Anti-herpes activity of the total alkaloid fraction from the branches of Fusaea longifolia (Annonaceae) / Atividade anti-herpes da fração total de alcaloides dos ramos da Fusaea longifolia (Annonaceae)

The herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) occur worldwide. Infections caused by these viruses have great public health importance due to the growing resistance to the first-choice drug, acyclovir, especially in immunosuppressed patients. Alkaloids derived from species of Annonaceae have been reported as antiviral agents against HSV and others viruses. Within this context, we evaluated the antiviral activity of the total alkaloid fraction (TAF) extracted from the branches of Fusaea longifolia (Aubl.) Saff. (Annonaceae), a species native to the Amazon region, against the HSV-1 and HSV-2 viruses. The antiviral activity was evaluated through the plate reduction assay and the mode of action was investigated by a set of other assays. The TAF was active against the HSV-2 strain 333 and against the HSV-1 strains KOS and 29R (acyclovir resistant), with selectivity index values (SI = 50% cytotoxic concentration/50% effective concentration) of 5, 4 and 3, respectively. In the preliminary study of the anti-HSV-2 mode of action, TAF showed viral inhibitory effects if added up to 12 h post-infection, had virucidal activity and did not present viral inhibition in pre-treatment. Our results showed that the TAF exhibited anti-HSV activity. Regarding HSV-2, TAF acted after the viral infection and had virucidal activity. A mass spectrometry analysis revealed the presence of nine alkaloids in the TAF that had previously been reported for Annonaceae, including liriodenine, lysicamine and isoboldine, which have been described as potential anti-HSV-1 agents.(AU)

Os vírus herpes simplex tipo 1 (HSV-1) e tipo 2 (HSV-2) têm ampla ocorrência global. As infecções causadas por esses vírus têm grande importância em saúde pública devido à crescente resistência ao fármaco de primeira linha, aciclovir, principalmente em pacientes imunossuprimidos. Alcaloides derivados de espécies de Annonaceae têm sido relatados como agentes antivirais contra o HSV e outros vírus. Neste contexto, nós avaliamos a atividade antiviral da fração alcaloide total (TAF) dos ramos de Fusaea longifolia (Aubl.) Saff. (Annonaceae), uma espécie nativa da região amazônica, contra os vírus HSV-1 e HSV-2. A atividade antiviral foi avaliada através do ensaio de redução em placa e o modo de ação foi investigado por um conjunto de ensaios. O TAF foi ativo contra a cepa HSV-2 333 e contra as cepas HSV-1 KOS e 29R (resistente ao aciclovir), com valores de índice de seletividade (IS = 50% concentração citotóxica/50% concentração efetiva) de 5, 4 e 3, respectivamente. No estudo preliminar do modo de ação da atividade anti-HSV-2, o TAF inibiu a replicação viral quando adicionados até 12 h pós-infecção, apresentou atividade virucida e não apresentou inibição viral no pré-tratamento. Nossos resultados mostraram que o TAF exibiu atividade anti-HSV. Em relação ao HSV-2, o TAF atuou após a infecção viral e apresentou atividade virucida. Uma análise do TAF por espectrometria de massas identificou a presença de nove alcaloides, incluindo liriodenina, lisicamina e isoboldina, que já foram descritos como potenciais agentes anti-HSV-1.(AU)

Performance, carcass characteristics, and health parameters of growing and finishing pigs fed with diets supplemented with isoquinoline alkaloids and essential oils / Desempenho zootécnico, características de carcaça e parâmetros de saúde de suínos em crescimento e terminação submetidos a dietas suplementadas com alcaloides isoquinolínicos e óleos essenciais

The goal of this study was to evaluate, in a commercial herd, the use of isoquinoline alkaloids and carvacrol versus a preventive antibiotic program, such as feed additives, on the performance, carcass traits, and health status of pigs in the growing and finishing phase. There were 576 PIC immunocastrated males and females, at 70 days of age and 28.429 ± 2.302 kg of initial weight used. The experimental design was a 4 × 2 factorial randomized block, with four preventive programs, two sexes, and six repetitions per treatment (the pen with 12 animals of the same sex was the replicate). The treatments were T1 (positive control program with antibiotic shocks at preventive level), T2 (negative control with the absence of antibiotics as a growth promoter or as preventive), T3 (isoquinoline alkaloids at 100 to 150 g ton-1), T4 (isoquinoline alkaloids at 90 g ton-1 + carvacrol essential oil at 1 kg ton-1). T1 and T3 presented higher daily feed intakes, followed by T2, and T4 showed the worst feed consumption (P < 0.05). T1 showed higher daily weight gain compared to T4 (P < 0.05), without differences between T2 and T3. T2 showed better feed conversion than T1 and T3, but it was similar to T4. There were no effects of the treatments on the carcass traits. Intestinal crypt hyperplasia and crypt abscesses (lesions caused by Lawsonia intracellularis) were significantly higher for T2 and T3 compared to T1, which was similar to T4. T2 presented the highest carcass condemnation at slaughter (7%), differing (P < 0.05) from T1, T3, and T4 (1, 2, and 3%, respectively). Isoquinoline alkaloids are an alternative for antibiotic-free diets for pigs in the growing and finishing phase, preserving the performance and carcass indices and minimizing sanitary carcass condemnations at the slaughterhouse.(AU)

