Toxicological and pharmacological effects of pentacyclic triterpenes rich fraction obtained from the leaves of Mansoa hirsuta.

Mansoa hirsuta is a medicinal plant native to the Brazilian semi-arid region. This approach aimed to investigate the in vitro and in vivo toxicity and anti-inflammatory and analgesic actions of the M. hirsuta fraction (MHF). In vitro cell viability was assessed in 3T3 cells. In vivo, the acute toxicity test, a single dose of the MHF was administered. For the subchronic toxicity test, three doses of were administered for 30 days. Locomotion and motor coordination were assessed using open field and rota-rod. The anti-inflammatory activity was evaluated in carrageenan-induced paw edema and zymosan-induced air-pouch models. Myeloperoxidase (MPO) and total proteins were also measured. The antinociceptive activity MHF was determined using acid acetic-induced abdominal writhing and formalin models. In the cytotoxicity assay, MHF showed no significative impairment of cell viability and in the acute toxicity study, did not cause mortality or signs of toxicity. Repeated exposure to MHF did not cause relevant toxicological changes. The evaluation in the open field test showed that the MHF did not alter the locomotor activity and there was no change in motor coordination and balance of animals. MHF significantly reduced edema, MPO production, the migration of leukocytes and protein leakage. In addition, MHF reduced abdominal writhing and significantly inhibited the first and second stage of the formalin test. The results of this study indicated that MHF has an anti-inflammatory and analgesic potential without causing acute or subchronic toxic effects and it can be a promising natural source to be explored.

Antiulcer Activity and Potential Mechanism of Action of the Leaves of Spondias mombin L.

Spondias mombin L. is used in folk medicine for the treatment of inflammation and gastrointestinal diseases. Our study investigated the antiulcer activity of S. mombin ethanolic extract (SmEE) and its majority compounds gallic acid (GA) and ellagic acid (EA). Phytochemical characterization was performed by HPLC. The SmEE was screened for in vitro antioxidant activities using phosphomolybdenum, ABTS, DPPH, and FRAP assays. The antiulcer activity of SmEE, GA, EA, or GA + EA was evaluated by gastric lesion models induced by absolute ethanol and indomethacin. Following this, it is capable of stimulating mucus production, antisecretory capacity, and the influence of -SH groups and NO in the effect of SmEE. Its healing activity was demonstrated by acetic acid-induced chronic ulcer model. Anti-Helicobacter pylori activity was assessed by determining the MIC of the SmEE (64-1024 µg/mL). The HPLC results identified the presence of gallic acid and ellagic acid in SmEE. The extract showed antioxidant activity in vitro. SmEE (50, 100, and 200 mg/kg) reduced the area of ulcerative lesions induced by ethanol in 23.8, 90.3, and 90.2%, respectively. In NSAID model, the SmEE induced protection of 36.8, 49.4, and 49.9%, respectively. GA (10 mg/kg) or EA (7 mg/kg) or the association of GA + EA (10 + 7 mg/kg) inhibited the ethanol-induced lesions in 71.8, 70.9, and 94.9%, respectively, indicating synergistic action. SmEE (100 mg/kg) decreased acid secretion and H+ concentration in the gastric contents, increased levels of mucus, and showed to be dependent of -SH groups and NO on the protection of the gastric mucosa. In chronic ulcer model, SmEE reduced the gastric area lesion. SmEE showed anti-H. pylori activity. In conclusion, our study showed that SmEE has antiulcerogenic activity. GA and EA are isolated gastric protectors and, when associated, acted synergistically to protect the gastric mucosa.

Toxicity of soursop extracts to diamondback moth / Toxicidade de extratos de graviola sobre a traça-das-crucíferas

This study aimed to evaluate the effects of three solvent extractors (water, ethanol and hexane) of grounded seeds of soursop, Annona muricata L. (Annonaceae), in the mortality, biology and oviposition of Plutella xylostella L. (Lepidoptera: Plutellidae). The results showed that the LC50 and LC99 were 0.0133 and 0.084%, 0.025% and 0.196%, 2.33 and 35.22% for the ethanolic, hexanic and aqueous extracts, respectively. The organic extracts affected only the larval phase and reduced viability in more than 60%, but did not affect pupal stage of the remaining larvae. Furthermore, the ethanolic extract at lethal concentraction also affected negatively the embryonic phase. The results lead to the conclusion that the ethanolic extract of soursop grounded seeds is a viable alternative to control diamondback moth on vegetables.

