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Stingless bee honey (SBH) is gaining attention due to its nutritional, sensorial, and medicinal characteristics. This study focuses on the combination of physicochemical properties, antioxidant capacity, mineral profile, and mass spectrometry-based fingerprints, using a chemometric approach to differentiate SBH (n = 18) from three different Brazilian biogeographical zones (Caatinga, Cerrado, and Atlantic Forest). The physicochemical properties of SBH varied, resulting in a wide range of water activity, moisture, total soluble solids, pH, and total and free acidity. The Caatinga honey showed the highest and the lowest contents of phenolics and flavonoids, respectively. The antioxidant free-radical scavenging assays demonstrated that the Brazilian SBH has a high antioxidant potential. The mineral profile of honey samples from the Atlantic Forest revealed higher contents of Ca and Fe while the Cerrado and Caatinga honey showed the highest P contents. Partial Least-Squares Discriminant Analysis (PLS-DA) analysis separated the samples into three groups based on the biogeographical zones of harvest. The main separation factors between groups were the m/z 326 ion and the Fe content. Univariate analysis confirmed that Fe content is important for SBH discrimination. The present results indicate that the origin of SBH can be determined on the basis of mineral profile, especially Fe content.
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INTRODUCTION: Mass spectrometry in natural products research has been used as a first step to identify possible chemical structures and to guide subsequent efforts to isolate novel compounds. Preparations of Ampelozizyphus amazonicus Ducke (AA) are known for their high content of saponins, especially dammarane-type triterpenoid aglycones. In the Amazon, where it is known as "saracura-mirá", roots and bark are widely used for the treatment and prevention of malaria, while the wood is discarded. The extract prepared from the wood is also saponin-rich, but its exact chemical composition has not been described. OBJECTIVE: This study provides information on the chemical profiling and tentative structural identification of the major compounds (saponins) present in aqueous and ethanol extracts of bark and wood of AA by mass spectrometry. METHODS: The strategy used to identify compounds present in all samples was ultra-high-performance liquid chromatography with an ultraviolet detector coupled to tandem mass spectrometry (UHPLC-UV-MS/MS) for the analysis of fragmentation patterns through product ion scan using MZmine 2 software. Also, direct sample injection and electrospray ionisation combined with high-resolution mass spectrometry (DI-ESI-HRMS) measurements were performed. RESULTS: The extracts showed chemical similarity, and 95 saponins were tentatively identified in AA wood and bark, including 73 which are described for the first time as tentative structures for this plant species. CONCLUSION: This research describes a useful method for the fast and simultaneous tentative identification of major saponins in AA, contributing to the study of the chemical properties of this genus and family. Furthermore, it demonstrates the importance of the qualitative dereplication process, allowing a straightforward way to propose the tentative identification of compounds.
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Saponinas , Cromatografía Líquida de Alta Presión , Corteza de la Planta , Extractos Vegetales , Espectrometría de Masa por Ionización de Electrospray , Espectrometría de Masas en Tándem , MaderaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Jatropha curcas L. is a plant with high cultural significance for quilombola communities of Oriximiná (Pará State, Brazil). Although the plant is highly toxic, its seeds are used in these communities to treat tuberculosis and related diseases and symptoms. AIM OF THE STUDY: This study was designed to provide a scientific rationale for the traditional detoxification method and use of J. curcas seeds in quilombola communities of Oriximiná. MATERIALS AND METHODS: J. curcas seeds were manually separated into testa, tegmen, endosperm, and embryo, and then methanolic extracts of each sample were prepared. The traditional preparation of J. curcas seeds consists of a water extract of endosperms that is known as "milk of pinhão-branco". The content of phorbol esters (PEs) in the extracts was analyzed by High-Performance Liquid Chromatography with Diode-Array Detection (HPLC-DAD). The cytotoxic activity was evaluated in human monocytic cell line THP-1 by Resazurin Reduction Assay, and antimycobacterial activity was assessed by determining Minimal Inhibitory Concentration (MIC) values against H37Rv and BCG strains using the Resazurin Microtiter Assay (REMA). RESULTS: The content analysis revealed that the distribution of PEs within the seeds is not homogeneous. High contents were found in tegmens (4.22⯱â¯0.25-15.52⯱â¯0.06â¯mg/g) and endosperms (1.61⯱â¯0.07-5.00⯱â¯0.42â¯mg/g), while concentrations found in testas and embryos were all below 0.5â¯mg/g. The traditional preparation derived from the endosperm of J. curcas contained significantly less PEs than the endosperms (0.01⯱â¯0.005â¯mg/g). Against THP-1â¯cells, all the parts of the seed showed cytotoxic activity, while the traditional preparation was considered non-cytotoxic. Nevertheless, only the tegmen and endosperm of J. curcas were considered active against M. tuberculosis and M. bovis (MICâ¯=â¯200⯵g/mL). CONCLUSION: The results of this study indicated that the traditional processing performed by the quilombola people from Oriximiná is effective in reducing the toxicity of J. curcas seeds. Although inactive against mycobacteria, the extensive use of the traditional preparation and its low toxicity encourage further studies to investigate other biological activities.
