ABSTRACT
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.
Subject(s)
Aedes , Celastraceae , Maytenus , Insecticides/pharmacology , Anopheles , Plant Extracts/pharmacology , Plant Leaves , Mosquito Vectors , LarvaABSTRACT
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.
Subject(s)
Staphylococcus aureus/drug effects , Streptococcus pneumoniae , Plant Extracts/pharmacology , Maytenus/chemistry , Escherichia coli/drug effects , Klebsiella pneumoniae/drug effects , Anti-Bacterial Agents/pharmacology , Disk Diffusion Antimicrobial Tests , Anti-Bacterial Agents/isolation & purificationABSTRACT
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.
Subject(s)
Humans , Plasmodium falciparum/drug effects , Plant Extracts/pharmacology , Leishmania guyanensis/drug effects , Piper/chemistry , Fruit/chemistry , Antiprotozoal Agents/pharmacology , Toxicity Tests , Inhibitory Concentration 50 , Hep G2 Cells/drug effects , Antiprotozoal Agents/isolation & purificationABSTRACT
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.
Subject(s)
Molecular Sequence AnnotationABSTRACT
Abstract INTRODUCTION Maytenus guianensis is a member of the Celastraceae family that is used in traditional medicine, particularly for its anti-parasitic and anti-cancer effects. To explore the ethnopharmacological potential of this plant, the present study was designed to screen the in vitro antileishmanial activities of extracts and compounds isolated from M. guianensis. METHODS Maytenus guianensis stems and leaves were extracted in acetone, followed by the preparation of eluates and isolation of secondary metabolites using chromatography on a glass column with silica gel as the fixed phase. The chemical components were identified using spectroscopic methods, including one- and two-dimensional nuclear magnetic resonance of hydrogen-1 and carbon-13, mass spectroscopy, and infrared spectroscopy. The anti-Leishmania amazonensis activities of these eluates and compounds were evaluated by direct promastigote counting and viability assays. RESULTS It was found that the hexane bark eluate produced the strongest anti-L. amazonensis effect, with 90-100% inhibition of the promastigote form. The isolated metabolite that produced the best result was tingenone B, followed by a compound formed by the union of tingenone and tingenone B (80-90% inhibition). CONCLUSIONS Maytenus guianensis shows anti-parasite activity that warrants further investigation to determine the mechanisms underlying this antileishmanial effect and to evaluate the pharmacological potential of these eluates and isolated secondary metabolites, while minimizing any adverse effects.
Subject(s)
Leishmania braziliensis/drug effects , Plant Extracts/pharmacology , Maytenus/chemistry , Antiprotozoal Agents/pharmacology , Parasitic Sensitivity Tests , Antiprotozoal Agents/isolation & purificationABSTRACT
A preocupação em buscar novos fármacos para o tratamento da leishmaniose é cada vez maior em virtude da toxicidade dos existentes e do aumento da resistência do parasito, o que representa uma ameaça ao controle da doença. O presente estudo apresenta uma revisão bibliográfica sobre as plantas da Amazônia brasileira com potencial atividade leishmanicida in vitro. Constatouse uma grande diversidade de espécies vegetais da Amazônia brasileira com potencial para a investigação de novos fitoterápicos e metabólitos secundários com ação leishmanicida, além do tratamento de outras parasitoses negligenciadas. A presente revisão demonstrou que as espécies dos gêneros Casearia, Croton e Physalis são fortes candidatas para busca de novos fármacos, visto que apresentaram um IC50 menor que 1µg/mL em testes in vitro contra as formas promastigotas ou amastigotas de Leishmania spp. Ressalta-se a importância de estudos futuros sobre espécies que apresentem metabólitos terpenoides ou esteroides em virtude do potencial leishmanicida que têm demonstrado.
