Parkia from Cerrado: phytochemical bioprospection, toxicity and in vitro bioactivities of bark and flower extracts.

Parkia platycephala is the only species of the genus Parkia that is endemic to the brazilian Cerrado and the tree symbol of the state of Tocantins, but there are still few studies regarding its bioprospecting. In this study, we aimed to investigate the phytochemical composition, toxicity and bioactivities of the bark and flower of Parkia platycephala. Hot sequential extractions (Soxhlet) were performed using methanol and hydroethanolic solution (70%), after degreasing the sample (hexane). The presence of flavonoids, tannins, steroids and alkaloids was detected in the preliminary screening. Trilinolein, (Z)-9-octadecenamide, 3-O-methyl-d-glucose were detected by Gas Chromatography coupled to Mass Spectrometry (GC-MS). In the Liquid Chromatography with Diode Array Detector (LC-PDA) analysis, it was detected exclusively ferulic acid (bark) and ellagic acid (flower). The ethanolic extract of the bark (IC50=10.69 ± 0.35 µgmL-1) has an antioxidant potential (DPPH• radical) higher than that of the rutin standard (IC50=15.85 ± 0.08 µgmL-1). All extracts showed excellent anticholinesterase potential (Ellman), with emphasis on the ethanol extract of the flower (IC50 =5.34 ± 0.12 µgmL-1). Regarding toxicity (Artemia salina), the methanolic extract of the bark and the ethanolic extract of the flower presented high and moderate levels, respectively. Such results limit the concentrations of biological activities in this study, however, the antioxidant and anticholinesterase indices fall short of toxicity. The results demonstrated promising antioxidant and anticholinesterase activities of both the bark and the flower of Parkia platycephala.

Effect of carvacrol antioxidant capacity on oocyte maturation and embryo production in cattle.

Carvacrol (C10H14O), an efficient phenolic antioxidant substance for several cell types, may become a useful antioxidant for female germ cells and embryo culture. This study investigates the effects of carvacrol supplementation on bovine oocytes in in vitro maturation (IVM) and embryo production. In total, 1222 cumulus-oocyte complexes were cultured in TCM-199+ alone (control treatment) or supplemented with carvacrol at the concentrations of 3 µM (Carv-3), 12.5 µM (Carv-12.5), or 25 µM (Carv-25). After IVM, the oocytes were subjected to in vitro fertilization and embryo production, and the spent medium post-IVM was used for evaluating the levels of reactive oxygen species and the antioxidant capacity (2,2-diphenyl-1-picryl-hydrazyl-hydrate and 2,2'-azinobis-3-ethyl-benzothiozoline-6-sulphonic acid quantification). A greater (P < 0.05) antioxidant potential was observed in the spent medium of all carvacrol-treated groups compared with the control medium. Moreover, the addition of carvacrol to the maturation medium did not affect (P > 0.05) blastocyst production on days 7 and 10 of culture; however, the total number of cells per blastocyst was reduced (P < 0.05) in two carvacrol-treated groups (Carv-3 and Carv-25). In conclusion, carvacrol demonstrated a high antioxidant capacity in the spent medium after oocyte maturation; however, although embryo production was not affected, in general, carvacrol addition to IVM medium reduced the total number of cells per blastocyst. Therefore, due to the high antioxidant capacity of carvacrol, new experiments are warranted to investigate the beneficial effects of lower concentrations of carvacrol on embryo production in cattle and other species.

Oocyte in vitro maturation with eugenol improves the medium antioxidant capacity and total cell number per blastocyst.

This study investigates the impact of eugenol (EU) supplementation on bovine oocyte in vitro maturation (IVM) and antioxidant capacity, as well as in vitro embryo production and quality after conventional in vitro fertilization (IVF). A total of 1077 cumulus oocyte complexes were cultured in TCM-199+ without EU supplementation (control treatment) or supplemented with EU at the concentrations of 10 µM (EU-10), 20 µM (EU-20), or 40 µM (EU-40). After IVM, the oocytes were subjected to IVF and embryo culture. The addition of EU at 40 µM to the IVM medium improved (P < 0.05) the antioxidant capacity and cleavage rate when compared to the control treatment. Moreover, a positive correlation (r = 0.61, P < 0.03) was observed between cleavage rate and EU concentration. The addition of EU at concentrations of 10 and 20 µM decreased (P < 0.05) the calreticulin (CALR) levels in expanded blastocysts when compared to the control treatment and EU-40 treatment. However, the EU-10 and EU-20 treatments had a greater (P < 0.05) mean total cell number (TCN) per expanded blastocyst when compared to the control treatment and EU-40 treatment. In conclusion, the addition of EU to the enriched culture medium during IVM of bovine oocytes improved the antioxidant capacity of the spent medium, as well as the cleavage rate and embryonic quality (i.e., TCN/expanded blastocyst), and reduced the endoplasmic reticulum stress (i.e., CALR levels) in the embryos. Thus, we recommend enriching the IVM medium with 10 µM EU for in vitro bovine embryo production.

