In vitro activity of Amazon plant extracts against Enterococcus faecalis

Previous studies analyzing 2,200 plant extracts indicated anti-enterococcal activity in 25 extracts obtained from Brazilian forests' plants. In the present study, these extracts were subjected to microdilution broth assay (MDBA) and disk diffusion assay (DDA) using planktonic Enterococcus faecalis ATCC® 29212TM and were submitted to phytochemical analysis in TLC and HPLC. Three extracts obtained from Ipomoea alba (MIC < 40 µg/mL), Diclinanona calycina (MIC < 40 µg/mL) and Moronobea coccinea (40 < MIC < 80 µg/mL; MBC = 80 µg/mL) showed significant bactericidal activity in the MDBA and four extracts obtained from I. alba (14.04 ± 0.55 mm diameter) S. globulifera (14.43 ± 0.33 mm and 12.18 ± 0.28 mm diameter) and Connarus ruber var. ruber (13.13 ± 0.18 mm diameter) were active in DDA. Residues H2O obtained from Psidium densicomum (mean of 16.78 mm diameter) and from Stryphnodendron pulcherrimum (mean of 15.97 mm diameter) have shown an improved antibacterial activity after fractionation if compared to that obtained from the respective crude extracts. Antioxidant activity was observed in some residues of the active extracts. TLC analysis showed that phenolic compounds are likely to be found in active extracts. Three molecules were isolated from S. globulifera and were identified by 13C NMR lupeol, α-amyrin and 3β-hydroxyglutin-5-ene. The present chemical and biological findings suggest that these extracts are a potential source of new anti-Enterococcus compounds to be introduced in endodontic therapy.

Avaliação da atividade anti-helmíntica de extratos brutos de plantas da Floresta Amazônica e Mata Atlântica brasileira sobre Haemonchus contortus / Evaluation of the anti-helminthic activity of crude extracts from the Brazilian Amazon and Mata Atlântica plants against Haemonchus contortus

No mundo todo, as verminoses são causa de considerável prejuízo econômico na criação de ovinos. As perdas estão relacionadas ao retardo na produção, custos com tratamentos profiláticos e, em casos extremos, à morte dos animais. O objetivo deste trabalho foi verificar a ação anti-helmíntica de extratos vegetais sobre nematoides como alternativa terapêutica no tratamento da verminose em ovinos. Extratos orgânicos e aquosos foram obtidos de plantas nativas da Floresta Amazônica e Mata Atlântica, e foram testados na concentração de 100µg/mL em ensaios de toxicidade in vitro contra ovos de Haemonchus contortus e de 200µg/mL contra suas larvas. Na concentração estabelecida, apresentaram significante atividade relacionada à inibição de eclosão de ovos; em particular, o extrato orgânico de folhas e frutos de Trichilia sp. e o extrato aquoso dos órgãos aéreos de Phyllanthus attenuatus. Os resultados in vitro sugerem que extratos aquosos e orgânicos dessas plantas podem oferecer novas alternativas de controle da verminose em ovinos a partir de produtos naturais...

Helminthosis play a crucial role in small ruminant production leading to enormous economic losses particularly in areas where extensive grazing is practiced. It causes a loss of production through mortality, weight loss, reduced milk and wool production. Haemonchus contortus is a highly pathogenic small ruminant helminthes parasite, which is capable of causing acute diseases and high mortality. Therefore, there is an urgent need to seek alternative or complementary solutions to the control of parasitic nematodes of ruminants. The tropical forests concentrate the highest biodiversity in the world, particularly those located in Brazil, whose species richness is estimated to account for 20% of the total world richness and little is known about the chemical and pharmacological potentialities of Brazilian tropical forests. In this work, organic and aqueous extracts were tested on eggs and in the larval development test on Haemonchus contortus. The organic extract obtained from leaves and fruits of Trichilia sp. and the aqueous extract obtained from the aerial organs of Phyllanthus attenuates showed significant activity related to the inhibition of H. contortus egg eclosion. In vitro results suggest that both extracts, as well as eleven other active extracts, can offer alternatives in sheep worm control...

Influence of the intraperitoneal administration of antitumor Abarema auriculata extract on mice behavior

The organic extract EB689, obtained from the stem of Abarema auriculata (Benth.) Barneby & J.W.Grimes, Fabaceae, commonly known as "saboeiro-ferro", was chemically studied, as well as its influence over behavioral effects such as locomotion, emotionality and anxiety, after intra-peritonial administration were assessed. The open-field and elevated-plus maze were used in experiments divided into two stages. The first stage aimed for the identification of the main effects over behavior using a reduced number of animals against half-fold diluted doses of EB689. The same variables were also tested in a second stage of the experiment using the non-lethal intra-peritoneal dose of 4.8 mg/kg in a larger number of animals. It was observed that EB689 clearly decreased locomotion, which was probably caused by internal hemorrhage causing hypovolemic shock. Although it is the first time lupeol and eucryphin are described in A. auriculata, it is still not clear if they are involved in the toxicology of A. auriculata. The undesirable effects of EB689 are better understood, the basis for further pharmacological assays aiming antitumor activity are supported.

