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.

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.

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.

Protective effects of Baccharis dracunculifolia leaves extract against carbon tetrachloride- and acetaminophen-induced hepatotoxicity in experimental animals.

In this work we investigated the in vivo protective effects of Baccharis dracunculifolia leaves extract (BdE) against carbon tetrachloride (CCl4)- and acetaminophen (APAP)-induced hepatotoxicity. Total phenolic content, total flavonoid content, antioxidant DPPH radical scavenging activity, and HPLC analysis were performed. Our results showed that pretreatment with BdE significantly reduced the damage caused by CCl4 and APAP on the serum markers of hepatic injury, AST, ALT, and ALP. Results were confirmed by histopathological analysis. Phytochemical analysis, performed by HPLC, showed that BdE was rich in p-coumaric acid derivatives, caffeoylquinic acids and flavonoids. BdE also showed DPPH antioxidant activity (EC50 of 15.75±0.43 µg/mL), and high total phenolic (142.90±0.77 mg GAE/g) and flavonoid (51.47±0.60 mg RE/g) contents. This study indicated that B. dracunculifolia leaves extract has relevant in vivo hepatoprotective properties.

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.

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.

Solidagenone from Solidago chilensis Meyen inhibits skin inflammation in experimental models.

Solidagenone (SOL) is a labdane-type diterpenoid found in Solidago chilensis, a plant traditionally used to treat skin diseases, kidney pain and ovarian inflammation. In this study, the topical anti-inflammatory activity of SOL was evaluated using in vivo and in silico assays. Croton oil-, arachidonic acid (AA)- and phenol-induced ear oedema mouse models were applied in the in vivo studies. Myeloperoxidase (MPO) and N-acetyl-ß-D-glucosaminidase (NAG) activities and tumour necrosis factor alpha (TNF-α), interleukin-6 (IL-6) and nitric oxide (NO) levels were determined, as well as histopathological analyses were conducted. Interaction profiles between SOL and cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2), glucocorticoid receptor, estradiol-17-ß-dehydrogenase and prostaglandin-E(2)-9-reductase were established using molecular docking. SOL significantly inhibited croton oil-, AA- and phenol-induced ear oedema (P < .001) at doses of 0.1, 0.5 and 1.0 mg/ear. The MPO and NAG activities and TNF-α, IL-6 and NO levels were decreased (P < .001). The histopathological data revealed that inflammatory parameters (oedema thickness, leucocyte infiltration and vasodilatation) were reduced by treatment with SOL at doses of 0.1, 0.5 and 1.0 mg/ear. The docking study showed that SOL interacts with COX-1 and prostaglandin-E(2)-9-reductase through hydrogen bonding, inhibiting these enzymes. These results indicate that SOL may be a promising compound for the treatment of cutaneous inflammatory disorders and has potential as a topical anti-inflammatory agent.

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.

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.

Caracterização morfoanatômica das folhas de Eremanthus erythropappus (DC.) MacLeisch, Asteraceae / Leaf morpho-anatomical characterization of Eremanthus erythropappus (DC.) MacLeisch, Asteraceae

Eremanthus erythropappus (DC.) MacLeisch (Asteraceae), popularmente conhecida como "candeia-da-serra", é uma espécie utilizada na medicina tradicional como cicatrizante e antimicrobiano. O objetivo do presente trabalho foi comparar o número de tricomas glandulares nas folhas jovens e adultas de E. erythropappus, assim como realizar a caracterização morfoanatômica destas folhas. Secções transversais e paradérmicas das folhas foram submetidas às microtécnicas fotônicas e à microscopia eletrônica de varredura. A quantificação dos tricomas glandulares foi realizada em folhas jovens e adultas com auxílio de câmara clara. As folhas são alternas ou fasciculadas e a lâmina foliar possui epiderme uniestratificada, revestida por cutícula delgada e lisa e mesofilo dorsiventral. Em ambas as faces da epiderme, ocorrem estômatos predominantemente anomocíticos e tricomas glandulares inseridos em depressões. Na face abaxial observam-se numerosos tricomas tectores. O parênquima paliçádico é uniestratificado e o parênquima voltado para a face abaxial é formado por três a cinco camadas de células com disposição compacta. As folhas jovens e adultas apresentam respectivamente 21,78±5,83 e 17,80±6,69 tricomas glandulares na face adaxial. A análise morfoanatômica das folhas de E. erythropappus mostra-se um método rápido e prático para a identificação e controle de qualidade de espécies vegetais utilizadas na terapêutica.

