Chemical composition and biological activity of Baccharis erioclada DC. essential oil

Abstract The chemically complex essential oils of Baccharis species are associated with several biological activities, such as antimicrobial and antiulcerous properties. However, few studies have investigated Baccharis erioclada DC. Therefore, in this study, we aimed to characterize the essential oil of B. erioclada and evaluate its antioxidant, antimicrobial, and hemolytic potential. The essential oil was extracted by hydrodistillation using a Clevenger apparatus and analyzed via gas chromatography-mass spectrometry (GC-MS). Phosphomolybdenum complex formation, reducing antioxidant power, and thiobarbituric acid reactive substances (TBARS) methods were used to determine antioxidant potential. To evaluate the essential oil's antimicrobial activity, minimum inhibitory concentrations (MIC) in Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Candida albicans were calculated. Hemolytic activity was determined in sheep red blood cells. Thirty-one compounds were identified via GC-MS analysis, representing 81.60% of the total essential oil. These compounds included: turmerone (27.97%), fokienol (13.47%), ledol (9.78%), and santalol (5.35%). The class of compounds identified was the oxygenated sesquiterpenes (62.52%). Antioxidant activity was confirmed via phosphomolybdenum complex formation and TBARS methods. Moderate antimicrobial activity and low hemolysis rates were displayed at concentrations of 250 and 500 µg/mL

Co-Loaded Curcumin and Methotrexate Nanocapsules Enhance Cytotoxicity against Non-Small-Cell Lung Cancer Cells.

Background: As part of the efforts to find natural alternatives for cancer treatment and to overcome the barriers of cellular resistance to chemotherapeutic agents, polymeric nanocapsules containing curcumin and/or methotrexate were prepared by an interfacial deposition of preformed polymer method. Methods: Physicochemical properties, drug release experiments and in vitro cytotoxicity of these nanocapsules were performed against the Calu-3 lung cancer cell line. Results: The colloidal suspensions of nanocapsules showed suitable size (287 to 325 nm), negative charge (-33 to -41 mV) and high encapsulation efficiency (82.4 to 99.4%). Spherical particles at nanoscale dimensions were observed by scanning electron microscopy. X-ray diffraction analysis indicated that nanocapsules exhibited a non-crystalline pattern with a remarkable decrease of crystalline peaks of the raw materials. Fourier-transform infrared spectra demonstrated no chemical bond between the drug(s) and polymers. Drug release experiments evidenced a controlled release pattern with no burst effect for nanocapsules containing curcumin and/or methotrexate. The nanoformulation containing curcumin and methotrexate (NCUR/MTX-2) statistically decreased the cell viability of Calu-3. The fluorescence and morphological analyses presented a predominance of early apoptosis and late apoptosis as the main death mechanisms for Calu-3. Conclusions: Curcumin and methotrexate co-loaded nanocapsules can be further used as a novel therapeutic strategy for treating non-small-cell lung cancer.

Development of W1/O/W2 emulsion with gallic acid in the internal aqueous phase.

The aim of this work is to develop a W1/O/W2 multiple emulsion with gallic acid in the internal aqueous phase (W1). A quantification method for gallic acid using HPLC-UV was developed and validated. In the first step, a simple W1/O emulsion was prepared with distilled water, polyglycerol polyricinoleate, sodium chloride, gallic acid and pH 5.0 sodium acetate buffer system. The second step consisted of adding the simple emulsion to the external aqueous phase (W2) composed of distilled water, polysorbate 80 and xanthan gum. The multiple emulsion showed pseudoplastic behavior. After 28 days of analysis the multiple emulsion presented a stability index of 75% without pH variation, 89.61% of gallic acid concentration, 59.62% of antioxidant activity in the phosphomolybdenum complex assay and 80.58% of DPPH scavenging activity. It is concluded that the W1/O/W2 emulsion developed was stable for 28 days and maintained more than 50% of gallic acid antioxidant capacity.