Biofilm of Candida albicans: formation, regulation and resistance.

Candida albicans is the most common human fungal pathogen, causing infections that range from mucous membranes to systemic infections. The present article provides an overview of C. albicans, with the production of biofilms produced by this fungus, as well as reporting the classes of antifungals used to fight such infections, together with the resistance mechanisms to these drugs. Candida albicans is highly adaptable, enabling the transition from commensal to pathogen due to a repertoire of virulence factors. Specifically, the ability to change morphology and form biofilms is central to the pathogenesis of C. albicans. Indeed, most infections by this pathogen are associated with the formation of biofilms on surfaces of hosts or medical devices, causing high morbidity and mortality. Significantly, biofilms formed by C. albicans are inherently tolerant to antimicrobial therapy, so the susceptibility of C. albicans biofilms to current therapeutic agents remains low. Therefore, it is difficult to predict which molecules will emerge as new clinical antifungals. The biofilm formation of C. albicans has been causing impacts on susceptibility to antifungals, leading to resistance, which demonstrates the importance of research aimed at the prevention and control of these clinical microbial communities.

Bioactivity and Toxicity of Senna cana and Senna pendula Extracts.

This work investigated the content of total polyphenolic compounds and flavonoids as well as their toxicity and larvicidal and acetylcholinesterase inhibitory activities. The antioxidant activities of two medicinal Senna species extracts (Senna cana and Senna pendula) were also investigated. The ethanol extract of the leaves of S. cana and the ethanol extract of the branches of S. pendula presented the best performance in the DPPH/FRAP and ABTS/ORAC assays, respectively. For the inhibition of acetylcholinesterase, the hexane extract of the flowers of S. pendula presented the lowest IC50 value among the ethanol extracts of the leaves of S. cana and showed the best performance in some assays. The hexane extract of the leaves of S. pendula and the hexane extract of the branches of S. cana were moderate to Artemia salina Leach. In the quantification of phenols and flavonoids, the ethanol extract of the leaves of S. cana presented the best results. The ethanol extracts of the leaves of S. cana were found to be rich in antioxidants, phenolic compounds, and flavonoids. These results indicate the antioxidant potential of the extracts of Senna species and can be responsible for some of the therapeutic uses of these plants.

Involvement of mast cells, CD68+ and VEGF+ expressions in response to Himatanthus drasticus commercial latex in mice wound healing model / Envolvimento de mastócitos, expressão de CD68+ e VEGF+ em resposta ao látex comercial de Himatanthus drasticus em modelo de cicatrização em camundongos

This study aimed to evaluate Himatanthus drasticus latex in a mice wound healing experimental model. Animals were divided into four groups (n=7) according to the treatments: GI - saline 0.9% (control), GII - mineral oil (vehicle), GIII - H. drasticus commercial latex (HdCL) and GIV - H. drasticus mixed isolated fraction (MIF, 1 mg/mL). The treatments were applied topically once daily, 50 µL for 14 consecutive days. Macroscopic lesions were evaluated, considering parameters such as swelling, redness, granulation tissue and reepithelialization. VEGF+, CD68+ expressions and mast cells (Toluidin blue stain) were evaluated. HdCL induced higher contraction and exuberant granulation tissue (P > 0.05). HdCL showed a mild inflammatory process while MIF induced intense infiltrate inflammatory predominantly by lymphocytes, vascular congestion, bleeding and did not presented full reepithelialization. Reorganization of collagen fibers (red picrosirius stain) was observed. CD68+ expression and mast cells were presented as moderate, intense and mild in GI, GIII and GIV, respectively. Neovascularization occurred in all groups, while VEGF+ expression was intense in MIF in relation to HdCL. We concluded that HdCL presents wound healing potential, through modulation of mast cells, CD68+ and VEGF+ expressions that can be associated to triterpenes presence according MIF isolated from HdCL.(AU)

