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Palicourea rigida Kunth (Rubiaceae), also called “bate-caixa” or “douradao”, has been used as antihypertensive, antiulcerogenic, anti-inflammatory and analgesic by traditional communities. Pharmacological potential of the ethanol extract from P. rigida (EEPR) and two quercetin derivatives were investigated. Using the high performance liquid chromatography (HPLC) assay, EEPR was analyzed. Phenolic contents (total phenolic and flavonoids) were quantified by spectrophotometric methods. 2,2-diphenyl-1-pycrilhydrazil (DPPH), iron reducing power and β-carotene/linoleic acid bleaching tests were applied to estimate the antoxidant capacity of EEPR. Nociception (acetic acid-induced writhing, formalin and hot plate) and inflammation (carrageenan-induced paw edema and pleurisy) assays were performed. Molecular docking was used to measure the interactions’ profiles of ligands (rutin and quercetin) and cyclooxigenases (COX-1 and COX-2). HPLC analysis identified rutin and quercetin derivatives. Expressive levels of total phenolic and flavonoids and a promising antioxidant effect were measured. EEPR, rutin and quercetin reduced the abdominal contortions. EEPR was effective against both phases of formalin, while rutin and quercetin inhibited the second phase. The latency time on hot plate significantly increased after treatment with EEPR. Inflammatory parameters (paw edema, exudate volume and leukocyte infiltrate) were diminished by EEPR, rutin and quercetin. The molecular docking showed that rutin and quercetin are capable of complexing with COX-1 and COX-2 favorably through physical-chemical interactions. The results suggest that EEPR showed a relevant pharmacological potential, which may be related to action of rutin and quercetin derivatives. Key words: Palicourea rigida, rutin, quercetin, antioxidant, antinociception, inflammation.

The present study investigated the in- vivo and vitro bioactivities of the essential oil of Duguetia lanceolata branches (EODL) and caryophyllene oxide (CO). The chemical composition of EODL was analyzed by GC and GC/MS. Acetic acid-induced writhing, formalin, hot plate and tail-immersion methods were used to evaluate the antinociceptive effect in mice. Anti-inflammatory activity was tested by carrageenan-induced paw edema and pleurisy in rats, and in mouse models of acute ear inflammation induced by croton oil and arachidonic acid. 2,2-Diphenyl-1-picrylhydrazyl (DPPH), reducing power and 𝛽-carotene bleaching assays were used to determine the antioxidant bioactivity. i¢-Elemene, caryophyllene oxide and i¢-eudesmol were the major components found in EODL. When tested, EODL and CO reduced the number of writhes and both phases of the time of paw licking, while the reaction time on a hot plate and the pain latency duration by the tail-immersion assay were increased. EODL and CO were effective against the paw edema, exudate volume, leucocyte migration and ear edema. EODL and CO also showed in vitro antioxidant activity. These results suggest that caryophyllene oxide is one of the active compounds found in EODL and could partially justify the bioactivity of this oil. Key words: Duguetia lanceolata, essential oil, caryophyllene oxide, antinociceptive activity, anti-inflammatory activity, antioxidant activity.

Palicourea rigida Kunth is traditionally used for the treatment of skin diseases, kidney pains and ovarian inflammation. Based on these traditional uses, this study evaluated the topical anti-inflammatory activity of the ethanol extract from P. rigida leaves (EEPR) and identified bioactive compounds. Ear edema was induced in Swiss mice by the topical application of Croton oil, arachidonic acid, phenol and capsaicin. Histopathological analysis and myeloperoxidase and N-acetyl-β-D-glucosaminidase activities were determined. EEPR was characterized by UHPLC-UV-MS HPLC and the isolated compound was identified through 1H and 13C nuclear magnetic resonance and mass fragmentation. Interaction profiles between quercetin 3-O-β-D-glucoside and cyclooxygenase-1 and -2 were established by molecular docking. EEPR significantly inhibited ear edema induced by Croton oil (p

Bryophyllum pinnatum (Lam.) Oken (Crassulaceae), popularly known in Brazil as "folha-da-fortuna", is a plant species used in folk medicine for the external and internal treatment of inflammation, infection, wound, burn, boil, ulcers and gastritis, and several other diseases. The present study aimed to perform the chemical characterization and the evaluation of the topical anti-inflammatory effect of the ethanol extract of Bryophyllum pinnatum leaves (EEBP) in acute and chronic mice ear edema models induced by different irritant agents.The EEBP chemical characterization was performed by HPLC-UV DAD. Ear edema on Swiss mice was induced by the topical application of Croton oil (single and multiple applications), arachidonic acid, phenol, capsaicin and ethyl phenylpropiolate (EPP). The topical anti-inflammatory effect of EEBP was evaluated by measuring the ear weight (acute inflammation models) and thickness (chronic inflammation model). Histopathological analyses of ear tissue samples sensitized with Croton oil (single and multiple applications) were also performed.The flavonoids rutin, quercetin, luteolin and luteolin7-O-β-d-glucoside were detected in EEBP. Topical application of EEBP significantly (P0.001) inhibited the ear edema induced by Croton oil single application (inhibition of 57%), arachidonic acid (inhibition of 67%), phenol (inhibition of 80%), capsaicin (inhibition of 72%), EPP (inhibition of 75%) and Croton oil multiple application (55% after 9 days). Histopathological analyses confirmed the topical anti-inflammatory effect of EEBP since it was observed reduction of edema, epidermal hyperplasia, inflammatory cells infiltration and vasodilation.The results suggest that EEBP is effective as a topical anti-inflammatory agent in acute and chronic inflammatory processes possibly due to inhibition of arachidonic acid pathway, which justify the traditional use of Bryophyllum pinnatum as a remedy for skin disorders.