Componentes químicos del aceite esencial de Ocotea paranaensis (Lauraceae) y sus propiedades antioxidantes, anticancer y antimicrobianas / Chemical constituents of Ocotea paranaensis (Lauraceae) essential oil and their antioxidant, anticancer and antimicrobial properties

La composición química del aceite esencial obtenido de las ramas de Ocotea paranaensis se estudió por cromatografía de gases/espectrometría de masas (CG/MS). Se identificaron veintisiete compuestos, que comprenden el 94,82% de los componentes totales. El aceite se caracterizó por una concentración relativamente alta de sesquiterpenos (62,96%), sesquiterpenos oxigenados (33,33%) y diterpeno (3,70%). En cuanto a los compuestos principales, se destacaron Z-nerolidol (19,16%), germacreno D (12,92%) y α-bulnesene (8,47%), que correspondieron al 40,55% de las sustancias encontradas. El aceite esencial analizado de Ocotea paranaensis tiene una buena acción reductora de fosfomolibdeno y es moderadamente tóxico para la Artemia salina (LC50 = 147,91 µg/mL). Mostró potencial hemolítico y actividad moderada contra Staphylococcus aureus (concentración inhibitoria mínima MIC = 250 µg/mL) y Pseudomonas aeruginosa (MIC = 500 µg/mL). No se observaron resultados satisfactorios de citotoxicidad en el linaje H460 y HeLa.

The chemical composition of the essential oil obtained from the branches of Ocotea paranaensis was studied by gas chromatography/mass spectrometry (GC/MS). Twenty-seven compounds, comprising 94.82% of the total components, were identified. The oil showed relatively high concentration of sesquiterpenes (62.96%), oxygenated sesquiterpenes (33.33%), and diterpene (3.70%). Regarding the major compounds, Z-nerolidol (19.16%), germacrene D (12.92%) and α-bulnesene (8.47%) could be highlighted, which corresponded to 40.55% of the substances that were found. The essential oil from Ocotea paranaensis has phosphomolybdenum reducing action and is moderately toxic to the Artemia salina (LC50 = 147.91 µg/mL). It showed haemolytic potential and moderate activity against Staphylococcus aureus, (minimum inhibitory concentration MIC = 250 µg/mL) and Pseudomonas aeruginosa (MIC = 500 µg/mL). No satisfactory cytotoxicity results were observed in lineage H460 and HeLa.

Comparison of two oral health-related quality-of-life measures in elderly patients: the influence of missing teeth, and socio demographic factors / Comparação entre dois instrumentos de avaliação de qualidade de vida em pacientes idosos: a influência da perda de dentes e fatores sociodemográficos

Objective: The Oral Health Impact Profile-14 (OHIP14) and the Geriatric/General Oral Health Assessment Index (GOHAI) have never been compared to a group of the same subjects in the Brazilian population. The aim of the study was to compare the OHIP-14 and GOHAI measures. Material and Methods: 129 independently living people over the age of 60 were included in the study. The GOHAI and OHIP-14 measures were used. Other variables were included: age, gender, education, number of missing teeth, annual household income and frequency of dentist visits. Results: The mean age of respondents was 65 years. The internal reliability (Cronbach's alpha) showed a high internal consistency for both measures. Spearman's rank correlation coefficient between the GOHAI and OHIP-14 scores was 0.73. Using the additive method of creating scores, none of the respondents had the GOHAI score of zero, indicating no impact from oral conditions, while 9.3% of them had an OHIP-14 score of zero. Dental status, age, gendler and frequency of dental visit were significantly associated with the results ofthe GOHAI and the OHIP-14 (Kruskal­Wallis test, Mann­Whitney U test). Conclusions: There was a strong correlation between the GOHAI and the OHIP14. Both instruments demonstrated good discriminant properties and helped capture the respondents' oral health problems. (AU)

