Neuropharmacological effects in mice of Lychnophora species (Vernonieae, Asteraceae) and anticonvulsant activity of 4,5-di-O-[E]-caffeoylquinic acid isolated from the stem of L. rupestris and L. staavioides.
Aiming at contributing with the search for neuroactive substances from natural sources, we report for the first time antinociceptive and anticonvulsant effects of some Lychnophora species. We verify the protective effects of polar extracts (600 mg/kg, intraperitoneally), and methanolic fractions of L. staavioides and L. rupestris (100 mg/kg, intraperitoneally) in pentylenetetrazole-induced seizures on mice. Previously, a screening was accomplished, evaluating the antinociceptive central activity (hot plate test), with different extracts of L. rupestris, L. staavioides and L. diamantinana. It was possible to select the possible extracts of Lychnophora with central nervous system activity. Some of the active extracts were submitted to fractionation and purification process and the methanolic fractions of L. rupestris (stem) and L. staavioides (stem), with anticonvulsant properties (100 mg/kg, intraperitoneally), yielded 4,5-di-O-[E]-caffeoylquinic acid. This substance was injected intraperitoneally in mice and showed anticonvulsant effect against pentylenetetrazole-induced seizures at doses of 25 and 50 mg/kg. It has often been shown that seizures induced by pentylenetetrazole are involved in inhibition and/or attenuation of GABAergic neurotransmission. However, other systems of the central nervous system such as adenosinergic and glutamatergic could be involved in the caffeoylquinic acid effects. Further studies should be conducted to verify that the target receptor could be participating in this anticonvulsant property. Although other investigations have reported a series of biological activities from Lychnophora species, this is the first report of central analgesic and anticonvulsant activity in species of this genus.
Taleb-Contini
Silvia H
SH
Laboratory of Organic Chemistry, Department of Physics and Chemistry, Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, SP, Brazil.
Santos
Wagner F
WF
Mortari
Márcia R
MR
Lopes
Norberto P
NP
Lopes
João L C
JL
D000700:Analgesics / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D000818:Animals; D000927:Anticonvulsants / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D019659:Asteraceae / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D008297:Male; D051379:Mice; D009005:Monosaccharides / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D010146:Pain / Q000188:drug therapy; D010147:Pain Measurement; D010433:Pentylenetetrazole; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D018547:Plant Stems; D011801:Quinic Acid / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000302:isolation & purification / Q000494:pharmacology; D012640:Seizures / Q000188:drug therapy
C500583:4,5-di-O-(E)-caffeoylquinic acid; D000700:Analgesics; D000927:Anticonvulsants; D009005:Monosaccharides; D010936:Plant Extracts; D011801:Quinic Acid; D010433:Pentylenetetrazole