Mutagenic Evaluation of Fluoxetine and Fluoxetine-Galactomannan Complex Through the Analysis of Chromosomal Aberrations in Human Peripheral Leukocytes and Salmonella typhimurium/Microssome Assay / Avaliação Mutagênica de Fluoxetina e Complexo Fluoxetina-Galactomanana Através da Análise de Aberrações Cromossômicas em Leucócitos Periféricos Humanos e em Salmonella typhimurium / Ensaio Microssômico

Objectives: The purpose of this study was to evaluate the mutagenic potential of fluoxetine and fluoxetine-galactomannan. Methods: Chromosomal aberration test and Salmonella typhimurium/microsome mutagenicity assay. Results: The results showed that fluoxetine (250 µg/mL) can cause chromosomal breaks of treated leukocytes and increase the frequency of reversion of the tester strains of S. typhimurium / microsome assay only at the highest concentration (5 mg/mL), while fluoxetine encapsulated in galactomannan did not cause these changes (leukocytes and S. typhimuriums strains). Conclusion: In summary, fluoxetine showed a mutagenic effect detectable only at high concentrations in both eukaryotic and prokaryotic models. Furthermore, the fluoxetine/galactomannan complex, in this first moment, prevented the mutagenicity attributed to fluoxetine, emphasizing that the present encapsulation process can be an alternative in preventing these effects in vitro.

Objetivos: avaliar o potencial mutagênico da fluoxetina e da fluoxetina-galactomanana. Métodos: Teste de aberração cromossômica e ensaio de mutagenicidade de Salmonella typhimurium /microssoma. Resultados: a fluoxetina (250 µg/mL) pode causar quebras cromossômicas de leucócitos tratados e aumentar a frequência de reversão das cepas testadoras de S. typhimurium /microssoma apenas na concentração mais alta (5 mg/mL), enquanto a fluoxetina encapsulada em galactomanano não causou essas alterações (leucócitos e cepas de S. typhimurium). Conclusão: a fluoxetina mostrou um efeito mutagênico detectável apenas em altas concentrações em modelos eucarióticos e procarióticos. Além disso, o complexo fluoxetina/galactomanan, neste primeiro momento, evitou a mutagenicidade atribuída à fluoxetina, ressaltando que o presente processo de encapsulamento pode ser uma alternativa na prevenção desses efeitos in vitro.

Gastroprotective effect of hydroalcoholic extract from Agaricus blazei Murill against ethanol-induced gastric ulcer in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: The use of mushrooms in medicine is quite old and the first report about the use of genus Agaricus in treatment of ulcers occurred in Byzantine period. This mushroom is widely consumed as food, tea, food supplements, as well as nutraceutical and cosmeceutical applications, being cultivated and appreciated in several countries such as Brazil, Korea, Japan and China. AIM OF THE STUDY: This study aimed to characterize the chemical profile and the potential gastroprotective effect of hydroalcoholic extract from Agaricus blazei Murill (HEAb). MATERIALS AND METHODS: The extract was chemically characterized by elemental analysis, UPLC-QTOF-MSE, Nuclear Magnetic Resonance (NMR) and high-performance liquid chromatography (HPLC) techniques to elucidate the metabolites present in the extract. The quantification of phenolic compounds and the in vitro antioxidant activities were performed and the gastroprotective effect of this extract was evaluated against ethanol-induced gastric ulcer model. HEAb was administered by gavage at 5, 25 and 50 mg kg-1 and N-acetylcysteine at 300 mg kg-1 (positive control). Furthermore, the pathways of nitric oxide (NO), Cyclic Guanylate Monophosphate (cGMP), prostaglandins (PGs) and the involvement of ATP-sensitive K+ Channels were modulated. RESULTS: Mannitol, malic acid, pyroglutamic acid, L-agaritine and L-valine were putatively identified by UPLC-QTOF-MSE in HEAb. In addition, it was possible to identify mannitol by the intense signals in the NMR spectra, being still quantified as the main compound in the extract by HPLC. The contents of total phenols and flavonoids corroborated with the good antioxidant activity of HEAb. This study observed that HEAb at 25 and 50 mg kg-1 had gastroprotection effect demonstrated by the reduction of histopathological parameters and the reduction of mastocytosis in the stomach of mice. CONCLUSIONS: In this study was possible to conclude that HEAb has gastroprotective effect related to the involvement of NO and PG pathways in the ethanol-induced gastric ulcer model in mice.