Objetivo: O Perfil de Impacto na Saúde Oral-14 (OHIP14) e o Índice Geral de Avaliação de Saúde Oral em Geriatria (GOHAI) nunca foram comparados a um grupo dos mesmos sujeitos na população brasileira. O objetivo do estudo foi comparar as medidas OHIP-14 e GOHAI. Material e Métodos: 129 pessoas independentes com idade superior a 60 anos foram incluídas no estudo. Foram utilizadas as medidas GOHAI e OHIP-14. Outras variáveis foram incluídas: idade, sexo, escolaridade, número de dentes ausentes, renda familiar anual e frequência de visitas ao dentista. Resultados: a média de idade dos entrevistados foi de 65 anos. A confiabilidade interna (alfa de Cronbach) mostrou uma alta consistência interna para ambas as medidas. O coeficiente de correlação de Spearman entre os escores GOHAI e OHIP-14 foi de 0,73. Utilizando o método aditivo de criação de escores, nenhum dos entrevistados obteve pontuação zero no GOHAI, indicando nenhum impacto das condições bucais, enquanto 9,3% deles tiveram pontuação zero no OHIP-14. O estado dentário, a idade, o sexo e a frequência da visita foram significativamente associados aos resultados do GOHAI e do OHIP-14 (teste de Kruskal-Wallis, teste de Mann-Whitney U). Conclusões: Houve uma forte correlação entre o GOHAI e o OHIP-14. Ambos os instrumentos demonstraram boas propriedades discriminantes e ajudaram a capturar os problemas de saúde bucal dos entrevistados. (AU)

Phytochemical and morpho-anatomical study of the vegetative organs of Psychotria fractistipula L. B.Sm., R.M. Klein & Delprete (Rubiaceae)

Psychotria fractistipula L.B.Sm, R.M. Klein & Delprete (Rubiaceae) is found in the existing Atlantic Forest in the South of Brazil, in the Paraná and Santa Catarina States. The members of Rubiaceae are characterized chemically by the presence of alkaloids, some pharmacological properties of which include antifungal, antibacterial, analgesic, antioxidant, antimutagenic, and antiviral activities. In this study, we report the results of anatomical, morphological, and histochemical analyses of the leaves and stems of the Rubiaceae family member, P. fractistipula. The anatomical analysis involved of light microscopy and scanning electron microscopy. Morpho-anatomical and histochemical characterization were made using standard methodology. The isolated compounds were identified by Nuclear Magnetic Resonance spectroscopic analysis. The following structures are highlighted as the distinctive features of the species: presence of petiolate leaves and a petiole base, leaf blade with smooth cuticle on both surfaces, paracytic stomata, and, dorsiventral mesophyll and presence of trichomes on the leaves and stems. Phytosteroids, identified as β-sitosterol and campesterol, were observed in the hexane fraction of the stem. Future studies should focus on the isolation of other fractions of interest and their characterization through specific biological and cytotoxicity assays.

PEG-PCL Nanocapsules Containing Curcumin: Validation of HPLC Method for Analyzing Drug-loading Efficiency, Stability Testing and Cytotoxicity on NIH-3T3 Cell Line

Abstract Curcumin (CUR) shows potential use for treating cancer. However, CUR has low solubility and reduced bioavailability, which limit its clinical effect. Therefore, the development of nanocarriers can overcome these problems and can ensure the desired pharmacological effect. In addition, it is mandatory to prove the quality, the efficacy, and the safety for a novel nanomedicine to be approved. In that sense, this paper aimed (a) to prepare CUR-loaded polyethylene glycol-poly(ε-caprolactone) nanocapsules; (b) to validate an analytical method by high performance liquid chromatography (HPLC) for quantifying CUR in these nanoformulations; (c) to evaluate the physicochemical stability of these formulations; and to investigate their cytotoxicity on NIH-3T3 mouse fibroblast cells. The HPLC method was specific to CUR in the loaded nanocapsules, linear (r = 0.9994) in a range of 10.0 to 90.0 µg.mL-1 with limits of detection and quantification of 0.160 and 0.480 µg.mL-1, respectively. Precision was demonstrated by a relative standard deviation lower than 5%. Suitable accuracy (102.37 ± 0.92%) was obtained. Values of pH, particle size, polydispersity index, and zeta potential presented no statistical difference (p > 0.05) for CUR-loaded nanoparticles. No cytotoxicity was observed against NIH-3T3 mouse embryo fibroblast cell line using both the tetrazolium salt and sulforhodamine B assays. In conclusion, a simple and inexpensive HPLC method was validated for the CUR quantification in the suspensions of nanocapsules. The obtained polymeric nanocapsules containing CUR showed suitable results for all the performed assays and can be further investigated as a feasible novel approach for cancer treatment.

