RESUMO
INTRODUCTION: Bioprospection of plant products is used to discover new insecticides. METHODS: The larvicidal activity of ethanolic extract and triterpene (tingenone B) from the bark of Maytenus guianensis and their effect on pupation and emergence were evaluated against Aedes aegypti. RESULTS: Crude extract LC50 was 11.3 ppm and caused ejection of the larvae intestine; tingenone B LC50 was 14.8 ppm. Pupation was reduced by 20% and 10%, respectively; however, the emergence was not affected. CONCLUSIONS: The crude bark extract exhibited a higher larvicidal effect against the vector.
Assuntos
Aedes , Anopheles , Celastraceae , Inseticidas , Maytenus , Animais , Inseticidas/farmacologia , Larva , Mosquitos Vetores , Extratos Vegetais/farmacologia , Folhas de PlantaRESUMO
Abstract INTRODUCTION: Bioprospection of plant products is used to discover new insecticides. METHODS: The larvicidal activity of ethanolic extract and triterpene (tingenone B) from the bark of Maytenus guianensis and their effect on pupation and emergence were evaluated against Aedes aegypti. RESULTS: Crude extract LC50 was 11.3 ppm and caused ejection of the larvae intestine; tingenone B LC50 was 14.8 ppm. Pupation was reduced by 20% and 10%, respectively; however, the emergence was not affected. CONCLUSIONS: The crude bark extract exhibited a higher larvicidal effect against the vector.
Assuntos
Aedes , Celastraceae , Maytenus , Inseticidas/farmacologia , Anopheles , Extratos Vegetais/farmacologia , Folhas de Planta , Mosquitos Vetores , LarvaRESUMO
Leishmaniases, caused by Leishmania spp., are among the most prevalent infectious diseases in the world and their treatment may present high toxicity and side/adverse effects. This study evaluated the antileishmanial activity of the Hexanic Eluate subfraction from Maytenus guianensis bark (HEMg) incorporated in microparticles of PLGA. One batch of microparticles produced contained HEMg (HEMgP) and another contained the PLGA polymer alone (PCTE). The microparticles were characterized in regards to diameter, Zeta potential, encapsulation rate and morphology and their cytotoxicity was evaluated against J774 macrophages. The infection assay employing peritoneal macrophages witth L. amazonensis and cytokine dosages were performed on the cell supernatants. The groups of infected BALB/C mice were treated, euthanized and the parasite load and cytokine production were evaluated. The diameters and zeta potential were: 4⯵m and -11.6â¯mV (PCTE) and 7.8⯵m and -26.7â¯mV (HEMgP). The encapsulation rate was â 15% and the morphology of the particles was spherical and homogeneous. In the infection assay, HEMgP inhibited the amastigotes by 70% (24â¯h) and 59% (48â¯h) and induced IL-12 and TNF-α production. HEMg in solution reduced the number of parasites in the lymph nodes by 50% and HEMgP administration increased the levels of IL-12 and TNF-α cytokines in lymph nodes and in the lesion site. When encapsulated, HEMg maintained its antileishmanial activity, but in a more attenuated and sustained form over time, showing promise as complementary/alternative therapy against cutaneous leishmaniasis.
Assuntos
Antiprotozoários/farmacologia , Leishmania mexicana/efeitos dos fármacos , Maytenus/química , Casca de Planta/química , Extratos Vegetais/farmacologia , Animais , Biodegradação Ambiental , Linhagem Celular , Micropartículas Derivadas de Células/química , Micropartículas Derivadas de Células/ultraestrutura , Concentração Inibidora 50 , Linfonodos/parasitologia , Macrófagos Peritoneais/efeitos dos fármacos , Macrófagos Peritoneais/parasitologia , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Microscopia Eletrônica de VarreduraRESUMO
INTRODUCTION: This aim of this study was to evaluate the antibacterial activity of fractions and isolates of Maytenus guianensis, a plant species used in Amazonian folk medicine. METHODS: A disk diffusion technique was used to investigate the antibacterial potential. RESULTS: The hexanic fractions and tingenone B isolate showed inhibitory effects against Staphylococcus aureus and Streptococcus pneumoniae. CONCLUSIONS: These results indicate the antibacterial potential of this species and will enable future studies to identify novel therapeutic alternatives from this species.
Assuntos
Antibacterianos/farmacologia , Escherichia coli/efeitos dos fármacos , Klebsiella pneumoniae/efeitos dos fármacos , Maytenus/química , Extratos Vegetais/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Streptococcus pneumoniae/efeitos dos fármacos , Antibacterianos/isolamento & purificação , Testes de Sensibilidade a Antimicrobianos por Disco-DifusãoRESUMO
Abstract INTRODUCTION This aim of this study was to evaluate the antibacterial activity of fractions and isolates of Maytenus guianensis, a plant species used in Amazonian folk medicine. METHODS A disk diffusion technique was used to investigate the antibacterial potential. RESULTS The hexanic fractions and tingenone B isolate showed inhibitory effects against Staphylococcus aureus and Streptococcus pneumoniae. CONCLUSIONS These results indicate the antibacterial potential of this species and will enable future studies to identify novel therapeutic alternatives from this species.