Hypolipidemic and reduced nitrergic effects of p-hydroxycinnamic diesters extracted from Copernicia prunifera in mice challenged by a high-fat diet.

Dyslipidemia is a chronic non-transmissible condition that has increased due to an unhealthy lifestyle. Statins have been used as the standard treatment to control hyperlipidemia. However, side effects and high costs may be associated with its prolonged treatment, so plants derivatives have been an attractive therapy to overcome these problems. Among the compounds extracted from plants, the p-hydroxycinnamic diesters (HCE), present in carnauba wax (CW), have been found with good pharmacological properties. Therefore, this study aimed to evaluate the potential anti-hypercholesterolemic and possible toxicological effects of HCE in C57BL/6J mice under a high-fat (HF) diet. Male C57BL/6J mice were fed during 60 days under the HF diet and therefore were either treated with HCE (200 and 400 mg/kg) or simvastatin (20 mg/kg) or received saline (controls) by gavage for 30 days under the same diet. HCE treatment was able to reduce serum total cholesterol and LDL levels. Besides, this compound increased liver X receptor (LXR) and but not significantly affected IL-1ß and TNF-α liver mRNA transcription activity. In conclusion, HCE treatment was found safe and may attenuate the deleterious effects of dyslipidemia due to chronic feeding with western diets.

Chemopreventive effect of troxerutin against hydrogen peroxide-induced oxidative stress in human leukocytes through modulation of glutathione-dependent enzymes.

Troxerutin is a natural flavonoid present abundantly in tea, coffee, olives, wheat, and a variety of fruits and vegetables. Due to its diverse pharmacological properties, this flavonoid has aroused interest for treatment of various diseases, and consequently prompted investigation into its toxicological characteristics. The aim of this study was to evaluate the genotoxic and mutagenic effects and chemoprotective activity attributed to troxerutin using human peripheral blood leukocytes (PBLs) through several well-established experimental protocols based upon different parameters. Data demonstrated that troxerutin (100 to 1000 µM) induced no marked cytotoxic effect on PBLs after 24 hr, and did not produce strand breaks and mutagenicity. Regarding chemoprevention, this flavonoid attenuated cytotoxicity, genotoxicity, and mutagenicity initiated by hydrogen peroxide (H2O2) in human PBLs. Further, troxerutin demonstrated no marked cytotoxic effect on PBLs and exerted a protective effect against oxidative stress induced by H2O2 through modulation of GSH-dependent enzymes.

Role of Rutin in 5-Fluorouracil-Induced Intestinal Mucositis: Prevention of Histological Damage and Reduction of Inflammation and Oxidative Stress.

Intestinal mucositis, characterized by inflammatory and/or ulcerative processes in the gastrointestinal tract, occurs due to cellular and tissue damage following treatment with 5-fluorouracil (5-FU). Rutin (RUT), a natural flavonoid extracted from Dimorphandra gardneriana, exhibits antioxidant, anti-inflammatory, cytoprotective, and gastroprotective properties. However, the effect of RUT on inflammatory processes in the intestine, especially on mucositis promoted by antineoplastic agents, has not yet been reported. In this study, we investigated the role of RUT on 5-FU-induced experimental intestinal mucositis. Swiss mice were randomly divided into seven groups: Saline, 5-FU, RUT-50, RUT-100, RUT-200, Celecoxib (CLX), and CLX + RUT-200 groups. The mice were weighed daily. After treatment, the animals were euthanized and segments of the small intestine were collected to evaluate histopathological alterations (morphometric analysis); malondialdehyde (MDA), myeloperoxidase (MPO), and glutathione (GSH) concentrations; mast and goblet cell counts; and cyclooxygenase-2 (COX-2) activity, as well as to perform immunohistochemical analyses. RUT treatment (200 mg/kg) prevented 5-FU-induced histopathological changes and reduced oxidative stress by decreasing MDA concentrations and increasing GSH concentrations. RUT attenuated the inflammatory response by decreasing MPO activity, intestinal mastocytosis, and COX-2 expression. These results suggest that the COX-2 pathway is one of the underlying protective mechanisms of RUT against 5-FU-induced intestinal mucositis.