Objetivou-se avaliar o látex de Himatanthus drasticus em feridas induzidas experimentalmente em camundongos. Os animais foram divididos em quatro grupos (n=7): GI - salina 0,9% (controle), GII - óleo mineral (veículo), GIII - látex comercial de H. drasticus (HdCL) e GIV - fração isolada mista de H. drasticus (MIF, 1mg/mL). Os tratamentos foram aplicados topicamente uma vez ao dia (50µL), durante 14 dias consecutivos. Lesões macroscópicas, as expressões de VEGF+, CD68+ e a participação dos mastócitos (coloração azul de toluidina) foram avaliadas. HdCL induziu maior contração e tecido de granulação exuberante (P >0,05). HdCL induziu leve processo inflamatório enquanto MIF promoveu intenso infiltrado inflamatório predominantemente linfocítico, congestão vascular, hemorragia e reepitelização parcial. Observou-se reorganização das fibras colágenas (coloração picrosírius). A expressão de CD68+ e os mastócitos apresentaram-se moderados, intensos e leves em GI, GIII e GIV, respectivamente. A neovascularização foi observada em todos os grupos, enquanto a expressão de VEGF+ foi mais intensa em MIF em relação a HdCL. Conclui-se que HdCL apresenta potencial de cicatrização por meio da modulação dos mastócitos e das expressões de CD68+ e VEGF+, o que pode estar associado à presença de triterpenos de acordo com MIF isolada de HdCL.(AU)

Efeito do extrato etanólico bruto e das frações da Hyptidendron canum (Pohl ex Benth. ) Harley em brânquias de Oreochromis niloticus L / Effect of the crude ethanol extract and fractions of Hyptidendron canum (Pohl ex Benth. ) Harley on the gills of Oreochromis niloticus L

Alguns problemas relacionados à criação intensiva de peixes estão mais evidentes devido ao aumento da aquicultura em todo o mundo, destacando-se os distúrbios nutricionais e o aumento de doenças nos sistemas de produção. Com isso as pesquisas envolvendo produtos derivados de plantas vem ganhando espaço nessa área. A Hyptidendron canum é uma planta utilizada na medicina popular como antimalárica, anti-inflamatória, antiulcerativa e anti-hepatotóxica. Objetivou-se, neste trabalho, avaliar os efeitos celulares e teciduais do extrato etanólico bruto e das frações hexano, clorofórmio e acetato de etila da H. canum nas brânquias de Oreochromis niloticus L. Para isso, o extrato etanólico e as frações foram administrados no peixe através da ração. Após 24 horas da ingestão da ração, os peixes foram sacrificados e o segundo arco branquial de cada um foi processado histologicamente e corado com tricômico de Masson e Hematoxilina e Eosina (HE). Pela análise qualitativa das brânquias ao microscópio de luz, observou-se que o extrato bruto e as três frações promoveram, em diferentes intensidades nas lamelas, descamação e destacamento do epitélio respiratório, alteração da curvatura, desorganização do eixo, hiperplasia celular do tecido epitelial interlamelar e vasodilatação nas lamelas e no vaso central do filamento. Os resultados deste experimento mostraram que o extrato etanólico bruto e as três frações de H. canum promoveram processos inflamatórios e/ou lesões sistêmicas, dose dependente para O. niloticus.

Some problems related to intensive fish farming are more evident because of the increased aquaculture worldwide, and we highlight the nutritional disorders and the increase of diseases in the production systems. Thus, research involving plant-derived products has been increasing in this area. The Hyptidendron canum is a plant used in folk medicine as an antimalarial, anti-inflammatory, anti-ulcer and antihepatotoxic agent. This study proposes to evaluate the cellular and tissue effects of the crude ethanol extract and the hexane, chloroform and ethyl acetate fractions of H. canum on the gills of Oreochromis niloticus L. The ethanol extract and fractions were administered through the feed of the fish. Twenty-four hours later, the fish were sacrificed and their second gill arch dissected. Histological analyses were performed using Masson's trichrome and Haematoxylin and Eosin (H&E). The qualitative analysis of the material showed that the crude extract and the three fractions caused varying degrees of peeling and detachment of the lamellar respiratory epithelium, alterations in the curvature and axis of the gill, cell hyperplasia in the interlamellar epithelium and lamellar vasodilation, as well as vasodilation in the central vessel of the filament. The results of this experiment showed that the crude ethanol extract and the three fractions of H. canum promoted inflammation and/or systemic lesions, dose dependent, for O. niloticus.

