Identification of compounds from Palicourea rigida leaves with topical anti-inflammatory potential using experimental models.

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-ß-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-ß-D-glucoside and cyclooxygenase-1 and -2 were established by molecular docking. EEPR significantly inhibited ear edema induced by Croton oil (p < 0.001), arachidonic acid (p < 0.01), phenol (p < 0.001) and capsaicin (p < 0.01 or p < 0.001). Histopathological analysis showed a reduction of edema, inflammatory cell infiltration and vasodilation. Additionally, the myeloperoxidase and N-acetyl-ß-D-glucosaminidase activities were decreased (p < 0.001). From spectroscopic data, quercetin 3-O-ß-D-glucoside was the identified compound. This compound can to interact with cyclooxygenase-1 and -2 through van der Waals interactions and dipole-dipole and hydrogen bonding's, demonstrating inhibition of these enzymes. The results indicate that EEPR is a source of active compounds with topical anti-inflammatory activity, justifying the traditional use of P. rigida and showing that this species has a therapeutic potential to treat skin inflammatory processes.

Evidence of Bioactive Compounds from Vernonia polyanthes Leaves with Topical Anti-Inflammatory Potential.

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-ß-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.

Bioactivities of the ethanol extract from Ageratum fastigiatum branches: antioxidant, antinociceptive and anti-inflammatory.

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.

Antinociceptive and anti-inflammatory activities of the sesame oil and sesamin.

Sesame oil is widely consumed as nutritious food, cooking oil, and in pharmaceuticals and food. In this study, the antinociceptive and anti-inflammatory properties of the sesame oil and sesamin were investigated. The sesame oil and sesamin reduced the number of abdominal contortions at the doses 100, 200, or 400 mg/kg. The first and second phases of the time paw licking were inhibited by sesame oil and sesamin (100, 200, or 400 mg/kg). After 90 min of treatment, sesame oil and sesamin increased the reaction time on a hot plate (200 or 400 mg/kg). Considering the tail-immersion assay, the sesame oil and sesamin produced significant effect after 60 min at the doses of 100, 200, or 400 mg/kg. After 4 h of application of the carrageenan, the sesame oil and sesamin were effective against the paw edema. The exudate volume and leucocyte migration were also reduced by sesame oil and sesamin. These results suggest that sesamin is one of the active compounds found in sesame oil and justify the antinociceptive and anti-inflammatory properties of this product.

Anti-inflammatory effects of Bryophyllum pinnatum (Lam.) Oken ethanol extract in acute and chronic cutaneous inflammation.

ETHNOPHARMACOLOGICAL RELEVANCE: 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. MATERIALS AND METHODS: 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. RESULTS: The flavonoids rutin, quercetin, luteolin and luteolin7-O-ß-d-glucoside were detected in EEBP. Topical application of EEBP significantly (P<0.001) 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. CONCLUSIONS: 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.

Chemical composition and biological activities of essential oils of Eremanthus erythropappus (DC) McLeisch (Asteraceae).

The chemical composition of the essential oils obtained by hydrodistillation of different parts of Eremanthus erythropappus, including leaves, branches and inflorescences, was investigated by Gas Chromatography and Gas Chromatography/Mass Spectrometry. The antimicrobial activity of the oils was assessed by the disc diffusion and microdilution methods, while the antioxidant activity was evaluated by DPPH and reducing power tests. The main compounds found in the essential oils derived from the inflorescences and leaves were ß-caryophyllene, germacrene-D, α-copaene and ß-pinene. α-Bisabolol was the major component in the branches. The oils were active against Staphylococcus aureus, Streptococcus pyogenes and fungi, but not Escherichia coli and Pseudomonas aeruginosa. The MIC values ranged from 0.01 to 0.50 mg/mL. Using the DPPH test, the IC50 values ranged from 38.77 ± 0.76 to 102.24 ± 1.96 µg/mL, while the reducing power test produced IC50 values between 109.85 ± 1.68 and 169.53 ± 0.64 µg/mL. The results revealed that the E. erythropappus oils are new promising potential sources of antimicrobial and antioxidant compounds with good future practical applications for human health.

Vernonia condensata Baker (Asteraceae): a promising source of antioxidants.

The present study evaluated the antioxidant potential of Vernonia condensata Baker (Asteraceae). Dried and powdered leaves were exhaustively extracted with ethanol by static maceration followed by partition to obtain the hexane, dichloromethane, ethyl acetate, and butanol fractions. Total phenols and flavonoids contents were determined through spectrophotometry and flavonoids were identified by HPLC-DAD system. The antioxidant activity was assessed by DPPH radical scavenging activity, TLC-bioautography, reducing power of Fe(+3), phosphomolybdenum, and TBA assays. The total phenolic content and total flavonoids ranged from 0.19 to 23.11 g/100 g and from 0.13 to 4.10 g/100 g, respectively. The flavonoids apigenin and luteolin were identified in the ethyl acetate fraction. The IC50 of DPPH assay varied from 4.28 to 75.10 µg/mL and TLC-bioautography detected the antioxidant compounds. The reducing power of Fe(+3) was 19.98 to 336.48 µg/mL, while the reaction with phosphomolybdenum ranged from 13.54% to 32.63% and 56.02% to 135.00% considering ascorbic acid and rutin as reference, respectively. At 30 mg/mL, the ethanolic extract and fractions revealed significant effect against lipid peroxidation. All these data sustain that V. condensata is an important and promising source of bioactive substances with antioxidant activity.