Effect of Cilostazol-Loaded PCL/PEG Nanocapsules on Abdominal Aortic Tunics and Lipid Profile of Wistar Rats

Abstract Cilostazol (CLZ) is a phosphodiesterase III inhibitor with antiplatelet and vasodilator properties. It has been recently verified that CLZ plays a significant role in the arteries by inhibiting the proliferation and growth of muscle cells, increasing the release of nitric oxide by the endothelium and promoting angiogenesis. Considering these promising effects, the use of nanocapsules may be an interesting strategy to optimize its pharmacokinetics and pharmacodynamics at the vascular level for preventing atherosclerosis. The aim of this study was to evaluate the effect of cilostazol-loaded nanocapsules in the abdominal aortic tunics and on the lipid profile of Wistar rats in order to investigate its potential role in the prevention of atherosclerosis. Thirty-two animals were divided into four groups of eight animals, with 30-day treatment. Group 1 received nanoencapsulated CLZ; Group 2, control nanocapsules with no drug; Group 3, propylene glycol and water; and Group 4, a solution of CLZ in propylene glycol and water. After 30 days, there was no statistically significant difference between the groups regarding the cellularity and thickness of the arterial tunics of the abdominal aorta. However, the group that received nanoencapsulated CLZ (Group 1) had an improvement in HDL-c and triglyceride values compared to unloaded nanocapsules (Group 2).

Chemical composition, phytotoxic potential, biological activities and antioxidant properties of Myrcia hatschbachii D. Legrand essential oil

Myrcia hatschbachii D. Legrand (Myrtaceae) is a native and endemic species from Brazil. This study investigated the essential oil composition, phytotoxic potential, in vitro toxicity, antioxidant properties and antibacterial activity of species. Chromatographic analysis of essential oil identified trans-calamanene, (E)-caryophyllene and spathulenol as major components. Antioxidant capacity was determined by the DPPH• scavenging method and phosphomolybdenum complex formation assay. Antibacterial activity was evaluated using the Minimal Inhibitory Concentration test, demonstrating that the essential oil was active toward Enterococcus faecalis and Staphylococcus aureus. Phytotoxic activity of essential oil was analyzed by testing interference on germination and growth of Lactuca sativa, demonstrating significant inhibition of the hypocotyls and radicles of seeds. Preliminary toxicity studies were determined using Artemia salina, resulting in an LC50 of 409.92 µg/mL, and through hemolytic activity. The results of the phytotoxic activity point to a possible application for Myrcia hatschbachii in the development of natural herbicides and the in vitro toxicity assays suggests the performance of antitumoral activity tests, having in mind the prospection of antineoplastic drugs.

Long-lasting anti-platelet activity of cilostazol from poly(ε-caprolactone)-poly(ethylene glycol) blend nanocapsules.