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Jatropha , Medicina Tradicional , Ésteres del Forbol , Extractos Vegetales , Semillas/química , Antibacterianos/análisis , Antibacterianos/farmacología , Antibacterianos/toxicidad , Brasil , Supervivencia Celular/efectos de los fármacos , Humanos , Pruebas de Sensibilidad Microbiana , Mycobacterium bovis/efectos de los fármacos , Mycobacterium bovis/crecimiento & desarrollo , Mycobacterium tuberculosis/efectos de los fármacos , Mycobacterium tuberculosis/crecimiento & desarrollo , Ésteres del Forbol/análisis , Ésteres del Forbol/farmacología , Ésteres del Forbol/toxicidad , Extractos Vegetales/química , Extractos Vegetales/farmacología , Extractos Vegetales/toxicidad , Células THP-1RESUMEN
Lippia species share various pharmacological activities and are used in traditional cooking and medicine worldwide. Combined chromatographic techniques such as column chromatography, high-performance liquid chromatography, and countercurrent chromatography led to the purification of two new antifungal phenylpropanoid glycosides, lippiarubelloside A (1) and lippiarubelloside B (2), by bioactivity-directed fractionation of an ethanol-soluble extract from Lippia rubella, in addition to the known active related compounds forsythoside A (3), verbascoside (4), isoverbascoside (5), and poliumoside (6). The structures of compounds 1 and 2 were determined by comparison of their NMR spectroscopic data with the prototype active compound 4. Cryptococcus neoformans, which causes opportunistic lung infections, was sensitive to compounds 1-6 in the concentration range of 15-125 µg/mL. A synergistic effect (FICindex = 0.5) between 3 and amphotericin B was demonstrated. The glycosylated flavonoids pectolinarin (7), linarin (8), and siparunoside (9) were also isolated.
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Antifúngicos/farmacología , Glicósidos/farmacología , Lippia/química , Fenilpropionatos/farmacología , Antifúngicos/química , Candida/efectos de los fármacos , Cryptococcus/efectos de los fármacos , Glicósidos/química , Fenilpropionatos/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Análisis Espectral/métodosRESUMEN
ABSTRACT The bioavailability, toxicity, and therapeutic efficacy of a drug is directly related to its administration route. The pulmonary route can be accessed by inhalation after fumigation, vaporization or nebulization. Thus, pharmacological and toxicological evaluation accessed by an apparatus specifically designed and validated for this type of administration is extremely important. Based on pre-existing models, an inhalation chamber was developed. This presents a central structure with five animal holders. The nebulized air passes directly and continuously through these holders and subsequently to an outlet. Evaluation of its operation was performed using clove essential oil, a nebulizer, and a flow meter. The air within the chamber was collected by static headspace and analyzed by gas chromatography with a flame ionization detector. For this purpose, a 2.5 minutes chromatographic method was developed. The air flow in each of the five outputs was 0.92 liters per minute. During the first minute, the chamber became saturated with the nebulized material. Homogeneous and continuous operation of the chamber was observed without accumulation of volatile material inside it for 25 minutes. The inhalation chamber works satisfactorily for in vivo tests with medicines designed to be administrated by inhalation.