Troxerutin Prevents 5-Fluorouracil Induced Morphological Changes in the Intestinal Mucosa: Role of Cyclooxygenase-2 Pathway.

Intestinal mucositis is a common complication associated with 5-fluorouracil (5-FU), a chemotherapeutic agent used for cancer treatment. Troxerutin (TRX), a semi-synthetic flavonoid extracted from Dimorphandra gardneriana, has been reported as a potent antioxidant and anti-inflammatory agent. In the present study, we aimed to evaluate the effect of TRX on 5-FU-induced intestinal mucositis. Swiss mice were randomly divided into seven groups: Saline, 5-FU, TRX-50, TRX-100, TRX-150, Celecoxib (CLX), and CLX + TRX-100. The weight of mice was measured daily. After treatment, the animals were euthanized and segments of the small intestine were collected to evaluate histopathological alterations (morphometric analysis), levels of malondialdehyde (MDA), myeloperoxidase (MPO), glutathione (GSH), mast and goblet cell counts, immunohistochemical analysis, and cyclooxygenase-2 (COX-2) activity. Compared to the saline treatment, the 5-FU treatment induced intense weight loss and reduction in villus height. TRX treatment (100 mg/kg) prevented the 5-FU-induced histopathological changes and decreased oxidative stress by decreasing the MDA levels and increasing GSH concentration. TRX attenuated inflammatory process by decreasing MPO activity, intestinal mastocytosis, and COX-2 expression. TRX also reversed the depletion of goblet cells. Our findings suggest that TRX at a concentration of 100 mg/kg had chemopreventive effects on 5-FU-induced intestinal mucositis via COX-2 pathway.

Photoprotective potential of medicinal plants from Cerrado biome (Brazil) in relation to phenolic content and antioxidant activity.

Photooxidative damage affects cellular lipids, proteins and DNA in addition to being involved in the pathobiochemistry of erythema formation, premature skin aging, photodermatoses development and skin cancer. Phenolic compounds, flavonoids and hydroxycinnamic acid esters protect plant tissues against harmful UV-radiation. This study aimed to evaluate the sun protection factor of several Brazilian plant extracts in relation to UVB radiation absorption, which causes skin cancer, and to correlate the findings with their antioxidant activity, as well as with total phenol and flavonoid content. The antioxidant activity of the extracts were evaluated using the DPPH radical scavenging test. The photoprotective effect was evaluated using the methodology developed by Mansur. The antioxidant activity from the extracts showed IC50 values ranging from 4.91 to 132.24 µg/mL when compared to the standard quercetin with an IC50 of 5.01 µg/mL; the phenolic content varied from 3.77 to 57.14 mg GAE/g extract while flavonoid content varied from 1.80 to 5.89 mg EQ/g extract. Almost all extracts showed a potential for UVB radiation absorption in accordance with the ANVISA (Agência Nacional de Vigilância Sanitária) technical regulation for cosmetic sunscreens. The extracts with greater sun protection factors were those originating from Lippia microphylla (SPF = 26.82) and Dimorphandra gardneriana (SPF = 20.12). A sun protection factor of 15 or higher contributes to protect the skin, where the presence of sakuranetin flavonoids and quercetin glycosides contribute to this action.

Corrigendum to "Antihypercholesterolemic Effects of Fruit Aqueous Extract of Copernicia prunifera (Miller) H. E. Moore in Mice Diet-Induced Hypercholesterolemia".

[This corrects the article DOI: 10.1155/2017/6376173.].

Antihypercholesterolemic Effects of Fruit Aqueous Extract of Copernicia prunifera (Miller) H. E. Moore in Mice Diet-Induced Hypercholesterolemia.

