Spiranthera odoratissima A. St. Hil. (manacá) is used in folk medicine to treat renal and hepatic diseases, stomachache, headaches and rheumatism. A central nervous system (CNS) depressant effect of the hexane fraction from the ethanolic extract of this plant has been described. β-caryophyllene, the main component of this essential oil, is a sesquiterpene compound with anti-inflammatory properties that has been found in essential oils derived from several medicinal plants. This work is aimed to evaluate the pharmacological activity of the essential oil obtained from S. odoratissima leaves (EO) and its major component on the murine CNS; we aimed to evaluate a possible anxiolytic-like effect and the underlying mechanisms involved. In an open field test, EO (500 mg/kg) and β-caryophyllene (50, 100 and 200 mg/kg) increased the crossing frequency (P<0.05) and, EO (250 and 500 mg/kg) and β-caryophyllene (200 mg/kg) increased the time spent in the center (P<0.05) without altering total crossings of the open field. EO and β-caryophyllene did not alter the number of falls in the rota-rod test (P>0.05). In the pentobarbital-induced sleep test, EO (500 mg/kg) and β-caryophyllene (200 and 400 mg/kg) decreased the latency to sleep (P<0.05), and EO (125, 250 and 500 mg/kg) (P<0.001) and β-caryophyllene (200 and 400 mg/kg) (P<0.05 and P<0.001) increased the sleep time. In anxiety tests, EO (500 mg/kg) and β-caryophyllene (100 and 200 mg/kg) increased head-dipping behavior (P<0.05) in the hole-board test, entries (P<0.05) into and time spent (P<0.05) on the open arms of the elevated plus maze (EPM), and number of transitions (P<0.05) and time spent in the light compartment (P<0.05) of a light-dark box (LDB). We further investigated the mechanism of action underlying the anxiolytic-like effect of EO and β-caryophyllene by pre-treating animals with antagonists of benzodiazepine (flumazenil) and 5-HT(1A) (NAN-190) receptors prior to evaluation using EPM and LDB. The anxiolytic-like effects of EO were significantly reduced by pre-treatment with NAN-190 (P<0.05) but not flumazenil (P>0.05). The anxiolytic-like effects of β-caryophyllene were not blocked by either NAN-190 or flumazenil (P>0.05). In conclusion, these results suggest that the essential oil derived from S. odoratissima produces an anxiolytic-like effect without altering motor performance and that this effect is mediated by 5-HT(1A) but not via benzodiazepine receptors. In addition, the major component, β-caryophyllene, also has an anxiolytic-like effect that may contribute to the effects of EO, but this effect does not seem to be mediated via 5-HT(1A) or benzodiazepine receptors.

Preparations from Pimenta pseudocaryophyllus (Gomes) L.R. Landrum (Myrtaceae) have been widely used in Brazilian folk medicine. This study aims to evaluate the antimicrobial activity of the crude ethanol extracts, fractions, semipurified substances, and essential oils obtained from leaves of two chemotypes of P. pseudocaryophyllus and to perform the antinociceptive and anti-inflammatory screening. The ethanol extracts were purified by column chromatography and main compounds were spectrally characterised (1D and 2D 1H and 13C NMR). The essential oils constituents were identified by GC/MS. The broth microdilution method was used for testing the antimicrobial activity. The abdominal contortions induced by acetic acid and the ear oedema induced by croton oil were used for screening of antinociceptive and anti-inflammatory activities, respectively. The phytochemical analysis resulted in the isolation of pentacyclic triterpenes, flavonoids, and phenol acids. The oleanolic acid showed the best profile of antibacterial activity for Gram-positive bacteria (31.2–125 μg mL−1), followed by the essential oil of the citral chemotype (62.5–250 μg mL−1). Among the semipurified substances, Ppm5, which contained gallic acid, was the most active for Candida spp. (31.2 μg mL−1) and Cryptococcus spp. (3.9–15.6 μg mL−1). The crude ethanol extract and fractions from citral chemotype showed antinociceptive and anti-inflammatory effects.

EMN have significant antinociceptive and anti-inflammatory effects, which appear to be, at least in part, due to the presence of allantoin. However, allantoin is not responsible for the EMN central antinociceptive activity. Allantoin has peripheral antinociceptive activity that involves the opioid receptor and ATP-sensitive K(+)channels. Opioid receptors are also involved in the EMN antinociceptive activity. These findings support the use of Memora nodosa in popular medicine and demonstrate that this plant has therapeutic potential for the development of antinociceptive and anti-inflammatory phytomedicines.

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Nonsteroidal anti-inflammatory drugs are commonly used worldwide; however, they have several adverse effects, evidencing the need for the development of new, more effective and safe anti-inflammatory and analgesic drugs. This research aimed to design, synthesize and carry out a pharmacological/toxicological investigation of LQFM-102, which was designed from celecoxib and paracetamol by molecular hybridization. To evaluate the analgesic effect of this compound, we performed formalin-induced pain, hot plate and tail flick tests. The anti-inflammatory effect of LQFM-102 was evaluated in carrageenan-induced paw oedema and pleurisy tests. The biochemical markers indicative of toxicity-AST, ALT, GSH, urea and creatinine-as well as the index of gastric lesion after prolonged administration of LQFM-102 were also analyzed. In addition, the interaction of LQFM-102 with COX enzymes was evaluated by molecular docking. In all experimental protocols, celecoxib or paracetamol was used as a positive control at equimolar doses to LQFM-102. LQFM-102 reduced the pain induced by formalin in both phases of the test. However, this compound did not increase the latency to thermal stimuli in the hot plate and tail flick tests, suggesting an involvement of peripheral mechanisms in this effect. Furthermore, LQFM-102 reduced paw oedema, the number of polymorphonuclear cells, myeloperoxidase activity and TNF-α and IL-1β levels. Another interesting finding was the absence of alterations in the markers of hepatic and renal toxicity or lesions of gastric mucosa. In molecular docking simulations, LQFM-102 interacted with the key residues for activity and potency of cyclooxygenase enzymes, suggesting an inhibition of the activity of these enzymes.

LQFM-015 demonstrated inhibition of both PLA₂ and COX enzymes; thus, the moderate antinociceptive effect of this compound could be attributed to its anti-inflammatory activity.

Acetic acid-induced writhing, hot-plate, carrageenan-induced pleurisy, formalin-induced pain, croton oil-induced ear edema, vascular permeability tests and phospholipase A 2 activity assay were used to study the analgesic and/or antiinflammatory activity of the hydromethanolic fraction of ethanolic extract from Spiranthera odoratissima A. St.-Hil., Rutaceae, leaves (HMF) and its subfraction (sub-Fr 10-28 ). HMF and sub-Fr 10-28 reduced the leukocyte migration on the carrageenaninduced pleurisy test; sub-Fr 10-28 reduced the pain reaction time in the second phase of formalin-induced pain, as well as the ear edema and vascular permeability. Both HMF and sub-Fr 10-28 inhibited the phospholipase A 2 activity. These results suggest that the analgesic effect of this plant could be, in part, due to an anti-inflammatory action produced by the inhibition of phospholipase A 2 activity.