Eremanthus erythropappus (DC.) MacLeisch (Asteraceae), commonly known as 'candeia-da-serra', is a plant used in folk medicine as wound healing and antimicrobial. The aim of this study was to compare the number of glandular trichomes between the young and the mature leaves, as well as to perform the morpho-anatomical characterization of E. erythropappus leaves. Transverse and paradermal sections of the leaves were prepared according to light and scanning microtechniques for the morpho-anatomical characterization. The quantification of glandular trichomes on the adaxial surface of the epidermis was evaluated in young and mature leaves with camera lucida. The leaves are alternate or fasciculate and the blade has uniseriate epidermis coated with thin and smooth cuticle and dorsiventral mesophyll. There are predominantly anomocytic stomata on both surfaces, as well as glandular trichomes located in epidermal depressions. Various non-glandular trichomes are encountered on the abaxial surface. The palisade parenchyma consists of a single layer of cells and the parenchyma which is faced to the abaxial surface comprehends three to five layers of cells in compact arrangement. The young and mature leaves showed, respectively, 21.78±5.83 e 17.80±6.69 glandular trichomes on the adaxial side. The morpho-anatomical analysis of E. erythropappus leaves has proved to be a practical and rapid method for the identification and quality control of the vegetal species used for medical purposes.

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.

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.

Atividades farmacológicas dos extratos de Zanthoxylum chiloperone (Rutaceae) / Pharmacological activities of Zanthoxylum chiloperone (Rutaceae) extracts

Neste trabalho foram avaliadas as atividades antinociceptiva e antiinflamatória dos extratos das folhas de Zanthoxylum chiloperone. Os ensaios foram realizados pelos testes de contorções abdominais induzidas por ácido acético, tempo da lambida da pata induzida por formalina, edema de pata e pleurisia induzidas por carragenina, usando os extratos hexânico, em acetato de etila e etanólico administrados nas doses de 100 e 200 mg/kg. As doses testadas reduziram, significativamente, as contorções abdominais, o tempo de lambida da pata, o edema de pata, o volume do exsudato e a migração leucocitária. Estes resultados sugerem que os extratos de Z. chiloperone possuem constituintes com atividades antinociceptiva e antiinflamatória.

In this work the antinociceptive and anti-inflammatory activities of the extracts of leaves from Zanthoxylum chiloperone were evaluated. The tests were carried out by acetic acid writhing, formalin-induced paw licking, carrageenan-induced rat paw edema and pleurisy methods, using hexane, ethyl acetate and ethanol extracts administered in the doses of 100 and 200 mg/kg. The doses inhibited, significantly, the contortions, the paw lick, the paw edema, the volume of the exsudate and the leukocytes migration. These results suggest that the extracts from Z. chiloperone possess constituents with antinociceptive and anti-inflammatory activities.

Investigação das atividades analgésica e antiinflamatória do extrato metanólico dos rizomas de Echinodorus grandiflorus / Investigation of analgesic and anti-inflammatory activities of Echinodorus grandiflorus rhizomes methanol extract

O presente trabalho investigou as atividades analgésica e antiinflamatória do extrato metanólico de rizomas de Echinodorus grandiflorus. Para isto, foram realizados os testes de contorções abdominais induzidas por ácido acético; tempo da lambida da pata induzida por formalina; edema de pata e pleurisia induzidas por carragenina. As doses de 100, 200 e 400 mg/kg inibiram as contorções em 34,30 por cento, 35,84 por cento e 36,07 por cento, respectivamente. O tempo de lambida da primeira fase foi reduzido nas doses de 200 e 400 mg/kg, enquanto a segunda fase teve redução em 400 mg/kg. As doses testadas diminuíram o edema, enquanto o volume do exsudato foi reduzido em 24,61 por cento na dose de 400 mg/kg. As doses de 200 e 400 mg/kg diminuíram a migração leucocitária. Os resultados indicam que o extrato de E. grandiflorus testado pode constituir alvo potencial para uso em terapias da dor e da inflamação.

The present work investigated the analgesic and anti-inflammatory activities of the methanol extract of the rhizomes of Echinodorus grandiflorus. For this purpose, acetic acid writhing, paw licking induced by formalin, carrageenan-induced rat paw edema and pleurisy tests were performed. The doses of 100, 200 and 400 mg/kg inhibited the contortions 34.30 percent, 35.84 percent and 36.07 percent, respectively. The lick of the paw 1st phase was reduced at the doses of 200 and 400 mg/kg, while the 2nd phase had reduction at 400 mg/kg. All doses inhibited the paw edema, while the volume of the exsudate was reduced 24.61 percent in the dose of 400 mg/kg. The doses of 200 and 400 mg/kg decreased the leukocytes migration. The results indicate that the methanol extract of E. grandiflorus can constitute target potential for use in therapies of the pain and inflammation.