O presente trabalho teve como objetivo avaliar o efeito de extratos de sementes de graviola, Annona muricata L. (Annonaceae) obtidos com diferentes solventes sobre Plutella xylostella L. (Lepidoptera: Plutellidae). Foram estimadas as concentrações letais de três solventes extratores (água, hexano e etanol) e seus efeitos na biologia e oviposição. Os valores estimados das concentrações letais foram de 0,013 e 0,084%; 0,025 e 0,196%; 2,33 e 35,22%, para as CL50 e CL99 do extrato etanólico, hexânico e aquoso, respectivamente. Os extratos orgânicos afetaram apenas a fase larval e reduziu a viabilidade em mais de 60%, mas não afetou a fase pupal das lagartas remanescentes. Além disso, o extrato etanólico na concentração letal se mostrou eficiente afetando negativamente a fase embrionária. Conclui-se que o extrato etanólico da graviola é uma alternativa viável no controle da traça.

Hepatic fatty acid profile of rats fed a triheptanoin-based ketogenic diet / Perfil de ácidos grasos de hígados de ratones alimentados con una dieta cetogénica basada en triheptanoína

Objective: the aim of this study was to evaluate the influence of consumption of a ketogenic diet supplemented with triheptanoin, a medium-chain anaplerotic triacylglycerol, on the liver fatty acid profile of Wistar rats. Methods: three groups of male Wistar rats (n=10) were submitted to an AIN-93 control diet, a triheptanoin-based ketogenic diet, or a soybean oil-based ketogenic diet for 60 days. Excised livers were subjected to lipid extraction and methylation to obtain fatty acids methyl esters, which were subjected to gas chromatography-mass spectrometry. Results and discussion: compared to the rats fed the control diet, those fed ketogenic diets showed a significant reduction in the concentrations of 9-hexadecenoic and 9-octadecenoic acids, whereas those fed triheptanoin showed increased levels of octadecanoic acid. Conclusion: changes in the liver fatty acid profiles of the rats fed a triheptanoin-based or a soybean oil-based ketogenic diet did not seem to be related to the dietary fat source, but rather to the characteristics of the ketogenic diets themselves (AU)

Objetivo: el objetivo de este estudio fue evaluar la influencia del consumo de una dieta cetogénica complementada con triheptanoína, un triacilglicerol de cadena media y anaplerótico, en el perfil de ácidos grasos del hígado de ratones Wistar. Métodos: tres grupos de ratones Wistar machos (n=10) fueron sometidos durante 60 días a una dieta AIN-93 de control, una dieta cetogénica basada en triheptanoína o una dieta cetogénica a base de aceite de soja. Los hígados fueron escindidos y sometidos a extracción de lípidos y metilación para obtener los ésteres metílicos de ácidos grasos, que se sometieron a cromatografía de gas-espectrometría de masa. Resultados y discusión: en comparación con los ratones alimentados con la dieta de control, los de ambas dietas cetogénicas mostraron una reducción significativa en las concentraciones de los ácidos grasos 9-hexadecenoico y 9-octadecenoico, mientras que los alimentados con triheptanoína mostraron niveles de ácido octadecenoico aumentados. Conclusión: los cambios en los perfiles de ácidos grasos del hígado de los ratones alimentados con dietas cetogénicas no están relacionados con la fuente de grasa de la dieta (triheptanoína o aceite de soja), sino más bien con la concentración total de lípidos (AU)

Cocos nucifera Linn. (Palmae) husk fiber ethanolic extract: antioxidant capacity and electrochemical investigation.

