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Croton blanchetianus Baill, commonly known as “marmeleiro”, is native to the Brazilian Caatinga is traditional used to treat joint pain and gastrointestinal disorders. The aim of the study was identify the chemical constituents by HPLC-DAD and determine the antioxidant activity of the spray-dried extract (SDE) aqueous (AqF) and ethyl acetate (EAF) fractions obtained from the leaves of C. blanchetianus; and to determine the acute (single dose, 2000 or 5000 mg/kg, p.o) and subacute (repeated dose, 250, 500 and 1000 mg/kg, p.o) toxicities, and genotoxicity (1000 and 2000 mg/kg, p.o) of the EAF in mice. In the acute oral toxicity assay the LD50 was determined as > 5000 mg/kg. In the subacute toxicity, changes in weight gain, food and water intake, hematological, organ coefficients, oxidative stress parameters were not observed; however, changes in transaminases and leukocyte infiltration in the liver were observed at the highest dose. The genotoxicity test showed that high concentrations of EAF were not genotoxic in micronucleus and comet assays. The enrichment process was confirmed by HPLC and five flavonoids were identified. Our results provide evidence that the EAF was safe to use, although a long-term dose of 1000 mg/kg in should be avoided.

Members of the Psidium genus have been suggested in ethnobotanical research for the treatment of various human diseases, and some studies have already proven their popular uses through research, such as Psidium glaziovianum, which is found in Brazil's northeast and southeast regions and has antinociceptive and anti-inflammatory properties; however, the safety of use has not yet been evaluated.This study investigated the safety of using essential oil obtained from P. glaziovianum leaves (PgEO) in vitro and in vivo models.Cytotoxicity was evaluated in murine erythrocytes, while acute toxicity, genotoxicity (comet assay) and mutagenicity (micronucleus test) studies were performed using Swiss albino mice.In the cytotoxicity assay, the hemolysis rate indicated a low capacity of PgEO to cause cell lysis (0.33-1.78%). In the acute oral toxicity study, animals treated with up to up to 5000 mg/kg body weight did not observe mortality or physiological changes. Neither dosage caused behavioral problems or death in mice over 14 days. The control and 2,000 mg/kg groups had higher feed intake and body weight than the 5,000 mg/kg PgEO group. Erythrocyte count, hemoglobin level, mean corpuscular volume, and MCV decreased, but serum alanine and aspartate aminotransferases increased. In the genotoxic evaluation, 5000 mg/kg PgEO enhanced nucleated blood cell DI and DF.The present study describes that PgEO can be considered well tolerated in acute exposure at doses up to 2000 mg/kg, however the dose of 5000 mg/kg of PgEO should be used with caution.

Eugenia pohliana (Myrtaceae) is used in folk medicine by communities in Brazil. However, there are no reports on its biological activity. This is the first to identify the components of E. pohliana essential oil (EpEO) and evaluate their antinociceptive and anti-inflammatory activities in an in vivo model at doses of 25, 50, and 100 mg/kg. The essential oil (EO) was obtained by hydrodistillation, and the analysis was performed by gas chromatography coupled with mass spectrometry. Antinociceptive activity was evaluated by writhing tests, tail movement, and formalin (neurogenic and inflammatory pain); naloxone was used to determine the nociception mechanism. Anti-inflammatory activity was assessed by edema and peritonitis tests. We found that (E)-β-caryophyllene (BCP) (15.56%), δ-cadinene (11.24%) and α-cadinol (10.89%) were the major components. In the writhing test, there was a decrease in writhing by 42.95–70.70%, in the tail movement, an increase in latency time by 69.12–86.63%, and in the formalin test, there was a reduction in pain neurogenic by 29.54–61.74%, and inflammatory pain by 37.42–64.87%. The antinociceptive effect of EpEO occurs through the activation of opioid receptors. In addition to antinociceptive activity and mechanism, a reduction in inflammation by 74.93‒81.41% was observed in the paw edema test and inhibition of the influx of leukocytes by 51.86‒70.38% and neutrophils by 37.74‒54.72% in the peritonitis test. It was concluded that EpEO has antinociceptive pharmacological properties with opioid and anti-inflammatory actions, and that its use does not cause hemolytic damage or behavioral change.