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Animales , Conejos , Ratas , Administración por Inhalación , Nebulizadores y Vaporizadores , Aceites Volátiles/administración & dosificación , Diseño de Equipo , Factores de Tiempo , Cromatografía Líquida de Alta Presión , Syzygium/químicaRESUMEN
The bioavailability, toxicity, and therapeutic efficacy of a drug is directly related to its administration route. The pulmonary route can be accessed by inhalation after fumigation, vaporization or nebulization. Thus, pharmacological and toxicological evaluation accessed by an apparatus specifically designed and validated for this type of administration is extremely important. Based on pre-existing models, an inhalation chamber was developed. This presents a central structure with five animal holders. The nebulized air passes directly and continuously through these holders and subsequently to an outlet. Evaluation of its operation was performed using clove essential oil, a nebulizer, and a flow meter. The air within the chamber was collected by static headspace and analyzed by gas chromatography with a flame ionization detector. For this purpose, a 2.5 minutes chromatographic method was developed. The air flow in each of the five outputs was 0.92 liters per minute. During the first minute, the chamber became saturated with the nebulized material. Homogeneous and continuous operation of the chamber was observed without accumulation of volatile material inside it for 25 minutes. The inhalation chamber works satisfactorily for in vivo tests with medicines designed to be administrated by inhalation.
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Administración por Inhalación , Diseño de Equipo , Nebulizadores y Vaporizadores , Aceites Volátiles/administración & dosificación , Animales , Cromatografía Líquida de Alta Presión , Ratones , Ratas , Syzygium/química , Factores de TiempoRESUMEN
ABSTRACT Commercial antiparasitics have been the main tool to control parasites, but due to the resistance development, plant extracts have been widely investigated to find new molecules. The present study aimed to investigate the in vitro acaricide and anthelmintic activities of the essential oil from the aerial parts of Hesperozygis myrtoides (A.St.-Hil. ex Benth.) Epling, Lamiaceae. The essential oil was obtained by hydrodistillation analyzed by GC-FID and GC-MS. Four tests were conducted in vitro to screen the antiparasitic action of the essential oil. The evaluation on Rhipicephalus (Boophilus) microplus was performed with the adult immersion test at concentrations ranging from 0.391 to 25 mg/ml and the larval packet test from 3.125 to 100 mg/ml. For Haemonchus contortus the egg hatch test was performed from 0.012 to 25 mg/ml and the larval development test from 0.003 to 0.4 mg/ml. The LC50 and LC90 values were calculated by Probit. The main components identified in the essential oil were isomenthone (47.7%), pulegone (21.4%), limonene (7.7%), isomenthyl acetate (6.8%) and neoisomenthol (3.9%). In the larval packet test the LC50 and LC90 were 13.5 and 21.8 mg/ml, respectively. In egg hatch test, the LC50 and LC90 were 0.249 and 0.797 mg/ml, respectively, while in the larval development test were 0.072 and 0.167 mg/ml, respectively. This is the first report of the H. myrtoides evaluation against those parasites. The anthelmintic results proved its efficacy on H. contortus encouraging new research with a focus on their main bioactives.