Coleoptera associated with pig carcass exposed in a forest reserve, Manaus, Amazonas, Brazil / Coleoptera associados a carcaça de porco em reserva florestal, Manaus, Amazonas, Brasil

The Coleoptera fauna of forensic importance associated with Sus scrofa Linnaeus, 1758 carcass decomposition in Ducke Reserve, Manaus, Brazil, was determined. A total of 41 species, belonging to six families and 11 subfamilies were collected. Staphylinidae presented the higher richness with 17 species sampled, followed by Histeridae, with 11 and Scarabaeidae with nine species. Euspilotus azureus (Sahlberg, 1823) (Histeridae), Aleochara sp. (Staphylinidae) and Oxelytrum cayennense (Stürm, 1826) (Silphidae) occurred in all stages of decomposition. Omalodes lucidus Erichson, 1824 and Scapomegas auritus Marseul, 1855 (Histeridae) are recorded for the first time in the Amazon, being also reported for the first time associated with a decomposing carcass. The fauna differs from those of other Brazilian regions, emphasizing the importance of studies to determine the regional insect fauna of forensic importance that can be used in criminal investigations.

A fauna de Coleoptera de importância forense foi analisada na Reserva Ducke, Manaus, Brasil, durante a decomposição de carcaça de Sus scrofa Linnaeus, 1758. Foram coletadas 41 espécies, pertencentes a seis famílias e 11 subfamílias. Staphylinidae apresentou a maior riqueza com 17 espécies, seguida por Histeridae, com 11 e Scarabaeidae com nove espécies. Euspilotus azureus (Sahlberg, 1823) (Histeridae), Aleochara sp. (Staphylinidae) e Oxelytrum cayennense (Stürm, 1826) (Silphidae) ocorreram em todos os estágios de decomposição. Omalodes lucidus Erichson, 1824 e Scapomegas auritus Marseul, 1855 (Histeridae) são registrados pela primeira vez na Amazônia, sendo também a primeira amostragem na qual essas espécies são encontradas em carcaça em decomposição. A fauna difere das de outras regiões do Brasil, ressaltando a importância de estudos regionais para posterior utilização como provas forenses.

Concentração inibitória mínima e concentração bactericida mínima de três extratos vegetais antibacterianos selecionados da Floresta Amazônica e da Mata Atlântica brasileiras / Minimal inhibitory concentration and minimal bactericidal concentration results from three selected antibacterial plant extracts from the Amazon and Atlantic Brazilian rain forests

Introdução - Em trabalho prévio, 705 extratos vegetais oriundos de plantas amazônicas e da Mata Atlântica foram triados no teste antibacteriano da microdiluição em caldo. No presente trabalho, os extratos ativos foram identificados e submetidos à avaliação da concentração mínima inibitória e da concentração bactericida mínima usando o mesmo modelo experimental. Material e Métodos - Foi utilizado o ensaio da microdiluição em caldo, que consiste em se avaliar a susceptibilidade das bactérias aos extratos vegetais em meio ágar caldo, em microplacas de 96 poços. Resultados = Os extratos orgânicos obtidos de Rapanea parvifolia (MY841), Smilax rufescens (SM53) e Ruizterania retusa (VO581) mostraram atividade antibacteriana. MY841 e SM53 mostraram atividade contra Enterococcus faecalis CIM = 30 ?g/ml; CBM = 60 ?g/ml e CIM = 80 ?g/ml; CBM = 90 ?g/ml, respectivamente) e VO581 mostrou atividade contra Staphylococcusaureus (CIM = 140 ?g/ml; CBM = 160 ?g/ml) e leve atividade contra Pseudomonas aeruginosa (CIM = 200 ?g/ml; CBM = 380 ?g/ml). Conclusões - Estes três extratos apresentaram atividade importante contra as bactérias testadas, devendo, portanto, ser fracionados e os compostos majoritários avaliados.