Cilostazol (CLZ) acts as a vasodilator and antiplatelet agent and is the main drug for the treatment of intermittent claudication (IC) related to peripheral arterial disease (PAD). The usual oral dose is 100 mg twice a day, which represents a disadvantage in treatment compliance. CLZ presents several side effects, such as headache, runny nose, and dizziness. This paper aimed to obtain novel polymeric nanocapsules prepared from poly(ε-caprolactone)-poly(ethylene glycol) (PCL-PEG) blend containing CLZ. Nanocapsules showed pH values between 6.1 and 6.3, average size lower than 137 nm, low polydispersity index (<0.22) and negative zeta potential. These nanoformulations demonstrated spherical shape with smooth surface. Results achieved by X-ray diffraction (XRD) and differential scanning calorimetry (DSC) indicated drug amorphization compared to pure CLZ. Fourier-transformed infrared spectroscopy (FTIR) showed no chemical bonds between drug and polymers. Formulations presented suitable stability for physical parameters. The in vitro drug release demonstrated prolonged release with no burst effect. Drug release was controlled by both mechanisms of polymer relaxation/degradation and Fickian diffusion. Moreover, chosen CLZ-loaded nanocapsules provided an in vivo prolonged antiplatelet effect for CLZ statistically similar to aspirin. These formulations can be further used as a feasible oral drug delivery carrier for controlled release of CLZ in order to treat PAD and IC events.

Ocotea nutans (Nees) Mez (Lauraceae): chemical composition, antioxidant capacity and biological properties of essential oil

The present study was undertaken to assess the potential uses of the essential oil obtained from Ocotea nutans (Nees) Mez. The hydrodistilled essential oil from O. nutans leaves was analyzed by gas chromatography-mass spectrometry. Fifty-eight compounds representing 87,29% of the total leaf essential oil components were identified, of which biciclogermacrene(11.41%), germacrene-D (4.89%), bisabolol-11-ol(3.73%) and spathulenol (3.71%) were the major compounds. The essential oil from O. nutans were tested for antibacterial activity using the minimum inhibitory concentracion (MIC) method, Artemia salina method, larvicidal activity in Aedes aegypti, and antioxidant capacity.The antioxidant activity measured by the phosphomolybdenum complex and Prussian blue method had positive results. The minimum inhibitory concentration for the microorganisms tested allowed moderate inhibitionfor Enterococcus faecalis (MIC=500 µg/mL). Artemia salina were toxic to the organisms in the study (LC50= 71,70 µg /mL). The essential oil showed remarkable larvicidal activity potencial (LC50= 250 µg/mL). The present results showed thatO. nutans essential oil has potential biological uses

Composition, antioxidant properties, and biological activities of the essential oil extracted from Ocotea diospyrifolia (Meisn.) Mez

The article has aimed to characterize the essential oil extracted from Ocotea diospyrifolia (Meisn.) Mez. leaves, in terms of its chemical composition and antioxidant, hemolytic, and phytotoxic potentials, as well as its toxicity against Artemia salina. The major constituents identified by CG-MS were d-elemene, spathulenol, and b-atlantol. When screened for potential biological activities, the essential oil presented low toxicity against Artemia salina, and a capacity of lysing red blood cells. Also, the evaluation of its in vitro antioxidant activity, using the phosphomolybdenum method, showed better results when compared to butylhydroxytoluene (BHT) and rutin. In conclusion, the results obtained showed certain in vitro toxicity, leading to an interesting target for cytotoxicity evaluations of carcinoma cells.

Spray-dried Eudragit® L100 microparticles containing ferulic acid: Formulation, in vitro cytoprotection and in vivo anti-platelet effect.

This paper aimed to obtain new spray-dried microparticles containing ferulic acid (FA) prepared by using a methacrylic polymer (Eudragit® L100). Microparticles were intended for oral use in order to provide a controlled release, and improved in vitro and in vivo biological effects. FA-loaded Eudragit® L100 microparticles were obtained by spray-drying. Physicochemical properties, in vitro cell-based effects, and in vivo platelet aggregation were investigated. FA-loaded Eudragit® L100 microparticles were successfully prepared by spray-drying. Formulations showed suitable encapsulation efficiency, i.e. close to 100%. Microparticles were of spherical and almost-spherical shape with a smooth surface and a mean diameter between 2 and 3µm. Fourier-transformed infrared spectra demonstrated no chemical bond between FA and polymer. X-ray diffraction and differential scanning calorimetry analyses indicated that microencapsulation led to drug amorphization. FA-loaded microparticles showed a slower dissolution rate than pure drug. The chosen formulation demonstrated higher in vitro cytoprotection, anti-inflammatory and immunomodulatory potential and also improved in vivo anti-platelet effect. These results support an experimental basis for the use of FA spray-dried microparticles as a feasible oral drug delivery carrier for the controlled release of FA and improved cytoprotective and anti-platelet effects.