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The aim of this work was to develop and characterize nanoparticles as carriers of lapazine, a phenazine derived from ß-lapachone; its antimycobacterial activity is described for the first time as a potential treatment for tuberculosis. The lapazine was synthesized, and by using gas chromatography coupled to a flame ionization detector, it was possible to evaluate its purity degree of almost 100%. For better elucidation of the molecular structure, mass spectroscopy and 1H NMR were carried out and compared to the literature values. Lapazine was assayed in vitro against H37Rv Mycobacterium tuberculosis and a rifampicin-resistant strain, with minimum inhibitory concentration values of 3.00 and 1.56 µg mL(-1), respectively. The nanoparticles showed a polydispersity index of 0.16,mean diameter of 188.5 ± 1.7 mm, zeta potential of -15.03 mV, and drug loading of 54.71 mg g(-1) for poly-ε-caprolactone (PCL) nanoparticles and a polydispersity index of 0.318,mean diameter of 197.4 ± 2.7 mm, zeta potential of -13.43 mV and drug loading of 137.07 mg g(-1) for poly(DL-lactide-co-glycolide) (PLGA) nanoparticles. These results indicate that both polymeric formulations have good characteristics as potential lapazine carriers in the treatment of tuberculosis.
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Antituberculosos/síntesis química , Antituberculosos/farmacología , Ácido Láctico/química , Nanopartículas/química , Fenazinas/síntesis química , Fenazinas/farmacología , Poliésteres/química , Ácido Poliglicólico/química , Antituberculosos/química , Liberación de Fármacos , Cinética , Pruebas de Sensibilidad Microbiana , Mycobacterium tuberculosis/efectos de los fármacos , Nanopartículas/ultraestructura , Tamaño de la Partícula , Fenazinas/química , Copolímero de Ácido Poliláctico-Ácido Poliglicólico , Electricidad Estática , Difracción de Rayos XRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Malaria is the most important parasitic disease in the world, including in the Amazon region, due to its high incidence. In addition, malaria is difficult to control because of the geographical characteristics of the endemic Amazon region. The quilombola communities of Oriximina, located in remote rainforest areas, have extensive experience with medicinal plants due to their close contact with and dependence on local biodiversity as a therapeutic resource. To search for active bioproducts against malaria, based on in vitro tests using blood culture-derived parasites and plants selected by an ethno-directed approach in traditional quilombola communities of Oriximiná, in the Amazon region of Brazil. MATERIALS AND METHODS: Ethnobotanical data were collected from 35 informants in the quilombola communities of Oriximiná, Brazil, by a free-listing method for the survey of species locally indicated to be effective against malaria and related symptoms. Data were analyzed by salience index (S) and major use agreement. The activity of extracts from 11 plants, selected based on their Salience values (four plants with S>1; seven plants with S<0.1), was measured in vitro in cultures of W2 clone Plasmodium falciparum parasites resistant to chloroquine. RESULTS: Thirty-five ethnospecies comprising 40 different plants belonging to 23 botanical families and 37 genera were listed as antimalarials by the ethno-directed approach. Among these, 11 species selected based on their S values were assayed against P. falciparum. The most active plant extracts, with an IC50 as low as 1.6µg/mL, were obtained from Aspidosperma rigidum (Apocynaceae), Bertholletia excelsa (Lecythidaceae) and Simaba cedron (Simaroubaceae), all of which displayed an S value>1. CONCLUSION: A strong correlation between the consensus of the informants from quilombola communities living in a malaria endemic area and the salience index indicating antiplasmodial activity was observed, where the ethnospecies mostly cited to be effective against malaria produced the most active plant extracts in vitro. It was also evident from the data that these groups approached the treatment of malaria with an holistic view, making use of purgative, depurative, emetic and adaptogen plants.
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Malaria/tratamiento farmacológico , Fitoterapia , Plantas Medicinales , Adulto , Anciano , Anciano de 80 o más Años , Antimaláricos/farmacología , Brasil , Etnofarmacología , Femenino , Humanos , Concentración 50 Inhibidora , Masculino , Medicina Tradicional , Persona de Mediana Edad , Extractos Vegetales/farmacología , Plasmodium falciparum/efectos de los fármacos , Adulto JovenRESUMEN
Infusions and decoctions of three chemotypes of Lippia alba (Mill.) N. E. Brown (Verbenaceae) were investigated for their quantitative profiles by HPLC-DAD-ESI-MS analyses. An RP-HPLC method was developed which permitted the quality control of the preparations. The correct choice of the column allowed the detailed characterization of the constituents in a total analysis time of 35 min. The HPLC method was accordingly validated for linearity range, LOD, LOQ, accuracy and precision. For the quantitative analysis the three major phytochemical groups were taken into consideration, namely iridoids, phenylpropanoids and flavonoids. Comparative quantitative analyses revealed significant differences among the chemotypes that should be taken into account in the uses of the herbal teas. The developed HPLC-UV assay proved to be an efficient and alternative method for the discrimination of the three chemotypes. This is the first report of detailed analysis of the chemical composition of the constituents of L. alba chemotypes' teas.