The present study aims to determine the antioxidant capacity of the ethanolic extracts of husk fiber of four coconut (Cocos nucifera L.) varieties (yellow dwarf, green dwarf, giant and hybrid) and to evaluate the electrochemical behavior of these extracts on a glassy carbon electrode and on a modified glassy carbon electrode. The highest values of total phenolic content were obtained for the hybrid (531 ± 24 mg GAE g(-1) dry extract) and yellow dwarf (501 ± 29 mg GAE g(-1) dry extract) varieties and the lowest was for the green dwarf variety with 58 ± 9 mg GAE g(-1) dry extract. The ability of the extracts to scavenge DPPH˙ radicals was in the order of giant > yellow dwarf > hybrid > green dwarf and the IC50 values varied from 8.6 to 55.9 µg mL(-1). All varieties showed reducing potential by the use of FRAP and CUPRAC methods, with the lowest performance obtained for the green dwarf variety. Additionally, through the use of mimetic biomembranes, ethanolic extracts of coconut husk were shown to protect lipids against oxidative damage independent of the variety. The main antioxidants identified in the extract of yellow dwarf variety by UPLC-MS were quercetin and catechin. Cyclic voltammetric studies of the ethanolic extracts on glassy carbon electrode confirmed the presence of easily oxidized compounds, and the high antioxidant capacity of the varieties. This capacity was expressed as mg quercetin equivalents g(-1) dry extract and ranged from 25.9 up to 53.5 mg QE g(-1). A poly-xanthurenic acid (poly-Xa)/multi-walled carbon nanotube (MWCNT) / glassy carbon modified electrode (poly-Xa/MWCNT/GCE) was used for this purpose. Our findings suggest that these extracts are potentially important antioxidant supplements for the everyday human diet, pharmaceutical and cosmetic industries, thereby aggregating value to the enormous amount of waste from the coconut industry, mostly used for burning purposes.

Antispasmodic effect of 4'-methylepigallocatechin on guinea pig ileum.

The antispasmodic effect of 4'-methylepigallocatechin (MEC), which was isolated from Maytenus rigida Mart (Celestraceae), was investigated in vitro in guinea pig intestinal segments. In the isolated ileum, MEC (1 nM-100 µM) did not modify the ileal spontaneous tonus or the electrically elicited contractions. MEC (8 µM) significantly (p<0.01) reduced the submaximal contractions induced by histamine (2 µM), carbachol (100 µM) and BaCl2 (0.03 M). An additive relaxing action (p<0.001) was observed by co-incubation of verapamil (10 nM) and MEC (8 µM). Although MEC (1 nM-100 µM) did not modify the contractions elicited by 60 mM KCl, it significantly reduced the CaCl2 contractile response without changing the EC50 (effective concentration of CaCl2 causing 50% of maximum response). In brief, these results show that MEC has a potent ileal spasmolytic effect and blocks spasms induced by specific and nonspecific stimuli. Importantly, the spasmolytic effects were attained at low concentrations and might be related to the symptomatic relief of abdominal pain that is obtained from the use of the M. rigida stem bark.

Consumo de café segundo métodos de preparo da bebida e associação com perfil lipídico sérico em hipertensos e diabéticos / Intake of different coffee preparations and its association with the serum lipid profile of diabetics and hypertensive individuals

OBJETIVO: Verificar o consumo da bebida café segundo a quantidade ingerida e os métodos de preparo, e sua associação com o perfil lipídico sérico de hipertensos e diabéticos. MÉTODOS: Foram coletados, por meio de entrevista, dados demográficos, de estilo de vida e de consumo alimentar, aferidas medidas antropométricas e colhido sangue para análise de perfil lipídico sérico. Análise descritiva, testes t de Student, qui-quadrado e de correlação linear de Pearson foram utilizados com 5 por cento de probabilidade de erro experimental. RESULTADOS: Foram avaliados 182 indivíduos hipertensos e diabéticos tipo 2, consumidores de café, distribuídos em dois grupos segundo o método de preparo da bebida: à brasileira e fervido. Os grupos foram semelhantes quanto aos dados demográficos, antropométricos, de estilo de vida, de consumo alimentar e de perfil lipídico sérico. A quantidade per capita de pó utilizado no método à brasileira e no fervido foi de M=7,52, DP=4,99g e M=7,91, DP=5,87g, respectivamente. O volume ingerido e a frequência de consumo dos indivíduos do grupo à brasileira foi de M=517,3, DP=402,7mL e M=2,14, DP=1,06 vezes/dia, e para os consumidores de café fervido, M=513,4, DP=409,8mL e M=2,2, DP=0,94 vezes/dia. Não houve associação significativa entre a quantidade ingerida da bebida café e o perfil lipídico sérico. CONCLUSÃO: Não houve associação entre o consumo de café à brasileira ou fervido e o perfil lipídico sérico, possivelmente em função da quantidade consumida e/ou da diluição utilizada. Se, por um lado, os resultados não permitem desestimular o consumo da bebida na quantidade ingerida pela população estudada, como medida de prevenção cardiovascular, por outro lado autorizam concluir que há necessidade de avançar nessa linha de investigação.