In this study, the toxicity and antinociceptive effects of the ethanolic extract of Croton blanchetianus leaves were investigated in mice. Phytochemical analysis was performed by thin layer chromatography (TLC) and high–performance liquid chromatography (HPLC) revealed the presence of alkaloids, reducing sugars, cinnamic derivatives, flavonoids, saponins, condensed tannins, terpenes, and steroids. Acute toxicity was evaluated by administration of a single dose of 2000 or 5000 mg/kg b.w. (per os or i.p.). The extract (50, 100, and 200 mg/kg per os) was evaluated for genotoxicity through micronucleus and comet assays, and antinociceptive effects using different tests. No death was observed but increased serum levels of hepatic and renal markers, hematological changes, and histological alterations in the lung and kidney were observed exclusively with intraperitoneal administration. Oral administration did not result in genotoxicity in bone marrow or peripheral blood cells. The extract reduced the number of abdominal writhings by 47.16–88.81%, increased the latency time (up to 2.13 times) in the tail–immersion test, and decreased the paw licking time by as much as 74.07% and 97.76% in the first and second phases of the formalin test, respectively. This work contributes to the determination of safety and pharmacological potential for C. blanchetianus leaves.

The ethanolic extract from Croton blanchetianus leaves has been shown to have antinociceptive activity in mice. Here, we investigated the antinociceptive activity of an ethyl acetate fraction (EAF) from this extract in mice and the possible pathways involved in the analgesic effect. Adverse effects on behavior and motor coordination were also evaluated. The EAF was characterized by liquid chromatography coupled with mass spectrometry and evaluated (12.5, 25, and 50 mg/kg per os) in the acetic acid-induced abdominal writhing, formalin, hot plate, and tail immersion assays. Naloxone, atropine, glibenclamide, prazosin, or yohimbine was pre-administered to mice to investigate the involved pathways in the formalin test. The open-field, rotarod, and elevated plus-maze tests were used to assess behavior and locomotion. The main components of the EAF were quercetin-3-O-(2-rhamnosyl) rutinoside, hyperoside, quercetin rutinoside pentoside, and quercetin hexoside deoxyhexoside. EAF showed antinociceptive effects in all models and was effective against both neurogenic and inflammatory pain. The reversion of the effects in the formalin test by naloxone and atropine revealed that the EAF acted via the opioid and cholinergic systems. In the open-field test, the behavior of the animals treated with the EAF was like that of control, except at the highest dose, when hypnosis, eyelid ptosis, decreased walking, hygiene, and rearing behaviors were observed. No muscle relaxant effect was observed, but an anxiogenic effect was observed at all doses. This study provides new scientific evidence on the pharmacological properties of C. blanchetianus leaves and their potential for the development of phytomedicines with analgesic properties.

The purpose of this study was to analyses the influence of seasonal variation on the chemical composition and antimicrobial, antioxidant and cytotoxicity activities of the essential oil (EO) extracted from the leaves of Eugenia pohliana. Chemical characterization of the samples - by gas chromatography-mass spectrometry - found 35 and 38 components for summer and winter, respectively, of the EO from E. pohliana leaves, totaling 47 different compounds. Analysis of antioxidant capacity (DPPH, ABTS and TAC) revealed that the summer EO showed greater free radical scavenging capacity than the winter. Similarly, the summer EO exhibited superior antimicrobial potential (MIC=128-512 μg/mL and MMC=128-1024 μg/mL, compared to the winter EO (128-2048 μg/mL and 256-2048 μg/mL, respectively). Results showed that both oils had a low potential to cause hemolysis. This study provides new scientific evidence on the influence of seasonality on the pharmacological properties of E. pohliana leaves and its potential for the development of herbal medicines.

Myrciaria pilosa is a tree species of the Brazilian Caatinga biome. This paper is the first report on the chemical composition and the antimicrobial and antivirulence activities of essential oil extracted from its leaves. The oil was extracted by hydrodistillation. Chemical composition determined by GC–MS and CG–FID revealed 63 compounds; the sesquiterpenes guaiol (13.17%) and (E)-β-caryophyllene (11.26%) dominated. Antimicrobial activity against strains of Staphylococcus aureus was evaluated by the broth microdilution method. It showed minimum inhibitory concentrations (MIC) of 5 μg/mL against evaluated strains and minimum bactericidal concentrations (MBC) ranging from 10 to 20 μg/mL. Evaluation of antivirulence activity showed reductions of 92.0% and 47.2%, respectively, in haemolytic action and production of staphyloxanthin. These findings show that the essential oil of M. pilosa has potential as an antimicrobial drug to control infection by multi-resistant strains of S. aureus.