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Bebidas/análisis , Cromatografía Líquida de Alta Presión/métodos , Lippia/química , Brasil , Flavonoides/análisisRESUMEN
Lippia origanoides Kunth. Verbenaceae, is of great importance in the Brazilian traditional medicine. Because of it, this work had the purpose to contribute to the ethnopharmacological knowledge of L. origanoides through an ethnobotanical survey conducted within quilombola (maroon) communities of Oriximiná, Pará, Brazil. Among 254 plants cited in the survey, L. origanoides stood out among the ten most versatile species. The agreed main uses were to treat menstrual cramps, stomachache, and baby and postpartum colic. This could indicate a consensus of the informants to possible antispasmodic, anti-inflammatory and analgesic activities of L. origanoides.Therefore, anti-inflammatory and analgesic activities of L. origanoides extract (aerial parts) were assessed through thermal (hot plate) and chemical (formalin and acetic acid) models of nociception. A dose-dependent reduction in acetic acid-induced writhing was observed after treating mice with L. origanoides extract. The same extract also inhibited significantly formalin-induced licking response and proved to have a central antinociceptive effect, in the hot plate test. This work demonstrates that L. origanoides is used specially by quilombola women from Oriximiná for disorders of the genitourinary system and that biological activities of this species could contribute to these uses. Furthermore, it was also observed antispasmodic, analgesic and antimicrobial uses of other species of the genus Lippia (Goniostachyum section), rich in thymol and carvacrol.
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ETHNOPHARMACOLOGICAL RELEVANCE: Several medicinal plants are traditionally traded in open-air markets in Rio de Janeiro State (Brazil) to treat tuberculosis (TB) and related symptoms. AIMS OF THE STUDY: Conduct a survey in the open-air markets of 20 cities of Rio de Janeiro State to find medicinal plants that are popularly used to treat tuberculosis and other related diseases and assess their in vitro antimycobacterial activity. MATERIALS AND METHODS: We used direct observation and semi-structured interviews and asked herbalists to list species (free listing) in order to gather data about the plant species most commonly used for lung problems. We calculated a Salience Index and acquired two species of "erva-de-passarinho" (mistletoe), Struthanthus marginatus and Struthanthus concinnus (Loranthaceae), commonly used to treat tuberculosis for a bioassay-guided isolation of the antimycobacterial active principles. Extracts, fractions and isolated compounds of both species were assayed in vitro against susceptible (H37Rv) and rifampicin-resistant (ATCC 35338) Mycobacterium tuberculosis strains. RESULTS: From the interviews, we generated a list of 36 plant species belonging to 12 families. The mistletoes Struthanthus marginatus and Struthanthus concinnus showed high Salience Index values among plants used to treat tuberculosis. Bioassay-guided fractionation of hexane extracts from both species led to the isolation and/or identification of steroids and terpenoids. The Minimum Inhibitory Concentration (MIC) of the extracts and isolated compounds ranged from 25 to 200 µg/mL. Some of the isolated compounds have been previously assayed against Mycobacterium tuberculosis, others are reported here for the first time (obtusifoliol: MIC H37Rv 50 µg/mL, MIC ATCC 35338 12.5 µg/mL; 3-O-n-acil-lup-20(29)-en-3ß,7ß,15α-triol: MIC H37Rv 200 µg/mL, MIC ATCC 35338 100 µg/mL). CONCLUSIONS: This study demonstrated the importance of ethnobotanical surveys in markets as a source for new drugs and also for scientific validation of folk medicine.
