Couroupita guianensis bark decoction: From Amazonian medicine to the UHPLC-HRMS chemical profile and its role in inflammation processes and re-epithelialization.

ETHNOPHARMACOLOGICAL RELEVANCE: In the Amazon rainforest, the shamans of the Mayantuyacu site use the healing virtues of decoctions and teas from different parts of the Couroupita guianensis Aubl. (Lecythidaceae) trees as remedies in Ashaninka medicine. However, composition of the remedy and the underlying mechanism remain unclear. AIM OF THE STUDY: This study was designed to compare the metabolite profile of Couroupita guianensis bark decoction produced by Amazonian shamans with that obtained under standardised laboratory conditions and to investigate biological properties of both decoction and isolated constituents in skin wound healing process and inflammation. MATERIALS AND METHODS: The chemical analyses were carried out by Ultra-High-Performance Liquid Chromatography coupled with UV and High-Resolution Mass Spectrometry detectors (UHPLC-UV-HRMS). 1D and 2D-NMR experiments were performed to identify the main decoction constituents. The decoction and pure compound effect on keratinocyte migration was determined by the in vitro wound healing model; the mechanism of action was elucidated by western blot analysis. RESULTS: UHPLC-UV-HRMS analysis revealed the occurrence of polyphenolic compounds as catechins, ellagitannins and, notably, of unusual sulphated derivatives of ellagic acid isolated for the first time from Couroupita guianensis bark. A new natural sulphated molecule [4-(2″-O-sulphate- ß-D-glucuronopyranosyl) ellagic acid] was identified as the potential active compound responsible for the efficacy of bark decoction stimulating wound healing in human HaCaT keratinocytes. The molecular mechanism involved the induction of pro-migratory pathways mediated by ERK and AKT phosphorylation and the increase of MMP2 expression in HaCaT cells. At the same time, the treatment inhibited inflammation interfering with NFkB activation. CONCLUSION: Beyond identifying a new bioactive compound, the overall results scientifically validate the traditional use of Couroupita guianensis bark decoction as an anti-inflammatory remedy. Moreover, the beneficial effects on keratinocytes suggest promising therapeutic applications in skin diseases.

Biological applications of green synthesized lanthanum oxide nanoparticles via Couroupita guianensis abul leaves extract.

In this work, extract from leaves of Couroupita guianensis (C.guianensis) abul was used as a potential reducing agent for the synthesis of lanthanum oxide (La2O3) nanoparticles (NPs). In addition, the morphology and several physicochemical properties of the La2O3 NPs were improved by introducing the ionic liquid of 1-butyl 3-methyl imidazolium tetra fluoroborate (BMIM BF4) as a stabilizing agent. The structure of the La2O3 (without ionic liquid) and IL-La2O3 (with ionic liquid) NPs were analyzed by X-ray diffraction (XRD). The chemical composition of the synthesized NPs was analyzed using the energy dispersive X-ray (EDX) and X-ray photoelectron spectroscopy (XPS) studies. Optical and morphological studies were also performed. The antibacterial, antioxidant, anti-inflammatory, anti-diabetic and anticancer properties of the La2O3 and IL-La2O3 NPs were evaluated.

Phytochemical profile and ethnopharmacological applications of Lecythidaceae: An overview.

ETHNOPHARMACOLOGICAL RELEVANCE: The family Lecythidaceae has about 25 genera and 400 identified species, which are distributed especially in the pantropical region, mostly found in the tropics of Central and South America, Southeast Asia and Africa. The third most abundant family in Amazonian forests and the genus Eschweilera, with the large number of species in Lecythidaceae. AIM OF THE REVIEW: The present review compiles information since the 1934s about of ethnopharmacology, and chemical constituents of species of Lecythidaceae, as well as a summary of the bioactivities shown by the extracts, fractions, and secondary metabolites. MATERIALS AND METHODS: All relevant information on ethnopharmacology, and chemical constituents of species of Lecythidaceae were gathered from electronic databases including Web of Science, Science Direct, Elsevier, ResearchGate, and Google Scholar. Information was also obtained from local books, PhD. and MSc. Dissertations. RESULTS: The phytochemical diversity of the family was demonstrated with 180 different metabolites that have been reported from 25 species, most of them being triterpenes or flavonoids. The pharmacological studies carried out with the extracts, fractions and compounds showed promising antibacterial, antifungal, anti-inflammatory, antinociceptive, cytotoxic and antioxidant activities. CONCLUSION: The present review provides an insight into ethnopharmacology, phytochemistry and pharmacology of species of Lecythidaceae. Based on the pharmacological studies it has been found that different plant species of Lecythidaceae possess a wide range of bioactivities such as anti-arthritic, anti-inflammatory, antileishmanial, antibacterial and antifungal. These activities are due to the presence of bioactive compounds including triterpenoids and their glycosides derivatives, flavonoids, steroids, sesquiterpenoids, alkaloids, and other compounds. However, there are many plants, which have not been assessed pharmacologically and hence warrant further studies.