The present objective of the investigation is to evaluate the antihypercholesterolemic activity of the aqueous fruit pulp extract (APE) of Copernicia prunifera (Miller) H. E. Moore (Arecaceae family). Various chemical characterization methods like thin layer chromatography, Fourier transform infrared spectroscopy, 1H and 13C NMR, and molecular weight by gel permeation chromatography have been employed to characterize the extracted pectin. The present study demonstrated that hypercholesterolemic diet (HD) created hypercholesterolemia, caused significant increases in body weight, total cholesterol, and low-density lipoprotein, and caused decreases in high-density lipoprotein in serum compared with SD group. Two doses (APE 150 and 300 mg/Kg b.w./day) were administered to hyperlipidemic mice for 90 days. APE reversed body weight changes, changed serum lipids to normal values, and significantly inhibited the changes of lipid peroxidation and inflammation in the liver tissues. The renal parameters analyzed (urea and creatinine) altered by diet were reverted to normal values. Our results revealed that aqueous fruit pulp extracts of carnauba reduced hypercholesterolemia showing a potential preventive effect against cardiovascular diseases without side effects cause.

Antioxidant activity and physicochemical analysis of passion fruit (Passiflora glandulosa Cav) pulp native to Cariri region / Atividade antioxidante e análise físico-química da polpa do maracujá (Passiflora glandulosa Cav) nativo da região do Cariri

The objective of this study was to determine the proximal composition, the physical and chemical characteristics and the in vitro antioxidant capacity (DPPH, ABTS and FRAP) of the pulp of the wild passion fruit (Passiflora glandulosa Cav.) from Cariri region, Ceara, Brazil. The results showed that the proximal composition and the caloric value of this passion fruit are similar to other species, but with a high ascorbic acid content. The fruit pulp showed low level of antioxidant activity and low level of polyphenolic compounds followed by three methodologies used. Due to high levels of titratable acidity (3.52) and total soluble solids (17.80° Brix), this fruit can be considered as a high value fruit for commerce. However, it is a species of passion fruit with few studies described in the literature, and more research is needed to assess its nutritional and functional potential.

O objetivo do estudo foi determinar a composição centesimal, as características físicas e químicas e a capacidade antioxidante (DPPH, ABTS e FRAP) in vitro da polpa do maracujá-do-mato (Passiflora glandulosa Cav.) da região do Cariri, Ceará, Brasil. Os resultados demonstraram que a composição centesimal e o valor calórico desse tipo de maracujá são similares a outras espécies, mas com nível elevado de ácido ascórbico. A polpa apresentou baixo teor de polifenóis e baixa atividade antioxidante para as três metodologias aplicadas. Em razão dos altos níveis de acidez titulável (3,52) e sólidos solúveis totais (17,80° Brix), este fruto pode ser considerado como um fruto de alto valor para o comércio. Porém, esta é uma espécie de maracujá pouco descrita na literatura, sendo necessárias mais análises para avaliar seu potencial valor nutricional e funcional.

Screening of Bioactivities and Toxicity of Cnidoscolus quercifolius Pohl.

The caatinga, an exclusively Brazilian biome, is one of the most endangered vegetation systems in the planet. To be exploited rationally, its potential needs to be scientifically demonstrated. Among these is the faveleira, used in northeastern Brazil. It stands out for its extraordinary drought resistance and medicinal properties. The objective of this study was to assess the therapeutic potential of compounds extracted from Cnidoscolus quercifolius Pohl in preventing disease and its rational use as a herbal therapeutic tool. The methodology began with the collection and herborization of the plant material, to obtain the chemical compounds, preliminary phytochemical analysis, and extraction of the constituents of the active extracts. To determine the biological activities the authors conducted investigation of antioxidant and antimicrobial activities, inhibition capacity of the acetylcholinesterase enzyme, and initial assessment of toxicity of the extracts. The results demonstrated great potential as an antimicrobial agent, an important antioxidant capacity, and acetylcholinesterase inhibition response with no significant difference compared with the reference drug. The authors expect to develop a new herbal product, resulting in lower production costs and that, consequently, could be commercialized in more accessible form to the population, highlighting the risk reduction of contraindication of this category of medications.

Carnauba wax p-methoxycinnamic diesters: Characterisation, antioxidant activity and simulated gastrointestinal digestion followed by in vitro bioaccessibility.