Subject(s)
Leishmaniasis , Ethnopharmacology , Drug TherapyABSTRACT
The preoccupation to find new drugs for the treatment of malaria is increasing steadily due to the resistance of the parasite, which is a threat to disease control, The present study describes a literature review on the antimalarial ethnopharmacology (Anti-Plasmodium falciparum - in vitro) of the Brazilian Amazon plants, It was found a great diversity of plant species in the Brazilian Amazon with potential for research of new herbal and secondary metabolites with antiplasmodial action, in addition to treating other neglected parasitic diseases, However, for these studies is needed in addition to financial support, the interaction between different laboratories and research groups for the formation of multidisciplinary and interdisciplinary teams, which will enhance the research level in the region and increase the likelihood of new antimalarial drugs discovery...
Está cada vez maior a necessidade em se buscar novos fármacos para o tratamento da malária, principalmente devido à resistência do parasito, o que é uma ameaça ao controle da doença. O presente estudo descreve uma revisão bibliográfica sobre a etnofarmacologia antimalárica (Anti-Plasmodium falciparum - in vitro) de plantas da Amazônia brasileira. Constatou-se uma grande diversidade de espécies vegetais na Amazônia brasileira com potencial para a investigação de novos fitoterápicos e metabólitos secundários com ação antiplasmodial, além do tratamento de outras parasitoses negligenciadas. Porém, para a realização desses estudos são necessários além de apoio financeiro, a interação entre diferentes laboratórios e grupos de pesquisa para a formação de equipes multidisciplinares e interdisciplinares, o que irá potencializar o nível da pesquisa na região e aumentar a probabilidade de descoberta de novos fármacos antimaláricos...
Subject(s)
Humans , Antimalarials/pharmacology , Ethnopharmacology/trends , Malaria, Falciparum/drug therapy , Brazil , Drug ResistanceABSTRACT
Abstract The species Maytenus guyanensis Klotzsch ex Reissek, Celastraceae, present a wide variety of possible pharmacological activities and its roots and stems are used by popular medicine in the western Amazon rainforest. Few studies have demonstrated the genotoxic safety of the popular use of this species, and owing to this, the present study aimed to perform an analysis of the acute genotoxicity in vivo of the aqueous extract of M. guyanensis. Male and female mice from Mus musculus species, of weights ranging from 20 to 40 g, organized in eight groups with different treatments were used. The aqueous extracts of the bark of M. guyanensis were administered orally by gavage with 0.1 ml of the test substance per 10 g of the animal, followed by performance of comet assay in peripheral blood, PCE/NCE correlation and occurrence of micronuclei in the bone marrow. It was found that the aqueous extract of M. guyanensis, with ten times higher concentration than those used in ethnopharmacology, did not present genotoxic effect and, moreover, it has antigenotoxic action in mice treated acutely. Further studies regarding bioaccumulation and chronic effects of this species are suggested, in order to improve the understanding of its mechanism of action, ensuring the efficacy and safety of its utilization and developing phytotherapics and drugs.
ABSTRACT
Copaifera spp. is a common tree species found in the tropical region of Latin America, popularly known as copaiba or pau-d'alho. Oil-resin from different Copaifera species and its components present several biological activities such as antimicrobial, anti-inflammatory, antioxidant and insecticidal, including larvicidal activity against mosquitoes. Thus, bark and leaf ethanolic extracts, oil-resin, essential oil and alepterolic acid from Copaifera multijuga Hayne, Fabaceae, were tested as larvicides against the main malaria vector in the north of Brazil, Anopheles darlingi and also Aedes aegypti, the dengue vector. A. darlingi larval mortality was significantly higher than A. aegypti for most tested compounds. Bark and leaf extracts resulted in lower Lethal Concentrations (LC50) values for A. darlingi, 3 and 13 ppm, respectively, while the essential oil provided the lowest LC50 value for A. aegypti, 18 ppm. Despite of that, the lowest LC values were from the alepterolic acid for both species, i.e. 0.9 and 0.7 ppm for A. darlingi and A. aegypti, respectively.
