Search

Morbidity and mortality of the infected patients by multidrug-resistant bacteria have increased, emphasizing the urgency of fight for the discovery of new innovative antibiotics. In this sense, natural products emerge as valuable sources of bioactive compounds. Among the biodiversity, Eryngium pristis Cham. & Schltdl. (Apiaceae Lindl.) is traditionally used to treat thrush and ulcers of throat and mouth, as diuretic and emmenagogue, but scarcely known as an antimicrobial agent. With this context in mind, the goals of this study were to investigate the metabolic profile and the antibacterial activity of ethanolic extract (EE-Ep) and hexane (HF-Ep), dichloromethane (DF-Ep), ethyl acetate (EAF-Ep) and butanol (BF-Ep) fractions from E. pristis leaves. Gas Chromatography-Mass Spectrometry (GC-MS) was performed to stablish the metabolic profile and revealed the presence of 12 and 14 compounds in EAF-Ep and HF-Ep, respectively. β-selinene, spathulenol, globulol, 2-methoxy-4-vinylphenol, α-amyrin, β-amyrin, and lupeol derivative were some of phytochemicals identified. The antibacterial activity was determined by Minimal Inhibitory Concentration (MIC) using the broth micro-dilution against eight ATCC® and five methicillin-resistant Staphylococcus aureus (MRSA) clinical strains. HF-Ep was the most effective (MIC ≤ 5,000 µg/µL), being active against the largest part of tested Gram-positive and Gram-negative bacterial strains, including MRSA, with exception of Escherichia coli (ATCC 25922) and Pseudomonas aeruginosa (ATCC 9027) and (ATCC 27853). These results suggest that E. pristis is a natural source of bioactive compounds for the search of new antibiotics which can be an interesting therapeutic approach to recover patients mainly infected by MRSA strains.

O servico farmaceutico na Unidade Basica de Saude (UBS) do Sistema Unico de Saude (SUS) no Brasil garante o acesso a medicamentos de qualidade e contribui para o uso racional para que o paciente seja o principal beneficiario. O objetivo deste estudo foi descrever a importância da assistencia farmaceutica (AF) no funcionamento geral das UBSs com um enfoque nos servicos farmaceuticos. Os dados coletados foram organizados a partir de uma revisao da literatura em diferentes fontes bibliograficas. Os achados mostraram que a UBS e a principal porta de entrada para o sistema de saude e que deve funcionar em conformidade com as normas preconizadas pelo Ministerio da Saude do Brasil. Alem disso, e essencial a participacao do profissional farmaceutico na gestao clinica dos medicamentos para o desenvolvimento de atividades voltadas aos cuidados farmaceuticos do paciente. Portanto, a AF consiste em um conjunto de acoes relacionadas a promocao, protecao e recuperacao da saude, individual e coletiva, tendo o medicamento como insumo essencial e visando ao acesso e uso racional.

Rutin is a flavonoid used in clinical practice to treat capillary fragility and prevent bleeding due to its wide variety of pharmacological actions, including antioxidant, anti-inflammatory, anti-allergic, antiproliferative, and anticarcinogenic activities. In this study, the biopharmacotechnical and physical properties of film-coated tablets containing rutin marketed in drugstores were evaluated. Using samples from three batches called A, B and C, we determined the average weight, disintegration time, hardness, content and dissolution profile, and kinetics of the tablets. The samples demonstrated average weight of 457.45 ± 12.32 to 449.15 ± 8.95 mg; disintegration time, 30.17 ± 2.14 to 15.17 ± 2.14 min; hardness, 1.92 ± 0.55 to 1.69 ± 0.36 Kgf; and rutin content, 18.34 ± 1.21 to 15.66 ± 1.29 mg. After 90 min, the dissolution profile showed 52.65, 41.80, and 79.2% for A, B, and C, respectively. The results imply that the non-conformities of the tested products can significantly compromise the drug’s therapeutic efficacy.

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.

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.

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 β-caryophyllene, germacrene-D, α-copaene and β-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.

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.

The present study evaluated the antioxidant potential ofVernonia condensataBaker (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 IC50of DPPH assay varied from 4.28 to 75.10 µg/mL and TLC-bioautography detected the antioxidant compounds. The reducing power of Fe+3was 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 thatV. condensatais an important and promising source of bioactive substances with antioxidant activity.

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.

Essential oils of Duguetia lanceolata barks, obtained at 2 (T2) and 4 h (T4), were identified by gas chromatography and gas chromatography/mass spectrometry. β-Elemene (12.7 and 14.9%), caryophyllene oxide (12.4 and 10.7%) and β-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.

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.

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.

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%, 69,34% e 70,07%, 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% (100 mg/kg) e 47,62% (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%, 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% (100 mg/kg) and 47.62% (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.