Spray-dried solid dispersions containing ferulic acid: comparative analysis of three carriers, in vitro dissolution, antioxidant potential and in vivo anti-platelet effect.

This article aimed to improve the relative solubility and dissolution rate of ferulic acid (FA) by the use of spray-dried solid dispersions (SDs) in order to ensure its in vitro antioxidant potential and to enhance its in vivo anti-platelet effect. These SDs were prepared by spray-drying at 10 and 20% of drug concentration using polyvinylpyrrolidone K30 (PVP-K30), polyethylene glycol 6000 (PEG 6000) and poloxamer-188 (PLX-188) as carriers. SDs and physical mixtures (PM) were characterized by SEM, XRPD, FTIR spectroscopy and TGA analysis. Spray-dried SDs containing FA were successfully obtained. Relative solubility of FA was improved with increasing carrier concentration. PVP-K30 and PEG 6000 formulations showed suitable drug content values close to 100%, whereas PLX-188 presented mean values between 70 and 90%. Agglomerates were observed depending on the carrier used. XRPD patterns and thermograms indicated that spray-drying led to drug amorphization and provided appropriate thermal stability, respectively. FTIR spectra demonstrated no remarkable interaction between carrier and drug for PEG 6000 and PLX-188 SDs. PVP-K30 formulations had changes in FTIR spectra, which denoted intermolecular O-H•••O = C bonds. Spray-dried SDs played an important role in enhancing dissolution rate of FA when compared to pure drug. The free radical-scavenging assay confirmed that the antioxidant activity of PEG 6000 10% SDs was kept. This formulation also provided a statistically increased in vivo anti-platelet effect compared to pure drug. In summary, these formulations enhanced relative solubility and dissolution rate of FA and chosen formulation demonstrated suitable in vitro antioxidant activity and improved in vivo anti-platelet effect.

A Stability-Indicating HPLC-DAD Method for Determination of Ferulic Acid into Microparticles: Development, Validation, Forced Degradation, and Encapsulation Efficiency.

A simple stability-indicating HPLC-DAD method was validated for the determination of ferulic acid (FA) in polymeric microparticles. Chromatographic conditions consisted of a RP C18 column (250 mm × 4.60 mm, 5 µm, 110 Å) using a mixture of methanol and water pH 3.0 (48 : 52 v/v) as mobile phase at a flow rate of 1.0 mL/min with UV detection at 320 nm. The developed method was validated as per ICH guidelines with respect to specificity, linearity, limit of quantification, limit of detection, accuracy, precision, and robustness provided suitable results regarding all parameters investigated. The calibration curve was linear in the concentration range of 10.0-70.0 µg/mL with a correlation coefficient >0.999. Precision (intraday and interday) was demonstrated by a relative standard deviation lower than 2.0%. Accuracy was assessed by the recovery test of FA from polymeric microparticles (99.02% to 100.73%). Specificity showed no interference from the components of polymeric microparticles or from the degradation products derived from acidic, basic, and photolytic conditions. In conclusion, the method is suitable to be applied to assay FA as bulk drug and into polymeric microparticles and can be used for studying its stability and degradation kinetics.

