Our results indicate that the ethanolic extract of Zanthoxylum rhoifolium exhibits a significant gastroprotection, because it inhibits the formation of gastric lesions using different models. The release of the nitric oxide, the opening of the K(ATP) channels, the participation of the non-protein sulfhydril groups (NP-SH), catalase and the increase of mucous secretion seem to be involved in the gastroprotection activity of the EEZR. Nevertheless, this activity does not seem to be related to antisecretory mechanisms.
Context: The essential oil (EO) from Thymus capitatus Hoff. et Link. (Lamiaceae) has been traditionally used for its medicinal properties, such as anti-inflammatory, analgesic, antioxidant and antimicrobial properties.Objective: Characterize the constituents from T. capitatus EO and further evaluate the antinociceptive activity by in vivo and in vitro procedures.Materials and methods: Gas chromatography–mass spectrometry was used to identify and quantify the constituents of the T. capitatus EO. The antinociceptive activity was evaluated in vivo by the glutamate-induced nociception model in male Swiss mice (25 g), at doses of 3, 6 and 12 mg/kg, 1 h before evaluation of the licking time response (0–15 min). The mechanism of T. capitatus EO (1–500 μg/mL) on the isolated nerve excitability of Wistar rat (300 g) was assessed by the single sucrose technique.Results and discussion: The EO of T. capitatus presented 33 components, mainly monoterpenes and sesquiterpenes, carvacrol (ca. 80%) was its major constituent. T. capitatus EO induced antinociception in orally treated mice (3, 6, and 12 mg/kg) reducing the licking time from control (100.3 ± 11.9 s) to 84.8 ± 12.2, 62.7.6 ± 9.9, and 41.5 ± 12.7 s, respectively (n = 8; p < 0.05). Additionally, we have demonstrated that T. capitatus EO (500 μg/mL) decreased the compound action potential amplitude (VCAP) of about 80.0 ± 4.3% from control recordings (n = 4; p < 0.05). Such activity was presumably mediated through a voltage-gated Na+ channels.Conclusions: The present study demonstrated the antinociceptive activity of Thymus capitatus essential oil, which acts via peripheral nervous excitability blockade.
Pharmacological treatment of inflammatory pain is usually done by administration of
non-steroidal anti-inflammatory drugs (NSAIDs). These drugs present high efficacy,
although side effects are common, especially gastrointestinal lesions. One of the
pharmacological strategies to minimize such effects is the combination of drugs and
natural products with synergistic analgesic effect. The monoterpene terpinolene (TPL)
is a chemical constituent of essential oils present in many plant species, which have
pharmacological activities, such as analgesic and anti-inflammatory. The association
of ineffective doses of TPL and diclofenac (DCF) (3.125 and 1.25 mg/kg
po, respectively) presented antinociceptive and anti-inflammatory
effects in the acute (0, 1, 2, 3, 4, 5 and 6 h, after treatment) and chronic (10
days) inflammatory hyperalgesia induced by Freund's complete adjuvant (CFA) in the
right hind paw of female Wistar rats (170-230 g, n=6-8). The mechanical hyperalgesia
was assessed by the Randall Selitto paw pressure test, which determines the paw
withdrawal thresholds. The development of edema was quantified by measuring the
volume of the hind paw by plethismography. The TPL/DCF association reduced
neutrophils, macrophages and lymphocytes in the histological analysis of the paw,
following a standard staining protocol with hematoxylin and eosin and the counts were
performed with the aid of optical microscopy after chronic oral administration of
these drugs. Moreover, the TPL/DCF association did not induce macroscopic gastric
lesions. A possible mechanism of action of the analgesic effect is the involvement of
5-HT2A serotonin receptors, because ketanserin completely reversed the
antinociceptive effect of the TPL/DCF association. These results suggest that the
TPL/DCF association had a synergistic anti-inflammatory and analgesic effect without
causing apparent gastric injury, and that the serotonergic system may be involved in
the antinociceptive effect of this association.
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