The beneficial biological effects of cinnamic acid derivatives and the lack of studies on the antioxidant activity and bioavailability of cinnamic esters from carnauba wax, diesters were extracted from carnauba wax powder. Their structural, physical and morphological characteristics, antioxidant activity and in vitro bioaccessibility were measured. p-Methoxycinnamic diester (PCO-C) was identified, which has a crystalline, apolar structure and exhibited significant antioxidant activity (107.27 ± 3.92 µM Trolox/g of dry weight) before and after simulated in vitro gastrointestinal digestion and 32.46% bioaccessibility. In human cells, PCO-C (250 µg/mL) inhibited the production of intracellular reactive oxygen species, with an effect similar to that of Trolox (80 µM). Thermogravimetric analysis showed that PCO-C had high thermal stability and high UV absorption between 250 and 350 nm. These results indicate that this compound is promising as an antioxidant for pharmaceutical and food industry applications, such as the development of active packaging and functional foods.

Occurrence of fungi and aflatoxins B in nuts and products marketed the Brazilian northeastern regions / Ocorrência de fungos e aflatoxinas do tipo B em castanhase produtos comercializados no nordeste brasileiro

Aflatoxin contamination has been considered as a public health problem, especially in tropical countries, including Brazil. In order to investigate the presence of type B aflatoxins in products marketed in the city of Fortaleza, 23 samples were analyzed by thin layer chromatography.Visible fungal contamination in food was identified according to their macroscopic and microscopic features. The contamination by aflatoxins was detected in 8.7 % of 23 analyzedsamples, and 12.5 % of Brazilian nuts samples were positive for AFB1 (<8 µg/kg) and for AFB2 in a contamination rate above the allowed value (16 µg/kg). Among the peanut samples,33.3 % were positive to AFB1 and AFB2, also in a contamination rate (317.1 µg/kg) which was higher than that recommended by ANVISA. The isolation and morphological characteristics of fungi detected mainly in Brazilian nuts with peel showed the occurrence of the followingspecies: Aspergillus flavus, Aspergillus niger, Mucor sp, Cladosporium sphaerospermum, Cladosporium cladosporoides, Fusarium sp, Aspergillus terreus and bacteria of Actinomycetes phylum. These findings indicate that it is needed to apply the mostly effective quality monitoringof food available to consumers.

A contaminação por aflatoxinas tem sido considerada um problema de saúde públicaprincipalmente em países tropicais, incluindo o Brasil. Com o intuito de investigar a presença de aflatoxinas do tipo B em produtos comercializados na cidade de Fortaleza, 23 amostrasforam analisadas por meio de cromatografia em camada delgada. Os fungos visivelmentepresentes em alimentos foram identificados de acordo com suas características macroscópicase microscópicas. A contaminação por aflatoxina foi detectada em 8,7 % das 23 amostrasanalisadas; e 12,5 % das amostras de castanha-do-Brasil apresentaram positividade paraAFB1 (<8 μg/kg) e para AFB2 com taxa de contaminação acima do valor permitido (16 μg/kg). Quanto às amostras de amendoim, 33,3 % apresentaram positividade para AFB1 e AFB2, também com nível de contaminação (317,1 μg/kg) acima do preconizado pela ANVISA. O isolamento e a caracterização morfológica dos fungos encontrados principalmente nas castanhas-do-Brasilcom casca revelaram a presença das espécies: Aspergillus flavus, Aspergillus niger, Mucor sp, Cladosporium sphaerospermum, Cladosporium cladosporoides, Fusarium sp, Aspergillus terreuse bactérias do filo Actinomicetos. Estes resultados demonstram que há necessidade de fiscalização mais efetiva da qualidade dos alimentos oferecidos aos consumidores.

Occurrence of fungi and aflatoxins B in nuts and products marketed the Brazilian northeastern regions / Ocorrência de fungos e aflatoxinas do tipo B em castanhas e produtos comercializados no Nordeste brasileiro

Aflatoxin contamination has been considered as a public health problem, especially in tropical countries, including Brazil. In order to investigate the presence of type B aflatoxins in products marketed in the city of Fortaleza, 23 samples were analyzed by thin layer chromatography. Visible fungal contamination in food was identified according to their macroscopic and microscopic features. The contamination by aflatoxins was detected in 8.7 % of 23 analyzed samples, and 12.5 % of Brazilian nuts samples were positive for AFB1 (<8 µg/kg) and for AFB2 in a contamination rate above the allowed value (16 µg/kg). Among the peanut samples, 33.3 % were positive to AFB1 and AFB2, also in a contamination rate (317.1 µg/kg) which was higher than that recommended by ANVISA. The isolation and morphological characteristics of fungi detected mainly in Brazilian nuts with peel showed the occurrence of the following species: Aspergillus flavus, Aspergillus niger, Mucor sp, Cladosporium sphaerospermum, Cladosporium cladosporoides, Fusarium sp, Aspergillus terreus and bacteria of Actinomycetes phylum. These findings indicate that it is needed to apply the mostly effective quality monitoring of food available to consumers.

