Ellman's method. Purification of the MeOH extract of P. saxatile allowed the isolation of phenolic compounds. Among them, the compounds that most effectively inhibited lipopolysaccharide-induced NO production were caffeic acid and methylchlorogenic acid, with IC50 values of 7 microg/mL and 12 microg/mL, respectively. Luteolin and 3,5-dicaffeoylquinic acid exhibited the most promising activity against AChE with an IC50 of 25.2 and 54.5 microg/mL, respectively, while caffeic acid and luteolin exhibited higher activity against BChE with an IC50 of 32.2 and 37.2 microg/mL, respectively.
Conforti
Filomena
F
Department of Pharmaceutical Sciences, University of Calabria, Rende, Italy. filomena.conforti@unical.it
Rigano
Daniela
D
Formisano
Carmen
C
Bruno
Maurizio
M
Loizzo
Monica Rosa
MR
Menichini
Francesco
F
Senatore
Felice
F
D000110:Acetylcholinesterase / Q000187:drug effects; D000544:Alzheimer Disease / Q000188:drug therapy*; D000818:Animals; D019659:Asteraceae / Q000737:chemistry*; D002091:Butyrylcholinesterase / Q000187:drug effects; D002460:Cell Line; D002800:Cholinesterase Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D051379:Mice; D009569:Nitric Oxide / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D010936:Plant Extracts / Q000627:therapeutic use*
D002800:Cholinesterase Inhibitors; D010936:Plant Extracts; D009569:Nitric Oxide; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase