Chemical prospecting and antioxidant, anticholinesterase and antifungal activity of ethanol extracts from Senna Mill. species. (Fabaceae) / Prospecção química, atividade antioxidante, anticolinesterásica e antifúngica de extratos etanólicos de espécies de Senna Mill. (Fabaceae)

The objective of this work was to evaluate the chemical profile, total phenol content and the antioxidant, antiacetylcholinesterase and antifungal activities of ethanol extracts from leaves (EEF) and stem (EEC) of five species of Senna, as well as to evaluate the correlation between the content of total phenols with the DPPH free radical scavenging activity and with the inhibition of the acetylcholinesterase AChEI enzyme. The phytochemical test showed the presence of secondary metabolites in all extracts. The EEF and EEC of Senna trachypus, stood out for presenting the highest values of total phenols. S. trachypus EEF and EEC showed the best action on the acetylcholinesterase enzyme. All species showed antioxidant activity, especially the EEF from S. trachypus. A strong correlation was observed for the variables total phenols and antioxidant activity (r = -0.71), very strong for total phenols and anti-acetylcholinesterase (r = -0.84) and moderate activity for antioxidant and anti-acetylcholinesterase activity (r = 0.43). Only S. trachypus extracts showed activity against all dermatophytes, when compared to the other species. The species S. trachypus was considered the most promising plant for further studies, in order to find compounds with pharmacological actions.

O objetivo deste trabalho foi avaliar o perfil químico, teor de fenóis totais e as atividades antioxidante, antiacetilcolinesterásica e antifúngica dos extratos etanólicos das folhas (EEF) e do caule (EEC) de cinco espécies de Senna, bem como avaliar a correlação entre o conteúdo de fenóis totais com a atividade sequestradora do radical livre DPPH e com a inibição da enzima acetilcolinesterase AChEI. No teste fitoquímico, evidenciou-se a presença de metabólitos secundários em todos os extratos. Os EEF e EEC de Senna trachypus, destacaram-se por apresentar os maiores valores de fenóis totais. Os EEF e EEC de S. trachypus mostraram a melhor ação sobre a enzima acetilcolinesterase. Todas as espécies apresentaram atividade antioxidante, em especial o EEF de S. trachypus. Foi observado correlação forte para as variáveis fenóis totais e atividade antioxidante (r = -0,71), muito forte para fenóis totais e antiacetilcolinesterase (r = -0,84) e atividade moderada para atividade antioxidante e antiacetilcolinesterase (0,43). Apenas os extratos de S. trachypus apresentaram atividade contra todos os dermatófitos, quando comparado às demais espécies. A espécie S. trachypus foi considerada a planta mais promissora para estudos subsequentes, a fim de encontrar compostos com ações farmacológicas.

Caryocar coriaceum Wittm. fruit extracts as Leishmania inhibitors: in-vitro and in-silico approaches.

Leishmaniasis is a group of neglected diseases caused by parasites of the Leishmania genus. The treatment of Leishmaniasis represents a great challenge, because the available drugs present high toxicity and none of them is fully effective. Caryocar is a botanical genus rich in phenolic compounds, which leaves extracts have already been described by its antileishmanial action. Thus, we investigated the effect of pulp and peel extracts of the Caryocar coriaceum fruit on promastigote and amastigote forms of Leishmania amazonensis. Both extracts had antipromastigote effect after 24, 48, and 72 h, and this effect was by apoptosis-like process induction, with reactive oxygen species (ROS) production, damage to the mitochondria and plasma membrane, and phosphatidylserine exposure. Knowing that the fruit extracts did not alter the viability of macrophages, we observed that the treatment reduced the infection of these cells. Thereafter, in the in vitro infection context, the extracts showed antioxidant proprieties, by reducing NO, ROS, and MDA levels. Besides, both peel and pulp extracts up-regulated Nrf2/HO-1/Ferritin expression and increase the total iron-bound in infected macrophages, which culminates in a depletion of available iron for L. amazonensis replication. In silico, the molecular modeling experiments showed that the three flavonoids presented in the C. coriaceum extracts can act as synergistic inhibitors of Leishmania proteins, and compete for the active site. Also, there is a preference for rutin at the active site due to its greater interaction binding strength.Communicated by Ramaswamy H. Sarma.

Anthelmintic activity of nanoencapsulated carvacryl acetate against gastrointestinal nematodes of sheep and its toxicity in rodents.

The objective of this study was to evaluate the efficacy of carvacryl acetate (CVA) and nanoencapsulated CVA (nCVA) on gastrointestinal nematodes of sheep. The CVA was nanoencapsulated with chitosan/gum arabic and the efficacy of nanoencapsulation (EE), yield, zeta potential, nanoparticle morphology and release kinetics at pH 3 and 8 were analyzed. Acute and subchronic toxicity were evaluated in rodents and reduction of egg counts in the faeces (FECRT) of sheep. The sheep were divided into four groups (n = 10): G1, 250 mg/kg CVA; G2, 250 mg/kg nCVA; G3, polymer matrix and G4: 2.5 mg/kg monepantel. EE and nCVA yield were 65% and 57%, respectively. The morphology of the nanoparticles was spherical, size (810.6±286.7 nm), zeta potential in pH 3.2 (+18.3 mV) and the 50% release of CVA at pHs 3 and 8 occurred at 200 and 10 h, respectively. nCVA showed LD50 of 2,609 mg/kg. CVA, nCVA and monepantel reduced the number of eggs per gram of faeces (epg) by 57.7%, 51.1% and 97.7%, respectively. The epg of sheep treated with CVA and nCVA did not differ from the negative control (P>0.05). Nanoencapsulation reduced the toxicity of CVA; however, nCVA and CVA presented similar results in the FECRT.

Anthelmintic activity of nanoencapsulated carvacryl acetate against gastrointestinal nematodes of sheep and its toxicity in rodents / Atividade anti-helmíntica do acetato de carvacrila nanoencapsulado sobre nematoides gastrintestinais de ovinos e toxicidade em roedores

Abstract The objective of this study was to evaluate the efficacy of carvacryl acetate (CVA) and nanoencapsulated CVA (nCVA) on gastrointestinal nematodes of sheep. The CVA was nanoencapsulated with chitosan/gum arabic and the efficacy of nanoencapsulation (EE), yield, zeta potential, nanoparticle morphology and release kinetics at pH 3 and 8 were analyzed. Acute and subchronic toxicity were evaluated in rodents and reduction of egg counts in the faeces (FECRT) of sheep. The sheep were divided into four groups (n = 10): G1, 250 mg/kg CVA; G2, 250 mg/kg nCVA; G3, polymer matrix and G4: 2.5 mg/kg monepantel. EE and nCVA yield were 65% and 57%, respectively. The morphology of the nanoparticles was spherical, size (810.6±286.7 nm), zeta potential in pH 3.2 (+18.3 mV) and the 50% release of CVA at pHs 3 and 8 occurred at 200 and 10 h, respectively. nCVA showed LD50 of 2,609 mg/kg. CVA, nCVA and monepantel reduced the number of eggs per gram of faeces (epg) by 57.7%, 51.1% and 97.7%, respectively. The epg of sheep treated with CVA and nCVA did not differ from the negative control (P>0.05). Nanoencapsulation reduced the toxicity of CVA; however, nCVA and CVA presented similar results in the FECRT.

Resumo O objetivo deste trabalho foi avaliar a eficácia do acetato de carvacrila (ACV) e do ACV nanoencapsulado (nACV) sobre nematóides gastrintestinais de ovinos. O ACV foi nanoencapsulado com quitosana/goma arábica e foi analisada a eficácia de nanoencapsulamento (EE), o rendimento, potencial zeta, morfologia das nanopartículas e cinética de liberação em pH 3 e 8. Foram avaliadas as toxicidades aguda e subcrônica em roedores e a redução da contagem de ovos nas fezes (RCOF) de ovinos. Os ovinos foram divididos em quatro grupos (n = 10): G1, 250 mg/kg ACV; G2, 250 mg/kg de nACV; G3, matriz polimérica e G4: 2,5 mg/kg de monepantel. A EE e o rendimento de nACV foram de 65% e 57%, respectivamente. A morfologia das nanopartículas foi esférica, tamanho (810,6±286,7 nm), potencial zeta no pH 3,2 (+18,3 mV) e a liberação de 50% de CVA nos pHs 3 e 8 ocorreu às 200 e 10 h, respectivamente. nACV apresentou DL50 de 2.609 mg/kg. ACV, nACV e o monepantel reduziram a contagem de ovos por grama de fezes (opg) em 57,7%, 51,1% e 97,7%, respectivamente. A contagem de opg de ovelhas tratadas com ACV e nCVA não diferiu do controle negativo (P>0,05). O nanoencapsulamento reduziu a toxicidade do AVC; no entanto, nACV e ACV apresentaram resultados semelhantes na RCOF.

Antifungal and Antioxidant Activities of Vernonia Chalybaea Mart. ex DC. Essential Oil and their Major Constituent β -caryophyllene

Abstract: This article describes the chemical composition of Vernonia chalybaea essential oil, and investigates its antimicrobial, antioxidant and hemolytic activities. The evaluation of the antifungal activity was performed by the broth microdilution method using strains of yeasts and dermatophytic fungi. The checkerboard technique to find antimicrobial modulatory effects was performed using ketoconazole as standard drug. The antioxidant activity was evaluated by DPPH scavenging assay and β-carotene/linoleic-acid system. The toxicity was characterized by the brine shrimp lethality test and hemolysis bioassays. The essential oil was obtained by hydrodistillation and analyzed by GC-MS method, showing to be rich in the sesquiterpenes β-caryophyllene (39.06%) and bicyclogermacrene (19.69%), and also demonstrated a relevant antifungal activity against strains of Trichophyton rubrum. In the modulatory activity assay, the essential oil of V. chalybaea and β-caryophyllene demonstrated a synergistic interaction with ketoconazole, with increasing of its antifungal action. The antioxidant activity was evidenced mainly by β-carotene/linoleic acid system, with IC50 value of 35.87 ± 0.32 µg/mL. The results suggest that V. chalybaea essential oil and β-caryophyllene are valuable natural medicinal agents with antioxidant and antimicrobial activities.

Anthelmintic activity of Eucalyptus citriodora essential oil and its major component, citronellal, on sheep gastrointestinal nematodes.

This study aimed to evaluate the anthelmintic activity of Eucalyptus citriodora essential oil and citronellal on sheep gastrointestinal nematodes. Essential oil composition was determined by gas chromatography mass spectrometry. The substances were evaluated in vitro using adult worm motility test (AWMT) and transmission electron microscopy (TEM). The acute toxicity test in mice and the fecal egg count reduction test (FECRT) in sheep were performed. Citronellal was confirmed as the essential oil major constituent (63.9%). According to the AWMT, 2 mg/mL of essential oil and citronellal completely inhibited Haemonchus contortus motility at 6 h post exposure. H. contortus exposed to essential oil and citronellal exhibited internal ultrastructural modifications. The lethal dose 50 values in mice were 5,000 and 2,609 mg/kg for essential oil and citronellal, respectively. E. citriodora essential oil reduced sheep epg at 14 days post treatment by 69.5% (P<0.05). No significant differences were observed in epg between the citronellal and negative control groups (P>0.05). The interaction between citronellal and other constituents in the essential oil may be relevant for its in vivo anthelmintic activity. Thus, E. citriodora essential oil and citronellal pharmacokinetic studies may help elucidate the anthelmintic activity of these compounds.

Anthelmintic activity of Eucalyptus citriodora essential oil and its major component, citronellal, on sheep gastrointestinal nematodes / Atividade anti-helmíntica do óleo essencial de Eucalyptus citriodora e seu componente majoritário, citronelal, sobre nematoides gastrintestinais de ovinos

Abstract This study aimed to evaluate the anthelmintic activity of Eucalyptus citriodora essential oil and citronellal on sheep gastrointestinal nematodes. Essential oil composition was determined by gas chromatography mass spectrometry. The substances were evaluated in vitro using adult worm motility test (AWMT) and transmission electron microscopy (TEM). The acute toxicity test in mice and the fecal egg count reduction test (FECRT) in sheep were performed. Citronellal was confirmed as the essential oil major constituent (63.9%). According to the AWMT, 2 mg/mL of essential oil and citronellal completely inhibited Haemonchus contortus motility at 6 h post exposure. H. contortus exposed to essential oil and citronellal exhibited internal ultrastructural modifications. The lethal dose 50 values in mice were 5,000 and 2,609 mg/kg for essential oil and citronellal, respectively. E. citriodora essential oil reduced sheep epg at 14 days post treatment by 69.5% (P<0.05). No significant differences were observed in epg between the citronellal and negative control groups (P>0.05). The interaction between citronellal and other constituents in the essential oil may be relevant for its in vivo anthelmintic activity. Thus, E. citriodora essential oil and citronellal pharmacokinetic studies may help elucidate the anthelmintic activity of these compounds.

Resumo Este trabalho objetivou avaliar a atividade anti-helmíntica do óleo essencial de Eucalyptus citriodora e citronelal sobre nematoides gastrintestinais de ovinos. A composição do óleo essencial foi determinada por cromatografia gasosa acoplada à espectrometria de massas. As substâncias foram avaliadas in vitro utilizando-se teste de motilidade de vermes adultos (AWMT) e microscopia eletrônica de transmissão (TEM). Teste de toxicidade aguda em camundongos e teste de redução da contagem de ovos fecais (FECRT) em ovinos foram realizados. Citronelal foi confirmado como componente majoritário do óleo essencial (63,9%). No AWMT, 2 mg/mL de óleo essencial e citronelal inibiram completamente a motilidade de H. contortus 6 h pós-exposição. H. contortus expostos ao óleo essencial e citronelal exibiram modificações ultraestruturais internas. Os valores da dose letal 50 em camundongos foram 5.000 e 2.609 mg/kg para óleo essencial e citronelal, respectivamente. Óleo essencial de E. citriodora reduziu opg de ovinos 14 dias pós-tratamento em 69,5% (P<0,05). Não houve diferença significativa de opg entre grupo controle negativo e citronelal (P>0,05). A interação entre citronelal e outros constituintes do óleo essencial pode ser relevante na atividade anti-helmíntica in vivo. Portanto, avaliação farmacocinética do óleo essencial de E. citriodora e citronelal pode auxiliar a elucidar a atividade anti-helmíntica desses compostos.

Different susceptibilities of Aedes aegypti and Aedes albopictus larvae to plant-derived products.

INTRODUCTION: Aedes aegypti and Aedes albopictus are important vectors that transmit arboviruses to human populations. METHODS: Natural products were obtained and tested against larvae collected from the field in Fortaleza, capital of Ceará state. RESULTS: The essential oils of Syzygium aromaticum (Ae. aegypti LC50 = 32.7 ppm and Ae. albopictus LC50 = 138.1 ppm) and Croton nepetaefolius (Ae. aegypti LC50 = 81.7 ppm and Ae. albopictus LC50 = 76.1 ppm) showed the most intense larvicidal activity. CONCLUSIONS: The essential oils and methyl esters showed greater larvicidal activity than did the ethanol extracts.

Different susceptibilities of Aedes aegypti and Aedes albopictus larvae to plant-derived products

Abstract INTRODUCTION: Aedes aegypti and Aedes albopictus are important vectors that transmit arboviruses to human populations. METHODS: Natural products were obtained and tested against larvae collected from the field in Fortaleza, capital of Ceará state. RESULTS: The essential oils of Syzygium aromaticum (Ae. aegypti LC50 = 32.7 ppm and Ae. albopictus LC50 = 138.1 ppm) and Croton nepetaefolius (Ae. aegypti LC50 = 81.7 ppm and Ae. albopictus LC50 = 76.1 ppm) showed the most intense larvicidal activity. CONCLUSIONS: The essential oils and methyl esters showed greater larvicidal activity than did the ethanol extracts.

Leishmanicidal and fungicidal activity of lipases obtained from endophytic fungi extracts.

This work describes the production of lipases from endophytic fungi: Vermisporium-like, Emericella nidulans, Dichotomophtora portulacae and D. boerhaaviae and the biological activity against the dermatophyte fungi Malassezia sp and Microsporum canis and the parasite Leishmania amazonensis. All fungal enzymes extract showed lipolysis action in the media that contains long carbon chain lipids. The proteomic analysis of lipases exhibits several molecules mostly ranging in size from 220 to 20 kDa, with clear differences in protein profile's yield. All fungal enzymes were competent to eliminate promastigote forms of Leishmania amazonensis at 5 mg.mL-1. The antileishmanial activity of lipases from Vermisporium-like, E. nidulans, D. portulacae and D. boerhaaviae in amastigote forms, promoted the reduction in viability of 78.88, 39.65, 63.17 and 98.13%, with selectivity index of 19.56, 30.68, 18.09 and 20.99. In relation to antifungal activity, Dichothomophtora enzymes demonstrate best action with MFC of 14.65 µg.mL-1 against Malassezia sp and Microsporum canis, respectively. These results allow us to infer that lipases from entophytic fungi displays activity against dermatophyte fungi (Malassezia sp. and Microsporum canis) as well as Leishmania.

Anthelmintic effect of thymol and thymol acetate on sheep gastrointestinal nematodes and their toxicity in mice.

Thymol is a monoterpene and acetylation form of this compound can reduce the toxicity and enhance its biological effects. The objective of this study was to evaluate the effect of thymol and thymol acetate (TA) on egg, larva and adult Haemonchus contortus and the cuticular changes, acute toxicity in mice and the efficacy on sheep gastrointestinal nematodes. In vitro tests results were analyzed by analysis of variance (ANOVA) and followed by comparison with Tukey test or Bonferroni. The efficacy of in vivo test was calculated by the BootStreet program. In the egg hatch test (EHT), thymol (0.5 mg/mL) and TA (4 mg/mL) inhibited larval hatching by 98% and 67.1%, respectively. Thymol and TA (8 mg/mL) inhibited 100% of larval development. Thymol and TA (800 µg/mL) reduced the motility of adult worms, by 100% and 83.4%, respectively. Thymol caused cuticular changes in adult worm teguments. In the acute toxicity test, the LD50 of thymol and TA were 1,350.9 mg/kg and 4,144.4 mg/kg, respectively. Thymol and TA reduced sheep egg count per gram of faeces (epg) by 59.8% and 76.2%, respectively. In in vitro tests thymol presented better anthelmintic activity than TA. However TA was less toxic and in in vivo test efficacy was similar.

Anthelmintic effect of thymol and thymol acetate on sheep gastrointestinal nematodes and their toxicity in mice / Efeito anti-helmíntico do timol e acetato de timila sobre nematoides gastrintestinais de ovinos e toxicidade em camundongos

Abstract Thymol is a monoterpene and acetylation form of this compound can reduce the toxicity and enhance its biological effects. The objective of this study was to evaluate the effect of thymol and thymol acetate (TA) on egg, larva and adult Haemonchus contortus and the cuticular changes, acute toxicity in mice and the efficacy on sheep gastrointestinal nematodes. In vitro tests results were analyzed by analysis of variance (ANOVA) and followed by comparison with Tukey test or Bonferroni. The efficacy of in vivo test was calculated by the BootStreet program. In the egg hatch test (EHT), thymol (0.5 mg/mL) and TA (4 mg/mL) inhibited larval hatching by 98% and 67.1%, respectively. Thymol and TA (8 mg/mL) inhibited 100% of larval development. Thymol and TA (800 µg/mL) reduced the motility of adult worms, by 100% and 83.4%, respectively. Thymol caused cuticular changes in adult worm teguments. In the acute toxicity test, the LD50 of thymol and TA were 1,350.9 mg/kg and 4,144.4 mg/kg, respectively. Thymol and TA reduced sheep egg count per gram of faeces (epg) by 59.8% and 76.2%, respectively. In in vitro tests thymol presented better anthelmintic activity than TA. However TA was less toxic and in in vivo test efficacy was similar.

Resumo Timol é um monoterpeno e a acetilação deste composto pode reduzir a toxicidade e potencializar os seus efeitos biológicos. O objetivo deste trabalho foi avaliar o efeito do timol e acetato de timolila (AT) sobre ovos, larvas e adultos de Haemonchus contortus e suas alterações cuticulares, toxicidade aguda em camundongos e a eficácia sobre nematoides gastrintestinais de ovinos. Os resultados dos testes in vitro foram analisados por análise de variância (ANOVA) e comparados pelo testes de Tukey ou Bonferroni. A eficácia do teste de redução da contagem de ovos nas fezes (RCOF) foi calculada pelo programa BootStreet. No teste de inibição da eclosão de ovos (TEO), timol (0,5 mg/mL) e AT (4 mg/mL) inibiram a eclosão das larvas em 98% e 67,1%, respectivamente. Timol e AT (8 mg/mL) inibiram 100% do desenvolvimento larval. Timol e AT (800 μg/mL) reduziram a motilidade dos nematoides adultos, em 100% e 83,4%, respectivamente. O timol provocou alterações cuticulares nos nematoides adultos. No teste de toxicidade aguda, a DL50 do timol e AT foi de 1.350,9 mg/kg e 4.144,4 mg/kg, respectivamente. Timol e AT reduziram a contagem de ovos por gramas de fezes (OPG) dos ovinos em 59,8% e 76,2%, respectivamente. Nos testes in vitro timol apresentou atividade melhor anti-helmíntica do que AT. Entretanto, AT foi menos tóxico do que o timol e no teste in vivo apresentaram eficácia semelhante.

Ethnobotanical study of medicinal plants in Imperatriz, State of Maranhão, Northeastern Brazil / Estudo etnobotânico de plantas medicinais em Imperatriz, Estado do Maranhão, Nordeste do Brasil

The study of medicinal plants reveals locally important plant species often useful for the discovery of new drugs. The objective of this research was to conduct an ethnobotanical survey of medicinal plants used by the population of the Imperatriz city, State of Maranhão, Northeastern Brazil. Two hundred and five interviews were conducted, resulting in the collection of 60 plant species from 31 plant families. The highest number of species belongs to Fabaceae, followed by Lamiaceae, Asteraceae and Euphorbiaceae. The most reported species were Chenopodium ambrosioides, Myracrodruon urundeuva, Lippia alba, and Plectranthus barbatus. The main plant parts used were leaves (63.3%), bark (16.7%), fruits (6.7%), roots (6.7%), seeds (3.3), stems (1.7%) and latex (1.7%). Major administration routes were by oral (81.7%) or nasal via (1.6%) and topical application (16.7%) The plants were used to mitigate various health problems including pain, asthma, hypertension, gastritis, inflammation, influenza, and tuberculosis. The collected data shows that local population uses medicinal plants for treatment of several diseases and this study can serve as a basis for future chemical and pharmacological investigation, which can lead to the discovery of new therapeutic agents.

O estudo de plantas medicinais são em geral significativos em revelar espécies de plantas localmente importantes, principalmente para a descoberta de fármacos. O objetivo desta pesquisa foi realizar um levantamento etnobotânico das plantas medicinais utilizadas pela população da cidade de Imperatriz no estado do Maranhão, Nordeste do Brasil. 205 entrevistas foram realizadas resultando na coleção de 60 espécies de 31 famílias de plantas. Fabaceae teve o maior número de espécies, seguido por Lamiaceae, Asteraceae e Euphorbiaceae. As espécies mais utilizadas foram Chenopodium ambrosioides, Myracrodruon urundeuva, Lippia alba e Plectranthus barbatus. As principais partes foram as folhas (63,3%), cascas (16,7%), frutos (6,7%), raízes (6,7%), sementes (3,3%), caule (1,7%) e látex (1,7%). As vias de administração mais frequentes foram oral (81,7%), tópica (16,7%) e nasal (1,6%). As plantas são utilizadas para diversos problemas de saúde como dores em geral, asma, hipertensão, gastrite, inflamação, gripe e tuberculose. Os dados mostram que população local utiliza plantas medicinais para tratamento de várias doenças e este estudo pode servir de base para estudos químicos e farmacológicos futuros que levem ao descobrimento de novos agentes terapêuticos.

In vitro effects of Coriandrum sativum, Tagetes minuta, Alpinia zerumbet and Lantana camara essential oils on Haemonchus contortus / Efeitos in vitro dos óleos essenciais de Coriandrum sativum, Tagetes minuta, Alpinia zerumbet e Lantana camara sobre Haemonchus contortus

Phytotherapy can be an alternative for the control of gastrointestinal parasites of small ruminants. This study evaluated the efficacy of Alpinia zerumbet, Coriandrum sativum, Tagetes minuta and Lantana camara essential oils by two in vitro assays on Haemonchus contortus, an egg hatch test (EHT) and larval development test (LDT). No effect was observed for L. camara in the EHT. A. zerumbet, C. sativum and T. minuta essential oils exhibited a dose-dependent effect in the EHT, inhibiting 81.2, 99 and 98.1% of H. contortus larvae hatching, respectively, at a concentration of 2.5 mg mL-¹. The effective concentration to inhibit 50% (EC50) of egg hatching was 0.94, 0.63 and 0.53 mg mL-¹ for A. zerumbet, C. sativum and T. minuta essential oils, respectively. In LDT, L. camara, A. zerumbet, C. sativum and T. minuta at concentration of 10 mg mL-¹ inhibited 54.9, 94.2, 97.8 and 99.5% of H. contortus larval development, presenting EC50 values of 6.32, 3.88, 2.89 and 1.67 mg mL-¹, respectively. Based on the promising results presented in this in vitro model, it may be possible use of these essential oils to control gastrointestinal nematodes. However, their anthelmintic activity should be confirmed in vivo.

Fitoterapia pode ser uma alternativa para o controle de parasitas gastrintestinais de pequenos ruminantes. Este estudo avaliou a eficácia dos óleos essenciais de Alpinia zerumbet, Coriandrum sativum, Tagetes minuta e Lantana camara sobre Haemonchus contortus através de dois testes in vitro, teste de eclosão dos ovos (TEO) e teste de desenvolvimento larval (TDL). Nenhum efeito foi observado para L. camara no TEO. Os óleos essenciais de A. zerumbet, C. sativum e T. minuta exibiram um efeito dose dependente no TEO inibindo a eclosão das larvas de H. contortus em 81,2, 99 e 98,1%, respectivamente, na concentração de 2,5 mg mL-¹. A concentração efetiva para inibir 50% (CE50) da eclosão dos ovos foi de 0,94, 0,63 e 0,53 mg mL-¹ para os óleos essenciais de A. zerumbet, C. sativum e T. minuta, respectivamente. No TDL, 10 mg mL-¹ de L. camara, A. zerumbet, C. sativum e T. minuta inibiram em 54,9, 94,2, 97,8 e 99,5% do desenvolvimento larvar, apresentando valores de CE50 de 6,32, 3,88, 2,89 e 1,67 mg mL-¹, respectivamente. Com base nos resultados promissores apresentados neste modelo in vitro, pode ser possível a utilização destes óleos essenciais para controlar os nematoides gastrintestinais. No entanto, a sua atividade anti-helmíntica deve ser confirmada in vivo.

In vitro efficacy of Coriandrum sativum, Lippia sidoides and Copaifera reticulata against Leishmania chagasi / Eficácia in vitro de Coriandrum sativum, Lippia sidoides e Copaifera reticulata sobre Leishmania chagasi

The increased incidence of visceral leishmaniasis (VL) in Brazil is due to a lack of effective disease control measures. In addition to that, no effective treatment exists for canine VL in response to synthetic drugs. Thus, the objective of this study was to evaluate the effect of the essential oils of Coriandrum sativum and Lippia sidoides, and oleoresin from Copaifera reticulata, on Leishmania chagasi promastigotes and amastigotes. We also examined the toxicity of these treatments on the murine monocyte cell line RAW 264.7. To determine the IC50 a MTT test (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) was performed on promastigotes, and an in situ ELISA assay was conducted on amastigotes. Here, we demonstrate that oleoresin from C. reticulata was effective against both promastigotes (IC50 of 7.88 µg.mL-1) and amastigotes (IC50 of 0.52 µg.mL-1), and neither of the two treatments differed significantly (p > 0.05) from pentamidine (IC50 of 2.149 µg.mL-1) and amphotericin B (IC50 of 9.754 µg.mL-1). Of the three plant oils tested, only oleoresin showed no toxicity toward monocyte, with 78.45% viability after treatment. Inhibition of promastigote and amastigote growth and the lack of cytotoxicity by C. reticulata demonstrate that oleoresin may be a viable option for analyzing the in vivo therapeutic effects of leishmanicidal plants.