O objetivo deste trabalho foi avaliar, em um rebanho comercial, o uso de alcalóides isoquinolínicos e do carvacrol frente a um programa preventivo com antibióticos, como aditivos alimentares, sobre o desempenho zootécnico, características de carcaça e o status de saúde de suínos em fase de recria e terminação. Foram utilizados 576 suínos PIC, machos imunocastrados e fêmeas, com 70 dias de idade e 28.429 ± 2.302 kg de peso médio inicial. O delineamento experimental foi em blocos casualizados, modelo fatorial 4 x 2, com quatro programas preventivos e dois sexos e 6 repetições por tratamento (baia com 12 animais do mesmo sexo representou a unidade experimental). Os tratamentos foram: T1 - Controle Positivo (programa com choque antibiótico em nível preventivo), T2 - Controle Negativo (ausência de aditivos promotores de crescimento ou preventivos), T3 - Alcalóides isoquinolínicos (100 a 150 g ton-1), T4 - Alcalóides isoquinolínicos (90 g ton-1) + Óleo essencial - carvacrol (1 kg ton-1). T1 e T3 apresentaram maior consumo diário de ração, seguidos de T2, sendo que T4 apresentou o pior consumo (P < 0,05). O ganho de peso diário foi maior para T1 em relação a T4 (P < 0,05), não sendo verificada diferença entre T1 versus T2 e T3. T2 apresentou melhor conversão alimentar que T1 e T3, não diferindo de T4. Não houve efeito dos tratamentos para as características da carcaça. A hiperplasia e o abscesso das criptas intestinais (lesões causadas pela Lawsonia Intracellularis) foram significativamente superiores para T2 e T3 comparado com T1, que foi semelhante a T4. T2 apresentou maiores condenações de carcaça ao abate (7%), diferindo (P < 0,05) de T1, T3 e T4, respectivamente, 1, 2 e 3%. Os alcaloides isoquinolínicos são uma alternativa para dietas isentas de antibióticos para suínos em fase de crescimento e terminação, preservando o desempenho e os índices de carcaça e minimizando as condenações sanitárias de carcaças no frigorífico.(AU)

Phytochemical profile and antifungal action of Anadenanthera colubrina extract on the quality of maize seeds

Maize (Zea mays L.) is among the most cultivated crops in the world and can be affected by several diseases, especially those transmitted by seeds. The study of alternatives to fungicides used for seed treatment has a promising field in essential oils. Thus, this study determined the phytochemical profile of the ethanolic extract from Anadenanthera colubrina (Vell.) Brenan and to evaluate its antifungal activity on the sanitary and physiological quality of maize seeds. The seeds used were of the Jaboatão cultivar, which were submitted to the following treatments: control (untreated seeds), commercial fungicide (dicarboximide) and A. colubrina extract at 200, 400, 600, 800, and 1,000 ppm. The seeds were subjected to sanitary and germination tests in a completely randomized experimental design. Phytochemical prospecting of A. colubrina extract indicated the presence of alkaloids, tannins, flavonoids and saponins, as well as the major compounds lupeol, gallic acid, ferulic acid, catechin and quercetin. The A. colubrina extract reduced the incidence of Aspergillus spp., including Aspergillus niger, Alternaria spp., Curvularia spp. and Fusarium spp. at all concentrations. The highest concentrations (800 and 1,000 ppm) of the A. colubrina extract reduced the incidence of Penicillium spp. and yielded an effective control of Rhizoctonia spp. The extract of A. colubrina did not present phytotoxic effect, guaranteeing the viability and vigor of maize seeds.

Isoquinolone alkaloids mitigate microscopic digestive tract lesions induced by sub-acute ruminal acidosis (SARA) in feedlot cattle / Alcaloides isoquinolínicos atenuam lesões microscópicas digestivas induzidas por acidose ruminal subaguda em bovinos confinados

Feedlot cattle is submitted to a diet rich in energy and reduced in fibres that induces the sub-acute ruminal acidosis (SARA) with its lesions and clinical signs. Recent studies have demonstrated some amelioration of this condition by the use of isoquinolone alkaloids found in Macleaya cordata (Papaveraceae) such as Sanguinarine and Chelerythrine. These compounds have demonstrated antimicrobial, antiinflammatory and immune-modulatory effects in both humans and animals The aim on this study, using histopathology and a score system, was to evaluate the differences between a non-treated and a treated group feed with these alkaloids, present in trade preparation Sangrovit-RS® as a source of sanguinarine (SG), chelerythrine (CH) and protropine (PA) standardized to 0.15% w/w SG, using feedlot cattle under a high-grain diet as an inflammatory model for gastrointestinal system. The samples of forestomachs were evaluated and graded using scores ranging from zero (0) to three (3) obtained at light-microscopic fields of 400X. Parameters such as inflammation, hydropic degeneration, hyperkeratosis, and vesicle formation were accessed in the different layers of the tissues, considering the severity and dispersion of the microscopic lesions. The soft tissues such as the abomasum, small intestine, cecum and colon had their total amount of inflammatory cells counted at light-microscopic fields of 200X. The rumen of the SG-CH-PRO-treated group showed a significant reduction in the epithelial hydropic degeneration scores (p ≤ 0.001) and lamina propria inflammation (p ≤ 0.001).The reticulum had a similar reduction in scores of epithelial (p ≤ 0.002) and stratum corneum hydropic degeneration (p ≤ 0.001), hyperkeratosis (p ≤ 0.002) and inflammation in lamina propria (p ≤ 0.001) and epithelium (p ≤ 0.002). The omasum had no significant differences. All non-keratinized tissues, except for ileum, had a significant decrease (p ≤ 0.001) in the total counting of inflammatory cells. In this trial, the feedlot cattle feed with high grain diet and treated with isoquinolone alkaloids expressed lesions that indicate ameliorations and worsening's. Ameliorating effects of the alkaloids were better demonstrated in tissues with reduced or no corneal layer in the mucosa and in the absence of a lipopolysaccharides rich acidic environment reinforcing the notion of the topic action, the dependence of the media pH and the time of exposure modulating the pharmacological mechanisms of these alkaloids. The observed cytolytic (oncolysis) effect in epithelial forestomachs cells under low pH values, worsening the osmotic status, should be considered before clinical applications.(AU)