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Antibacterianos , Magnoliopsida , Plantas Medicinales , Antibacterianos/farmacología , Brasil , Recolección de Datos , Conocimientos, Actitudes y Práctica en Salud , Humanos , Pruebas de Sensibilidad Microbiana , Mycobacterium tuberculosis/efectos de los fármacos , Fitoterapia , Componentes Aéreos de las Plantas , Extractos Vegetales/farmacologíaRESUMEN
The compound (±)-trans-4-hydroxy-6-propyl-1-oxocyclohexan-2-one [(±)-δ-lactone] was isolated from the plant Vitex cymosa Bertero, and determined to be the active principle. The present study aimed to evaluate the antinociceptive effect of (±)-δ-lactone and to elucidate its mechanism of action. Mice were subjected to in-vivo models of acute pain (acetic acid-induced abdominal writhing, formalin and hot-plate tests) and the open-field test. (±)-δ-Lactone, administered orally (6-900 µmol/kg), exerted a dose-dependent antinociceptive effect in the acetic acid-induced abdominal writhing, formalin and hot-plate tests. (±)-δ-Lactone administered by the intrathecal (i.t.) and subplantar (s.p.) routes (10-600 nmol) exerted concentration-dependent antinociceptive effects in the formalin test, showing its spinal and peripheral activity, respectively. In the hot-plate test, (±)-δ-lactone was also active when administered i.t., confirming its spinal effect. The previous intraperitoneal (i.p.) application of naloxone, yohimbine, mecamylamine or glibenclamide did not alter the effect produced by the i.t. administration of (±)-δ-lactone, whereas the previous application of atropine and L-arginine significantly reduced its effects in the formalin and hot-plate tests. The previous i.p. application of L-NAME enhanced the antinociceptive effect of the i.t. administration of (±)-δ-lactone in the formalin and hot-plate tests. The previous i.p. application of L-NAME and L-arginine increased and decreased, respectively, the activity of (±)-δ-lactone administered by s.p. administration. These results indicate that (±)-δ-lactone has significant spinal and peripheral antinociceptive activity, and that its effects are at least partially mediated by a reduced nitric oxide production/release, most likely through mechanisms involving the cholinergic system.
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Dolor Agudo/prevención & control , Analgésicos no Narcóticos/uso terapéutico , Neuronas Colinérgicas/efectos de los fármacos , Lactonas/uso terapéutico , Óxido Nítrico/antagonistas & inhibidores , Nervios Periféricos/efectos de los fármacos , Nervios Espinales/efectos de los fármacos , Dolor Agudo/metabolismo , Administración Oral , Analgésicos no Narcóticos/administración & dosificación , Analgésicos no Narcóticos/efectos adversos , Analgésicos no Narcóticos/antagonistas & inhibidores , Animales , Conducta Animal/efectos de los fármacos , Brasil , Neuronas Colinérgicas/metabolismo , Relación Dosis-Respuesta a Droga , Etnofarmacología , Conducta Exploratoria/efectos de los fármacos , Inyecciones Espinales , Inyecciones Subcutáneas , Lactonas/administración & dosificación , Lactonas/efectos adversos , Lactonas/antagonistas & inhibidores , Masculino , Ratones , Óxido Nítrico/metabolismo , Dimensión del Dolor/efectos de los fármacos , Nervios Periféricos/metabolismo , Nervios Espinales/metabolismo , Vitex/químicaRESUMEN
Tuberculosis (TB), caused by Mycobacterium tuberculosis, is the world's number one killer among infectious diseases. The search for new naturalproducts that can act as drugs against TB has received increased attention duringthe last years. In this work we describe the isolation and identification of the active antimycobacterial principles of the dichloromethane extract from Lippia lacunosa Mart. & Schauer, Verbenaceae. Compounds were evaluated for their in vitro activity against Mycobacterium tuberculosis (susceptible and rifampicin resistantstrain) using a redox bioassay. From the dichloromethane extract of L. lacunosa leaves, seven methoxy-flavones named cirsimaritin (1), eupatilin (2), eupatorin (3), salvigenin (4), 3'-O-methyl-eupatorin (5), 3',7-dimethoxy-5,6,4'- trihydroxyflavone (6), and 7'-O-methylapigenin (7), and one triterpene, named oleanolic acid (8), were isolated. All compounds were found to display antimycobacterial activity against susceptible strain, with MIC ranging from 25 to 200 µg/mL. None of them was active against rifampicin resistant strain. This is the first report in the antimycobacterial activity of 6-substituted flavones, as well as the first report of the occurrence of these substances in L. lacunosa.
