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Showing papers in "Revista Brasileira De Farmacognosia-brazilian Journal of Pharmacognosy in 2015"


Journal ArticleDOI
TL;DR: In this paper, the authors used HPLC-DAD-MS/MS analysis in the positive and negative ion modes to identify 39 flavonoids and eight phenolic acids in the extract of Securigera securidaca.
Abstract: Securigera securidaca (L.) Degen & Doefl., Fabaceae, has been widely used in the Iranian, Indian and Egyptian folk medicine as antidiabetic and anti-hyperlipidemic remedy. Phenolic profiling of the ethanolic extract (90%) of the flowers of S. securidaca was performed via HPLC-DAD-MS/MS analysis in the positive and negative ion modes. The total polyphenols and flavonoids in the flowers were determined colorimetrically, and the quantification of their components was carried out using HPLC-UV. Total phenolics and flavonoids estimated as gallic acid and rutin equivalents were 82.39 ± 2.79 mg/g and 48.82 ± 1.95 mg/g of the dried powdered flowers, respectively. HPLC-DAD-MS/MS analysis of the extract allowed the identification of 39 flavonoids and eight phenolic acids. Quantitative analysis of some flavonoids and phenolics (mg/100 g powdered flowers) revealed the presence of isoquercetrin (3340 ± 2.1), hesperidin (32.09 ± 2.28), naringin (197.3 ± 30.16), luteolin (10.247 ± 0.594), chlorogenic acid (84.22 ± 2.08), catechin (3.94 ± 0.57) and protocatechuic acid (34.4 ± 0.15), in the extract. Moreover, the acute toxicity, hypoglycemic and hypolipidemic effects of the extract were investigated using alloxan induced diabetes in rats in a dose of 100, 200, and 400 mg/kg bwt. The ethanolic extract was safe up to a dose of 2000 mg/kg. All tested doses of the flower extract showed marked decrease in blood glucose level by 31.78%, 66.41% and 63.8% at 100, 200 and 400 mg/kg bwt, respectively, at p < 0.05. Regarding the anti-hyperlipidemic effect, a dose of 400 mg/kg of the flower extract showed the highest reduction in serum triacylglycerides and total cholesterol levels (68.46% and 51.50%, respectively at p < 0.05). The current study proved the folk use of the flowers of S. securidaca as anti-diabetic and anti-hyperlipidemic agent which could be attributed to its high phenolic content.

134 citations


Journal ArticleDOI
TL;DR: This study contributes to nanobiotechnology of natural products, presenting a potential larvicidal nanoemulsion prepared with R. officinalis essential oil and describing easy technique which may be useful for integrative control programs.
Abstract: Nanotechnology has emerged as a promising area for innovative products, including insecticides. Dengue is a tropical disease which is considered a critical health problem in developing countries, due to negative impacts to the environment caused by synthetic chemicals used for vector control (Aedes aegypti). Thus, developing of natural products based insecticidal are considered very promising. On this context, the aim of the present study was to obtain an O/W nanoemulsion containing Rosmarinus officinalis L., Lamiaceae, essential oil and evaluate its larvicidal activity against A. aegypti. Low energy method was employed, allowing achievement of small droplets. The nanoemulsion also presented low polydispersity and mean droplet below 200 nm, even after 30 days of storage. Potential mortality levels were observed after 24 h (80 ± 10%) and 48 h (90 ± 10%) in A. aegypti larvae at final concentration of 250 ppm, related to R. officinalis essential oil. This study contributes to nanobiotechnology of natural products, presenting a potential larvicidal nanoemulsion prepared with R. officinalis essential oil. Moreover, nanoemulsion production involved a non-heating procedure, describing easy technique which may be useful for integrative control programs.

132 citations


Journal ArticleDOI
TL;DR: TE-OE was the most promising among the evaluated oils: it afforded the lowest IC50 values for B16F10 cells and HT29 cells, as well as selectivity indices of 2.61 and 2.81, respectively, suggesting that TE-OE may be used to treat cancer without affecting normal cells.
Abstract: This study evaluated the cytotoxicity activity of the essential oils of Tagetes erecta L., Asteraceae (TE-OE), Tetradenia riparia (Hochst.) Codd, Lamiaceae (TR-OE), Bidens sulphurea (Cav.) Sch. Bip., Asteraceae (BS-OE), and Foeniculum vulgare Mill., Apiaceae (FV-OE), traditionally used in folk medicine, against the tumor cell lines murine melanoma (B16F10), human colon carcinoma (HT29), human breast adenocarcinoma (MCF-7), human cervical adenocarcinoma (HeLa), human hepatocellular liver carcinoma (HepG2), and human glioblastoma (MO59J, U343, and U251). Normal hamster lung fibroblasts (V79 cells) were included as control. The cells were treated with essential oil concentrations ranging from 3.12 to 400 µg/ml for 24 h. The cytotoxic activity was evaluated using the XTT assay; results were expressed as IC50, and the selectivity index was calculated. The results were compared with those achieved for classic chemotherapeutic agents. TE-OE was the most promising among the evaluated oils: it afforded the lowest IC50 values for B16F10 cells (7.47 ± 1.08 µg/ml) and HT29 cells (6.93 ± 0.77 µg/ml), as well as selectivity indices of 2.61 and 2.81, respectively. The major BS-EO, FV-EO and TE-EO chemical constituents were identified by gas chromatography mass spectrometry as being (E)-caryophyllene (10.5%), germacrene D (35.0%) and 2,6-di-tert-butyl-4-methylphenol (43.0%) (BS-EO); limonene (21.3%) and (E)-anethole (70.2%) (FV-EO); limonene (10.4%), dihydrotagetone (11.8%), α-terpinolene (18.1%) and (E)-ocimenone (13.0%) (TE-EO); and fenchone (6.1%), dronabinol (11.0%), aromadendrene oxide (14.7%) and (E,E)–farnesol (15.0%) (TR-EO). 2,6-di-tert-butyl-4-methylphenol (43.0%), (E)-anethole (70.2%) and α-terpinolene (18.1%), respectively. These results suggest that TE-OE may be used to treat cancer without affecting normal cells.