As dietas para bovinos confinados possuem alta quantidade de alimentos energéticos com menor quantidade de alimentos volumosos (fibras), favorecendo a indução de acidose ruminal subaguda com formação de lesões gastrointestinais e sintomas clínicos deletérios. Recentes trabalhos têm demonstrado alguma amenização desta condição pelo uso de alcaloides isoquinolínicos encontrados na Macleaya cordata (Papaveraceae) tais como a sanguinarina e a cheleretrina, os quais tem demonstrado efeitos anti-inflamatórios, antimicrobianos e imuno modulatórios em humanos e animais. O objetivo deste estudo foi, através da histopatologia e de um sistema de escores, avaliar as diferenças entre um grupo não tratado e um grupo tratado com alcaloides isoquinolínicos, presentes na formulação Sangrovit RS® como fonte de sanguinarina (SG), chelerethrina (CH) and protropina (PA) padronizadas em 0,15 % w/w SG, usando bovinos em confinamento recebendo uma dieta rica em grãos como modelo inflamatório para o sistema gastrointestinal. Amostras dos pré-estômagos foram avaliadas por escores variando de zero a três, obtidos por microscopia de luz em diferentes campos em aumentos de 400X. Inflamação, degeneração hidrópica, hiperqueratose e formação de vesículas foram avaliadas nas diferentes camadas dos pré-estômagos tendo em vista a intensidade e a extensão das lesões. Tecidos não queratinizados como abomaso e intestino delgado, ceco e cólon tiveram seu total de células inflamatórias contadas por microscopia de luz em diferentes campos com aumentos de 200X. No rumem do grupo tratado houve uma redução significante no número de campos contendo degeneração hidrópica epitelial (p ≤ 0,001) e inflamação de lâmina própria (p ≤ 0,001). O retículo teve uma redução similar nos escores scores de degeneração hidrópica epitelial (p ≤ 0.002), degeneração hidrópica no estrato córneo (p ≤ 0.001), hiperqueratose (p ≤ 0.002) e inflamação na lamina própria (p ≤ 0.001) e inflamação epitelial (p ≤ 0.002). Não foram encontradas diferenças significantes no omaso. Todos os tecidos não queratinizados, exceto pelo íleo, tiveram uma redução significativa (p ≤ 0.001) no total de células inflamatórias. Neste experimento, bovinos em confinamento recebendo dieta rica em grãos e tratados com alcaloides isoquinolínicos tiveram lesões que tiveram melhoras e pioras. Os efeitos de melhora foram melhor demonstrados em tecidos sem camada córnea e na ausência de um meio ácido rico em lipopolisacarídeos, reforçando a noção da ação tópica, da dependência do pH do meio e do tempo de exposição modulando os mecanismos farmacológicos destes alcalóides. O efeito citolítico (oncólise) sobre células epiteliais de pré-estômagos em baixos valores de pH, piorando o estado osmótico das células, deveria ser considerado antes das aplicações clínicas.(AU)

Bufotenine, a tryptophan-derived alkaloid, suppresses the symptoms and increases the survival rate of rabies-infected mice: the development of a pharmacological approach for rabies treatment

Between 40,000-70,000 people die yearly of rabies, an incurable disease. Besides post-bite vaccination, no treatment is available for it. Methods: First, virus dilution for antiviral effects in mice was determined. Then, animals were treated as follows: control (NaCl 250 µL/animal/day); bufotenine (0.63, 1.05 and 2.1 mg in 250 µL of NaCl/animal/day); rabies (10-6,82CVS dilution); and test (10-6,82 CVS dilution and bufotenine, in the above-mentioned doses). Animals were observed daily for 21 days or until the 3rd stage of rabies infection. Twitch-tension and liposome studies were applied to understand the possible interaction of bufotenine with receptors, particularly acetylcholine. Results: Bufotenine was able to increase the survival rate of intracerebrally virus-infected mice from 15 to 40%. Bufotenine did not seem to interfere with the acetylcholine response in the skeletal muscle, indicating that its mechanism of action is not blocking the virus entrance due to nAChR antagonism. By analyzing liposomes, we could observe that bufotenine did not passively penetrates cell membranes, indicating the necessity of complementary structures to cell penetration. Conclusions: Bufotenine is a promising candidate for drug development. After further chemical modification, it might be possible to dissociate minor side effects, increase efficiency, efficacy and pharmacokinetics, yielding a true anti-rabies drug.(AU)

Anti-tick effect and cholinesterase inhibition caused by Prosopis juliflora alkaloids: in vitro and in silico studies / Efeito carrapaticida e inibição da acetilcolinesterase por alcaloides de Prosopis juliflora: estudos in vitro e in silico

We investigated the in vitro acaricide activity of the methanolic extract (ME) and alkaloid-rich fraction (AF) of Prosopis juliflora on Rhipicephalus microplus and correlated this effect with acetylcholinesterase (AChE) inhibition. The acaricide activity was evaluated using adult and larval immersion tests. Also, we studied the possible interaction mechanism of the major alkaloids present in this fraction via molecular docking at the active site of R. microplus AChE1 (RmAChE1). Higher reproductive inhibitory activity of the AF was recorded, with effective concentration (EC50) four times lower than that of the ME (31.6 versus 121 mg/mL). The AF caused mortality of tick larvae, with lethal concentration 50% (LC50) of 13.8 mg/mL. Both ME and AF were seen to have anticholinesterase activity on AChE of R. microplus larvae, while AF was more active with half-maximal inhibitory concentration (IC50) of 0.041 mg/mL. The LC-MS/MS analyses on the AF led to identification of three alkaloids: prosopine (1), juliprosinine (2) and juliprosopine (3). The molecular docking studies revealed that these alkaloids had interactions at the active site of the RmAChE1, mainly relating to hydrogen bonds and cation-pi interactions. We concluded that the alkaloids of P. juliflora showed acaricide activity on R. microplus and acted through an anticholinesterase mechanism.(AU)