Activity of cycloartane-type triterpenes and sterols isolated from Musa paradisiaca fruit peel against Leishmania infantum chagasi.

UNLABELLED: The aim of the study was to evaluate in vitro the antileishmanial activity of triterpenes and sterols isolated from Musa paradisiaca (banana) fruit peel used traditionally to treat leishmaniasis. The compounds were isolated from the ethanolic extract of the peel of the banana fruit by column chromatography. The chemical structure of compounds was determined by (1)H and (13)C - nuclear magnetic resonance spectroscopy. The cytotoxicity was measured in RAW 264.7 cells and LLC-MK2. Leishmanicidal activity against L. infantum chagasi promastigotes was performed by the MTT colorimetric method and activity against amastigotes was assayed in mammalian cells using in situ ELISA method. Five compounds were identified, consisting of three triterpenes: cycloeucalenone, 31-norcyclolaudenone and 24-methylene-cicloartanol and a mixture of two sterols: beta-sitosterol and stigmasterol. With the exception of cycloeucalenone, all compounds showed statistically similar activity against promastigote to pentamidine. While, acting against amastigotes, excluding 31-norcyclolaudenone, other compounds showed activity similar to amphotericin B. All compounds showed low cytotoxicity in mammalian cells. CONCLUSION: This study partially confirms the use of Musa paradisiaca in folk medicine against leishmaniasis. Further in vivo studies are necessary to evaluate the efficacy.

Correlação entre as atividades antiradical, antiacetilcolinesterase e teor de fenóis totais de extratos de plantas medicinais de farmácias vivas / Correlation between the anti-radical, anti-acetylcholinesterase activities and phenolic content of some extracts of live herbal pharmacies in the Northeast of Brazil

O objetivo deste trabalho foi avaliar a correlação entre o conteúdo de fenóis de extratos de 18 plantas medicinais comuns nas Farmácias Vivas com a atividade sequestradora do radical livre DPPH e com a inibição da enzima acetilcolinesterase. Maiores conteúdos de fenóis totais foram encontrados nas plantas: Eugenia uniflora, Lippia alba, Lippia microphylla, Mentha x villosa, Ocimum gratissimum e Ocimum selloi. As espécies que apresentaram maior atividade antioxidante, semelhante a quercetina, foram: Spondias mombim, Malphigia glabra, L. alba e Croton zenhtneri,. As plantas Cecropia pachystachia, L. alba, L. microphylla, M. glabra, O. gratissimum e Plectranthus ornatus mostraram maiores halos de inibição da enzima acetilcolinesterase. Combinando as duas ações, as plantas mais ativas foram a M. glabra e a L. alba e somente a segunda correlaciona-se diretamente com o maior teor de fenóis totais. Através deste estudo, M. glabra e L. alba foram consideradas as plantas mais promissoras para estudos subsequentes a fim de encontrar novos compostos com ação potencial contra a doença de Alzheimer.

The purpose of this study was to evaluate the phenolic content of 18 medicinal plant extracts of "Live Pharmacies" and correlate them with their free radical scavenging activity and inhibition of the acetylcholinesterase enzyme. Higher amounts of phenolic compounds were found in the following plants: Eugenia uniflora, Lippia alba, Lippia microphylla, Mentha x villosa, Ocimum gatissimum, and Ocimum selloi. The species that showed higher anti-radical activity were Croton zenhtneri, Lippia alba, Malphigia glabra, and Spondias mombim, similar to quercetin. The plants Cecropia pachystachia, L. alba, L. microplylla, M. glabra, O. gratissimum, and Plectranthus ornatus showed larger inhibition zones of the acetylcholinesterase enzyme. By correlating the two actions L. alba and M. glabra are common as more active to both tests and only L. alba correlates directly with the phenolic content. Through this study, L. alba and M. glabra are considered the most promising plants for further studies to find new compounds with potential action against Alzheimer's disease.

Toxicity of Brazilian plant seed extracts to two strains of Aedes aegypti (Diptera: Culicidae) and nontarget animals.

Seed ethanolic extracts of 21 Brazilian plants were evaluated for ovicidal, larvicidal, and pupicidal activities against insecticide-susceptible (SS) and field-collected (FC) strains of Aedes aegypti (L.) (Diptera: Culicidae), as well as for their effects on nontarget organisms. Myracrodruon urundeuva Fr. Allemao extract was highly toxic to both mosquito strains. Schinopsis brasiliensis Engler extract showed low toxicity and was 38-68 times less toxic to Ae. aegypti larvae than was M. urundeuva extract. The pupicidal activity (LC50) of 14 plant seed extracts ranged between 9 and 433/g/ml, and toxicities were comparable to both mosquito strains. Piptadenia moniliformis Benth. and Luetzelburgia auriculata (Allemao) Ducke extracts showed the highest activities against pupae of FC and SS strains. None of the extracts showed 100% ovicidal activity. In addition, the active extracts did not show high acute toxicity to mice (LD50 > 1.5 g/kg), except that of Enterolobium contortisiliquum (Vell.) Morong. Most of the active extracts exhibited low toxicity against brine shrimp (Artemia sp.) nauplii. The extracts of M. urundeuva, P. moniliformis, and L. auriculata are promising sources of recognized classes of insecticidal compounds with good selectivity against immature stages of Ae. aegypti.

Antiviral activities of extracts and phenolic components of two Spondias species against dengue virus

In recent years, the search for natural plant products to fight viral diseases has been increasing. In this work, two Spondias species, namely S. mombin and S. tuberosa, found in Ceará state (Brazil), and their main phenolic components were evaluated against dengue virus. In vitro antiviral tests were performed against type-2 dengue virus by the MTT method and standard cytopathic effect reduction assay in C6/36 cells. Cytotoxicity was also evaluated by MTT. The presence of phenolic compounds quercetin, rutin, and ellagic acid in plant extracts was characterized by HPLC analysis. Both Spondias species extracts and components were nontoxic to the cells whereas rutin and quercetin displayed relevant antiviral activity with IC50 of 362.68 µg/mL and 500 µg/mL, respectively.

Análise tecidual e celular das brânquias de Oreochromis niloticus L. tratadas com extrato etanólico bruto e frações das folhas da pitanga (Eugenia uniflora L. ) - Myrtaceae / Tissue and cell analysis of Oreochromis niloticus L. gill treated with crude ethanol extract and fractions from pitanga (Eugenia uniflora L. ) leaves Myrtaceae

Eugenia uniflora L. (Myrtaceae) é uma planta que ocorre no bioma Cerrado e é utilizada popularmente no tratamento de diarréias, inflamações, hiperglicemia e hipertensão. Estudos prévios revelaram atividade antimicrobiana da E. uniflora in vitro. Tendo em vista o uso popular, este trabalho objetivou avaliar as possíveis atividades celulares e teciduais sistêmicas do extrato bruto e das frações das folhas dessa planta em brânquias de Oreochromis niloticus L. (tilápia nilótica). Para isso, o extrato etanólico e as frações das folhas dessa planta foram administrados no peixe, por via oral, adicionadas à ração. Após um período de 24 horas, os peixes foram sacrificados e o segundo arco branquial de cada peixe foi dissecado, fixado em formalina neutra, desidratado, incluído em parafina e cortado. Nas análises histológicas, utilizaram-se tricômico de Masson e hematoxilina e eosina (HE). Pelas análises qualitativas na microscopia de luz, concluiu-se que o extrato etanólico bruto e as frações das folhas da E. uniflora apresentaram efeito sistêmico nas tilápias nilóticas atingindo as brânquias. As ações tóxicas como destacamento e descamação do epitélio respiratório e hiperplasia das células do epitélio interlamelar, foram mais pronunciadas nas tilápias que ingeriram maiores concentrações. Este trabalho colaborou para identificar o efeito vasodilatador dessa planta, e contribuiu para estabelecer a tilápia nilótica como sistema-modelo para testes com princípios ativos de plantas. Espera-se, com esses testes, viabilizar o uso de plantas como medicamentos para tratamentos de peixes, a manutenção da saúde de animais em cultivo intensivo e extensivo, a partir do qual se possibilite emprego alternativo aos medicamentos sintéticos.

