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

Abstract

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.

Histolocalization of chemotaxonomic markers in Brazilian Vernonieae (Asteraceae)

“…It is well know that Lychnophorinae produce metabolites of therapeutic importance, such as terpenoids (mono‐, sesqui‐, di‐ and triterpenes and sesquiterpene lactones) and phenolic compounds (flavonoids and cinnamic acid derivatives) (Vichnewski & Gilbert, ; Vichnewski et al ., ; Herz et al ., ; Dias Barros et al ., ; Oliveira et al ., ; Grael et al ., ; Dos Santos et al ., ; Kanashiro et al ., ; Taleb‐Contini et al ., ; Silvério et al ., ; Keles et al ., ; Dos Santos et al ., ; Baldin et al ., ; De Souza et al ., ; Abreu et al ., ; Silvério et al ., ; Gouvea et al ., ; Saúde‐Guimarães, Raslan & Oliveira, ). In addition, many studies have investigated the chemotaxonomy of Lychnophorinae because of the chemical richness that characterizes the subtribe (Bohlmann et al ., , b; Herz et al ., ; Bohlmann et al ., ; Zdero et al ., ; Bohlmann et al ., ; Bohlmann & Jakupovic, ; Borella et al ., ; Lunardello et al ., ; Borella et al ., ; Vichnewski et al ., ; Sacilotto, Sartori & Vichnewski, ; Sartori et al ., ; Sakamoto et al ., , ; Keles et al ., ; Sakamoto et al ., ; Souza et al ., ; Lusa et al ., ).…”

The role of polar phytocomplexes on anticonvulsant effects of leaf extracts of <I>Lippia alba</I> (Mill.) N.E. Brown chemotypes

“…[22] Moreover, it is known that phenylpropanoids derived from caffeic acid exhibit neuroprotective effects. [23,24] Regarding the anticonvulsant molecular mechanism, the 80% ethanolic extract of L. alba LP3 chemotype, one of the most effective anticonvulsants evaluated and also that obtained in a larger amount, inhibited GABA uptake and GABA binding in a dose-dependent manner. These data suggest that the presence of non-volatile compound(s), probably phenylpropanoids, flavonoids and inositols, might function as GABA agonist(s) or GABA uptake inhibitor(s) leading to an enhanced and sustained GABA inhibitory activity, which could play a role in L. alba anticonvulsant molecular mechanism.…”

Chemical Ecology and Volatile Terpenes Biosynthesis of "Arnicas-da-Serra" from Brazil

“…31 -Capacidade anticonvulsivante de ácido cafeoilquínico de Lychnophora rupestris e L. staavioides. 32 -Efeito antihipernociceptivo de derivado do bisabolano, em modelo in vitro, majoritário na fração volátil de folhas de Lychnophora ericoides. 20 -Capacidade anti-carcinogênica Lychnophora ericoides.…”