Methanolic extract of Cariniana rubra Gardner ex Miers stem bark negatively regulate the leukocyte migration and TNF-α and up-regulate the annexin-A1 expression.

ETHNOPHARMACOLOGICAL RELEVANCE: Cariniana rubra Gardner ex Miers (Lecythidaceae), is a native and endemic tree in Brazil, whose inner stem bark decoction preparation is used in folk medicine to treat various inflammatory disorders. Previous scientific reports confirmed its popular use as an anti-inflammatory, without, however, evaluating its action mechanisms. AIM: The objective of this study was to determine the cytotoxicity and anti-inflammatory mechanism of action of the methanolic extract of Cariniana rubra (MECr), using experimental models in vivo and in vitro, as well as to identify secondary metabolites present in the extract. MATERIAL AND METHODS: The MECr was prepared by maceration of inner stem bark powder in methanol (1:10 w/v). The in vitro cytotoxicity effect was evaluated in CHO-k1 cells. The Hippocratic screening test was conducted to evaluate the acute toxicity of MECr in mice. The actions of MECr on leukocyte migration, cytokine levels (IL-1ß and TNF-α) and annexin-A1 (AnxA1) expression, were carried out on lambda-type carrageenan air pouch inflammation model in Swiss mice. Additionally, the phytochemical analysis of MECr was carried out by thin-layer chromatography (TLC) and spectrometric mass analysis with electrospray ionization ESI(-)/MS and gas chromatography-mass spectrometry (GC-MS). RESULTS: Treatment of CHO-k1 cells for 24 h with MECr did not cause cytotoxicity (IC50 > 200 µg/mL), however, the MECr was shown to be cytotoxic after 72 h of cell exposure (IC50 = 19.90 ± 3.51 µg/mL). In the Hippocratic test, oral treatment of mice with 750, 1500, or 3000 mg/kg of MECr did not show any histopathological changes and mortality during the 14 days of observation. In the carrageenan air pouch inflammation model, MECr reduced (p < 0.001) polymorphonuclear migration (57.7% and 57.8%), leukocyte monocyte migration (74.5% and 61.8%) in the air pouch cavity and in the skin tissue, respectively. MECr also inhibited TNF-α concentration in the air cavity wash (3.2%, p < 0.01) and increased expression of the AnxA1 protein (26.9%, p < 0.01) in the skin tissue, particularly in neutrophils. ß-sitosterol (1.95%), gallic acid (1.24%), ß-amyrin (0.87%) and stigmasterol (0.66%) were identified as the major constituents in methanolic extract. CONCLUSION: MECr exhibits significant anti-inflammatory action at least by increasing AnxA1 expression and by inhibiting the release of TNF-α pro-inflammatory cytokine and leukocyte migration, which is probably linked to the presence of identified biologically active compounds, especially gallic acid and terpenes. We believe that the results of this study provide a pharmacological basis for the MECr to be considered as a potential therapeutic agent for the treatment of inflammatory diseases.

Stability of a Natural-Based Cream Containing Lecythis pisonis Extract.

The outer pericarps of Lecythis pisonis Camb. are by-products with a high content of antioxidant substances. The goal of the present study was to analyze the incorporation of L. pisonis pericarp extract in an all-natural formulation. Physical-chemical and organoleptic characteristics and Challenge tests were evaluated before and after the stability test of the cosmetic formulation. The instability of the formulation increased with the increase of the concentration of the extract. The physical-chemical and organoleptic parameters did not present alterations after the stability test. The extract of the outer pericarp of L. pisonis seems to be compatible with the cream formulation. However, the concentration should be analyzed to not interfere with the stability of the product. The natural formulation developed is under the legal requirements of the National Agency of Sanitary Monitoring of Brazil (Agência Nacional de Vigilância Sanitária), presenting an efficient conservation system.