Assuntos
Staphylococcus aureus/efeitos dos fármacos , Streptococcus pneumoniae , Extratos Vegetais/farmacologia , Maytenus/química , Escherichia coli/efeitos dos fármacos , Klebsiella pneumoniae/efeitos dos fármacos , Antibacterianos/farmacologia , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Antibacterianos/isolamento & purificaçãoRESUMO
INTRODUCTION: This study assessed the activity of compounds from Piper tuberculatum against Plasmodium falciparum and Leishmania guyanensis. METHODS: The effects of compounds from P. tuberculatum fruits on P. falciparum and L. guyanensis promastigote growth in vitro were determined. Hemolytic action and cytotoxicity in HepG2 and J774 cells were measured. RESULTS: Three compounds showed strong antiplasmodial activity and one compound showed strong antileishmanial activity. Two compounds were non-toxic to HepG2 cells and all were toxic to J774 cells. The compounds showed no hemolytic activity. CONCLUSIONS: The tested compounds from P. tuberculatum exhibited antiparasitic and cytotoxic effects.
Assuntos
Antiprotozoários/farmacologia , Frutas/química , Leishmania guyanensis/efeitos dos fármacos , Piper/química , Extratos Vegetais/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Antiprotozoários/isolamento & purificação , Células Hep G2/efeitos dos fármacos , Humanos , Concentração Inibidora 50 , Testes de ToxicidadeRESUMO
Abstract INTRODUCTION This study assessed the activity of compounds from Piper tuberculatum against Plasmodium falciparum and Leishmania guyanensis. METHODS The effects of compounds from P. tuberculatum fruits on P. falciparum and L. guyanensis promastigote growth in vitro were determined. Hemolytic action and cytotoxicity in HepG2 and J774 cells were measured. RESULTS Three compounds showed strong antiplasmodial activity and one compound showed strong antileishmanial activity. Two compounds were non-toxic to HepG2 cells and all were toxic to J774 cells. The compounds showed no hemolytic activity. CONCLUSIONS The tested compounds from P. tuberculatum exhibited antiparasitic and cytotoxic effects.
Assuntos
Humanos , Plasmodium falciparum/efeitos dos fármacos , Extratos Vegetais/farmacologia , Leishmania guyanensis/efeitos dos fármacos , Piper/química , Frutas/química , Antiprotozoários/farmacologia , Testes de Toxicidade , Concentração Inibidora 50 , Células Hep G2/efeitos dos fármacos , Antiprotozoários/isolamento & purificaçãoRESUMO
The strategies to control the cattle tick, Rhipicephalus microplus are based mainly on the use of synthetic pesticides. However, the emergence, establishment, and development of resistance of ticks is rendering the main chemical groups ineffective. Finding new molecules to effectively control infestations by R. microplus is necessary to maintain the productivity of cattle herds, particularly of taurine breeds established in equatorial and tropical regions of the world. Ethanol extracts from the leaves, stems, and fruits of Piper tuberculatum were evaluated in bioassays at concentrations of 50, 25, 12.50, 6.25, 3.12 and 1.56 mg mL-1. The concentrations lethal to 50% of the individuals (LC50) of tick larvae after 24 hours of exposure were 3.62, 3.99 and 5.30 mg mL-1 for fruit, stem and leaf extracts, respectively. Against the engorged females, the highest efficacy rates were obtained at the concentration of 50 mg mL-1, corresponding to 71.57%, 68.38% and 37.03% of the fruit, leaf and stem extracts, respectively. The main effect of the ethanol extracts was on the egg hatching rate of ticks, with a reduction of 55.63% for the fruit and leaf extracts, and 20.82% for the stem extract. The results show that P. tuberculatum is a promising source of molecules for use as active ingredients in pesticide formulations for R. microplus control.(AU)
Estratégias de controle do carrapato dos bovinos, Rhipicephalus microplus, fundamentam-se na utilização de pesticidas. Os principais grupos químicos utilizados atualmente mostram-se ineficazes devido ao surgimento de populações resistentes. A pesquisa de novas moléculas com eficiência acaricida é uma necessidade para manutenção da produtividade dos rebanhos bovinos estabelecidos em regiões de clima tropical. Avaliamos a atividade de Piper tuberculatum para o controle de fêmeas ingurgitadas e larvas de R. microplus através de bioensaios de imersão de adultos e de pacotes de larvas. As concentrações avaliadas foram de 50; 25; 12,50; 6,25; 3,12 e 1,56 mg mL-1 de extrato etanólico de folha, talo e fruto de P. tuberculatum. As concentrações letais para 50% dos indivíduos (CL50) após 24 horas de exposição de larvas de R. microplus foram 3,62; 3,99 e 5,30 mg mL-1 para os extratos etanólicos de fruto, talo e folha, respectivamente. Para fêmeas ingurgitadas, a maior eficácia resultou da concentração de 50 mg mL-1 de extrato de fruto (71.57%). O principal efeito dos extratos etanólicos de P. tuberculatum foi sobre a eclodibilidade, com uma redução de 55.63% para extratos de fruto e folha. P. tuberculatum mostra-se promissora como fonte de moléculas candidatas a uso em pesticidas, em formulações destinadas ao controle das infestações de R. microplus.(AU)