Eugenia uniflora L. (Myrtaceae) is a plant found in the Cerrado biome and traditionally used in the treatment of diarrheas, inflammations, hyperglycemia and hypertension. Previous studies have revealed in vitro antimicrobial activity of E. uniflora. Considering its popular use, this study aimed to assess possible systemic cellular and tissue activities of the crude extract and the fractions from the leaves of this plant on Oreochromis niloticus L. (Nile tilapia) gill. Thus, ethanol extract and fractions from the leaves of this plant were orally administered to the fish in their rations. After 24 hours, the fish were sacrificed and the second gill arch of each fish was dissected, fixed in neutral formalin, dehydrated, embedded in paraffin and sectioned. Masson's trichome and hematoxylin and eosin (HE) were used in the histological analyses. Qualitative analyses using a light microscope led to the conclusion that the crude ethanol extract and the fractions from E. uniflora leaves presented systemic effect on Nile tilapias, affecting the gills. Toxic actions such as respiratory epithelium detachment and lifting, and hyperplasia of interlamellar epithelial cells were more pronounced in the tilapias that ingested higher concentrations. This study helped to identify the vasodilator effect of this plant and contributed to the definition of the Nile tilapia as a model system for testing plant active principles. These tests are expected to make feasible not only the use of plants as fish medication but also the maintenance of the health of animals in intensive and extensive cultures through the possible use of alternatives to synthetic medication.

Extratos vegetais usados no controle de dípteros vetores de zoonoses / Plant extracts used in the control of dipteran vectors of zoonosis

Os insetos são importantes transmissores de doenças que cada vez mais ocorrem em áreas periurbanas ou urbanas, devido à introdução ou reaparecimento de seus respectivos vetores. As estratégias de controle das doenças transmissíveis por vetores biológicos são de difícil execução, principalmente quando associadas à existência de reservatórios domésticos e silvestres e aos aspectos ambientais. O uso de inseticidas direcionado ao combate de formas adultas de dípteros vetores tem sido freqüente. Entretanto, o amplo uso dos inseticidas sintéticos desde a descoberta do DDT para o controle de pragas domésticas e da agricultura, como também de vetores que transmitem doenças ao homem, levou a uma maior preocupação em relação à toxicidade e impacto ambiental destes agentes. Além disso, a resistência a inseticidas tornou-se uma preocupação crescente na agricultura, economia e na saúde pública. Um grande número de diferentes espécies de plantas representando diferentes áreas geográficas ao redor do mundo tem se mostrado capaz de causar efeitos letais e subletais sobre insetos. Esta revisão aborda a utilização de extratos de plantas com potencial no controle de dípteros vetores de zoonoses.

Insects are important transmitters of diseases increasingly occurring in peri-urban or urban areas due to the introduction or the reemergence of their respective vectors. Strategies to control diseases transmitted by biological vectors are difficult to implement, especially when associated with the existence of domestic and wild reservoirs and environmental aspects. The use of insecticides against adult forms of dipteran vectors has been frequent. However, the widespread use of synthetic insecticides since the discovery of DDT to control domestic and agricultural pests, as well as vectors that transmit diseases to humans, has led to greater concern for the toxicity and environmental impact of these agents. Moreover, resistance to insecticides has become an increasing concern in agriculture, economy and public health. A large number of different plant species representing different geographical areas around the world have been capable of causing lethal and sublethal effects on insects. This review addresses the use of potential plant extracts to control dipteran vectors of zoonosis.

Croton sonderianus essential oil samples distinctly affect rat airway smooth muscle.