OBJECTIVE: This study determined the amount of coffee consumed, the preparation methods and the association between coffee intake and the serum lipid profile of diabetics and hypertensive individuals. METHODS: Interviews were done to collect demographic and lifestyle data and food intake. Blood was collected to determine serum lipid profiles and anthropometric characteristics were measured. Descriptive analysis and the Student's t-test, chi-square test and Pearson's linear correlation were used with p£0.05 to establish statistical significance. RESULTS: A total of 182 hypertensive and type-2 diabetic individuals who consumed coffee were evaluated and categorized according to the preparation method: Brazilian or boiled. The population had similar demographics, anthropometrics, lifestyles, food habits and serum lipid profiles. The per capita amount of powder ingested when the Brazilian preparation method (uses a filter) was used compared with boiling was M=7.52, SD=4.99g and M=7.91, SD=5.87g, respectively. In both groups, those levels were obtained in accordance with the estimated daily intake volume of the drink. The volume ingested by individuals in the "Brazilian" group and intake frequency were: M=517.3, SD=402.7mL and M=2.14, SD=1.06 times/day and in the "boiled" group: M=513.4, SD=409.8mL, and M=2.2 SD=0.94 times/day. There was no significant association between coffee intake and serum lipid profile. CONCLUSION: There was no association between coffee intake and serum lipid profile in the studied population, possibly because of the amount consumed and/or dilution used. If, on the one hand, the results do not allow us to discourage consumption in the amounts consumed by the studied population as a way to prevent cardiovascular disease, on the other hand, it is clear that this line of research requires further investigation.

Café e saúde humana: um enfoque nas substâncias presentes na bebida relacionadas às doenças cardiovasculares / Coffee and human health: a focus on the substances of the beverage related to cardiovascular disease

O café é a bebida mais consumida no Brasil e no mundo ocidental. O fato de ser uma bebida tão popular, aliado à sua importância econômica, explica o interesse por estudos sobre o café, desde a sua composição até seus efeitos na saúde humana. Dentre as diversas substâncias presentes na composição química do café, além dos nutrientes, destacam-se a cafeína, os diterpenos cafestol e kahweol e os ácidos clorogênicos, o que faz do café uma importante fonte dietética destes compostos. Muitos estudos têm verificado a influência de seus constituintes na saúde, principalmente a cafeína vs a elevação da pressão arterial; o cafestol e o kahweol vs a dislipidemia; e ácidos clorogênicos vs proteção cardiovascular, por suas propriedades antioxidantes. Este artigo tem como objetivo apresentar de forma sucinta a importância da bebida e sua composição química, os mecanismos fisiológicos envolvidos na elevação da pressão arterial e do colesterol sérico atribuíveis ao café, bem como estudos selecionados que verificaram a associação do consumo da bebida com estas doenças cardiovasculares.

Coffee is the most consumed beverage in the Western world, including Brazil. The fact that it is one the most popular beverages and its worldwide consumption and economic importance explain the interest for studies on coffee, from its composition to its effects on human health. In addition to the nutrients, its various components include caffeine, the diterpenes cafestol and kahweol, and chlorogenic acids, with coffee being an important dietary source of these compounds. Many studies have verified the association between its constituents and health, especially caffeine and high blood pressure, cafestol and kahweol and dyslipidemias, and chlorogenic acids and cardiovascular protection from their antioxidant properties. This article aims to succinctly present the importance and composition of the drink, the physiological mechanisms involved in the increased blood pressure and serum cholesterol attributed to coffee, and selected studies that verified the association between coffee consumption and these cardiovascular diseases.