Assuntos
Animais , Rhipicephalus , Controle de Ácaros e Carrapatos/métodos , Acaricidas/análise , Piperaceae/toxicidade , BioensaioRESUMO
ABSTRACT The strategies to control the cattle tick, Rhipicephalus microplus are based mainly on the use of synthetic pesticides. However, the emergence, establishment, and development of resistance of ticks is rendering the main chemical groups ineffective. Finding new molecules to effectively control infestations by R. microplus is necessary to maintain the productivity of cattle herds, particularly of taurine breeds established in equatorial and tropical regions of the world. Ethanol extracts from the leaves, stems, and fruits of Piper tuberculatum were evaluated in bioassays at concentrations of 50, 25, 12.50, 6.25, 3.12 and 1.56 mg mL-1. The concentrations lethal to 50% of the individuals (LC50) of tick larvae after 24 hours of exposure were 3.62, 3.99 and 5.30 mg mL-1 for fruit, stem and leaf extracts, respectively. Against the engorged females, the highest efficacy rates were obtained at the concentration of 50 mg mL-1, corresponding to 71.57%, 68.38% and 37.03% of the fruit, leaf and stem extracts, respectively. The main effect of the ethanol extracts was on the egg hatching rate of ticks, with a reduction of 55.63% for the fruit and leaf extracts, and 20.82% for the stem extract. The results show that P. tuberculatum is a promising source of molecules for use as active ingredients in pesticide formulations for R. microplus control.
RESUMO Estratégias de controle do carrapato dos bovinos, Rhipicephalus microplus, fundamentam-se na utilização de pesticidas. Os principais grupos químicos utilizados atualmente mostram-se ineficazes devido ao surgimento de populações resistentes. A pesquisa de novas moléculas com eficiência acaricida é uma necessidade para manutenção da produtividade dos rebanhos bovinos estabelecidos em regiões de clima tropical. Avaliamos a atividade de Piper tuberculatum para o controle de fêmeas ingurgitadas e larvas de R. microplus através de bioensaios de imersão de adultos e de pacotes de larvas. As concentrações avaliadas foram de 50; 25; 12,50; 6,25; 3,12 e 1,56 mg mL-1 de extrato etanólico de folha, talo e fruto de P. tuberculatum. As concentrações letais para 50% dos indivíduos (CL50) após 24 horas de exposição de larvas de R. microplus foram 3,62; 3,99 e 5,30 mg mL-1 para os extratos etanólicos de fruto, talo e folha, respectivamente. Para fêmeas ingurgitadas, a maior eficácia resultou da concentração de 50 mg mL-1 de extrato de fruto (71.57%). O principal efeito dos extratos etanólicos de P. tuberculatum foi sobre a eclodibilidade, com uma redução de 55.63% para extratos de fruto e folha. P. tuberculatum mostra-se promissora como fonte de moléculas candidatas a uso em pesticidas, em formulações destinadas ao controle das infestações de R. microplus.
Assuntos
Anotação de Sequência MolecularRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: 3ß,6ß,16ß-Trihydroxylup-20(29)-ene (TTHL) is a triterpene isolated from the flowers of Combretum leprosum, a plant used in folk medicine in the north of Brazil for the treatment of skin disorders. AIM OF THE STUDY: In the present study, TTHL was evaluated as a potential topical anti-inflammatory and anti-proliferative agent through in vivo and in vitro models. MATERIAL AND METHODS: Anti-inflammmatory and anti-proliferative effects of TTHL were assessed using Swiss mice in acute and chronic models of skin inflammation induced by 12-O-tetradecanoylphorbol-acetate (TPA) application. Anti-proliferative activity was proved through in vitro experiments with the HaCaT human keratinocyte cell line. RESULTS: Treatment with TTHL inhibited inflammatory parameters such as oedema formation and cellular infiltration in acute and chronic models. In the chronic model, TTHL also inhibited epidermal hyperproliferation, as evidenced by reduction of epidermis thickness and proliferating cell nuclear antigen expression. The anti-proliferative effect was confirmed by the capability of TTHL in reducing the proliferation and inducing cell apoptosis of HaCaT cells. Suggesting a mechanism of action, TTHL showed activation of corticosteroid receptors, but without the induction of corticosteroid-related cutaneous side effects. CONCLUSION: Our results demonstrate consistent anti-inflammatory and anti-proliferative activity and assign TTHL as a valuable tool in the development of a new treatment for skin inflammatory and proliferative diseases, such as psoriasis.