A atividade carrapaticida in vitro do extrato metanólico (EM) e da fração de alcaloides (FA) de Prosopis juliflora foi investigada, frente ao Rhipicephalus microplus, e relacionada com a inibição da enzima acetilcolinesterase (AChE). A predição in silico das interações de alcaloides dessa fração com a AChE1 de R. microplus (RmAChE1) foi realizada por acoplamento molecular. A atividade carrapaticida foi avaliada, utilizando-se os ensaios de imersão de adultos e larvas. Maior efeito sobre parâmetros reprodutivos de teleóginas foi verificado para a FA, com valor de Concentração Efetiva 50% (CE50) (31.6 mg/mL), quatro vezes menor do que o valor do EM (121 mg/mL). A FA induziu mortalidade de larvas (Concentração Letal de 50% - CL50 = 13,8 mg/mL). A inibição da atividade da AChE de larvas do carrapato foi observada para EM e FA, sendo a FA mais ativa (Concentração Inibitória 50%- CI50 de 0,041mg/mL). As análises químicas da FA permitiram a identificação dos alcaloides prosopina (1), juliprosinina (2) e juliprosopina (3). No ensaio in silico, observou-se que esses alcaloides podem interagir com o sítio ativo da RmAChE1, principalmente por ligações de hidrogênio e interações cátion-pi. Os alcaloides de P. juliflora têm atividade carrapaticida contra R. microplus, atuando através do mecanismo anticolinesterásico.(AU)

Protein identification from the parotoid macrogland secretion of Duttaphrynus melanostictus

Bufonid parotoid macrogland secretion contains several low molecular mass molecules, such as alkaloids and steroids. Nevertheless, its protein content is poorly understood. Herein, we applied a sample preparation methodology that allows the analysis of viscous matrices in order to examine its proteins. Methods: Duttaphrynus melanostictus parotoid macrogland secretion was submitted to ion-exchange batch sample preparation, yielding two fractions: salt-displaced fraction and acid-displaced fraction. Each sample was then fractionated by anionic-exchange chromatography, followed by in-solution proteomic analysis. Results: Forty-two proteins could be identified, such as acyl-CoA-binding protein, alcohol dehydrogenase, calmodulin, galectin and histone. Moreover, de novo analyses yielded 153 peptides, whereas BLAST analyses corroborated some of the proteomic-identified proteins. Furthermore, the de novo peptide analyses indicate the presence of proteins related to apoptosis, cellular structure, catalysis and transport processes. Conclusions: Proper sample preparation allowed the proteomic and de novo identification of different proteins in the D. melanostictus parotoid macrogland secretion. These results may increase the knowledge about the universe of molecules that compose amphibian skin secretion, as well as to understand their biological/physiological role in the granular gland.(AU)

Ipomoea brasiliana poisoning on buck reproduction / Efeitos da intoxicação por Ipomoea brasiliana na reprodução de caprinos

Swainsonine-containing plants comprise a group of important poisonous plants in Brazil. This research aimed to characterize both the behavioral changes related to reproduction and appearance of lesions in the reproductive system of bucks poisoned by Ipomoea brasiliana. I. brasiliana plants were collected and administered at a dose of 4g/kg (800µg swainsonine/kg) to two groups of bucks for 45 days. Goats from Group I were euthanized on the 46th day of the experiment, and goats from Group II were euthanized on the 120th day. Group III was composed of goats that did not receive I. brasiliana and were euthanized on the 120th day of the experiment. Reproductive behavioral changes were observed starting on day 20 and were characterized by an absence of courtship behavior, and Flehmen reflex, decrease or loss of libido and inability to perform mating. After 120 days, Group II goats showed no regression of the changes in their reproductive behavior or improvement of their seminal parameters. The main defects observed in the sperm of goats that consumed I. brasiliana were cytoplasmatic droplets, bent tails and detached tails. The main histopathological findings were reported in tests, with cytoplasmic vacuolization of germline and Sertoli cells, generalized impairment of spermatogonia maturation with exfoliation of degenerative cells, cell fragments, rare abnormal spermatocytes in the seminiferous lumen and disappearance of Leydig cells. Results of this study confirmed the hypothesis that I. brasiliana causes testicular degeneration in male goats.(AU)

Este trabalho teve como objetivo caracterizar as mudanças comportamentais relacionadas a reprodução e lesões no sistema reprodutor de caprinos intoxicados por Ipomoea brasiliana. A planta foi coletada e administrada na dose de 4g/kg (800g swainsonina/kg) para dois grupos de caprinos durante 45 dias. Os caprinos do Grupo I foram eutanasiados no 46º dia do experimento e os caprinos do Grupo II no 120º dia. O Grupo III foi constituído por caprinos que não receberam I. brasiliana e foram eutanasiados no 120º dia de experimento. Alterações comportamentais reprodutivas foram observadas a partir de 20 dias de experimento e consistiram em ausência do comportamento de corte, ausência de reflexo de Flehmen, diminuição ou perda de libido e incapacidade de realizar a monta natural. Após 120 dias, os caprinos do Grupo II não apresentaram regressão de alterações reprodutivas. Os principais defeitos observados no sêmen dos caprinos que consumiam I. brasiliana foram gotas citoplasmáticas, caudas dobradas e caudas destacadas. Os principais achados histopatológicos consistiram em vacuolização citoplasmática das células da linhagem germinativa e células de Sertoli; comprometimento generalizado da maturação das espermatogônias com esfoliação de células degeneradas; presença de fragmentos celulares e raros espermatócitos anormais no lúmen dos túbulos seminíferos e ausência de células de Leydig. Os resultados confirmam a hipótese de que o consumo de I. brasiliana causa degeneração testicular em caprinos.(AU)