113 citations


Journal ArticleDOI
TL;DR: The present work aims to review the main nanotechnological approaches used for association of different plant extracts and the main achievements from using these technologies, especially liposomes, nanoemulsions and nanoparticles.
Abstract: Depending on the method of extraction, plant extracts can contain an enormous variety of active molecules, such as phenolic compounds, essential oils, alkaloids, among others. In many cases, from a pharmacological point of view, it is interesting to work with crude extract or fractions instead of a single isolated compound. This could be due to multi-targeting effect of the extract, lack of knowledge of the active compounds, synergistic effect of the extract compounds, among others. In any case, in order to achieve a final product some issues must be overcome, including poor stability, solvent toxicity, and low solubility of the bioactive compound. Recently many nanotechnology-based strategies have been proposed as an alternative to solve these problems, especially liposomes, nanoemulsions and nanoparticles. In this sense, the present work aims to review the main nanotechnological approaches used for association of different plant extracts and the main achievements from using these technologies.

75 citations


Journal ArticleDOI
TL;DR: In this paper, the influence of leaf age on methylxanthine and total phenolic contents by High Performance Liquid Chromatography and Ultraviolet Spectroscopy, as well as on free radical scavenging capacity, of aqueous extracts of I. paraguariensis leaves was investigated.
Abstract: Yerba-mate (Ilex paraguariensis A. St. Hil., Aquifoliaceae) is a South American native species that is widely used for its industrial potential in the preparation of drinks, teas and cosmetics. Its properties are directly related to the presence of its chemical constituents, such as saponins, methylxanthines and phenolic compounds. This study aimed to investigate the influence of leaf age on methylxanthine and total phenolic contents by High Performance Liquid Chromatography and Ultraviolet Spectroscopy, as well as on free radical scavenging capacity, of aqueous extracts of I. paraguariensis leaves. The results showed great variability in all the metabolites measured. Leaf ageing significantly increased the methylxanthine content and total phenolic content of the extracts. Free radical scavenging capacity was also significantly affected (p < 0.05) by leaf age. A positive correlation was observed, between the antioxidant activity and total phenolic content.

55 citations


Journal ArticleDOI
TL;DR: The first study relating detailed isolation, cultivation and biological evaluation (cytotoxic, antifungal and antibacterial) of endophytes Penicillium decaturense and P. waksmanii from the Brazilian marine red alga B. tenella is reported, corroborated that this species could be a pharmaceutical source from marine environment.
Abstract: Marine environment is one of the most important sources regarding natural products research. Besides, marine microorganisms have been denominated as a talented natural source for discovery of new leads. Although the association of macroalgae and fungi has been described regarding ecological issues, there is a lack of studies about marine seaweed endophytic fungi. In this context, the goal of this study was to evaluate cytotoxic, antifungal and antibacterial activities of endophytic fungi isolated from the Brazilian marine seaweed Bostrychia tenella (J.V. Lamouroux) J. Agardh (Ceramiales, Rhodophyta). Forty-five endophytic microorganism strains were isolated from B. tenella. Crude extracts and organic fractions of ten selected strains were obtained after growth in rice medium. Samples were evaluated for cytotoxicity, antifungal and antibacterial assays. Penicillium strains showed positive results in a diversity of assays, and other five strains were active in at least one test. In addition, cytochalasin D was isolated from Xylaria sp. This alga is composed of a microbiological potential, since its endophytic strains exhibited remarkable biological properties. Moreover, cytochalasin D isolation has confirmed chemical potential of marine endophytic strains. This is the first study in which cultured fungi isolates from the Brazilian macroalga B. tenella were evaluated concerning biological properties. Results corroborated that this species could be a pharmaceutical source from marine environment. Furthermore, Acremonium implicatum is being firstly described as marine endophyte and Xylaria sp., Trichoderma atroviride and Nigrospora oryzae as marine seaweed endophytes. Thus, this work reports the first study relating detailed isolation, cultivation and biological evaluation (cytotoxic, antifungal and antibacterial) of endophytes Penicillium decaturense and P. waksmanii from the Brazilian marine red alga B. tenella. We are also reporting the isolation of cytochalasin D, a known antitumor and antibiotic compound, from Xylaria sp. strain. Despite widespread prevalence in terrestrial and marine habitats, this present work describes the first occurrence of cytochalasin D as a metabolite from marine seaweed endophyte.

53 citations


Journal ArticleDOI
TL;DR: In this paper, Schinus molle L. and Schinus terebinthifolius Raddi, Anacardiaceae, leaves and fruit hydrodistillation, as well as, their chemical composition and extraction kinetic were evaluated.
Abstract: Essential oils extracted from Schinus molle L. and Schinus terebinthifolius Raddi, Anacardiaceae, leaves and fruit hydrodistillation, as well as, their chemical composition and extraction kinetic were evaluated. For this proposal, 6 h extraction and aliquots collected at sequencing different times (0.5, 1, 2, 4 and 6 h) were carried out allowing calculating accumulated content (% w/w) and verifying essential oil chemical profile. β-caryophyllene (35.2%), α-pinene (28.1%) and germacrene D (15.5%) represent S. terebinthifolius dried leaves essential oil major components, as well as, α-pinene (44.9%), germacrene D (17.6%) and β-pinene (15.1%) in the fruit. Cubenol (27.1%), caryophyllene oxide (15.3%) and spathulenol (12.4%) represent S. molle dried leaves essential oil major components, and β-pinene (36.3%) α-pinene (20.3%), germacrene D (12.1%) and spathulenol in the fruit. Essential oil extraction kinetics showed a hyperbolic distribution; monoterpene content presented exponential decay in time function and sesquiterpene showed exponential growth. Faster monoterpene extraction than the sesquiterpene extraction was observed, however, both presented increasing exponential distribution.

52 citations


Journal ArticleDOI
TL;DR: It is proven that horse chestnut seed extract not only significantly improves subjective symptoms in patients with chronic venous insufficiency like calf spasm, leg pain, pruritus, fatigue, but it also reduced leg volume, the ankle and calf circumference.
Abstract: The extract from horse chestnut seeds (Aesculus hippocastanumL., Sapindaceae), standardised for the content of aescin, is used as the treatment for chronic venous insufficiency. It has anti-inflammatory and anti-oedematous properties and indicates a positive effect on the venous tone, rheological properties, and blood coagulability. The mechanism of horse chestnut seed extract/aescin activity was proposed on the basis of in vitro and in vivo studies, and its effectiveness was documented with numerous randomised clinical trials. The results of the studies have proven that horse chestnut seed extract not only significantly improves subjective symptoms in patients with chronic venous insufficiency like calf spasm, leg pain, pruritus, fatigue, but it also reduced leg volume, the ankle and calf circumference. The preparations containing horse chestnut seed extract are very popular and they have similar effectiveness as compression therapy and a preparation with O-(β-hydroxyethyl)-rutosides. Moreover, horse chestnut seed extract has been proven to be safe and very well tolerated. The study was to present the results of the studies that have been conducted so far and that have confirmed the effectiveness of use of horse chestnut seed extract or aescin as the treatment for chronic venous insufficiency.

51 citations


Journal ArticleDOI
TL;DR: The chemical component and biological activity of T. pagdeni propolis depend on flora area of bee collection and bee species as mentioned in this paper, and the most potent activity of propolis extract was investigated for bioactive compounds and their quantity.
Abstract: The chemical component and biological activity of propolis depend on flora area of bee collection and bee species. In the study, the propolis from three stingless bee species, Lepidotrigona ventralis Smith, Lepidotrigona terminata Smith, and Tetragonula pagdeni Schwarz, was collected in the same region of mangosteen garden from Thailand. Total phenolic content, alpha glucosidase inhibitory effect, and free-radical scavenging activity using FRAP, ABTS, DPPH assays were determined. The most potent activity of propolis extract was investigated for bioactive compounds and their quantity. The ethanol extract of T. pagdeni propolis had the highest total phenolic content 12.83 ± 0.72 g of gallic acid equivalents in 100 g of the extract, and the strongest alpha glucosidase inhibitory effect with the IC50 of 70.79 ± 6.44 µg/ml. The free-radical scavenging activity evaluated by FRAP, ABTS, DPPH assays showed the FRAP value of 279.70 ± 20.55 µmol FeSO4 equivalent/g extract and the IC50 of 59.52 ± 10.76 and 122.71 ± 11.76 µg/ml, respectively. Gamma- and alpha-mangostin from T. pagdeni propolis extract were isolated and determined for the biological activity. Gamma-mangostin exhibited the strongest activity for both alpha glucosidase inhibitory effect and free-radical scavenging activity. Using HPLC quantitative analysis method, the content of gamma- and alpha-mangostin in the extract was found to be 0.94 ± 0.01 and 2.77 ± 0.08% (w/w), respectively. These findings suggested that T. pagdeni propolis may be used as a more suitable raw material for nutraceutical and pharmaceutical products and these mangostin derivatives as markers.

46 citations


Journal ArticleDOI
TL;DR: The principal botanical aspects, ethnopharmacological information and evaluation of the bioactive and pharmacological properties of Cordia, its phytochemical constituents and the most common classes of secondary metabolites identified are described.
Abstract: Species of the genus Cordia, Boraginaceae, are widely studied with regard to the various ethnobotanical and ethnopharmacological aspects. They are found principally in tropical and subtropical regions of the American, Asian and African continents, where they occur in various countries. In the genus Cordia, there are many species cultivated for ornamental plants, wood and medicinal applications, where they are extensively utilized by traditional communities. In the last decades, scientific studies of Cordia species have intensified, demonstrating the great interest in phytochemical, biological and pharmacological studies. In this review, we describe the principal botanical aspects, ethnopharmacological information and evaluation of the bioactive and pharmacological properties of Cordia, its phytochemical constituents and the most common classes of secondary metabolites identified. The information reported in this work contributes scientifically to recognizing the importance of the genus Cordia as a target in the search for new biotechnological investments.

43 citations


Journal ArticleDOI
TL;DR: Together, new insights of Meliaceae members demonstrating as a potential source as antimicrobial agents using in vitro studies are provided.
Abstract: Drug resistance to human infectious diseases caused by pathogens lead to premature deaths through out the world. Plants are sources for wide variety of drugs used for treating various diseases. Systematic screening of medicinal plants for the search of new antimicrobial drug candidates that can inhibit the growth of pathogens or kill with no toxicity to host is being continued by many laboratories. Here we review the phytochemical investigations and biological activities of Meliaceae. The mahogany (Meliaceae) is family of timber trees with rich source for limonoids. So far, amongst the different members of Meliaceae, Azadirachta indica and Melia dubia have been identified as the potential plant systems possessing a vast array of biologically active compounds which are chemically diverse and structurally complex. Despite biological activities on different taxa of Meliaceae have been carried out, the information of antibacterial and antifungal activity is a meager with exception to Azadirachta indica. Together we provide new insights of Meliaceae members demonstrating as a potential source as antimicrobial agents using in vitro studies.

Journal ArticleDOI
TL;DR: The topical formulation containing SLN-Curcuminoids showed good spreadability and stability when subjected to mechanical stress test, and can be used in further in vivo studies for the treatment of inflammatory reactions, in special for radiodermitis.
Abstract: Solid lipid nanoparticles incorporating Curcuma longa L., Zingiberaceae, curcuminoids were produced by the hot melt emulsion method. A Box–Behnken factorial design was adopted to study the nanoparticles production at different levels of factors such as the percentage of curcuminoids, time of homogenization and surfactant ratio. The optimized nanoparticles were incorporated into hydrogels for stability, drug release and skin permeation tests. The average nanoparticle sizes were 210.4 nm; the zeta potential of −30.40 ± 4.16; the polydispersivity was 0.222 ± 0.125. The average encapsulation efficiency of curcumin and curcuminoids was 52.92 ± 5.41% and 48.39 ± 6.62%, respectively. Solid lipid nanocapsules were obtained with curcumin load varying from 14.2 to 33.6% and total curcuminoids load as high as 47.7%. The topical formulation containing SLN-Curcuminoids showed good spreadability and stability when subjected to mechanical stress test remained with characteristic color, showed no phase separation and no significant change in pH. As a result of slow release, the nanoparticles were able to avoid permeation or penetration in the pig ear epidermis/dermis during 18 h. The topical formulation is stable and can be used in further in vivo studies for the treatment of inflammatory reactions, in special for radiodermitis.

Journal ArticleDOI
TL;DR: It is suggested that the in vivo sedative effect of the P. quadrangularis extract and its main flavonoid apigenin maybe be due to an enhancement of the GABAergic system.
Abstract: In the current study we showed that oral administration of an aqueous extract of Passiflora quadrangularis L, Passifloraceae, pericarp results in a significant prolongation of the sleep duration in mice evaluated in the ethyl ether-induced hypnosis test which indicates sedative effects Apigenin, the main flavonoid of the extract, induced a similar sedative response when applied alone, at a dose equivalent to that found in the extract, suggesting that apigenin is mediating the sedative effects of P quadrangularis extract In addition, the sedative effect of apigenin was blocked by pretreatment with the benzodiazepine antagonist flumazenil (1 mg/kg), suggesting an interaction of apigenin with gamma-aminobutyric acid type A (GABAA) receptors However, apigenin at concentrations 01–50 µM failed to enhance GABA-induced currents through GABAA receptors (α1β2γ2S) expressed in Xenopus oocytes Nevertheless, based on our results, we suggest that the in vivo sedative effect of the P quadrangularis extract and its main flavonoid apigenin maybe be due to an enhancement of the GABAergic system

Journal ArticleDOI
TL;DR: The available evidences suggest that the complementary effects of silymarin and vitamin C proved to be capable of ameliorating acetaminophen-mediated hepatic oxidative damage and the probable mechanism is via antioxidative action.
Abstract: Oxidative insult by free radicals has been implicated in drug-induced hepatic damage and this has resulted in frequent episodes of liver disorders. Therapeutic efficacy of antioxidants may provide a possible solution to this menace. This study was carried out to investigate the effect of combined administration of silymarin and vitamin C in rescuing acetaminophen-induced hepatotoxicity in rats. Hepatotoxic rats were orally administered with silymarin and vitamin C at 100 and 200 mg/kg body weight, respectively. At the end of the experiment, liver function indices, antioxidant parameters and histological analysis were evaluated. We observed that the significantly increased (p < 0.05) activities of alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase, as well as levels of thiobarbituric acid reactive substances and serum total bilirubin, were markedly reduced following co-administration of silymarin and vitamin C. The compounds also effectively reversed the reduced activities of superoxide dismutase, catalase, glutathione peroxidase, glutathione S-transferase and total protein concentration in the hepatotoxic rats. These findings are indicative of hepatoprotective and antioxidant attributes of the two compounds which are also supported by the histological analysis. The available evidences in this study suggest that the complementary effects of silymarin and vitamin C proved to be capable of ameliorating acetaminophen-mediated hepatic oxidative damage and the probable mechanism is via antioxidative action.