Antitubercular compounds isolated and characterized in Tithonia diversifolia and Couroupita guianensis.

Background: Tuberculosis (TB) has become a public health challenge in the current scenario with a single causative agent, Mycobacterium tuberculosis (MTB) causing the highest morbidity and mortality affecting almost 1.7 million of the population. Furthermore, there has been no novel drug discovery for the past five decades, and the emergence of latent, multiple drug-resistant, and extensively drug-resistant species has given rise to an alarming necessity for a novel compound/s for treating this highly untamable microbe. In developing countries, plant-based drugs have shown promising results in combating TB or its symptoms; naturally occurring secondary metabolites can act as lead-drug molecules or can be co-administered with conventional drugs. Therefore, the present study was focused to identify and characterize potential antimycobacterial compounds found in the screened ethnobotanical plants, Tithonia diversifolia (TD) and Couroupita guianensis (CG). These plants are used for treating respiratory disorders and allergies in the traditional medicinal systems. Methods: These plant leaf extracts were detected and purified using chromatographic techniques for potent antitubercular phytochemicals, and the purified eluents were tested on Mycobacterium smegmatis (MSM) as a surrogate for MTB; further, the fractions inhibiting growth of MSM were characterized through gas chromatography-mass spectrometry. A toxicity test of the purified samples was also assessed by an in vitro 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide reduction and hemolytic assays. Results: The analyzed plant extracts showed the presence of a C-15 sesquiterpene, zingiberene in TD, and a phthalate ester, bis (2-ethylhexyl) phthalate, in CG leaf extracts. The toxicity assessment proved the purified fractions to be moderately toxic at higher concentrations (≥100 µg/mL). Conclusion: Therefore, the identified compounds can be promising antitubercular agents; however, further in vivo investigations will add substantial value to the compounds being pharmacologically useful.

Potencial antimicrobiano do extrato metanólico de Cariniana parvifolia contra patógenos alimentares / Antimicrobial potential of metanolic extract of Cariniana Parvifolia against food pathogens

O presente estudo objetivou avaliar a atividade antimicrobiana do extrato de Cariniana parvifolia contra dois importantes patógenos em alimentos. Para isso, o extrato foi diluído em DMSO nas concentrações 250 mg/mL a 1,95 mg/mL e a atividade antibacteriana foi testada frente as cepas padrões de Escherichia coli ATCC25922 e Staphylococcus aureus ATCC43300por meio da técnica de microdiluição em placa.A concentração inibitória mínima obtida para ambas as cepas foi de 250 mg/mL, enquanto a concentração bactericida mínima foi > 250 mg/mL para S. aureus e 250 mg/mL para E. coli. O extrato metanólico de Cariniana parvifolia apresenta atividade antimicrobiana contra os patógenos S. aureus e E. coli na concentração de 250 mg/mL.

Alternative vibro-dynamic compression processing of wood-cement composites using Amazonian wood

Wood-cement composite (WCC) is a potential construction material for tropical regions, due to its physico-mechanical properties and resistance to decay and fungi attack. However it is important to test alternative production methods and wood materials that are easier and cheaper than those traditionally used, in order to create a higher demand for this product. The aim of this work was to evaluate the use of wood from four Amazonian species (Eschweilera coriaceae, Swartzia recurva, Manilkara amazonica and Pouteria guianensis) in the production of wood-cement composites through a vibro-dynamic compression process, an alternative method to the use of a hydraulic press. The inhibition degree caused by the wood to the cement cure, measured by the factor CA, indicated that all species were compatible with Portland cement (CP II-Z). WCC with densities higher than 1,100 kg m-3 (produced with E. coriaceae and S. recurva particles) showed compressive strength values higher than 10 MPa, which fulfills the minimum requirement for lightweitgh reinforced concrete blocks for structural use. (AU)