Uso de extrato aquoso de pimenta malagueta (Capsicum frutescens L. ) em testes de sobrevivência sobre Achatina fulica (Bowdich, 1822) (Mollusca, Gastropoda) / Effect of use of aqueous chilli pepper (Capsicum frutescens l. ) on survival of Achatina fulica(Bowdich, 1822) (Mollusca, Gastropoda) molluscicidal activity

Achatina fulica (Bowdich, 1822) é um molusco pulmonado terrestre originário do Leste-Nordesteda África, que se disseminou por todo o mundo, como praga agrícola e hospedeiro de váriasdoenças de interesse médico-veterinário, foi introduzido no Brasil por volta de 1980 por criadores doParaná, visando substituir o escargot Helix aspersa (Müller, 1774), embora exista relato da introduçãodesse molusco na Região Sudeste por volta da década de 1970. Com o insucesso na comercializaçãodessa espécie, foi solto no ambiente sem qualquer cuidado, causando assim um desequilíbrio nafauna nativa. Produtos sintéticos foram usados para tentar conter esse molusco, mas sem êxito, alémde serem inviavelmente mais caros. O uso de produtos naturais vem sendo estudado há vários anostentando chegar a uma substância que não agrida o meio ambiente e outras espécies. Com isso Capsicumfrutescens L. (Solanaceae) conhecida popularmente como pimenta malagueta, possui algumassubstâncias como alcaloides, compostos fenólicos e taninos, que sugere-se que possuam uma supostataxa moluscicida. Nesse trabalho utilizou-se do método direto, que consiste da aplicação do extratoaquoso diretamente sobre os moluscos. O experimento foi realizado no Laboratório de Zoologia dosInvertebrados do CES-JF, além da triagem fitoquímica concomitante para identificação dos principaiscompostos presentes no extrato aquoso. Este trabalho objetivou-se em testar o extrato aquoso deC. frutescens sobre a sobrevivência de indivíduos de 30 e 120 dias de idade, utilizando-se de noveconcentrações, 10g/L, 9g/L, 8g/L, 7g/L, 6g/L, 5g/L, 4g/L, 3g/L e 2g/L, o acompanhamento deu-sedurante 30 dias.

Achatina fulica (Bowdich, 1822)is a terrestrial pulmonary mollusk originating in East-Northeast Africa, which spreads throughout theworld as an agricultural pest and host of several zoonoses of medical and veterinary interest, includingthe nematodes Angiostrongylus cantonensis and Angiostrongylus. costaricensis. It was introducedin Brazil around 1980, replacing the Helix aspersa escargot (Müller, 1774), but there is another reportof the introduction of the mollusk in the Southeast Region in 1970’s. With the failure to commercializethis species, it was released in the environment without care, thu s causing an imbalance in nativefauna. Synthetic products were used to control this mollusk, but without success, besides being unviableand more expensive. The use of ecological products have been studied for several years and havereached an area that does not please the environment or any other species. Thus, Capsicum frutescensL. popularly known as chilli pepper, has several compounds like alkaloids, phenolic compoundsand tannins, which have a molluscicide potential. In this work, the direct method was applied, whichconsists of the application of the aqueous extract on the mollusks. The experiment was conductedin the Laboratory of Zoology of the Invertebrates of the CES-JF, and a phytochemical screening wascarried out to identify the main non-aqueous extract compounds. The aim of this work was to test theaqueous extract of C. frutescens on the survival of individuals of 30 and 120 days of age, using nineconcentrations, 10g/L, 9g/L, 8g/L, 7g/L and 6g/L. 5g/L, 4g/L, 3g/L and 2g/L. Follow-up occurred for 30days. The results were efficient in snails of 30 days of age, causing 100% mortality, no group control.In individuals of 120 days of age concentrations 10g/L, 9g/L, 8g/L, 7g/L acted as molluscicide, causing100 % of mortality. There are no concentrations.

Uso de extrato aquoso de pimenta malagueta (Capsicum frutescens L. ) em testes de sobrevivência sobre Achatina fulica (Bowdich, 1822) (Mollusca, Gastropoda) / Effect of use of aqueous chilli pepper (Capsicum frutescens l. ) on survival of Achatina fulica(Bowdich, 1822) (Mollusca, Gastropoda) molluscicidal activity.

Achatina fulica (Bowdich, 1822) é um molusco pulmonado terrestre originário do Leste-Nordesteda África, que se disseminou por todo o mundo, como praga agrícola e hospedeiro de váriasdoenças de interesse médico-veterinário, foi introduzido no Brasil por volta de 1980 por criadores doParaná, visando substituir o escargot Helix aspersa (Müller, 1774), embora exista relato da introduçãodesse molusco na Região Sudeste por volta da década de 1970. Com o insucesso na comercializaçãodessa espécie, foi solto no ambiente sem qualquer cuidado, causando assim um desequilíbrio nafauna nativa. Produtos sintéticos foram usados para tentar conter esse molusco, mas sem êxito, alémde serem inviavelmente mais caros. O uso de produtos naturais vem sendo estudado há vários anostentando chegar a uma substância que não agrida o meio ambiente e outras espécies. Com isso Capsicumfrutescens L. (Solanaceae) conhecida popularmente como pimenta malagueta, possui algumassubstâncias como alcaloides, compostos fenólicos e taninos, que sugere-se que possuam uma supostataxa moluscicida. Nesse trabalho utilizou-se do método direto, que consiste da aplicação do extratoaquoso diretamente sobre os moluscos. O experimento foi realizado no Laboratório de Zoologia dosInvertebrados do CES-JF, além da triagem fitoquímica concomitante para identificação dos principaiscompostos presentes no extrato aquoso. Este trabalho objetivou-se em testar o extrato aquoso deC. frutescens sobre a sobrevivência de indivíduos de 30 e 120 dias de idade, utilizando-se de noveconcentrações, 10g/L, 9g/L, 8g/L, 7g/L, 6g/L, 5g/L, 4g/L, 3g/L e 2g/L, o acompanhamento deu-sedurante 30 dias. (AU)