Residues of Citrus sinensis (L) Osbeck as agents that cause a change in antioxidant defense in plants / Resíduos de Citrus sinensis (L) Osbeck como agentes que causam uma alteração na defesa antioxidante em plantas

This work aimed to verify the allelopathic potential of the extract of Citrus seeds, for the purpose of adding a sustainable value to the fruit seeds toward their use as industrial residues. The extract was obtained with a Soxhlet apparatus by using hexane, chloroform, and methanol as solvents. The hexane extract of the Citrus seeds primarily consisted of linoleic acid (36.6%), followed by α-linoleic acid (25.3%), oleic acid (17.8%), palmitic acid (9.7%), and estearic acid (3.3%). The analysis results indicate that the oil is similar to those used in the cosmetics and food industries and has an economic value from its industrial application. In addition, the use of the oil causes changes in the oxidant balance, germination, and growth of plants...

Este trabalho teve como objetivo verificar o potencial alelopático do extrato de sementes de Citrus, com o objetivo de agregar valor sustentável para a semente de frutas para a sua utilização como resíduo industrial. O extrato foi obtido com aparelho de Soxhlet, utilizando hexano, clorofórmio e metanol como solventes. O extrato hexânico das sementes de Citrus constituiu principalmente por ácido linoleico (36,6%), seguido por ácido α-linoleico (25,3%), ácido oleico (17,8%), ácido palmítico (9,7%) e ácido esteárico (3,3%). As análises indicam que o óleo é semelhante aos utilizados na indústria de cosméticos e de alimentos, tem valor econômico para a utilização na indústria e seu uso provoca alterações no equilíbrio oxidativo, germinação e crescimento...

Chemical review and studies related to species from the genus Tynanthus (Bignoniaceae)

Species from the Bignoniaceae Family, including the genus Tynanthus, are very prevalent in the tropical Americas, with specimens found in a large part of the Brazilian territory. These plants are commonly used in traditional medicine for several purposes, and some studies have described their chemical structure, in addition to other reports related to some species from this genus. This review aimed to gather information from published works concerning species of the genus Tynanthus, as well as to detect flaws in research related to these plants, which may have great biological and pharmaceutical importance. Also, this review points out some common chemical characteristics of these species, providing information that may help new researchers to improve their knowledge about these plants.

As espécies da família Bignoniaceae possuem grande predominância na região da América tropical e entre elas, as espécies do gênero Tynanthus, com representantes em grande parte do território brasileiro. Estas plantas são comumente utilizadas na medicina tradicional para os mais diversos fins e algumas pesquisas já descrevem a constituição química além de outros estudos relacionados a alguns integrantes deste gênero. Este trabalho de revisão teve como objetivo reunir informações de trabalhos publicados a respeito das espécies do gênero Tynanthus e permitiu detectar a deficiência nas pesquisas relacionadas a estas plantas, que podem trazer consigo grande importância biológica e farmacológica. Além disto, este trabalho tornou possível apontar algumas características químicas em comum entre as espécies, trazendo informações que podem auxiliar novos pesquisadores que procuram melhorar seus conhecimentos acerca destas plantas.

Production and characterization of alginate-starch-chitosan microparticles containing stigmasterol through the external ionic gelation technique

Stigmasterol - a plant sterol with several pharmacological activities - is susceptible to oxidation when exposed to air, a process enhanced by heat and humidity. In this context, microencapsulation is a way of preventing oxidation, allowing stigmasterol to be incorporated into various pharmaceutical forms while increasing its absorption. Microparticles were obtained using a blend of polymers of sodium alginate, starch and chitosan as the coating material through a one-stage process using the external gelation technique. Resultant microparticles were spherical, averaging 1.4 mm in size. Encapsulation efficiency was 90.42% and method yield 94.87%. The amount of stigmasterol in the oil recovered from microparticles was 9.97 mg/g. This technique proved feasible for the microencapsulation of stigmasterol.