Eugenia gracillima is widely used by the population in the manufacture of pulps and jellies, with popular reports of its use in the treatment of infections in the urinary system, respiratory and dermatological problems. A previous study reports that EO from E. gracillima leaves proved to be a promising antioxidant agent in combating the promastigote forms of protozoa. Despite this, this species has been little studied due to its pharmacological properties.In this study, an essential oil extracted (EO) from Eugenia gracillima leaves was evaluated for its acute toxicity and anti-inflammatory, antinociceptive and behavioral effects in mice.The EO was obtained by hydrodistillation, and the composition analysis was performed by gas chromatography coupled to mass spectrometry. Acute toxicity assessment was performed with observation of hematological parameters and histopathological evaluation, as well as tests to investigate antinociceptive, anti-inflammatory activities and behavioral effects.Chromatographic analysis showed D-germacrene (16.10%), γ-muurolene-g (15.60%) and bicyclogermacrene (8.53%) as the majority of compounds. In the toxicity evaluation, no death or physiological changes were observed in mice treated with a single oral dose of up to 5000 mg/kg, and it did not lyse erythrocytes in vitro. The hematological parameters evaluated were not changed after treatment; however, 5,000 mg/kg promoted an increase in transaminase levels. In the histopathological evaluation, only the animals that received the dose of 5000 mg/kg showed discrete leukocyte infiltration around the centrilobular vein in the liver. Antinociceptive activity was detected through tests of acetic acid-induced writhing, formalin, and tail flick, promoted in part by the opioid receptor pathway. In the evaluation of anti-inflammatory activity, a reduction in inflammation was observed in the paw edema test and a decrease in the migration of leukocytes and neutrophils in the peritonitis test. The open field and elevated plus maze tests showed that EO did not affect the animals' motor functions or exploratory activity.It was concluded that the essential oil of E. gracillima has potential for the development of pharmaceutical formulations with analgesic and anti-inflammatory actions in non-toxic concentrations.

Eugenia uniflora (Myrtaceae) is a species native to Brazil and has a traditional use in the treatment of inflammation.To evaluate the anti-inflammatory and antinociceptive effects, and the involvement of opioid receptors in the antinociceptive activity of extract and fractions from Eugenia uniflora leaves.TLC and HPLC were used to characterize the spray-dried extract (SDE) and fractions. In the in vivo assays, Swiss (Mus musculus) mice were used. Carrageenan-induced hind-paw edema and carrageenan-induced peritonitis models were used to determine the anti-inflammatory effect of the extract (50, 100, or 200 mg/kg). Acetic acid-induced writhing, tail-flick, and formalin tests were used to determine the antinociceptive effect of the extract (50, 100, or 200 mg/kg). The aqueous (AqF) and ethyl acetate (EAF) fractions (6.25, 12.5, and 25 mg/kg) were then combined with naloxone to evaluate the involvement of opioid receptors in the antinociceptive activity.In this work, the TLC and HPLC analysis evidenced the enrichment of EAF, which higher concentration of gallic acid (5.29 ± 0.0004 %w/w), and ellagic acid (1.28 ± 0.0002 %w/w) and mainly myricitrin (8.64 ± 0.0002 %w/w). The extract decreased the number of total leukocytes and neutrophils in the peritoneal cavity (p 0.05), at doses of 100 and 200 mg/kg and showed significant inhibition in the increase of paw edema volume (p 0.05). The treatment per oral route (doses of 50, 100, and 200 mg/kg) significantly reduced the nociceptive response in acetic acid-induced abdominal writhing (p 0.05). The effect of the extract on the tail-flick test showed a significant increase in latency time of animals treated at doses of 200 and 100 mg/kg (p 0.05). The extract and ethyl acetate fraction reduced the nociceptive effect in both phases of formalin at all tested doses. The naloxone reversed the antinociceptive effect of EAF, suggesting that opioid receptors are involved in mediating the antinociceptive activity of EAF of E. uniflora in the formalin test.The current study demonstrates the anti-inflammatory and analgesic activities of water: ethanol: propylene glycol spray-dried extract from E. uniflora leaves using in vivo pharmacological models in mice. Our findings suggest that spray-dried extract and ethyl acetate fraction exhibit peripheral and central antinociceptive activity with the involvement of opioid receptors that may be related to the presence of flavonoids, mainly myricitrin.