The present study was designed to investigate the antioxidant, antinociceptive and anti-inflammatory activities of the ethanol extract from Ageratum fastigiatum branches. Phytochemical screening and total phenol and flavonoid contents were determined. The antioxidant activity was assessed by 2,2-diphenyl-1-pycrilhydrazin (DPPH) and iron reducing power methods. The antinociceptive effect was evaluated using the acetic acid-induced writhing, formalin, hot plate and tail immersion assays; while the carrageenan-induced paw edema and pleurisy tests were performed to examine the anti-inflammatory activity against acute inflammation. The extract revealed the presence of flavonoids, tannins, coumarins, terpenes, sterols and saponins. Expressive levels of total phenols and flavonoids and a promising antioxidant effect were quantified. At the doses of 50, 100 and 200 mg/kg, the extract inhibited the writhing, reduced both phases of paw licking time and increased the reaction time on the hot plate. In the tail immersion test, the extract (50, 100 and 200 mg/kg) caused a significant inhibition of pain. In these doses, the paw edema, exudate volume and leucocyte mobilization were significantly reduced. These results suggest that A. fastigiatum can be an active source of substances with antioxidant, antinociceptive and anti-inflammatory activities, adding scientific support to the appropriate use in the Brazilian folk medicine. RESUMO O presente estudo foi projetado para investigar as atividades antioxidante, antinociceptiva e anti-inflamatória do extrato etanólico dos galhos de Ageratum fastigiatum. Perfil fitoquímico e teores de fenois totais e flavonoids foram determinados. A atividade antioxidante foi avaliada por 2,2-difenil-1-picril-hidrazila (DPPH) e pelo método de poder de redução do ferro. O efeito antinociceptivo foi avaliado usando os ensaios de contorções abdominais induzidas por ácido acético, formalina, placa quente e imersão da cauda; enquanto os testes do edema de pata e pleurisia induzidos por carragenina foram realizados para examinar a atividade anti-inflamatória contra inflamação aguda. O extrato revelou a presença de flavonoides, taninos, cumarinas, terpenos, esteroides e saponina. Teores expressivos de fenóis totais e flavonoides e um promissor efeito antioxidante foram quantificados. Nas doses de 50, 100 e 200 mg/kg, o extrato inibiu as contorções, reduziu ambas as fases do tempo da lambida da pata e aumentou o tempo de reação sobre a placa quente. No teste de imersão da cauda, o extrato (50, 100 e 200 mg/kg) causou uma inibição significativa da dor. Nessas doses, o edema de pata, o volume do exsudato e a migração leucocitária foram significativamente reduzidos. Esses resultados sugerem que A. fastigiatum pode ser uma fonte de substâncias ativas com atividades antioxidante, antinociceptiva e anti-inflamatória, adicionando uma base científica para o uso na medicina popular brasileira.

The ethanol extract from Vernonia polyanthes leaves (EEVP) was investigated for antinociceptive and anti-inflammatory effects at the doses (p.o.) of 100, 200 and 400 mg/kg in animal models. The extract reduced the number of abdominal contortions by 16.75% and 31.44% at a dose of 200 and 400 mg/kg, respectively. The results obtained showed that EEVP exerted a significant antinociceptive effect in the two phases of formalin. The EEVP increased the reaction time on a hot plate at the doses of 100, 200 and 400 mg/kg after 90 min of treatment. The paw edema was reduced by EEVP at the doses of 100, 200 and 400 mg/kg after 4 h of application of carrageenan. Doses of 200 and 400 mg/kg, administered 4 h before the carrageenan injection, significantly reduced the exudate volume (29.25 and 45.74%, respectively) and leukocyte migration (18.19 and 27.95%, respectively). These results suggest that V. polyanthes can be an active source of substances with antinociceptive and anti-inflammatory activities.