Achatina fulica (Bowdich, 1822)is a terrestrial pulmonary mollusk originating in East-Northeast Africa, which spreads throughout theworld as an agricultural pest and host of several zoonoses of medical and veterinary interest, includingthe nematodes Angiostrongylus cantonensis and Angiostrongylus. costaricensis. It was introducedin Brazil around 1980, replacing the Helix aspersa escargot (Müller, 1774), but there is another reportof the introduction of the mollusk in the Southeast Region in 1970s. With the failure to commercializethis species, it was released in the environment without care, thu s causing an imbalance in nativefauna. Synthetic products were used to control this mollusk, but without success, besides being unviableand more expensive. The use of ecological products have been studied for several years and havereached an area that does not please the environment or any other species. Thus, Capsicum frutescensL. popularly known as chilli pepper, has several compounds like alkaloids, phenolic compoundsand tannins, which have a molluscicide potential. In this work, the direct method was applied, whichconsists of the application of the aqueous extract on the mollusks. The experiment was conductedin the Laboratory of Zoology of the Invertebrates of the CES-JF, and a phytochemical screening wascarried out to identify the main non-aqueous extract compounds. The aim of this work was to test theaqueous extract of C. frutescens on the survival of individuals of 30 and 120 days of age, using nineconcentrations, 10g/L, 9g/L, 8g/L, 7g/L and 6g/L. 5g/L, 4g/L, 3g/L and 2g/L. Follow-up occurred for 30days. The results were efficient in snails of 30 days of age, causing 100% mortality, no group control.In individuals of 120 days of age concentrations 10g/L, 9g/L, 8g/L, 7g/L acted as molluscicide, causing100 % of mortality. There are no concentrations.(AU)

Different leaf extracts from Brunfelsia uniflora in mice / Diferentes extratos das folhas de Brunfelsia uniflora em camundongos

In Brazil, at least 16 poisonous plant species can affect the central nervous system of livestock. Recently in the state of Piauí, Northeastern Brazil, Brunfelsia uniflora was reported as a cause of nervous signs in donkeys, cattle, and small ruminants. In order to assess the toxicity of B. uniflora extracts, 20 Swiss mice were distributed into four groups (n=5) receiving by gavage alkaloids, flavonoids, saponins, or saline (control group). After administration of the extracts in a single dose (5g kg-1), all mice were observed daily for clinical signs. Mice that received the extracts showed moderate to severe clinical signs, including piloerection, vocalization, and seizures. All mice dosed with saponins died between 10 and 20min after administration. Serum biochemical evaluation of animals that received saponins revealed slight increases in total protein levels and decreased magnesium and chlorite levels. In conclusion, saponins of B. uniflora leaves induced acute toxic neurological effects and death in mice.(AU)

No Brasil, pelo menos 16 espécies de plantas tóxicas podem afetar o sistema nervoso central dos bovinos. Recentemente no estado do Piauí, no Nordeste do Brasil, Brunfelsia uniflora foi relatada como causadora de sinais nervosos em jumentos, bovinos e pequenos ruminantes. Para avaliar a toxicidade de B. uniflora, 20 camundongos foram distribuídos em quatro grupos de cinco animais recebendo diferentes extratos da planta. Os extratos de alcalóides, flavonóides, saponinas ou solução salina (grupo controle) foram administrados por gavagem. Após a administração dos extratos, em dose única (5g kg-1), todos os animais foram observados diariamente. Os camundongos que receberam os extratos de B. uniflora apresentaram sinais clínicos moderados a graves, incluindo piloeração, vocalização e convulsões. Todos os camundongos que receberam extrato de saponinas morreram entre 10 e 20 minutos após. A avaliação bioquímica sérica dos animais que receberam saponinas, revelou discretos aumentos nos níveis de proteína total e diminuição nos níveis de magnésio e cloro. Conclui-se que, as saponinas presentes nas folhas de B. uniflora induzem efeitos neurológicos tóxicos agudos e, morte em camundongos.(AU)

Assessment of benzophenanthridine and protopine alkaloids in broiler challenged and not by Salmonella Heidelberg

Salmonellosis is a globally important zoonosis, and Salmonella Heidelberg is one of the most prevalent serovars in poultry production worldwide, as well as in food poisoning cases. Antimicrobial drugs were previously widely used to face health challenges in animal production; however, since their ban as performance enhancers, many alternative strategies have been proposed. One of these strategies is the use of plant extracts, such as those containing the alkaloids benzophenanthridine and protopine. These compounds have antimicrobial, anti-inflammatory, immunomodulation, and nutritional effects. The objective of the present study was to evaluate the effects of the supply of a product containing benzophenanthridine and protopine (Sangrovit(r)WS 100 g/1000 L of drinking water) to broilers during different rearing periods 1-21, 1-6 and 6-21 days of age challenged or not with Salmonella Heidelberg at six days of age. There was no effect of the product on the performance, jejunal morphometry, cecal goblet cell counts, or control of Salmonella spp. in broilers challenged or not with Salmonella Heidelberg. However, the group receiving the alkaloids from 1 to 21 days of age, compared with the control group, presented a numerical difference of 28 points in productive efficiency index, which directly impacts live production cost of live broiler, representing savings of R$ 0.11/kg of meat produced.