Journal ArticleDOI
TL;DR: In this article, the authors developed and validated an analytical method for the identification of the chemical marker of Schinopsis brasiliensis Engl., Anacardiaceae using HPLC-UV.
Abstract: The aim of this work was to develop and validate an analytical method for the identification of the chemical marker of Schinopsis brasiliensis Engl., Anacardiaceae. It would determine the total polyphenols and flavonoid content by spectrophotometric methodology in the dried extract of plant. The chromatographic profiles of S. brasiliensis were determined using HPLC-UV. The liquid chromatography method was conducted on a Phenomenex Gemini NX C18 column (250 × 4.6 mm, 5 μm). The mobile phase consisted of 0.05% orthophosphoric acid: methanol. The flow rate was 1 ml/min and effluents were monitored at 271 nm. The retention time for gallic acid was 8.5 min. The described method has the advantage of being both rapid and easy. Hence it can be applied for routine quality control analysis of herbal preparation containing S. brasiliensis.

Journal ArticleDOI
TL;DR: This paper reviews the literature about C15 acetogenins, focusing on their distribution, chemical and biological aspects, including their reported biological activities.
Abstract: Acetogenins are secondary metabolites derived from the polyketide pathway and their potential role as chemotaxonomical markers for red algae belonging to the Laurencia complex has been long pointed out. C15 acetogenins from algae are quite different from plant acetogenins: they are usually halogenated, and have an enyne or a bromoallene terminal group. Since they were first reported, laurencin and other algal acetogenins have inspired great curiosity among natural product chemists and also those working with synthesis. This paper reviews the literature about C15 acetogenins, focusing on their distribution, chemical and biological aspects, including their reported biological activities.

Journal ArticleDOI
TL;DR: Results have shown that C. langsdorffii leaves extract and isolated compounds from it, presented gastroprotective properties in different animal models of gastric ulcer, which may be associated with the ability of the extract to decrease gastric secretion and increase the mucus production.
Abstract: Gastric ulcer is a prevalent gastrointestinal disease, and the drugs currently used in the treatment produce several adverse effects. In this context, the search for new therapeutic antiulcer agents is essential, and medicinal plants have great potential. Here, we investigated the gastroprotective properties of Copaifera langsdorffii Desf., Fabaceae, hydroalcoholic extract obtained from leaves and its isolated compounds. The phytochemistry studies and the compounds isolations were performed using chromatographic and spectroscopic methodologies. The hydroalcoholic extract was evaluated using ethanol/HCl, non-steroidal anti-inflammatory drug, stress-induced-ulcer and chronic ulcer-model. The effects on gastric content volume, pH, total acidity and mucus stomach production were evaluated in the pylorus ligated-model. The C. langsdorffii extract obtained from leaves (50, 250 or 500 mg/kg) reduced the injured area compared to control group in all experiments. The extract showed a significant decrease in the total gastric juice acidity and an increase in mucus production (500 mg/kg) when compared to vehicle. Among isolated compounds (30 mg/kg) α-humulene, β-caryophyllene and caryophyllene oxide showed greater gastroprotective activity in the ethanol/HCl induced ulcer model. The data herein obtained shown that C. langsdorffii leaves extract and isolated compounds from it, presented gastroprotective properties in different animal models of gastric ulcer. These effects may be associated with the ability of the extract to decrease gastric secretion and increase the mucus production.

Journal ArticleDOI
TL;DR: In this article, a spray-drying technique was used to produce semipurified extract of guarana microparticles, which contained a combination of maltodextrin and gum arabic.
Abstract: Guarana (Paullinia cupana Kunth, Sapindaceae) is well known for its dietary and pharmaceutical potential, and the semipurified extract of guarana shows antidepressant and panicolytic effects. However, the low solubility, bioavailability and stability of the semipurified extract limit its use as a component of pharmaceutical agents. Delivery of the semipurified extract in a microparticle form could help to optimize its stability. In this study, microparticles containing semipurified extract of guarana were obtained by the spray-drying technique, using a combination of maltodextrin and gum arabic. The raw materials and microparticles produced were characterized by particle size analysis, differential scanning calorimetry, thermogravimetric analysis, and scanning electron microscopy. The drug content and antioxidant capacity were also evaluated. In vitro dissolution tests using flow cell dissolution apparatus, were carried out to investigate the influence of formulation parameters on the release of semipurified extract of guarana from the microparticles. The spray-drying technique and the processing conditions selected gave satisfactory encapsulation efficiency (80–110%) and product yield (55–60%). The mean diameter of microparticles was around 4.5 μm. The DPPH radical scavenging capacity demonstrated that microparticles can protect the semipurified extract of guarana from the effect of high temperatures during the process maintained the antioxidant capacity. Differential scanning calorimetry results indicated an interaction between semipurified extract of guarana and gum arabic: maltodextrin in the microparticles, and thermogravimetric analysis indicate that the profile curves of the microparticles are similar to the adjuvants used in drying, probably due to the higher proportion of adjuvants compared to semipurified extract of guarana. In vitro dissolution tests demonstrate that all formulations complete dissolution within 60 min. Microencapsulation improved the technological characteristics of the powders and preserved the antioxidant properties. The study demonstrated the feasibility of producing these microparticles for a one-step process using spray drying. The composition of each formulation influenced the physical and chemical characteristics. This spray-drying technique can be used as an efficient and economical approach to produce semipurified extract of guarana microparticles.