ABSTRACT
Este trabalho relata o estudo químico de duas plantas medicinais da Amazônia: Philodendron scabrum K. krause (Araceae) e Vatairea guianensis Aubl. (Fabaceae). As composições dos óleos essenciais dos cipós de P. scabrum e dos frutos de V. guianensis, respectivamente, foram analisadas em CG-DIC e CG-EM. Os constituintes majoritários dos cipós de P. scabrum foram óxido de cariofileno (19,42%), α-copaeno (16,08%) e ß-bisaboleno (10,01%); e nos frutos de V. guianensis foram o ácido (9Z)-octadecenoico (24,95%) e o ácido docosahexaenoico (24,17%). ß-sitosterol e o alquilresorcinol 1-hexadecanoil-2,6-dihidroxibenzeno foram isolados do extrato etanólico dos cipós de P. scabrum; e do extrato etanólico dos frutos de V. guianensis, foram isoladas as antraquinonas crisofanol e fisciona. As determinações estruturais foram baseadas em dados de RMN de ¹H e 13C. RMN, uni e bidimensional e comparação com dados da literatura.
This work describes the chemical study of two medicinal plants of the Amazon Philodendron scabrum K. Krause (Araceae) and Vatairea guianensis Aubl. (Fabaceae). Essential oils composition from stems of Philodendron scabrum K. Krause (Araceae) and fruits of Vatairea guianensis Aubl. (Fabaceae), respectively were analyzed in GC-FID and GC-MS. The major constituents from stems of P. scarabum were caryophyllene oxide (22.42%), α-copaene (16.08%) and ß-bisabolene (12.01%) and from fruits of V. guianensis were (9Z)-octadecenoic acid (24.95%) and docosahexenoic acid (24.17%). ß-sitosterol and alkylresorcinol 1-hexadecanoyl-2,6-dihydroxybenzene were isolated from ethanolic extracts from stems of P. scabrum and from ethanolic extracts from fruits of V. guianensis, the athraquinones chrysophanol and physcion were isolated. The structure of isolated compounds we determinate wered based on data from ¹H and 13C NMR, including two dimensional analyses and comparison with literature data.
Subject(s)
Ointment Bases , Anthraquinones , PhilodendronABSTRACT
Os óleos essenciais dos frutos e talos finos de Piper tuberculatum e das raízes de P. hispidum, coletados no estado de Rondônia, foram obtidos por hidrodestilação e analisados por GC e GC-MS. Foram identificados como constituintes majoritários, nos óleos dos frutos e talos finos de P. tuberculatum, o óxido de cariofileno (32,1 por cento) e (26,6 por cento) e o (E)-cariofileno (17,7 por cento) e (12,3 por cento), respectivamente. No óleo essencial das raízes de P. hispidum, foram identificados, como constituintes majoritários, o dilapiol (57,5 por cento), a elemicina (24,5 por cento) e o apiol (10,2 por cento). Do extrato etanólico dos frutos de P. tuberculatum, foram isolados os esteróides β-sitosterol e estigmasterol, as amidas piplartina e dihidropiplartina e um derivado do ácido cinâmico, o ácido 3,4,5-trimetoxi-dihidrocinâmico.
The essential oils of the fruits and fine stems of Piper tuberculatum and of the roots of P. hispidum, collected in the state of Rondônia, had been gotten by hydrodistillation and analyzed by GC and GC-MS. Caryophyllene oxide - 32,1 percent in fruits and 26,6 percent in fine stem, and (E)-caryophyllene - 17,7 percent in fruits and 12,3 percent in fine stems, were identified as the major constituents in such parts of P. tuberculatum. In the essential oil of the roots of P. hispidum, dillapiol (57,5 percent), elemicine (24,5 percent) and apiole (10,2 percent) were identified as the most abundant constituents. From the ethanolic extract of the fruits of P. tuberculatum, the steroids β-sitosterol and stigmasterol, the amides piplartine and dihidropiplartine and the derivative of the cinâmico acid 3,4,5-trimethoxy-dihidrocinâmic acid were isolated.