Compósito madeira-cimento é um potencial material de construção para regiões tropicais, devido a suas propriedades físico-mecânicas e resistência ao ataque de fungos e podridão. Contudo, é importante testar métodos alternativos de produção e madeiras que sejam mais simples e baratos do que os tradicionalmente usados, para que se alcance uma maior demanda para esse produto. O objetivo deste estudo foi avaliar o uso de madeira de quatro espécies amazônicas (Eschweilera coriaceae, Swartzia recurva, Manilkara amazonica e Pouteria guianensis) na produção de compósitos de madeira-cimento (WCC) pelo processo de compactação vibro-dinâmica, um método alternativo que dispensa o uso de prensas hidráulicas. O grau de inibição à pega do cimento causado pela presença da madeira foi medido pelo fator CA e indicou que todas as quatro espécies foram compatíveis com o cimento Portland (CP II-Z). Compósitos com massa específica superior a 1.100 kg m-3 (produzidas com partículas de E. coriaceae e S. recurva) apresentaram valores de compressão axial acima de 10 MPa, requisito mínimo para classificar como blocos de concreto reforçados leves de uso estrutural.(AU)

Biochemical, hematological, and hormonal profile of rats orally administered methanol stem bark extract of Napoleona vogelii Hook and Planch (Lecythidaceae).

Napoleona vogelii is used in traditional medicine for the management of stomach aches, ulcer, and cancers. This study was conducted to investigate the subchronic toxicological effect of methanol stem bark extract of N. vogelii on biochemical, hematological, and hormonal profile of male and female rats. Forty rats of both sexes were randomly divided into four groups of 10 rats each and were administered 100, 200, and 400 mg/kg of the extract p.o. for 90 d. Ten milliliter per kilogram of distilled water p.o. was administered to control rats. On hematological assessment, mean corpuscular hemoglobin concentration was significantly (p < 0.01) increased at 400 mg/kg compared to control. Biochemical assessment showed a significant increase (p < 0.05) in levels of alanine aminotransferase and aspartate aminotransferase at 200 and 400 mg/kg, respectively, compared to control. Hormonal assessment of male rats revealed a significantly (p < 0.0001) reduced level of testosterone at all treatment doses compared to control while estradiol was significantly (p < 0.05) reduced at 100 mg/kg, but significantly (p < 0.0001) increased at 200 and 400 mg/kg respectively compared to control in female rats. Findings from this study demonstrate that N. vogelli is relatively safe on oral acute exposure but may possess the potential to cause hepatic dysfunction and infertility in male rats by perturbations of the hypothalamic-pituitary axis while conversely enhancing fertility in female rats on subchronic administration.

Evaluation of the anti-asthmatic and antitussive potentials of methanol leaf extract of Napoleona vogelii in rodents.

Napoleona vogelii is used in ethnomedicine for the treatment of asthma and cough. This study evaluated antiasthmatic and antitussive properties of its methanol leaf extract (NVE) in rodents. Phytochemical screening was conducted using established methods. Acute oral toxicity test was done in mice and guinea pigs. Ovalbumin (OA)-sensitized guinea pigs were orally pretreated with 100, 200 or 400 mg/kg/day of NVE or 0.5 mg/kg/day of salbutamol for 14 days before exposure to 0.2% histamine aerosol. Latency to preconvulsive dyspnea (PCD), tracheal fluid volume (TFV), flow rate (FR), and tracheal morphometry (TM) were evaluated. Tracheal rings from sensitized guinea pigs were tested in organ baths for antispasmodic and spasmolytic effects. Citric acid and ammonium hydroxide cough models were used to evaluate antitussive effects in guinea pigs and mice respectively. Tannins, alkaloids, flavonoids, and phenolic substances were found in NVE. LD50 values in mice and guinea pigs were greater than 5000 mg/kg. NVE caused a significant (P < 0.05) increase in the latency to PCD and a decrease in TFV in the group treated with 200 mg/kg. TM indicated a reduction in airway narrowing in NVE-treated groups. The presence of NVE significantly attenuated responses of tracheal rings to carbachol. Its addition to carbachol precontracted rings resulted in significant relaxation. Emax for calcium concentration-response was significantly (P < 0.01) decreased in the presence of NVE. Cough bouts dose-dependently decreased significantly (P < 0.05) in guinea pigs and mice. We conclude that NVE seems safe and possesses anti-asthmatic effect that involves inhibition of calcium influx. It also has antitussive properties that may be peripherally mediated.