Journal ArticleDOI
TL;DR: A method to quantify both coumarin and chlorogenic acid and apply it to extracts of plants identified as M. glomerata, M. laevigata, or as guaco to determine the pattern of composition of these two species and to observe differences between oven-dried and lyophilized leaves is developed and validated.
Abstract: In Brazil, Mikania glomerata Spreng. and M. laevigata Sch. Bip. ex Baker, Asteraceae, known popularly as guaco, are widely used for colds and asthma. Although coumarin is adopted as the chemical marker of both species, it was not always detected in M. glomerata, for which chlorogenic acid was identified and quantified instead. The purpose of this study was to develop and validate a method to quantify both coumarin and chlorogenic acid and apply it to extracts of plants identified as M. glomerata, M. laevigata, or as guaco, to determine the pattern of composition of these two species and to observe differences between oven-dried and lyophilized leaves. A method using ultra-high resolution liquid chromatography–mass spectrometry (UHPLC–MS) in the full scan mode was validated for selectivity, matrix effect, linearity, limits of detection and quantification, precision and accuracy. The concentration of coumarin varied between species and samples, therefore these two species should not be used interchangeably. The concentration of chlorogenic acid was also determined for all samples. The UHPLC–MS method permitted the quantification of coumarin and chlorogenic acid in 16 samples of guaco and several commercial samples were possibly misidentified.

Journal ArticleDOI
TL;DR: The crude extract of M. taxifolia showed UV-A photoprotection and low eye irritation in the hen egg test-chorioallantoic membrane test, showing the possibility to use this extracts as a sunscreen in pharmaceutical preparations.
Abstract: The species Marcetia taxifolia (A. St.-Hil.) DC., Melastomataceae, which is endemic of the rupestrian fields of northeastern Brazil, contains a significant amount of flavonoids. In this work, the potential of the ethanolic extract of M. taxifolia as the active principle in a sunscreen photoprotection (UV-A and UV-B) formulation was investigated. The Liquid Chromatography High Performance-Diode Array Detector quantification (quercetin), total flavonoid content, antioxidant activity through 2.2-diphenyl-1- picrylhydrazil method, photoprotective activity against UV-B and UV-A radiation in vitro (spectrophotometric method) and potential for eye irritation using the methodology of the hen egg test-chorioallantoic membrane were performed in the extract. After that, the formulations were prepared using different concentrations of active ethanolic extract (5, 10, 20 and 30%) and the evaluation of the sun protection factor was carried out using the same methodology used for the crude extract. The crude extract showed UV-A photoprotection and low eye irritation in the hen egg test-chorioallantoic membrane test. All formulations containing M. taxifolia extract had ≥ 6 sun protection factor. Its shows the possibility to use this extracts as a sunscreen in pharmaceutical preparations.

Journal ArticleDOI
TL;DR: In this article, an UPLC-PDA method for quantification of eriodictyol in leaves of Vernonanthura tweedieana was developed and validated for specificity, linearity, precision (repeatability and intermediate precision), limit of detection (LOD) and limit of quantification (LOQ), accuracy and robustness.
Abstract: Vernonanthura tweedieana (Baker) H. Rob., Asteraceae, is used in the Brazilian folk medicine for the treatment of respiratory diseases. In this work the phytochemical investigation of its ethanol extracts as well as the development and validation of an UPLC-PDA method for the quantification of the eriodictyol from the leaves were performed. The phytochemical study for this species lead to the identification of ethyl caffeate, naringenin and chrysoeriol in mixture, eriodictyol from leaves, and the mixture of 3-hydroxy-1-(4-hydroxy-3,5-dimethoxyphenyl)-propan-1-one and evofolin B, apigenin, the mixture of caffeic and protocatechuic acid and luteolin from stems with roots, being reported for the first time for V. tweedieana, except for eriodictyol. The structural elucidation of all isolated compounds was achieved by 1H and 2D NMR spectroscopy, and in comparison with published data. An UPLC-PDA method for quantification of the eriodictyol in leaves of V. tweedieana was developed and validated for specificity, linearity, precision (repeatability and intermediate precision), limit of detection (LOD) and limit of quantification (LOQ), accuracy and robustness. In this study, an excellent linearity was obtained (r2 = 0.9999), good precision (repeatability RSD = 2% and intermediate precision RSD = 8%) and accuracy (average recovery from 98.6% to 99.7%). The content of eriodictyol in the extract of leaves of V. tweedieana was 41.40 ± 0.13 mg/g. Thus, this study allowed the optimization of a simple, fast and validated UPLC-PDA method which can be used to support the quality assessment of this herbal material.

Journal ArticleDOI
TL;DR: Hydroprophile–Lipophile Balance of evening primrose seeds oil was determined and pseudo-ternary diagram allowed delimitation of nanoemulsion region, contributing to nanobiotechnology of natural products.
Abstract: Evening primrose (Oenothera biennis L., Onagraceae) seeds oil has great economic importance due to its wide industrial application, mainly for medicines and nutraceutics. However, to our knowledge, it remains almost unexplored regarding development of innovative formulations, such as nanoemulsions. On the present study, required Hydroprophile–Lipophile Balance of evening primrose seeds oil was determined (HLB 12) and a stable nanoemulsion (Day 1: mean droplet size: 214.3 ± 0.69 nm, polydispersity index: 0.253 ± 0.012. Day 7: mean droplet size: 202.8 ± 0.23 nm, polydispersity index: 0.231 ± 0.008) was achieved. Moreover, pseudo-ternary diagram allowed delimitation of nanoemulsion region, contributing to nanobiotechnology of natural products.