Chemical composition and biological activities of the essential oils from Duguetia lanceolata St. Hil. barks.

Essential oils of Duguetia lanceolata barks, obtained at 2 (T2) and 4 h (T4), were identified by gas chromatography and gas chromatography/mass spectrometry. ß-elemene (12.7 and 14.9%), caryophyllene oxide (12.4 and 10.7%) and ß-selinene (8.4 and 10.4%) were the most abundant components in T2 and T4, respectively. The essential oils inhibited the growth of Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli and Candida albicans. The essential oils were cytotoxic against brine shrimp. The extraction time influenced the chemical composition and biological activities of essential oils obtained from the barks of D. lanceolata.

Antinociceptive and anti-inflammatory effects of ethanol extract from Vernonia polyanthes leaves in Rodents.

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.

Analgesic and anti-inflammatory properties of essential oil from Ageratum fastigiatum

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.

Caracterização morfoanatômica de Ageratum fastigiatum (Asteraceae) / Morpho-anatomical characterization of Ageratum fastigiatum (Asteraceae)

Ageratum fastigiatum (Gardn.) R. M. King et H. Rob. (Asteraceae), conhecido como "matapasto", é uma planta usada na medicina popular como cicatrizante e antimicrobiano. O objetivo deste trabalho foi realizar caracterização morfoanatômica da folha, dos ramos e da raiz de A. fastigiatum. Secções transversais e paradérmicas, coradas com safranina/azul de astra e azul de toluidina foram analisadas ao microscópio. As folhas são alternas ou fasciculadas; a inflorescência é constituída de capítulos; as flores com corola lilás; ausência de pápus. A raiz apresenta crescimento secundário na zona de ramificação com estruturas secretoras. O caule possui epiderme uniestratificada, estômatos, tricomas tectores simples e tricomas glandulares capitados. O pecíolo exibe contorno côncavo-convexo e a epiderme é unisseriada. A lâmina foliar é anfiestomática e o mesófilo dorsiventral. A epiderme possui células de contorno sinuoso e os estômatos são do tipo anomocítico. Os caracteres morfoanatômicos permitiram estabelecer parâmetros para identificação do A. fastigiatum.

Ageratum fastigiatum (Gardn.) R. M. King et H. Rob. (Asteraceae), known as "matapasto", is a plant used in the popular medicine as cicatrizant and antimicrobial. The aim of this work was to perform a morpho-anatomical characterization of the leaves, the stems and the roots from A. fastigiatum. Transversal and paradermic sections, stained with astra safranin/blue and toluidine blue were analyzed under a microscope. The leaves are alternate or fasciculate; the inflorescence is constituted of chapters; the flowers with lilac corolla; papus is absence. The root presents secondary growth in the ramification area with secretor structures. The stem possesses epidermis unistratified, stomata, simple non-glandular trichomes and capitates glandular trichomes. The petiole exhibits concave-convex outline and the epidermis is uniseriate. The blade leaf is hypostomatic; the mesophyll is dorsiventral. The epidermis possesses cells of sinuous outline and the stomata of the anomocytic type. The morpho-anatomical characters allowed establishing parameters for identification of A. fastigiatum.

Propriedades farmacológicas do extrato etanólico de Eremanthus erythropappus (DC. ) McLeisch (Asteraceae) / Pharmacological properties of the ethanol extract from Eremanthus erythropappus (DC. ) McLeisch (Asteraceae)

O presente trabalho investigou as propriedades antinociceptiva, antiinflamatória e antiulcerogênica do extrato etanólico dos galhos de E. erythropappus. Foram realizados os testes de contorções abdominais induzidas por ácido acético; tempo da lambida da pata induzida por formalina; placa quente; edema de pata induzido por carragenina; lesões ulcerativas induzidas por indometacina e etanol. As doses de 50, 100 e 200 mg/kg inibiram as contorções em 43,07 por cento, 69,34 por cento e 70,07 por cento, respectivamente. O tempo da lambida da pata foi reduzido em ambas as fases nas doses testadas, enquanto o tempo de latência da placa quente teve efeito significativo na dose de 200 mg/kg. O edema de pata foi reduzido em 23,81 por cento (100 mg/kg) e 47,62 por cento (200 mg/kg). O índice ulcerativo das lesões induzidas por indometacina foi reduzido na dose de 100 mg/kg e 200 mg/kg, enquanto a dose de 200 mg/kg teve efeito significativo sobre o volume e o pH do suco gástrico. O índice ulcerativo e o volume do suco gástrico, induzidos por etanol, foram reduzidos na dose de 200 mg/kg, enquanto o pH do suco gástrico aumentou nas doses de 100 e 200 mg/kg. Os resultados indicam que o extrato etanólico de E. erythropappus avaliado pode constituir alvo potencial para uso em terapias da dor, da inflamação e de úlcera.