A contaminação por aflatoxinas tem sido considerada um problema de saúde pública principalmente em países tropicais, incluindo o Brasil. Com o intuito de investigar a presença de aflatoxinas do tipo B em produtos comercializados na cidade de Fortaleza, 23 amostras foram analisadas por meio de cromatografia em camada delgada. Os fungos visivelmente presentes em alimentos foram identificados de acordo com suas características macroscópicas e microscópicas. A contaminação por aflatoxina foi detectada em 8,7 % das 23 amostras analisadas; e 12,5 % das amostras de castanha-do-Brasil apresentaram positividade para AFB1 (<8 µg/kg) e para AFB2 com taxa de contaminação acima do valor permitido (16 µg/kg). Quanto às amostras de amendoim, 33,3 % apresentaram positividade para AFB1 e AFB2, também com nível de contaminação (317,1 µg/kg) acima do preconizado pela ANVISA. O isolamento e a caracterização morfológica dos fungos encontrados principalmente nas castanhas-do-Brasil com casca revelaram a presença das espécies: Aspergillus flavus, Aspergillus niger, Mucor sp, Cladosporium sphaerospermum, Cladosporium cladosporoides, Fusarium sp, Aspergillus terreus e bactérias do filo Actinomicetos. Estes resultados demonstram que há necessidade de fiscalização mais efetiva da qualidade dos alimentos oferecidos aos consumidores.

Antiviral and Antioxidant Activities of Sulfated Galactomannans from Plants of Caatinga Biome.

Dengue represents a serious social and economic public health problem; then trying to contribute to improve its control, the objective of this research was to develop phytoterapics for dengue treatment using natural resources from Caatinga biome. Galactomannans isolated from Adenanthera pavonina L., Caesalpinia ferrea Mart., and Dimorphandra gardneriana Tull were chemically sulfated in order to evaluate the antioxidant, and antiviral activities and the role in the inhibition of virus DENV-2 in Vero cells. A positive correlation between the degree of sulfation, antioxidant and antiviral activities was observed. The sulfated galactomannans showed binding to the virus surface, indicating that they interact with DENV-2. The sulfated galactomannans from C. ferrea showed 96% inhibition of replication of DENV-2 followed by D. gardneriana (94%) and A. pavonina (77%) at 25 µg/mL and all sulfated galactomannans also showed antioxidant activity. This work is the first report of the antioxidant and antiviral effects of sulfated galactomannans against DENV-2. The results are very promising and suggest that these sulfated galactomannans from plants of Caatinga biome act in the early step of viral infection. Thus, sulfated galactomannans may act as an entry inhibitor of DENV-2.

Antiherpetic activity of an Agaricus brasiliensis polysaccharide, its sulfated derivative and fractions.

Agaricus brasiliensis is an edible mushroom, traditionally used for the treatment of several diseases. In this paper, a polysaccharide (PLS) from A. brasiliensis, its carboxymethylated (CPLS) and sulfated (SPLS) derivatives, as well as, fractions (F1-F3) obtained from the PLS were investigated for their effect in the replication of herpes simplex virus and bovine herpes virus in HEp-2 cell cultures. The PLS, SPLS and F3 inhibited both virus strains similarly, in a dose-dependent curve. F1, F2 and CPLS did not show significant effect even at higher concentrations. All the compounds showed neither virucidal or viral adsorption inhibition activities nor effect when cells were treated prior to infection. Our study demonstrated that the extracts of A. brasiliensis, can be promising for future antiviral drug design and its biotechnological production is economically feasible.

Different susceptibilities of Leishmania spp. promastigotes to the Annona muricata acetogenins annonacinone and corossolone, and the Platymiscium floribundum coumarin scoparone.

