Antinociceptive Properties of the Hydroalcoholic Extract, Fractions and Compounds Obtained from the Aerial Parts of Baccharis illinita DC in Mice

Abstract

The present study assessed the possible antinociceptive action of the hydroalcoholic extract, fractions and pure compounds obtained from the aerial parts of Baccharis illinita DC (Asteraceae) in behavioural models of chemical nociception in mice. The hydroalcoholic extract and fractions (hexane and aqueous but not EtOAc fraction) obtained from B. illinita (30-1000 mg/kg orally) produced a dose-related inhibition of the acetic acid-induced nociceptive response. However, the hexane fraction was more potent than the hydroalcoholic extract and the aqueous fraction. The hexane fraction derivatives baurenol, α -spinasterol and oleanolic acid (0.00001-10 mg/kg intraperitoneally) also caused potent inhibition of acetic acid-induced pain. The hexane fraction (300-1000 mg/kg orally) produced inhibition of both phases of formalininduced pain. Moreover, the hexane fraction (30-600 mg/kg orally) also caused a dose-dependent inhibition of glutamateinduced pain. Nevertheless, the hexane fraction only at the dose of 300 mg/kg orally, produced partial inhibition of the paw oedema caused by carrageenan. Furthermore, the hexane fraction (300 mg/kg orally) caused inhibition of the nociceptive response induced by intrathecal injection of N -methyl-d -aspartic acid, α -amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid, tumour necrosis factor-α and interleukin-1 β . In contrast, the hexane fraction did not affect the biting response induced by the metabotropic or ionotropic glutamatergic receptor agonist (±)-1-aminocyclopentane-trans -1,3-dicarboxylic acid and kainate, respectively. In addition, the antinociception caused by the hexane fraction (300 mg/kg orally) in the acetic acid test was not affected by intraperitoneal treatment of mice with naloxone (a non-selective opioid receptor antagonist). The precise mechanism responsible for the antinociceptive effect of the hexane fraction remains unclear, but appears to be partly associated with an inhibition of glutamatergic transmission and an inhibition of pathways dependent on proinflammatory cytokines. Finally, baurenol, α -spinasterol and oleanolic acid have an important role in the antinociceptive effects of the hexane fraction. Moreover, the antinociceptive action demonstrated in the present study supports the ethnomedical uses of this plant.The genus Baccharis belongs to the Asteraceae family and several species (e.g. Baccharis trimera ) are commercialized in Brazil. The species of the Baccharis genus have high economic and social value and are broadly distributed across the Brazilian states of Santa Catarina, Paraná, São Paulo and Rio Grande do Sul. In these states, species of Baccharis are used in folk medicine to treat widely varying diseases [1,2]. Baccharis illinita DC is an annual sub-shrub with yellowish flowers that grows in natural grasslands. This plant is popularly known in the south of Brazil as 'chá ventura' or 'erva milagrosa' and has been used in folk medicine as an anti-inflammatory, for the healing of skin and mucosal wounds, and for its gastroprotecti...

Identification of the Plant Steroid α-Spinasterol as a Novel Transient Receptor Potential Vanilloid 1 Antagonist with Antinociceptive Properties

“…Only the Dcm fraction and ␣-spinasterol reduced edema formation and spontaneous nociception. Our results are in accordance with previous findings that demonstrated that ␣-spinasterol exerted antinociceptive effects in different acute pain models, including glutamate-mediated spontaneous nociception and acetic acid-induced abdominal constriction (Meotti et al, 2006;Ribas et al, 2008;Freitas et al, 2009). However, the mechanisms underlying the antinociceptive effect of ␣-spinasterol remain to be elucidated.…”

Antinociceptive effectiveness of triterpenes from rosemary in visceral nociception

“…They are natural products structurally characterized by a basic backbone with 30 carbon atoms derived from the cyclization of squalene. Oleanolic acid and its isomer, ursolic acid, as well as micromeric acid have been found in species used around the world in folk medicine to relieve inflammation (Al-Sereiti et al, 1999;Peng et al, 2007) and nociception (Maia et al, 2006a, b;Kang et al, 2008;Freitas et al, 2009;Kawano et al, 2009;Muñ oz et al, 2011;AlvesRodrigues et al, 2012). A mixture of these triterpenes was reported to be the possibly responsible for the antinociceptive activity of Bouchea fluminensis (Verbenaceae) determined by using the hot plate and writhing tests in mice (Costa et al, 2003).…”

“…or, the NSAID acetylsalicylic acid (aspirin) ID 50 ¼24 mg/kg i.p. (Freitas et al, 2009). Furthermore, oleanolic acid (10-100 mg/kg, p.o.)…”

Antinociceptive, anti-inflammatory and antioxidant activities of aqueous extract from Remirea maritima (Cyperaceae)

“…Therefore, it is common to associate this model to that most closely resembling the clinical condition of pain, being a useful model for the investigation of potential analgesic drugs (Tjolsen et al, 1997;Freitas et al, 2009). In this assay, the aqueous extract was not able to reduce the antinociceptive response in any dose evaluated in the first phase.…”

“…The thermal stimulus of the hot plate test is employed to study the analgesic activity mediated by central mechanisms. It is an animal model that evaluates the antinociceptive activity of opioid drugs, but other drugs with central activity, such as sedatives and hypnotics show activity in the hot plate model (Freitas et al, 2009).…”