Assessment of benzophenanthridine and protopine alkaloids in broiler challenged and not by Salmonella Heidelberg

Salmonellosis is a globally important zoonosis, and Salmonella Heidelberg is one of the most prevalent serovars in poultry production worldwide, as well as in food poisoning cases. Antimicrobial drugs were previously widely used to face health challenges in animal production; however, since their ban as performance enhancers, many alternative strategies have been proposed. One of these strategies is the use of plant extracts, such as those containing the alkaloids benzophenanthridine and protopine. These compounds have antimicrobial, anti-inflammatory, immunomodulation, and nutritional effects. The objective of the present study was to evaluate the effects of the supply of a product containing benzophenanthridine and protopine (Sangrovit(r)WS 100 g/1000 L of drinking water) to broilers during different rearing periods 1-21, 1-6 and 6-21 days of age challenged or not with Salmonella Heidelberg at six days of age. There was no effect of the product on the performance, jejunal morphometry, cecal goblet cell counts, or control of Salmonella spp. in broilers challenged or not with Salmonella Heidelberg. However, the group receiving the alkaloids from 1 to 21 days of age, compared with the control group, presented a numerical difference of 28 points in productive efficiency index, which directly impacts live production cost of live broiler, representing savings of R$ 0.11/kg of meat produced.(AU)

Toxicidade de Ipomoea setifera

Ipomoea setifera é uma planta tropical pertencente à família Convolvulaceae. Os animais comem suas folhas e flores em períodos de estiagem pois a planta se mantêm verde durante todo o ano. Poucos são os relatos sobre a toxicidade da I. setifera. Análise química das folhas de I. setifera revelou a presença dos alcaloides nortropânicos calisteginas B1 e B2 que possuem atividade inibitória sobre as enzimas β-glicosidase, α e β-galactosidase e β-xilosidase, importantes para o adequado metabolismo de carboidratos. O objetivo desse estudo é realizar uma revisão sobre as propriedades químicas e toxicológicas das calisteginas presentes na I. setifera. (AU)

Ipomoea setifera is a tropical plant belonging to the Convolvulaceae family found mainly next to streams and rivers throughout the year. Few are the reports about the toxicity of I. setifera. On the other hand phytochemical analysis of the extracts revealed presence of nortropânicos alkaloids calystegines B1 and B2 in the leaves of I. setifera which promote inhibition of β-glycosidase, α and β-galactosidase, and β-xylosidase, important enzymes for an adequate metabolism of carbohydrates in the organism. So if objective of this study is to perform a literature on chemical and toxicological properties of calisteginas alkaloids of the I. setifera. (AU)

Toxicidade de Ipomoea setifera

Ipomoea setifera é uma planta tropical pertencente à família Convolvulaceae. Os animais comem suas folhas e flores em períodos de estiagem pois a planta se mantêm verde durante todo o ano. Poucos são os relatos sobre a toxicidade da I. setifera. Análise química das folhas de I. setifera revelou a presença dos alcaloides nortropânicos calisteginas B1 e B2 que possuem atividade inibitória sobre as enzimas β-glicosidase, α e β-galactosidase e β-xilosidase, importantes para o adequado metabolismo de carboidratos. O objetivo desse estudo é realizar uma revisão sobre as propriedades químicas e toxicológicas das calisteginas presentes na I. setifera.

Ipomoea setifera is a tropical plant belonging to the Convolvulaceae family found mainly next to streams and rivers throughout the year. Few are the reports about the toxicity of I. setifera. On the other hand phytochemical analysis of the extracts revealed presence of nortropânicos alkaloids calystegines B1 and B2 in the leaves of I. setifera which promote inhibition of β-glycosidase, α and β-galactosidase, and β-xylosidase, important enzymes for an adequate metabolism of carbohydrates in the organism. So if objective of this study is to perform a literature on chemical and toxicological properties of calisteginas alkaloids of the I. setifera.

Aspectos farmacológicos e toxicológicos de Psychotria colorata revisão / Pharmacological and toxicological aspects of Psychotria colorata review

Psychotria colorata popularmente conhecida como perpétua-do-mato e repolho, é uma planta da família Rubiaceae difundida na América do Sul e encontrada na região Amazônica do Brasil. A planta tem sido usada na medicina tradicional como analgésico para dores de ouvido e abdominais por "caboclos" de comunidades tradicionais rurais do estado do Pará, Brasil. No entanto, a ingestão da planta foi associada com a ocorrência de aborto em vacas. Além disso, a planta foi relatada por promover efeitos neurólogicos em camundongos. A análise fitoquímica das folhas de P. colorata revelou a presença de vários alcalóides pirrolidinoindolínicos, incluindo psicotridina, hodgkinsina, isocalicantina e calicantina, os quais estariam relacionados à atividade farmacológica e tóxica da planta. (AU)

Psychotria colorata popularly known as pérpetua do mato and repolho, is a plant of the family Rubiaceae widespread in South America, is found in Amazonian region of Brazil. The plant have been used in traditional medicine as painkiller for earache, abdominal pain by “caboclos” of traditional rural communities from the state of Pará, Brazil. However, ingestion of the plant was associated with the occurrence of abortions in cows. In addition, the plant has been related to promote neurological effects in mice. The phytochemical analysis from leaves of P. colorata revealed the presence of several pyrrolidinoindoline alkaloids, including psychotridine, hodgkinsine, isocalycanthine, calycanthine, which may be related to the pharmacological and toxic activity of the plant. (AU)

Possível toxicidade reprodutiva de S. guianensis revisão de literatura / Possible reproductive toxicity of S. guianensis - review