Estudo fitoquímico e avaliação das atividades moluscicida e larvicida dos extratos da casca do caule e folha de Eugenia malaccensis L. (Myrtaceae) / Phytochemical studies of the extracts of stem bark and leaves of Eugenia malaccensis L. (Myrtaceae) and evaluation of their molluscicidal and larvicidal activities

Eugenia malaccensis L. (Syzygium malaccensis Merr.& Perry), denominada comumente de jambo vermelho, é uma espécie arbórea de ocorrência comum no Brasil e faz parte das plantas medicinais do Estado de Alagoas. Estudos químicos anteriores com E. malaccensis foram realizados com plantas coletadas na Ásia, Oceania e na América Central. Este trabalho descreve o estudo químico do extrato etanólico das folhas e cascas de um espécimem coletado no Estado de Alagoas, Brasil. Considerando-se a escassa literatura sobre o potencial moluscicida e larvicida dessa espécie, buscou-se testar estas atividades contra caramujos Biomphalaria glabrata Say, e frente às larvas do mosquito Aedes aegypti L. Os extratos etanólicos da casca do caule e das folhas foram inativos frente às larvas de Aedes aegypti na concentração de 500 μg/mL, porém, ativos contra Biomphalaria glabrata (CL50 = 42,53 e 41,90 mg/mL, respectivamente). O estudo químico levou ao isolamento e identificação de 5,7,3',4',5'-penta-hidroxi-flavonol (1), 5,7,3',5'-tetra-hidroxi-4'-metoxi-flavonol (2), ácido 3,4,5-tri-hidroxibenzóico (3) e ácido 3-acetil-urs-12-en-28-óico (4) das folhas e da casca do caule. O composto 4 é isolado pela primeira vez no gênero Eugenia. As estruturas desses compostos foram estabelecidas através de estudos no IV, de RMN ¹H e 13C e comparação com dados da literatura.

Eugenia malaccensis L. (Syzygium malaccensis Merr. & Perry), popularly known in Brazil as jambo vermelho, is a very common tree and one of the medicinal plants of Alagoas State, Brazil. Previous chemical studies with E. malaccensis have been carried out with native plants from Asia, Oceania, and Central America. This work describes the chemical study of E. malaccensis L., a specimen collected in Alagoas State. Considering that studies on the molluscicidal and larvicidal potential of E. malaccensis were not reported, this work aimed to test its molluscicidal activity against Biomphalaria glabrata snails and larvicidal activity against Aedes aegypti mosquitos. The ethanolic stem bark and leaf extracts were inactive towards Aedes aegypti larvae. The ethanolic stem bark and leaf extract were active against Biomphalaria glabrata with CL50 = 42.53 and 41.90 mg/mL, respectively. 5,7,3',4',5'-Penta-hydroxy-flavonol (1), 5,7,3',5'-tetra-hydroxy-4'-methoxy-flavonol (2), 3,4,5-tri-hydroxybenzoic acid (3) and 3-acetyl-urs-12-en-28-oic acid (4) were isolated and identified from the leaves and stem bark. The acid 3b-O-acetyl-urs-12-en-28-oic is for the first time isolated from the genus Eugenia. The structures of the compounds have been established by IR, ¹H and 13C NMR spectral analysis and by comparison with literature data.

Anti-bacterial activity of some Brazilian medicinal plants.

Extracts from various organs of 25 plants of Brazilian traditional medicine were assayed with respect to their anti-bacterial activities against Escherichia coli, a susceptible strain of Staphylococcus aureus and two resistant strains of Staphylococcus aureus harbouring the efflux pumps NorA and MsrA. Amongst the 49 extracts studied, 14 presented anti-bacterial activity against Staphylococcus aureus, including the ethanolic extracts from the rhizome of Jatropha elliptica, from the stem barks of Schinus terebinthifolius and Erythrina mulungu, from the stems and leaves of Caesalpinia pyramidalis and Serjania lethalis, and from the stem bark and leaves of Lafoensia pacari. The classes of compounds present in the active extracts were determined as a preliminary step towards their bioactivity-guided separation. No extracts were active against Escherichia coli.

Multidrug resistance reversal agent from Jatropha elliptica.

As part of an ongoing project to identify plant natural products as resistance-modifying agents, bioassay-guided fractionation of an extract of Jatropha elliptica (Pohl) Muell Arg. led to the isolation of a penta-substituted pyridine, namely 2,6-dimethyl-4-phenyl-pyridine-3,5-dicarboxylic acid diethyl ester (8). The structure was established by spectroscopic methods. This known compound was assayed for in vitro antibacterial and resistance-modifying activities against strains of Staphylococcus aureus possessing the MsrA and NorA resistance efflux mechanisms. Antibiotic efflux studies indicated that (8) acts as an inhibitor of the NorA efflux pump and restores the level of intracellular drug concentration.