Leishmaniasis is a zoonotic disease that can manifest itself in visceral and cutaneous form. The aim of this study was to search for new leishmanicidal compounds. Preliminarily, Artemia salina assay was applied to compounds from two plants found in Northeastern Brazil, Platymiscium floribundum and Annona muricata. Then these compounds were tested against three Leishmania species (Leishmania donovani, Leishmania mexicana and Leishmania major). A screening assay using luciferase-expressing promastigote form were used to measure the viability of promastigote One coumarin, scoparone, isolated from P. floribundum and two acetogenins, annonacinone and corossolone isolated from A. muricata showed leishmanicidal activity in all species tested. Nevertheless, Leishmania species indicated different susceptibilities in relation to the tested compounds: L. mexicana was more sensitive to scoparone followed by L. major and L. donovani. The three species presented similar inhibition to corossolone and annonacinone. Acetogenin annonacinone (EC(50)=6.72-8.00 µg/mL) indicated high leishmanicidal activity; corossolone (EC(50)=16.14-18.73 µg/mL) and scoparone (EC(50)=9.11-27.51 µg/mL) moderate activity. A. saline larvae were less sensitive to the coumarin scoparone and acetogenin corossolone was the most toxic. In conclusion, the leishmanicidal activity demonstrated by the coumarin and acetogenins indicate these compounds for further studies aiming the development of new leishmanicidal agents.

Chemical composition, antioxidant and antibacterial activities of two Spondias species from Northeastern Brazil.

CONTEXT: The leaves of Spondias tuberosa Arr. Cam. (Anacardiaceae) and Spondias mombin L. have been traditionally used for medicinal purposes. Some studies reveal their antibacterial, antimicrobial, and antiviral properties. OBJECTIVE: Determine the chemical composition, antioxidant, and antimicrobial activities of Spondias species to justify its ethnopharmacological use. MATERIALS AND METHODS: Spondias species extracts were prepared with methanol:water 80:20 and analyzed by silica gel column chromatography and reversed phase liquid chromatography (HPLC). The antioxidant activity was evaluated by scavenging the radicals 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) and 2,2-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS•+) and measuring antimicrobial activity (agar well diffusion method, minimum inhibitory concentration and minimum bactericidal concentrations). RESULTS: The HPLC analysis of Spondias extracts demonstrated the occurrence of high yield of flavonoids. Found in S. mombin were quercetin (2.36 ± 0.01 mg/g) and ellagic acid (41.56 ± 0.01 mg/g) and in S. tuberosa species rutin (53.38 ± 1.71 mg/g), quercetin (24.46 ± 0.87 mg/g), and ellagic acid (169.76 ± 0.17 mg/g). The antibacterial activity of the extracts against the various bacteria strains varied from 8.8 to 20.1 mm. MIC values from 62.5 to 125 µg/mL were satisfactory when compared with other plant products. Medium DPPH scavenging activity IC50 for Spondias extracts varied from 0.042 to 0.558 mg/mL and for ABTS from 0.089 to 0.465 mg/mL. DPPH scavenging activity for constituent ellagic acid IC50 = 0.042 mg/mL and for quercetin IC50 = 0.081 mg/mL. DISCUSSION AND CONCLUSION: The chemical study of Spondias leaf extracts showed the occurrence of quercetin, rutin and ellagic acid, substances with relevant antioxidant and antimicrobial activities.

Antioxidant, larvicidal and antiacetylcholinesterase activities of cashew nut shell liquid constituents.

Anacardic acid, cardanol and cardol, the main constituents of natural cashew nut shell liquid (CNSL), were obtained by solvent extraction and assayed for antioxidant, larvicidal and antiacetylcholinesterase activity. Their relative percent composition was obtained by HPLC analysis. Antioxidant activity was assessed using the DPPH and ABTS(+) tests, which showed cardanol as the most active, followed by cardol and anacardic acid. The three CNSL components demonstrated good larvicidal activity against Aedes aegypti (LC(50)=12.40 for anacardic acid, 10.22 for cardol and 14.45 for cardanol) and exhibited inhibition zones for acetylcholinesterase enzymes in the TLC test similar to carbachol, which was used as standard. Based on the results, these multipotent compounds represent promising agents in the control of Ae. aegypti, the main dengue vector in Brazil.