Siparuna guianensis conhecida popularmente como negramina é uma planta usada na medicina popular para várias afecções, dentre elas, dores musculares, cefaleias e abortivas. Pecuaristas do estado do Tocantins relatam que a mesma causa mortes e abortamentos. Estudos fitoquímicos revelaram a presença de alcaloides na casca do fruto de S. guianensis que podem provocar as alterações reprodutivas. Assim, conclui-se que os efeitos abortivos atribuídos pelos produtores à planta podem estar relacionados a um efeito estrogênico dos alcaloides, por mecanismo semelhante ao dos piretroides, ao efeito hipotensor, sobre receptores adrenérgicos e serotoninérgicos, ou a um efeito deletério direto sobre o DNA. (AU)

Siparuna guianensis popularly known as negramina is a plant used in folk medicine for various diseases, among them, muscle aches, headache and abortion. Livestock producers in the state of Tocantins reported that the same cause deaths and abortifacient. Phytochemical studies revealed the presence of alkaloids in the fruit peel of S. guianensis that can cause reproductive changes. Thus, it is concluded that the abortifacient effects attributed by farmers to plant may be related to an estrogenic effect of alkaloids by a mechanism similar to the pyrethroids, the hypotensive effect of adrenergic and serotonergic receptors, or to a direct deleterious effect on DNA . (AU)

Possível toxicidade reprodutiva de S. guianensis – revisão de literatura / Possible reproductive toxicity of S. guianensis - review

Siparuna guianensis conhecida popularmente como negramina é uma planta usada na medicina popular para várias afecções, dentre elas, dores musculares, cefaleias e abortivas. Pecuaristas do estado do Tocantins relatam que a mesma causa mortes e abortamentos. Estudos fitoquímicos revelaram a presença de alcaloides na casca do fruto de S. guianensis que podem provocar as alterações reprodutivas. Assim, conclui-se que os efeitos abortivos atribuídos pelos produtores à planta podem estar relacionados a um efeito estrogênico dos alcaloides, por mecanismo semelhante ao dos piretroides, ao efeito hipotensor, sobre receptores adrenérgicos e serotoninérgicos, ou a um efeito deletério direto sobre o DNA.

Siparuna guianensis popularly known as negramina is a plant used in folk medicine for various diseases, among them, muscle aches, headache and abortion. Livestock producers in the state of Tocantins reported that the same cause deaths and abortifacient. Phytochemical studies revealed the presence of alkaloids in the fruit peel of S. guianensis that can cause reproductive changes. Thus, it is concluded that the abortifacient effects attributed by farmers to plant may be related to an estrogenic effect of alkaloids by a mechanism similar to the pyrethroids, the hypotensive effect of adrenergic and serotonergic receptors, or to a direct deleterious effect on DNA .

Aspectos farmacológicos e toxicológicos de Psychotria colorata – revisão / Pharmacological and toxicological aspects of Psychotria colorata – review

Psychotria colorata popularmente conhecida como perpétua-do-mato e repolho, é uma planta da família Rubiaceae difundida na América do Sul e encontrada na região Amazônica do Brasil. A planta tem sido usada na medicina tradicional como analgésico para dores de ouvido e abdominais por "caboclos" de comunidades tradicionais rurais do estado do Pará, Brasil. No entanto, a ingestão da planta foi associada com a ocorrência de aborto em vacas. Além disso, a planta foi relatada por promover efeitos neurólogicos em camundongos. A análise fitoquímica das folhas de P. colorata revelou a presença de vários alcalóides pirrolidinoindolínicos, incluindo psicotridina, hodgkinsina, isocalicantina e calicantina, os quais estariam relacionados à atividade farmacológica e tóxica da planta.

Psychotria colorata popularly known as pérpetua do mato and repolho, is a plant of the family Rubiaceae widespread in South America, is found in Amazonian region of Brazil. The plant have been used in traditional medicine as painkiller for earache, abdominal pain by “caboclos” of traditional rural communities from the state of Pará, Brazil. However, ingestion of the plant was associated with the occurrence of abortions in cows. In addition, the plant has been related to promote neurological effects in mice. The phytochemical analysis from leaves of P. colorata revealed the presence of several pyrrolidinoindoline alkaloids, including psychotridine, hodgkinsine, isocalycanthine, calycanthine, which may be related to the pharmacological and toxic activity of the plant.

Bufotenine is able to block rabies virus infection in BHK-21 cells

Background Rabies is a fatal zoonotic neglected disease that occurs in more than 150 countries, and kills more than 55.000 people every year. It is caused by an enveloped single stranded RNA virus that affects the central nervous system, through an infection initiated by the muscular nicotinic acetylcholine receptor, according to many authors. Alkaloids, such as acetylcholine, are widespread molecules in nature. They are present in numerous biological fluids, including the skin secretion of many amphibians, in which they act (together with proteins, peptides and steroids) as protection agents against predators and/or microorganisms. Among those amphibians that are rich in alkaloids, there is the genus Rhinella.Methods Bufotenine was isolated from Rhinela jimi skin secretion after a liquid-liquid partition (H2O:CH2Cl2) and reversed phase high-performance liquid chromatography analyses (RP-HPLC). Bufotenine was also extracted from seeds of Anadenanthera colubrina in acetone solution and purified by RP-HPLC, as well. Structural characterization was performed by mass spectrometry and nuclear magnetic resonance analyses. Cytotoxic tests of bufotenine were performed over baby hamster kidney (BHK-21) cells using MTT test. For the antiviral activity,Rabies virus strain Pasteur vaccine (PV) was used on fluorescence inhibition test and fluorescent foci inhibition test, with both simultaneous and time course treatment of the cells with the virus and bufotenine.Results In the present work we describe the effects of bufotenine, obtained either from toads or plants, that can inhibit the penetration of rabies virus in mammalian cells through an apparent competitive mechanism by the nicotinic acetylcholine receptor. Moreover, this inhibition was dose- and time-dependent, pointing out to a specific mechanism of action...(AU)