The present work investigated the antinociceptive, anti-inflammatory and antiulcerogenic activities of Eremanthus erythropappus ethanol extract. The tests were carried out by acetic acid writhing, paw licking induced by formalin, hot plate, indomethacin- and ethanol-induced ulcer. The doses of 50, 100 and 200 mg/kg inhibited the contortions in 43.07, 69.34 and 70.07 percent, respectively. Both phases of paw lick were reduced at the tested doses, while reaction time at hot plate had significant effect at 200 mg/kg. The paw edema was decreased in 23.81 percent (100 mg/kg) and 47.62 percent (200 mg/kg). The index of ulceration induced by indomethacin was reduced at the doses of 100 and 200 mg/kg, while 200 mg/kg decreased the gastric volume and pH. The index of ulceration and gastric volume induced by ethanol was reduced at 200 mg/kg, while the pH increased at 100 and 200 mg/kg. The results indicate that the ethanol extract from E. erythropappus may constitute a potential target for the use in therapies of the pain, inflammation and ulcer.

Antinociceptive and anti-inflammatory effects of the essential oil from Eremanthus erythropappus leaves.

The chemical composition of the essential oil from air-dried leaves of Eremanthus erythropappus was studied. The main compounds were beta-pinene (23.24%), beta-caryophyllene (22.92%), beta-myrcene (10.03%) and germacrene D (9.40%). The essential oil had an LD50 of 2.90 g kg(-1) in mice. Doses of 200 and 400 mg kg(-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 mg kg(-1)) and the second phase by 32.74% (200 mg kg(-1)) and 37.55% (400 mg kg(-1)). In the hot-plate test in mice, doses of 200 mg kg(-1) and 400 mg kg(-1) significantly increased the reaction time after 30, 60 and 90 min of treatment. Doses of 200 and 400 mg kg(-1) inhibited carrageenan-induced paw oedema in rats by 15.18% and 36.61%, respectively. Doses of 200 and 400 mg kg(-1) administered 4 h before intrapleural 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.

Propriedades biológicas das sementes de Joannesia princeps Vellozo / Biological properties of the Joannesia princeps Vellozo seeds

Este trabalho teve como objetivo avaliar as propriedades biológicas do extrato metanólico, obtido por Soxhlet, seguido de partição líquido/líquido (frações hexânica, diclorometânica, em acetato de etila, butanólica e residual) das sementes de Joannesia princeps. A atividade laxante foi avaliada pelo teste da motilidade intestinal em camundongos. O método de difusão em ágar utilizando Staphylococcus aureus ATCC 29737, Streptococcus mutans ATCC 25175, Escherichia coli ATCC 11229, Salmonella typhimurium ATCC 13111 e Pseudomonas aeruginosa ATCC 90271 e o bioensaio em Artemia salina foram utilizados para investigação da atividade antibacteriana e da toxidez, respectivamente. O extrato metanólico, as frações e a semente pulverizada aumentaram significativamente a motilidade intestinal. O extrato metanólico e a fração residual inibiram o crescimento de todas as amostras bacterianas de referência testadas, enquanto as frações hexânica e diclorometânica inibiram Staphylococcus aureus ATCC 29737, Salmonella typhimurium ATCC 13111 e Streptococcus mutans ATCC 25175. As frações em acetato de etila e butanólica foram ativas somente para S. aureus ATCC 29737. O extrato metanólico e as frações hexânica, diclorometânica e butanólica produziram CL50 de 56,28, 16,72, 14,82 e 67,29 ?g/mL, respectivamente. Os resultados mostraram que as sementes de J. princeps exibem atividades laxante e antibacteriana, sendo tóxicas para A. salina.

The aim of the present study was to evaluate the biological properties of the methanol extract, obtained by Soxhlet, followed by liquid/liquid partition with organic solvents (hexane, dichloromethane, ethyl acetate, butanol and residual fractions) of the Joannesia princeps seeds. Laxative activity was tested through the intestinal motility model in mice. The agar diffusion method using Staphylococcus aureus ATCC 29737, Streptococcus mutans ATCC 25175, Escherichia coli ATCC 11229, Salmonella typhimurium ATCC 13111 and Pseudomonas aeruginosa ATCC 90271and the Brine Shrimp Lethality bioassay were used to evaluate the antibacterial activity and the toxicity, respectively. The methanol extract, the fractions and the powder seeds increased the intestinal motility significantly. The methanol extract and residual fraction inhibited all reference strains tested, while the hexane, dichloromethane, ethyl acetate and butanol fractions inhibited only S. aureus ATCC 29737. The hexane and dichloromethane fractions were active against Salmonella typhimurium ATCC 13111 and Streptococcus mutans ATCC 25175. The methanol extract and hexane, dichloromethane and butanol fractions produced LC5056.28, 16.72, 14.82 and 67.29 ?g/mL, respectively. The results showed that J. princeps seeds present laxative and bacterial activities, being toxic to A. salina.