Sapucaia nut (Lecythis pisonis Cambess) and its by-products: A promising and underutilized source of bioactive compounds. Part II: Phenolic compounds profile.

In this study, the profile of the bioactive compounds of sapucaia nut (Lecythis pisonis Cambess) and its by-products have been investigated. The phenolic profile by LC-ESI-MS/MS, the total phenolic content, the condensed tannins and the antioxidant activity of the sapucaia nut and shell were determined. 14 phenolic compounds were identified in the sapucaia nut extract, primarily phenolic acids and flavonoids. Catechin, epicatechin, myricetin, ellagic acid and ferulic acid presented significant correlation to the antioxidant activity. The sapucaia shell contained 22 phenolic compounds, 13 of which were quantified. The sapucaia shell extract showed a high content of total phenolic compounds, a high condensed tannins content, and high antioxidant activity. The higher antioxidant activity of the shell can be associated with a higher content of phenolics. Overall, it can be concluded that the sapucaia nut is a raw material rich in phenolic compounds that present high antioxidant activity. The nuts and the cake may be used as a promising raw material for the food industry, while the shells could be an alternative source of natural antioxidants. Further use in the cosmetics and pharmaceutical industry may also be envisaged.

Sapucaia nut (Lecythis pisonis Cambess.) flour as a new industrial ingredient: Physicochemical, thermal, and functional properties.

The aim of this work was to investigate the physicochemical, thermal, and functional properties of partially defatted sapucaia nut (Lecythis pisonis Cambess.) flours (PDSF) degreased by subcritical propane (20-60 °C; 20-100 bar) and supercritical CO2 + ethanol (1:1 w/w) as co-solvent (60 °C; 200 bar) in comparison to the PDSF obtained through Soxhlet extraction with petroleum ether. Under the conditions studied herein, compressed propane has a minor effect on the granules' morphology (average particle size between 22 and 32 µm) or in the physicochemical characteristics of the PDSF. It caused a minimum impact on the nutritional profile of the samples; unlike, the thermogravimetric analysis revealed that there is an influence on the thermal stability of the PDSF. Functional characteristics, such as emulsifying (8-20 m2/g), foam (6-12%), and high water (0.35-1.38 g/g flour) and oil (0.72-1.57 g/g flour) absorption capacity, were observed in PDSF. Defatted flours were found to be effective in the production of emulsions with structures that showed micrometric-sized droplets (up to 85% droplet size <15.0 µm) with alleged stability. PDSF is a source of proteins (31-49%) and carbohydrates (17-31%), thus it can be used as an ingredient to produce foodstuff in bakery and confectionery aiming to increase their nutritional value and functional properties.

Sapucaia nut (Lecythis pisonis Cambess) and its by-products: A promising and underutilized source of bioactive compounds. Part I: Nutritional composition and lipid profile.

The nutritional composition of the sapucaia nut, cake and shell, the nut and cake minerals content and the lipid profile of the nut oil (fatty acids, tocopherols, phytosterols and triacylglycerols) were determined. The nuts and cake exhibited a high content of lipid (47.9 to 60.8 mg 100 g-1), protein (15.8 to 19.5 mg 100 g-1), dietary fiber (16.5 to 22.6 mg 100 g-1) and provided an excellent source of selenium (26.4 to 46.94 µg g-1). The oil contained a high amount of unsaturated fatty acids (39.7 to 45.4% of oleic and 32.2 to 46.6% of linoleic acids) and presented a high Oxidative Stability Index (8.57-12.95 h) indicating the presence of antioxidant compounds in the oil. The major triacylglycerols in the sapucaia oil were LLO, PLO, LOO, POO, OOO, PLL and LLL. The main bioactive lipids identified in the oil were γ-tocopherol (19.2 to 28.5 mg 100 g-1) and ß-sitosterol (92.8 to 194 mg 100 g-1). The results showed that the sapucaia nut and its by-products are a promising natural source of bioactive and nutritional compounds and when present in the diet can contribute to the maintenance of human health. In addition, the nut and by-product represents a promising raw material for the food industry.