Introduction - Up to 705 plant extracts from Amazon Rain Forest and Atlantic Rain Forest were screened against bacteria using the microdilution broth assay. In the present work, minimal inhibitory concentration and minimal bactericidal concentration were obtained from the three selected active extracts. Material and Methods - The microdilution broth assay used in the present analysis consists in evaluating small amounts of extract against the bacteria in agar broth medium in 96 well microplates. Results - Three organic extracts obtained from Rapanea parvifolia (MY841), Smilax rufescens (SM53) and Ruizterania retusa (VO581) showed antibacterial activity. MY841 and SM53 showed activity against Enterococcus faecalis MIC = 30 mg/ml; MBC = 60 mg/ml and MIC = 80 mg/ml; MBC = 90 mg/ml, respectively) and VO581 showed activity against Staphylococcus aureus (MIC = 140 mg/ml; MBC = 160 mg/ml) and a mild activity against Pseudomonas aeruginosa (MIC = 200 mg/ml; MBC = 380 mg/ml). Conclusions - The three extracts showed important activity against the bacteria, and they are going to be fractionated and the fractions evaluated against the antibacterial model. The major compounds are going to be isolated as well.

Discovery of new antitumoral and antibacterial drugs from brazilian plant extracts using high throughput screening: [review]

Plants have played a significant role in the treatment of cancer and infectious diseases for the last four decades. The discovery and introduction to market of paclitaxel, the vinca alkaloids, etoposide, and many antibacterial drugs support drug discovery programs based on natural products. Natural products have been rediscovered as important tools for drug development despite advances in combinatorial chemistry, due to the complex molecular structures able to interact with mammalian cell targets. The Brazilian flora, the most diverse in the world, has become an interesting spot to prospect for new chemical leads or hits due to its species diversity and associated chemical richness. Screening programs have been established in Brazil as a strategy to identify potentially active substances. High throughput screening techniques allow for the analysis of large numbers of extracts in a relatively short period of time, and can be considered one of the most efficient ways of finding new leads from natural products. An updated review of the current status of the biological screening program is presented and recent results from new antitumoral and antibacterial chemical leads are discussed.

Plantas são uma importante fonte de novos protótipos há pelo menos quatro décadas. A descoberta e introdução no mercado de paclitaxel, dos alcalóides da vinca, etoposídeo e muitos agentes antibacterianos têm servido de apoio ao desenvolvimento de programas de descobrimento de novos fármacos baseados em produtos naturais. Produtos naturais foram recentemente redescobertos como importante ferramenta na descoberta de novos fármacos devido às estruturas moleculares complexas capazes de interagir com alvos em células de mamíferos. A flora brasileira, a mais rica do mundo, tornou-se um importante sítio para prospecção de novos protótipos em decorrência da riqueza de espécies vegetais relacionada a uma possível diversidade química. Programas de triagem têm sido introduzidos no Brasil contrapondo a devastação de florestas relacionadas a atividades rurais, extrativismo madeireiro e mineral. Ensaios em larga escala permitem a análise de um grande número de amostras em um tempo relativamente pequeno, e pode ser considerado como o método mais eficaz para a descoberta de novos fármacos a partir de plantas. Dados atualizados relativos a programas de triagem que objetivam a identificação de novos protótipos antitumorais e antibacterianos são comentados.

Occurrence, body mass and biomass of Syntermes spp. (Isoptera: Termitidae) in Reserva Ducke, Central Amazonia

The leaf-feeding species Syntermes molestus and S. spinosus are two dominant termite species in Reserva Ducke in Central Amazonia; two other species (S. aculeosus, S. longiceps) exist in the area. All species except S. aculeosus were also found in urban areas. The workers of S. molestus and S. spinosus have average body dry weights of 4.5±0.2 and 13.1±1.4 mg, and the weight of their soldiers is 8.2±0.2 and 51.0±1.7 mg, respectively. Therefore, S. spinosus is among the largest termites of the world. In both species, fresh weight is about 4.7 higher than dry weight (a wider relation than in other termite species). The biomass of the populations of both species amounted to about 1 g m-2 (dry weight; indirect estimate), which rises previous assessments of the total termite biomass by about 36-45%, to a value of 3.0-3.5 g m-2.

As espécies comedoras de folhas Syntermes molestus and S. spinosus são duas espécies de cupins dominantes na Reserva Ducke na Amazônia Central; duas outras espécies (S. aculeosus, S. longiceps) existem na área. Todas as espécies (exceto S. aculeosus) são encontradas também em áreas urbanas. O peso seco médio do corpo dos operários de S. molestus e S. spinosus é de 4,5±0,2 e 13,1±1,4 mg, e dos soldados é de 8,2±0,2 and 51,0±1,7 mg, respectivamente. Por isto, S. spinosus está entre os maiores cupins do mundo. Em ambas espécies, o peso fresco é cerca de 4,7 vezes mais alto que o peso seco (uma proporção maior que em outras espécies de cupins). A biomassa das populações de ambas espécies foi avaliada em cerca de 1 g m-2 (peso seco; estimativa indireta), o que eleva estimativas anteriores da biomassa total de térmitas em cerca de 36-45%, a um valor de 3,0-3,5 g m-2.