O estigmasterol, um fitoesterol com diversas atividades farmacológicas, é suscetível à oxidação quando exposto ao ar, calor e umidade. Neste contexto, a microencapsulação é uma forma de proteção contra oxidação, permitindo a incorporação do estigmasterol em diversas formas farmacêuticas e aumentar sua absorção. As micropartículas foram obtidas por gelificação iônica externa, em uma etapa, utilizando como revestimento polímeros naturais de alginato de sódio, amido de milho e quitosana. As micropartículas apresentaram formato esférico com tamanho aproximado de 1,4 mm. O rendimento foi de 94,87% e a eficiência média de encapsulação de 90,42%. A quantidade de estigmasterol no óleo recuperado das micropartículas foi de 9,97 mg/g. O método mostrou-se viável para a microencapsulação do estigmasterol.

Antinociceptive effects of a chloroform extract and the alkaloid dicentrine isolated from fruits of Ocotea puberula.

The present work describes the chemical characterization of a chloroform fraction (CF) obtained from an extract of Ocotea puberula (Lauraceae) fruits, and preliminary antinociceptive analysis of CF and the alkaloid dicentrine, isolated from this fraction. CF (30-300 mg/kg, p. o.) caused dose-related inhibition of abdominal constrictions caused by acetic acid and also inhibited both phases of formalin-induced nociception. However, hexane or ethyl acetate fractions did not produce any effect. Antinociception caused by CF (100 mg/kg, p. o.) in the acetic acid test was not affected either by caffeine, an adenosine receptor antagonist, or by naloxone, an opioid receptor antagonist, and neither was associated with nonspecific effects such as muscle relaxation or sedation. Furthermore, dicentrine (30-300 mg/kg, p. o.) produced dose-related inhibition of acetic acid-induced pain without causing changes in the motor performance of mice. The results show, for the first time, that CF from Ocotea puberula fruits produced marked antinociception in different models of chemical pain, and this effect appears to be, at least in part, due to the presence of dicentrine. The mechanism by which CF and the alkaloid produced antinociception still remains unclear, but the adenosinergic or opioid system seems unlikely to be involved in this action.

Phytochemical constituents and preliminary toxicity evaluation of leaves from Rourea induta Planch. (Connaraceae) / Constituintes fitoquímicos e avaliação preliminar de toxicidade folhas de Rourea Induta Planch. (Connaraceae)

Most active plants are toxic at high doses and it is therefore important to investigate the preliminary toxicity of plant extracts. The Rourea induta species is a potential drug with no phytochemical or biological studies registered in the literature. Thus, a phytochemical study and a toxicity analysis of the ethanolic extract obtained from the leaves of Rourea induta Planch., Connaraceae, was run. A long chain hydrocarbon, n-tetracosane, and four flavonoids were identified: quercetin, and three glycosylated derivates, quercetin-3-O-α-arabinofuranoside, quercetin-3-O-β-xyloside and quercetin-3-O-β-galactoside. This is the first time these have been isolated in this species. The structures were elucidated by 13C NMR, ¹H NMR, UV and IR spectroscopy. The toxicity evaluation of extracts was performed by the brine shrimp method and determination of hemolytic activity. The samples demonstrated no toxic potential by the analyzed methods.

A maioria das plantas ativas é tóxica em doses elevadas, portanto, é importante a investigação da toxicidade preliminar dos extratos das plantas. A espécie Rourea induta é uma droga potencial que não apresenta estudo fitoquímico ou biológico descrito na literatura. Assim, um estudo fitoquímico e análises toxicológicas foram realizados com o extrato etanólico obtido das folhas de Rourea induta Planch., Connaraceae. Foram obtidos um hidrocarboneto de cadeia longa, n-tetracosano, e quatro flavonóides, quercetina e três derivados glicosilados, quercetina-3-O-α-arabinofuranosideo, quercetina-3-O-β-xilosideo e quercetina-3-O-β-galactosideo. Esta é a primeira vez que estes compostos são isolados nesta espécie. As estruturas foram elucidadas por espectroscopia de RMN-13C, RMN-¹H, ultravioleta e infravermelho. A avaliação da toxicidade dos extratos foi analisada pelo método da Artemia salina e atividade hemolítica. Nenhuma das amostras testadas apresentou um potencial tóxico pelos métodos analisados.