Green synthesis of magnetic Fe3O4 nanoparticles using Couroupita guianensis Aubl. fruit extract for their antibacterial and cytotoxicity activities.

In the present study, a sustainable green chemistry approach was established to fabricate magnetic Fe3O4 nanoparticles (Fe3O4NPs) using the aqueous fruit extract of edible C. guianensis (CGFE). Synthesized NPs were further confirmed with different high-throughput characterization techniques such as UV-visible spectroscopy, FT-IR, XPS, DLS and zeta potential analysis. Additionally, XRD, AFM, HRTEM and SQUID VSM demonstrate the generation of crystalline CGFe3O4NPs with mean diameter of 17 ± 10 nm. Interestingly, CGFe3O4NPs exhibit a stupendous bactericidal action against different human pathogens which depicts its antimicrobial value. A significant dose-dependent cytotoxic effect of CGFe3O4NPs was noticed against treated human hepatocellular carcinoma cells (HepG2).

Inhibition of proinflammatory mediators by coumaroyl lupendioic acid, a new lupane-type triterpene from Careya arborea, on inflammation-induced animal model.

ETHNOPHARMACOLOGICAL RELEVANCE: Careya arborea Roxb. (Lecythidaceae) is a large tree found throughout India in deciduous forests and grasslands. C. arborea is traditionally used in tumors, inflammation, anthelmintic, bronchitis, epileptic fits, astringents, antidote to snake-venom, skin disease, diarrhea, dysentery with bloody stools, dyspepsia, ulcer, tooth ache, and ear pain. AIM OF THE STUDY: In our previous work, the methanolic extract of Careya arborea stem bark showed significant anti-inflammatory activity. As a continuity of that work, this study aimed at the isolation and evaluation of the anti-inflammatory effect of coumaroyl lupendioic acid, a new lupane-type triterpene from Careya arborea stem bark. Further, to give an insight into the underlying mechanism of action of the compound on the modulation of proinflammatory mediators. MATERIALS AND METHODS: Methanolic extract of Careya arborea stem bark was suspended in water, and sequentially fractionated with n-hexane and ethyl acetate. Further ethyl acetate fraction was subjected to medium pressure liquid chromatography (MPLC) to isolate the active molecules. The isolated compounds were characterized by the various spectral techniques namely UV, IR, 1H NMR, 13C NMR, DEPT, 1H-1H COSY, HMBC and Mass spectral techniques. In vitro COX-1 and COX-2 enzyme inhibition assays using human whole blood was performed to investigate the inhibitory effect of the isolated compounds. The resulted potent COX-2 inhibitor of the isolated constituents compound 5, designated as coumaroyl lupendioic acid (CLA), was investigated in carrageenan induced inflammation and its effect was also compared with betulinic acid (BA) at the doses of 10 and 20mgkg-1, p.o. using indomethacin and celecoxib (10 and 20mgkg-1, p.o., respectively) as reference drugs. The effect of CLA on the production of NO, MPO, PGE2, TNF-α, IL-1ß and IL-6 were assessed. In addition, the histopathology and immunohistochemistry (NF-Ò¡B, COX-2 and TNF-α protein expression) in paw tissues were also carried out. RESULTS: The chromatographic fractionation of the methanolic extract resulted in isolation of six new derivatives of lupane type triterpenes for the first time from the stem bark of C. arborea; 3ß-hydroxy-lup-5,20 (29),21-trien-28-oic acid (Compound 1), 1, 3, 13, 16-tetrahydroxy-lup-9(11), 20(29)-diene-28-oic acid (Compound 2), 1, 7-di hydroxy betulinic acid (Compound 3), 3ß-O-dihydrocinnamyl betulinic acid (Compound 4), 3ß-O-trans-coumaryl-lup-6, 9(11), 20(29)-triene-27, 28-dioic acid (Compound 5), 16ß-hydroxy-2, 3-seco-lup-5, 20(29)-dien-2, 3, 28-trioic acid (Compound 6). Among the all isolated compounds 3ß-O-trans-coumaryl-lup-6, 9(11), 20(29)-triene-27, 28-olioic acid designated as coumaroyl lupendioic acid (CLA) showed higher COX-2 selectivity which is comparable to reference drug (celecoxib). CLA significantly reduced carrageenan induced inflammation whereas CLA revealed greater effect as compared to BA at the similar corresponding doses. Moreover, CLA significantly inhibited pro-inflammatory mediators elevated by carrageenan. CLA also preserved the tissue architecture as evidenced by the histopathology. Furthermore, immunohistochemical studies revealed that CLA significantly down regulated NF-Ò¡B, COX-2 and TNF-α protein expression. CONCLUSION: The study gives an insight into the molecular mechanisms of coumaroyl lupendioic acid and suggests that the down-regulations of proinflammatory mediators provide credence to the ethno botanical use of the plant in the management of inflammation.