The chemical composition of the essential oil from air-dried leaves of Eremanthus erythropappus was studied. The main compounds were β-pinene (23.24%), β-caryophyllene (22.92%), β-myrcene (10.03%) and germacrene D (9.40%). The essential oil had an LD50 of 2.90 gkg−1 in mice. Doses of 200 and 400 mgkg−1 inhibited 10.69% and 27.06% of acetic-acid-induced writhing in mice, respectively. In the formalin-induced nociception test in mice, the essential oil inhibited the first phase of paw licking by 29.13% (400 mgkg−1) and the second phase by 32.74% (200 mgkg−1) and 37.55% (400 mgkg−1). In the hot-plate test in mice, doses of 200 mgkg−1 and 400 mgkg−1 significantly increased the reaction time after 30, 60 and 90 min of treatment. Doses of 200 and 400 mgkg−1 inhibited carrageenan-induced paw oedema in rats by 15.18% and 36.61%, respectively. Doses of 200 and 400 mgkg−1 administered 4 h before intra-pleural injection of carrageenan significantly reduced exudate volume (by 20.20% and 48.70%, respectively) and leucocyte mobilization (by 5.88% and 17.29%, respectively). These results demonstrate that E. erythropappus has analgesic and anti-inflammatory properties, supporting the use of this plant in folk medicine.

Vernonia polyanthes Less. (Asteraceae), popularly known as “assa-peixe”, is a plant species used in Brazilian traditional medicine for the treatment of cutaneous damage, cicatrization, inflammation, and rheumatism. Based on these ethnopharmacological findings, the current study evaluated the topical anti-inflammatory effects of the hexane (HEVP) and ethyl acetate (EAEVP) extracts from V. polyanthes leaves in experimental models of skin inflammation. Chemical characterization was carried out by HPLC–UV/DAD analysis. Anti-inflammatory activity was evaluated using Croton oil-, arachidonic acid (AA)-, phenol-, ethyl phenylpropiolate (EPP)-, and capsaicin-induced ear edema models in mice. Histopathological evaluation and measurements of myeloperoxidase (MPO) and N-acetyl-β-d-glucosaminidase (NAG) enzymes were also performed. Rutin, luteolin, and apigenin were identified in EAEVP. Topically applied HEVP and EAEVP significantly (p < 0.05, p < 0.01 or p < 0.001) reduced edema induced by five different irritants at the doses tested (0.1, 0.5 and 1.0 mg/ear). Histopathological analysis revealed a reduction of edema, inflammatory cell infiltration, and vasodilation. In addition, the enzymes activity (MPO and NAG) in the ear tissues was reduced by the topical treatment of HEVP and EAEVP (p < 0.05, p < 0.01 or p < 0.001). The results suggest that V. polyanthes leaves are effective against cutaneous damage, which support its traditional use and open up new possibilities for the treatment of skin disorders.

In the current investigation, the antinociceptive and anti-inflammatory effects of the ethyl acetate and butanol fractions from Annona coriacea leaves were evaluated using standard experimental test models. The antinociceptive activity of A. coriacea was studied by acetic acid-induced writhing, formalin and hot-plate tests, and the anti-inflammatory activity was determined by carrageenan-induced rat paw edema and carrageenan-induced pleurisy. Inhibition of the acetic acid-induced abdominal contortions was observed at the doses of 50 and 100 mg/kg. After injection of formalin, the dose of 100 mg/kg inhibited the time spent paw licking in the first phase, while the second phase was inhibited at the doses of 10, 50 or 100 mg/kg. In the hot-plate assay, the reaction time was increased at 90 min in animals that received 100 mg/kg. Doses of 50 and 100 mg/kg inhibited carrageenan-induced paw edema, the exudate volume, and leucocyte migration. The present results demonstrate that fractions of A. coriacea have antinociceptive and anti-inflammatory effects, supporting the use of this plant in folk medicine.

The chemical composition, analgesic and anti-inflammatory properties of essential oil from Ageratum fastigiatum were investigated. The main compounds found in the essential oil were germacrene D, α-humulene and β-cedrene. The oil, with LD50 of 2.50 g/kg, inhibited the acetic acid-induced writhing at the dose of 200 mg/kg. In the formalin test, the oil inhibited the first phase (200 mg/kg) and the second phase (100 mg/kg and 200 mg/kg). In the hot plate test, after 30 and 60 min of treatment the doses of 100 and 200 mg/kg increased the reaction time. The antiedematogenic effect, reduction on the exudate volume and leukocyte mobilization were observed at the doses of 100 and 200 mg/kg. The results indicated that A. fastigiatum possessed the analgesic and anti-inflammatory properties that supported the popular medicinal use of the plant.A composição química e as propriedades analgésica e antiinflamatória do óleo essencial de Ageratum fastigiatum foram investigadas. Os principais constituintes do óleo essencial foram germacreno D, α-humuleno e β-cedreno. O óleo, com DL50 de 2,50 g/kg, inibiu as contorções abdominais induzidas por ácido acético na dose de 200 mg/kg. No teste da formalina, o óleo inibiu a primeira fase (200 mg/kg) e a segunda fase (100 e 200 mg/kg). O tempo de latência aumentou no teste da placa quente, após 30 e 60 minutos de tratamento, nas doses de 100 e 200 mg/kg. O efeito antiedematogênico, assim como a redução do volume do exsudato e da migração leucocitária foram observados nas doses de 100 e 200 mg/kg. Os resultados indicam que o A. fastigiatum possui propriedades analgésica e antiinflamatória, o que corrobora com o uso popular da planta.