Journal ArticleDOI
TL;DR: This review aims to provide up-to-date information on the traditional uses, pharmacology, clinical applications, and toxicology of Carthami flos in China and thereby to provide a basis for further investigation of its use to treat dissimilar diseases.
Abstract: Carthami flos, the dried floret of Carthamus tinctorius L., Asteraceae (safflower), has been widely used in traditional Chinese medicine to treat a broad range of ailments, such as coronary heart disease, angina pectoris, gynecologic disease, stroke, and hypertension. However, although several studies on Carthami flos have been done consecutively, the results are usually scattered across various documents. This review aims to provide up-to-date information on the traditional uses, pharmacology, clinical applications, and toxicology of Carthami flos in China and thereby to provide a basis for further investigation of its use to treat dissimilar diseases. Various ethnomedical uses of Carthami flos have been documented in many ancient Chinese books. Crude extracts and isolated compounds from Carthami flos show a broad range of pharmacological properties, such as protective effects on brain tissue, on osteoblasts, and in myocardial ischemia, as well as anti-inflammatory, antithrombotic, antitumor, and antidiabetic activities. To date, safflower and safflor yellow injections have been used to treat coronary heart disease, chronic pulmonary heart disease, cerebrovascular diseases, orthopedic diseases, and diabetes mellitus. Regarding the toxicology of Carthami flos, among the side effects that have been observed are allergic reaction, spermatogenetic failure, fatty liver, and nephrotoxicity.

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TL;DR: The chemical composition of the bioactive fraction was determined by gas chromatography–mass spectrometry (GC–MS); this fraction is solely composed of halogenated monoterpenes, therefore allowing assignment of acetylcholinesterase inhibition activity to them.
Abstract: Alzheimer's disease affects nearly 36.5 million people worldwide, and acetylcholinesterase inhibition is currently considered the main therapeutic strategy against it. Seaweed biodiversity in Brazil represents one of the most important sources of biologically active compounds for applications in phytotherapy. Accordingly, this study aimed to carry out a quantitative and qualitative assessment of Hypnea musciformis (Wulfen) J.V. Lamouroux, Ochtodes secundiramea (Montagne) M.A. Howe, and Pterocladiella capillacea (S.G. Gmelin) Santelices & Hommersand (Rhodophyta) in order to determine the AChE effects from their extracts. As a matter of fact, the O. secundiramea extract showed 48% acetylcholinesterase inhibition at 400 μg/ml. The chemical composition of the bioactive fraction was determined by gas chromatography–mass spectrometry (GC–MS); this fraction is solely composed of halogenated monoterpenes, therefore allowing assignment of acetylcholinesterase inhibition activity to them.

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TL;DR: Five lipid compounds isolated from soft coral E unicea sp.
Abstract: Biofilm has a primary role in the pathogenesis of diseases and in the attachment of multicellular organisms to a fouled surface. Because of that, the control of bacterial biofilms has been identified as an important target. In the present study, five lipid compounds isolated from soft coral Eunicea sp. and three terpenoids together with a mixture of sterols from Eunicea fusca collected at the Colombian Caribbean Sea showed different effectiveness against biofilm formation by three marine bacteria associated with immersed fouled surfaces, Ochrobactrum pseudogringnonense, Alteromona macleodii and Vibrio harveyi, and against two known biofilm forming bacteria, Pseudomonas aeruginosa ATCC 27853 and Staphylococcus aureus ATCC 25923. The pure compounds were characterized by NMR, HRESI-MS, HRGC-MS and optical rotation. The most effective compounds were batyl alcohol (1) and fuscoside E peracetate (6), acting against four strains without affecting their microbial growth. Compound 1 showed biofilm inhibition greater than 30% against A. macleodii, and up to 60% against O. pseudogringnonense, V. harveyi and S. aureus. Compound 6 inhibited O. pseudogringnonense and V. harveyi between 25 and 50%, and P. aeruginosa or S. aureus up to 60% at 0.5 mg/ml. The results suggest that these compounds exhibit specific biofilm inhibition with lower antimicrobial effect against the bacterial species assayed.

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TL;DR: This study demonstrates the first in vitro antileishmanial activity of the P. angustifolium essential oil, of which the phytochemical profile showed the presence of sesquiterpenes and monoterpenes.
Abstract: Piper angustifolium Lam., Piperaceae, popularly known as "matito", "pimenta-de-macaco", "pimenta-longa" or "jagurandi" in Brazil, has been commonly used in the treatment of cutaneous leishmaniasis-associated lesions, but there are few studies on the activity against visceral leishmaniasis-associated species. This study demonstrates the first in vitro antileishmanial activity of the P. angustifolium essential oil, of which the phytochemical profile showed the presence of sesquiterpenes and monoterpenes. The main compounds were spathulenol (23.8%) and caryophyllene oxide (13.1%). P. angustifolium essential oil was highly active [the half maximum inhibitory concentration = 1.43 μg/ml] against intracellular amastigotes of Leishmania infantum, the etiological agent of visceral leishmaniasis in the New and Old World. Activity was obtained 24 h after addition of the oil (6.25–50 μg/ml), with a reduction of 100% in the infection index at concentrations of 25 and 50 μg/ml. P. angustifolium essential oil showed low cytotoxicity for mammalian fibroblasts and macrophages (the half maximum inhibitory concentration values of 31.67 and 48.22 μg/ml, respectively), and it was 33 and 22 times more toxic to amastigotes than to mammalian cells, as indicated by selectivity indexes. The results demonstrated that P. angustifolium essential oil is a promising alternative for the study of potential drugs for visceral leishmaniasis.