In vitro anti-MRSA activity of Couroupita guianensis extract and its component Tryptanthrin.

Couroupita guianensis is known in Brazil as 'Abricó-de-Macaco' and it has some attributes such as: antihypertensive, analgesic and anti-inflammatory activities. This study evaluated the antimicrobial activity of ethanolic extract and fractions of C. guianensis flowers and isolation of bioactive component. These extracts and fractions were subjected to agar diffusion, MIC, TLC and bioautography to bacteria, filamentous fungi and yeasts. Among the fractions of EtOH extract, the DCM fraction was the most active, particularly against Methicillin-resistant Staphylococcus aureus (MRSA) with MIC of 156 µg/mL. The active compound in this fraction was identified as Tryptanthrin, which showed promising antibacterial activity for MRSA showing MIC of 62.5 µg/mL. Ultrastructural analysis of MRSA incubated in the presence of Tryptanthrin by transmission electron microscope showed significant alterations in the cellular structure. Cytotoxicity tests demonstrated that DCM fraction and Tryptanthrin showed low toxicity, which makes it a promising candidate for alternative therapies to control and combat diseases.

Neuroprotective effect of Sapucaia nuts (Lecythis pisonis)on rats fed with high-fat diet.

BACKGROUND: Lecythis pisonis Cambess is commonly known as "castanha de sapucaia" in Brazil. Chemical composition studies revealed that this nut is an excellent source of anti-oxidant minerals and of essential lipids. OBJECTIVE: The aim of the present study is to assess the anti-oxidant and anti-inflammatory effect of Lecythis pisonis Cambess on the brain tissue of Wistar rats. MATERIAL AND METHODS: The animals were divided in four experimental groups (n = 6), total of forty-eight rats. Treatments included the standard diet (AIN-93G) and high-fat food, supplemented with Sapucaianut from 14 to 28 days. The gene expression markers TNF-α, NFkB, ZnSOD and HSP-72 were defined through reverse transcriptase polymerase chain reaction (rtPCR). The anti-oxidant effect was assessed through the thiobarbituric acid-reactive substances (TBARS) and the measurement of the activity performed by superoxide dismutase enzymes. RESULTS: Accordingly, the gene expression of the inflammatory markers NFkB (p65) and TNF-αwas lower in rats fed on diets supplemented with "sapucaia", and they presented significant difference in the Tukey test (p < 0.05). The heat-shock HSP-72 protein and the ZnSOD enzyme raised the gene expression and showed significant statistical difference (p < 0.05) in both groups fed on Sapucaia nut-based diet. CONCLUSION: Thus, the nutritional properties of the Sapucaia nuts perform important neuroprotective activities because they modulated the anti-oxidant activity and the brain tissue inflammatory process in the assessed animals.

Multipurpose effectiveness of Couroupita guianensis-synthesized gold nanoparticles: high antiplasmodial potential, field efficacy against malaria vectors and synergy with Aplocheilus lineatus predators.