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Plants of the genus Psidium have been employed in "in natura" consumption and agroindustry, and owing to the diversity of phytochemicals, the development of new pharmaceutical forms has received remarkable research interest. In this study, the essential oil obtained from Psidium glaziovianum (PgEO) leaves were evaluated antinociceptive and anti-inflammatory activities were evaluated in mouse models. Initially, PgEO was characterized by gas chromatography-mass spectrometry and gas chromatography with flame ionization detection, and the profile was dominated by sesquiterpene compounds. In the evaluation of acute antinociceptive activity (abdominal contortions induced by acetic acid, formalin, tail immersion, and hot plate tests), PgEO promoted a reduction in nociception in the chemical and thermal models. Additionally, the potential underlying mechanism was investigated using pain pathway blockers, and the results revealed a combined action of opioidergic and muscarinic pathways. The anti-inflammatory potential was confirmed by anti-edematogenic action, reduced cell migration, pro-inflammatory cytokine production, and granuloma formation in chronic processes. This study provides evidence that PgEO can be effective for the treatment of pain and acute and chronic inflammation.

This work evaluated the antioxidant properties and in vivo antinociceptive and anti-inflammatory effects of extracts obtained from fruit peels of Myrciaria floribunda (H. West ex Willd.) O. Berg (Myrtaceae). This plant is popularly known in Brazil as Cambuí or camboim. Different extracts were submitted to comparative analysis to determine the content of selected phytochemical classes (levels of total phenols, flavonoids, and monomeric anthocyanins) and the in vitro antioxidant potentials. The extract with higher potential was selected for in vivo evaluation of its antinociceptive and anti-inflammatory action. Finally, the chemical characterization of this extract was performed by high-performance liquid chromatography (HPLC). MfAE (extract obtained using acetone as solvent) showed the higher levels of phenols (296 mg GAE/g) and anthocyanins contents (35.65 mg Cy-3-glcE/g) that were associated with higher antioxidant activity. MfAE also exhibited in vivo anti-inflammatory and analgesic propertiers. This fraction inhibited the inflammatory and neurogenic phases of pain, and this effect was reversed by naloxone (suggesting the involvement of opioidergic system). MfAE reduced the abdominal contortions induced by acetic acid. The HPLC analysis revealed the presence of gallic acid (and its derivatives) and ellagic acid. Taken together, these data support the use of M. floribunda fruit peels for development of functional foods and nutraceutics.

Eugenia stipitata is a Brazilian plant species used in traditional medicine for a wide range of ailments. Considering the biotechnological potential of herbal oils, in this study an essential oil was evaluated for toxicity, antinociceptive, antipyretic, and anti-inflammatory activity in mice model. The essential oil from Eugenia stipitata (EsEO) leaves was obtained by hydrodistillation and analyzed by gas chromatography-mass spectrometry. Abdominal contortion tests were performed to evaluate its antinociceptive activity. For estimating its anti-inflammatory activity, tests of paw edema, peritonitis, and protein denaturation were performed. The antipyretic effect was assessed with a yeast-induced pyrexia model. Artemia salina was used for environmental biomonitoring and preliminary toxicity. To analyse the safety of use; acute toxicity and hemolytic activity were performed. Majority of the compounds were identified by guaiol (13.77%), trans-caryophyllene (11.36%), and β-eudesmol (8.13%) e γ-eudesmol (6.55%). Essential Oil from E. stipitata promoted mortality of A. salina nauplii, with an LC50 of 812.45 μg/mL. No mice death(s) was noted with oral administration of the essential oil at 2000 and 5000 mg/kg, respectively; additionally, no alterations were observed with biochemical, hematological, and histopatological analyses. Markedly reduced abdominal contortion (54.1–56.6% inhibition) at all doses as compared with the negative control. Reduction in inflammation was also seen. In the paw edema test, a significant decrease in edema (88.66–96.94%) was observed. Whereas, in peritonitis; a reduction in the migration of total leukocytes (76.8–86.5%) and neutrophils (74.5–79.6%) was noted. Moreover, EsEO was capable of inhibiting protein denaturation (74.39–82.83%) as compared with the control (45.02–100%) at the concentrations evaluated. It also exerted an antipyretic effect after the first 1 h of evaluation, until the end of observation duration (4 h). The results suggested EsEO as a promising source of natural antinociceptive, anti-inflammatory, and antipyretic constituent for application in food and pharmaceutical industries.