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TL;DR: In this paper, Atemoya is an interspecific annonaceous hybrid between Annona cherimola mill and Annona squamosa L. Its phytochemical investigation led to seven alkaloids, including two aporphine (anonaine and asimilobine), three oxo-paraphine (lanuginosine, liriodenine and lysicamine), and two pro-proporphines (pronuciferine and stepharine).
Abstract: Atemoya is an interspecific annonaceous hybrid between Annona cherimola Mill. and Annona squamosa L. Its phytochemical investigation led to seven alkaloids, including two aporphine (anonaine and asimilobine), three oxoaporphine (lanuginosine, liriodenine and lysicamine) and two proaporphine (pronuciferine and stepharine). These alkaloids were identified by a series of spectrometric methods, mainly MS and NMR (1D and 2D), as well as by comparison with literature data. Our findings showed that this species is an important source of aporphine alkaloids and have high relationship with other Annona species.

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TL;DR: Results indicate that tagitinins exhibit anti-inflammatory action on human neutrophils, andtagitinin F was the only sesquiterpene lactone that decreased secretion of inflammatory products by neutrophil without inducing neutrophIL apoptosis.
Abstract: The tagitinins isolated of Tithonia diversifolia (Hemsl.) A. Gray, Asteraceae, are the most studied sesquiterpene lactones due to their wide spectrum of pharmacologic activities, especially related with nuclear factor-kappa B inhibition. Nevertheless, detailed studies about the mechanism of action of its active compounds are still lacking. Neutrophils perform a fundamental role in the inflammatory response to several etiologic factors. However, the effect of tagitinins on human neutrophil is not yet clearly known. We investigated the role of tagitinin C (1), tagitinin F (2) and tagitinin A (3) in activation and survival of human neutrophils to establish possible effects in their mechanisms of inflammation. Human neutrophils were purified from the peripheral blood and cultivated with tagitinins C (1), F (2) and A (3) in the presence or not of Escherichia coli lipopolysaccharide. The enzymatic activity, apoptosis and secretion of cytokines rate were determined after 18 h. Lipopolysaccharide-induced myeloperoxidase activity of human neutrophils was significantly inhibited only by tagitinin F (2). Apoptosis of neutrophils was increased in the presence of tagitinin C (1), and it occurred independently of the presence of lipopolysaccharide or dexamethasone. Tagitinins C (1), F (2) and A (3) decrease lipopolysaccharide-induced interleukin-6, interleukin-8 and Tumor necrosis factor alpha production by human neutrophils. Together, these results indicate that tagitinins exhibit anti-inflammatory action on human neutrophils. However, tagitinin F (2) was the only sesquiterpene lactone that decreased secretion of inflammatory products by neutrophils without inducing neutrophil apoptosis.

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TL;DR: In this paper, the authors used a modified active oxygen method with light irradiation, heating and oxygen flux to determine the antioxidant activity of green coffee oil microcapsules, which showed a 7-fold and 3-fold increase in antioxidant activity when compared to pure green coffee oils.
Abstract: The oil extracted by cold pressing unroasted coffee beans, known as green coffee oil, has been widely used for cosmetic purposes. The objective of this work was to prepare and characterize microcapsules containing green coffee oil and to verify its antioxidant activity under the effect of light, heat and oxygen. The encapsulating material was arabic gum and the microcapsules were obtained by spray drying an oil-in-water emulsion containing green coffee oil. The characterization of the microcapsules was performed by laser diffraction, scanning electron microscopy, differential scanning calorimetry and the antioxidant activity. The antioxidant activity was determined by a modified active oxygen method with light irradiation, heating and oxygen flux. The microparticles were effectively produced by the proposed spray drying method, which resulted in green coffee oil loads of 10 and 30%. The morphological evaluation of microcapsules showed spherical shape with smooth and non-porous surfaces, demonstrating the adequacy of arabic gum as encapsulating material. Calorimetric analysis of individual components and microcapsules with 10 and 30% green coffee oil showed diminished degradation temperatures and enthalpy, suggesting a possible interaction between arabic gum and green coffee oil. The antioxidant activities for pure green coffee oil and its microcapsules with loads of 10 and 30% showed high activity when compared to the reference antioxidant alfa-tocopherol. Microcapsules containing 10 and 30% of oil showed 7-fold and 3-fold increase in antioxidant activity when compared to pure green coffee oil. The new method for antioxidant activity determination proposed here, which applies heat, light and oxygen simultaneously, suggests a high improvement in encapsulated green coffee oil when compared to this active alone. The results showed herein indicate a promising industrial application of this microencapsulated green coffee oil.

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TL;DR: The oil from seeds of Dipteryx alata Vogel, Fabaceae, popularly known as baru, was extracted by hydraulic and continuous screw pressing as discussed by the authors, and eleven chemical constituents obtained by hydraulic pressing, including steroids, mono and sesquiterpenes and tocopherol derivatives were identified by gas chromatography-tandem mass spectrometry (GC-MS).
Abstract: The oil from seeds of Dipteryx alata Vogel, Fabaceae, popularly known as baru, was extracted by hydraulic and continuous screw pressing A total of eleven chemical constituents obtained by hydraulic pressing, including steroids, mono and sesquiterpenes and tocopherol derivatives were identified by gas chromatography–tandem mass spectrometry (GC–MS) Compounds limonene, β-elemene, γ-elemene, α-caryophyllene, β-caryophyllene, campesterol, stigmasterol, β-sitosterol and cycloartenol are being described for the first time in the baru oil