Mosquito-borne diseases represent a deadly threat for millions of people worldwide. According to recent estimates, about 3.2 billion people, almost half of the world's population, are at risk of malaria. Malaria control is particularly challenging due to a growing number of chloroquine-resistant Plasmodium and pesticide-resistant Anopheles vectors. Newer and safer control tools are required. In this research, gold nanoparticles (AuNPs) were biosynthesized using a cheap flower extract of Couroupita guianensis as reducing and stabilizing agent. The biofabrication of AuNP was confirmed by UV-vis spectrophotometry, Fourier transform infrared (FTIR) spectroscopy, transmission electron microscopy (TEM), energy-dispersive X-ray (EDX) spectroscopy, X-ray diffraction (XRD), zeta potential, and particle size analysis. AuNP showed different shapes including spheres, ovals, and triangles. AuNPs were crystalline in nature with face-centered cubic geometry; mean size was 29.2-43.8 nm. In laboratory conditions, AuNPs were toxic against Anopheles stephensi larvae, pupae, and adults. LC50 was 17.36 ppm (larva I), 19.79 ppm (larva II), 21.69 ppm (larva III), 24.57 ppm (larva IV), 28.78 ppm (pupa), and 11.23 ppm (adult). In the field, a single treatment with C. guianensis flower extract and AuNP (10 × LC50) led to complete larval mortality after 72 h. In standard laboratory conditions, the predation efficiency of golden wonder killifish, Aplocheilus lineatus, against A. stephensi IV instar larvae was 56.38 %, while in an aquatic environment treated with sub-lethal doses of the flower extract or AuNP, predation efficiency was boosted to 83.98 and 98.04 %, respectively. Lastly, the antiplasmodial activity of C. guianensis flower extract and AuNP was evaluated against CQ-resistant (CQ-r) and CQ-sensitive (CQ-s) strains of Plasmodium falciparum. IC50 of C. guianensis flower extract was 43.21 µg/ml (CQ-s) and 51.16 µg/ml (CQ-r). AuNP IC50 was 69.47 µg/ml (CQ-s) and 76.33 µg/ml (CQ-r). Overall, our results showed the multipurpose effectiveness of C. guianensis-synthesized AuNPs, since they may be proposed as newer and safer tools in the fight against CQ-r strains of P. falciparum and for field control of malaria vectors, in synergy with wonder killifish predators.

Chemical Constituents of Lecythispisonis (Lecythidaceae)--A New Saponin and Complete 1H and 13C Chemical Shift Assignments.

A novel triterpenoid saponin 3-O-ß-D-glucuronopyranosyl-(1' --> 3)-2α,19α-dihydroxyolean-12-en-28-oic acid [3-O-ß-D-glucuronopyranosyl-(1' --> 3)-arjunic acid, 1], ten known compounds [six triterpenoids: α-amyrin (2), ß-amyrin (3), germanicol (4), lupeol (5), friedelin (6), friedelanol (7); four steroids--campesterol (8), stigmasterol (9), sitosterol (10), cholesterol (11)], and a long chain alcohol n-eicosan-1-ol (12) were identified in the bark of Lecythis pisonis. The structures were established by 1D and 2D NMR spectroscopy (1H and 13C-NMR, DEPTQ, 1H-1H-COSY, NOESY, HSQC and HMBC), low (CG-MS) and high resolution mass spectrometry (HR-ESI-MS), and infrared (IR) spectral data involving comparison with the literature.

In vitro growth-inhibitory effect of Brazilian plants extracts against Paenibacillus larvae and toxicity in bees.

American foulbrood (AFB) is a serious worldwide spreading disease in bees caused by Paenibacillus larvae. Plants extracts are known to decrease or inhibit the growth of these bacteria. The purpose of this study was to evaluate the antimicrobial activity of Calendula. officinalis, Cariniana domestica, and Nasturtium officinale extracts against the P. larvae and to evaluate the toxicity of the extracts in bees. In vitro activity against P. larvae of the extracts was evaluated by micro dilution method and the minimal inhibitory concentrations (MICs) were also determined. The concentrations used in the toxicity test were established based on the MIC values and by the spraying application method. The P. larvae was susceptible to the evaluated crude extract of C. officinalis and N. officinale. To C. domestica, only the ethyl acetate (EtAc) fraction and n-butanol (BuOH) fractions had activity against P. larvae. Toxicity analysis in bees showed no toxicity for N. officinale crude extract and for C. domestica BuOH fraction during 15 days of treatment, however, some deaths of bees occurred during the first three days of treatment with C. officinalis and C. domestica EtAc fraction. The results with these species were firstly described and showed that N. officinale crude extract and C. domestica BuOH fraction both presented not toxic effects in the concentration tested by the spraying application method, and can be a useful alternative for treatment or prevention of AFB.