O aumento na incidência da Leishmaníase Visceral (LV) no Brasil deve-se à ineficácia das medidas de controle da doença. Além disso, não há tratamento efetivo para LV canina com drogas sintéticas. Assim, o objetivo deste trabalho foi avaliar o efeito dos óleos essenciais de Coriandrum sativum e de Lippia sidoides e do óleo-resina de Copaiferareticulata sobre promastigotas e amastigotas de Leishmania chagasi e analisar o grau de toxicidade sobre células monocíticas murinas RAW 264.7. Para determinar a CI50 sobre promastigotas foi usado teste MTT (brometo de 3-[4,5-dimetil-tiazol-2-il]-2,5-difeniltetrazólio) e sobre amastigotas foi realizado imunoensaio in situ pela técnica de ELISA. Os resultados obtidos comprovaram que o óleo-resina de C. reticulata foi o mais eficaz contra as formas promastigotas (CI50 de 7,88 µg.mL-1) e amastigotas (CI50 de 0,52 µg.mL-1) e em nenhum dos dois testes diferiu do controle pentamidina que obteve CI50 de 2,149 µg.mL-1, no teste sobre promastigotas, e anfotericina B que obteve CI50 de 9,754 µg.mL-1, nos testes com amastigotas (p > 0.05). Quanto à citotoxicidade apenas o óleo-resina não apresentou toxicidade com 78,45% de monócitos viáveis. Os resultados obtidos sobre promastigotas e amastigotas e a ausência de citotoxicidade do óleo-resina de C. reticulata evidenciam que este óleo-resina pode ser viável para a análise de seus efeitos terapêuticos em testes in vivo.

Plantas taniníferas e o controle de nematóides gastrintestinais de pequenos ruminantes / Tanniferous plants and control of gastrointestinal nematodes of small ruminants

Os nematóides gastrintestinais são responsáveis por acentuada redução na produtividade de ovinos e caprinos. Na tentativa de controlar esses parasitos, são utilizados diversos anti-helmínticos sintéticos, mas o desenvolvimento da resistência tem tornado esse controle pouco eficaz. Na busca por alternativas de controle dos nematóides gastrintestinais, a utilização de plantas taniníferas tem despertado interesse de pesquisadores em várias regiões do mundo. Essa revisão visa a abordar os diversos aspectos relacionados ao fornecimento dessas plantas a ovinos e caprinos, bem como os principais resultados obtidos em pesquisas utilizando taninos para o controle de nematóides de pequenos ruminantes.

The gastrointestinal nematodes are responsible for a marked reduction in the productivity of sheep and goats. In an attempt to control these parasites, different synthetic anthelmintics are used, but development of resistance has become this control little effective. In the search for alternatives to control these nematodes, the use of tanniferous plants has attracted attention from researchers in different regions of the world. This review aims to address the various aspects related to the administration of these plants to sheep and goats, and the main results obtained from studies using tannins to control nematodes in small ruminants.

Effect of six tropical tanniferous plant extracts on larval exsheathment of Haemonchus contortus.

Tanniferous plants represent a promising alternative for controlling gastrointestinal nematodes of small ruminants. This experiment evaluated the effects of extracts from the leaf and stem of Anadenanthera colubrina, Leucaena leucocephala and Mimosa tenuiflora on larval exsheathment of Haemonchus contortus in vitro and verified the role of tannins in this process. Third-stage larvae of H. contortus were incubated with extracts for 3 hours and were exposed to sodium hypochlorite solution. The extracts were tested at 300 µg.mL(-1) and accompanied by controls: phosphate buffer solution (PBS) and polyvinyl polypyrrolidone (PVPP). The larval exsheathment was evaluated for 60 minutes, and the results were subjected to the Kruskal-Wallis test (p < 0.05). The six extracts blocked larval exsheathment. After PVPP addition, a tannin inhibitor, the exsheathment percentage was similar to the PBS (p > 0.05), except for L. leucocephala and M. tenuiflora leaf extracts. However, pre-incubation with PVPP of these two extracts significantly changed larval exsheathment when compared to the non-treated extracts (p < 0.05). These results suggest that A. colubrina, L. leucocephala and M. tenuiflora could be useful in gastrointestinal nematode control and that tannins are probably the main compounds involved in the observed effects. However, in vivo and toxicological studies should be conducted.