Plants of the genus Croton have been used extensively in the northeast of Brazil for treating various clinical conditions. Previous studies have demonstrated that the essential oil of some specimens of Croton sp. have a relaxing effect on tracheal smooth muscle. Our study aimed to characterize the effects of Croton sonderianus essential oil samples, collected at 1:00 pm (EO-13) and 9:00 pm (EO-21), on rat tracheal smooth muscle. The two samples were submitted to gas chromatography (GC) and mass spectrometry (MS) analysis to identify their components. Rat tracheal smooth muscle strips were used to assess the biological activity. The major constituents of EO-21 were: spathulenol (18.32%), beta-caryophyllene (14.58%) and caryophyllene oxide (8.54%) and the major constituents of EO-13 were bicyclogermacrene (16.29%), beta-phellandrene (15.42%) and beta-caryophyllene (13.82%). These samples showed an antispasmodic effect on tracheal smooth muscle strips pre-contracted with high K+ concentration (80 mM) or with acetylcholine. EO-21 increased baseline tonus while EO-13 provoked a decrease. These results demonstrated that EO-13 and EO-21 have different chemical composition and showed myorelaxant activity. In conclusion, EO-13 and EO-21 may have potential therapeutic use in the treatment of bronchospasm.

Anthelmintic activity of Cocos nucifera L. on intestinal nematodes of mice.

In this study, we evaluated the anthelmintic activity of the liquid extracted from the bark of the green coconut (LBGC), as well as butanol extract obtained from LBGC, on mouse intestinal nematodes. Thirty-six naturally infected mice were distributed into six groups receiving the following treatments: Group I: 1000 mg/kg of LBGC; Group II: 2000 mg/kg of LBGC; Group III: 500 mg/kg of butanol extract; Group IV: 1000 mg/kg of butanol extract; Group V: 0.56 mg/kg febendazole; and Group VI: 3% dimethylsulfoxide. The chemical composition of the LBGC and its butanol extract was determined by phytochemical tests. A dose of 1000 mg/kg of butanol extract had 90.70% efficacy in reducing the mouse worm burden (p<0.05). Phytochemical tests revealed the presence of triterpens, saponnins and condensed tannins in the LBGC and butanol extracts. These results suggest that Cocos nucifera extracts may be useful in the control of intestinal nematodes.

Chemical composition of Eucalyptus spp. essential oils and their insecticidal effects on Lutzomyia longipalpis.

The chemical composition of essential oils from three species of plants belonging to the Eucalyptus genus was determined and, their insecticidal effects on egg, larva and adult phases of Lutzomyia longipalpis were assessed. The insects were collected in the municipality of Sobral in the State of Ceará, Brazil. Five treatments with different concentrations were performed along with two negative controls, distilled water and Tween 80 (3%), and a positive control, cypermethrin (0.196mg/ml). The tests were carried out in plastic pots internally coated with sterile plaster and filled with a substrate made of rabbit feces and crushed cassava leaves. The eggs, larvae and adults were sprayed with the oils. The hatched larvae were counted for 10 consecutive days and observed until pupation. Insect mortality was observed after 24, 48 and 72h. E. staigeriana oil was the most effective on all three phases of the insect, followed by E. citriodora and E. globulus oils, respectively. The major constituents of the oils were Z-citral and alpha-citral (E. staigeriana), citronellal (E. citriodora) and 1,8-cineole (E. globulus). The Eucalyptus essential oils constitute alternative natural products for the control of L. longipalpis since the median effective concentration (EC(50)) values revealed relevant action as compared with other natural products, some of their chemical constituents are already known for their insecticidal activity and these oils are produced in commercial scale in Brazil.

Anthelmintic activity of Cocos nucifera L. against sheep gastrointestinal nematodes.

The development of anthelmintic resistance has made the search for alternatives to control gastrointestinal nematodes of small ruminants imperative. Among these alternatives are several medicinal plants traditionally used as anthelmintics. This work evaluated the efficacy of Cocos nucifera fruit on sheep gastrointestinal parasites. The ethyl acetate extract obtained from the liquid of green coconut husk fiber (LGCHF) was submitted to in vitro and in vivo tests. The in vitro assay was based on egg hatching (EHT) and larval development tests (LDT) with Haemonchus contortus. The concentrations tested in the EHT were 0.31, 0.62, 1.25, 2.5 and 5 mg ml(-1), while in the LDT they were 5, 10, 20, 40 and 80 mg ml(-1). The in vivo assay was a controlled test. In this experiment, 18 sheep infected with gastrointestinal nematodes were divided into three groups (n=6), with the following doses administered: G1-400 mg kg(-1) LGCHF ethyl acetate extract, G2-0.2 mg kg(-1) moxidectin (Cydectin) and G3-3% DMSO. The worm burden was analyzed. The results of the in vitro and in vivo tests were submitted to ANOVA and analyzed by the Tukey and Kruskal-Wallis tests, respectively. The extract efficacy in the EHT and LDT, at the highest concentrations tested, was 100% on egg hatching and 99.77% on larval development. The parameters evaluated in the controlled test were not statistically different, showing that despite the significant results of the in vitro tests, the LGCHF ethyl acetate extract showed no activity against sheep gastrointestinal nematodes.