Effect of six tropical tanniferous plant extracts on larval exsheathment of Haemonchus contortus / Efeito de seis extratos de plantas taniníferas tropicais sobre o desembainhamento larvar de Haemochus contortus

Tanniferous plants represent a promising alternative for controlling gastrointestinal nematodes of small ruminants. This experiment evaluated the effects of extracts from the leaf and stem of Anadenanthera colubrina, Leucaena leucocephala and Mimosa tenuiflora on larval exsheathment of Haemonchus contortus in vitro and verified the role of tannins in this process. Third-stage larvae of H. contortus were incubated with extracts for 3 hours and were exposed to sodium hypochlorite solution. The extracts were tested at 300 µg.mL-1 and accompanied by controls: phosphate buffer solution (PBS) and polyvinyl polypyrrolidone (PVPP). The larval exsheathment was evaluated for 60 minutes, and the results were subjected to the Kruskal-Wallis test (p < 0.05). The six extracts blocked larval exsheathment. After PVPP addition, a tannin inhibitor, the exsheathment percentage was similar to the PBS (p > 0.05), except for L. leucocephala and M. tenuiflora leaf extracts. However, pre-incubation with PVPP of these two extracts significantly changed larval exsheathment when compared to the non-treated extracts (p < 0.05). These results suggest that A. colubrina, L. leucocephala and M. tenuiflora could be useful in gastrointestinal nematode control and that tannins are probably the main compounds involved in the observed effects. However, in vivo and toxicological studies should be conducted.

Plantas taniníferas representam uma promissora alternativa de controle dos nematóides gastrintestinais de pequenos ruminantes. Esse experimento avaliou in vitro os efeitos dos extratos das folhas e caules de Anadenanthera colubrina, Leucaena leucocephala e Mimosa tenuiflora sobre o desembainhamento larvar de Haemonchus contortus e verificou o papel dos taninos nesse processo. Larvas de terceiro estádio de H. contortus foram incubadas com 300 µg.mL-1 de extrato por 3 horas e expostas a uma solução de hipoclorito de sódio. O ensaio foi acompanhado por controles: solução salina tamponada com fosfato (PBS) e polivinilpolipirrolidona (PVPP). O desembainhamento larvar foi avaliado durante 60 minutos e os resultados submetidos ao teste Kruskal-Wallis (p < 0,05). Os seis extratos bloquearam o desembainhamento larvar. Após adição de PVPP, um inibidor de taninos, o percentual de desembainhamento foi similar ao PBS (p > 0,05), exceto nos extratos das folhas de L. leucocephala e M. tenuiflora. Entretanto, a pré-incubação desses dois extratos com PVPP alterou significativamente o desembainhamento quando comparado com extratos não-tratados (p < 0,05). Esses resultados sugerem que A. colubrina, L. leucocephala e M. tenuiflora podem ser úteis no controle de nematóides gastrintestinais e que os taninos são provavelmente os principais compostos envolvidos nos efeitos. Contudo, estudos toxicológicos e in vivo são necessários.

Antioxidant, larvicidal and antiacetylcholinesterase activities of cashew nut shell liquid constituents.

Anacardic acid, cardanol and cardol, the main constituents of natural cashew nut shell liquid (CNSL), were obtained by solvent extraction and assayed for antioxidant, larvicidal and antiacetylcholinesterase activity. Their relative percent composition was obtained by HPLC analysis. Antioxidant activity was assessed using the DPPH and ABTS(+) tests, which showed cardanol as the most active, followed by cardol and anacardic acid. The three CNSL components demonstrated good larvicidal activity against Aedes aegypti (LC(50)=12.40 for anacardic acid, 10.22 for cardol and 14.45 for cardanol) and exhibited inhibition zones for acetylcholinesterase enzymes in the TLC test similar to carbachol, which was used as standard. Based on the results, these multipotent compounds represent promising agents in the control of Ae. aegypti, the main dengue vector in Brazil.

Chemical composition, toxicity and larvicidal and antifungal activities of Persea americana (avocado) seed extracts.

The present study had the aim of testing the hexane and methanol extracts of avocado seeds, in order to determine their toxicity towards Artemia salina, evaluate their larvicidal activity towards Aedes aegypti and investigate their in vitro antifungal potential against strains of Candida spp, Cryptococcus neoformans and Malassezia pachydermatis through the microdilution technique. In toxicity tests on Artemia salina, the hexane and methanol extracts from avocado seeds showed LC50 values of 2.37 and 24.13 mg mL-1 respectively. Against Aedes aegypti larvae, the LC50 results obtained were 16.7 mg mL-1 for hexane extract and 8.87 mg mL-1 for methanol extract from avocado seeds. The extracts tested were also active against all the yeast strains tested in vitro, with differing results such that the minimum inhibitory concentration of the hexane extract ranged from 0.625 to 1.25mg L-(1), from 0.312 to 0.625 mg mL-1 and from 0.031 to 0.625 mg mL-1, for the strains of Candida spp, Cryptococcus neoformans and Malassezia pachydermatis, respectively. The minimal inhibitory concentration for the methanol extract ranged from 0.125 to 0.625 mg mL-1, from 0.08 to 0.156 mg mL-1 and from 0.312 to 0.625 mg mL-1, for the strains of Candida spp., Cryptococcus neoformans and Malassezia pachydermatis, respectively.