Anthelmintic activity of Lippia sidoides essential oil on sheep gastrointestinal nematodes.

Medicinal plants have been investigated for their anthelmintic properties and shown to be effective against eggs and larvae of gastrointestinal nematodes. The aim of this study was to evaluate the efficacy of the Lippia sidoides essential oil (LsEO) on sheep gastrointestinal nematodes. Initially, 44 naturally infected sheep were divided and treated with 200 microg kg(-1) ivermectin and 230 and 283 mg kg(-1) LsEO, respectively, plus the control. Fecal samples were collected from each animal to determine epg at 7, 14 and 21 days after treatment. In another test, 21 sheep were distributed and treated with 200 microg kg(-1) ivermectin, 283 mg kg(-1) LsEO and the control, respectively. Seven days after treatment, they were euthanized and necropsied to count and identify the nematodes from the abomasum, small and large intestines. In the first test, the efficacy of 230 and 283 mg kg(-1) LsEO and ivermectin was 38%, 45.9% and 40.2%, respectively, 7 days after treatment, and 30%, 54% and 39.6%, respectively, 14 days after treatment. In the second experiment, the respective efficacy of 283 mg kg(-1) LsEO and ivermectin was 56.9% and 34.4% against Haemonchus spp., and 39.3% and 63.6% against Trichostrongylus spp.

Antifungal activity of essential oils of Croton species from the Brazilian Caatinga biome.

AIMS: To find new antifungal agents among essential oils from Brazilian Croton species. METHODS AND RESULTS: Plant leaves were steam distilled and the obtained essential oils were analyzed by gas chromatography/mass spectroscopy. The main constituents were estragole and anethole for Croton zehntneri, methyl-eugenol and bicyclogermacrene for Croton nepetaefolius and spathulenol and bicyclogermacrene for Croton argyrophylloides. The antifungal activity of essential oils was evaluated against Candida albicans, Candida tropicalis and Microsporum canis by the agar-well diffusion method and the minimum inhibitory concentration (MIC) by the broth microdilution method. Essential oils of Croton species demonstrated better activity against M. canis. Among the three plants C. argyrophylloides showed the best results, with MIC ranging from 9 to 19 microg ml(-1). The acute administration of the essential oil up to 3 g kg(-1) by the oral route to mice was devoid of overt toxicity. CONCLUSIONS: The studied essential oils are active in vitro against the dermatophyte M. canis and present relative lack of acute toxicity in vivo. SIGNIFICANCE AND IMPACT OF THE STUDY: Because of its antifungal activity and low toxicity, the essential oils of studied Croton species are promising sources for new phytotherapeutic agents to treat dermatophytosis.

Effect of human renal cationic transporter inhibition on the pharmacokinetics of varenicline, a new therapy for smoking cessation: an in vitro-in vivo study.

Varenicline is predominantly eliminated unchanged in urine, and active tubular secretion partially contributes to its renal elimination. Transporter inhibition assays using human embryonic kidney 293 cells transfected with human renal transporters demonstrated that high concentrations of varenicline inhibited substrate uptake by hOCT2 (IC(50)=890 microM), with very weak or no measurable interactions with the other transporters hOAT1, hOAT3, hOCTN1, and hOCTN2. Varenicline was characterized as a moderate-affinity substrate for hOCT2 (K(m)=370 microM) and its hOCT2-mediated uptake was partially inhibited by cimetidine. Co-administration of cimetidine (1,200 mg/day) reduced the renal clearance of varenicline in 12 smokers, resulting in a 29.0% (90% CI: 21.5%-36.9%) increase in systemic exposure. This increase is not considered clinically relevant, as it should not give rise to safety concerns. Consequently, it can be reasonably expected that other inhibitors of hOCT2 would not cause greater renal interactions with varenicline than that seen with the efficient hOCT2 inhibitor cimetidine.