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The municipality of Oriximiná, Brazil, has 33 quilombola communities in remote areas, endowed with wide experience in the use of medicinal plants. An ethnobotanical survey was carried out in five of these communities. A free-listing method directed for the survey of species locally indicated against Tuberculosis and lung problems was also applied. Data were analyzed by quantitative techniques: saliency index and major use agreement. Thirty four informants related 254 ethnospecies. Among these, 43 were surveyed for possible antimycobacterial activity. As a result of those informations, ten species obtained from the ethnodirected approach (ETHNO) and eighteen species obtained from the random approach (RANDOM) were assayed against Mycobacterium tuberculosis by the microdilution method, using resazurin as an indicator of cell viability. The best results for antimycobacterial activity were obtained of some plants selected by the ethnopharmacological approach (50 percent ETHNO x 16,7 percent RANDOM). These results can be even more significant if we consider that the therapeutic success obtained among the quilombola practice is complex, being the use of some plants acting as fortifying agents, depurative, vomitory, purgative and bitter remedy, especially to infectious diseases, of great importance to the communities in the curing or recovering of health as a whole.
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Ocimum selloi, a traditional medicinal plant from Brazil, is sold in open-air markets at Rio de Janeiro State. Hesperozygis myrtoides is a very aromatic small bush found in the State of Minas Gerais, Brazil, growing at an altitude of 1800m. The chemical composition of both essential oils was analyzed as well as their antimicrobial activity against fungi and bacteria. For all specimens of Ocimum selloi obtained at open-air markets, methylchavicol was major compound found (93.6% to 97.6%) in their essential oils. The major compounds identified in the oil of H. myrtoides were pulegone (44.4%), isomenthone (32.7%), and limonene (3.5%). Both oils displayed antimicrobial activity against all tested microorganisms but Candida albicans was the most susceptible one. Combinations of the two oils in different proportions were tested to verify their antimicrobial effect against C. albicans, which, however, was not modified in any of the concentrations tested. The minimum inhibitory concentration (MIC) was determined to confirm the antimicrobial activity against C. albicans as well as other clinical isolates (C. glabrata, C. krusei, C. parapsilosis and C. tropicalis).
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Antibacterianos/aislamiento & purificación , Antifúngicos/aislamiento & purificación , Bacterias/efectos de los fármacos , Candida albicans/efectos de los fármacos , Lamiaceae/química , Aceites de Plantas/química , Terpenos/aislamiento & purificación , Antibacterianos/farmacología , Antifúngicos/farmacología , Brasil , Cromatografía de Gases y Espectrometría de Masas , Pruebas de Sensibilidad Microbiana , Hojas de la Planta/química , Aceites de Plantas/farmacología , Terpenos/química , Terpenos/farmacologíaRESUMEN
The diastereoselective synthesis of (+/-)-trans-4-hydroxy-6-propyl-1-oxocyclohexan-2-one, as a mixture trans:cis (3:1), was accomplished using a protocol that combine the Prins cyclization and RuO(4) oxidation. The synthesis this lactone allowed the elucidation of the correct structure of the substance isolated from the barks of Vitex cymosa. The delta-lactones mixture showed significant antinociceptive properties in preliminary tests using the tail flick model assay.
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Analgésicos/química , Analgésicos/uso terapéutico , Lactonas/química , Lactonas/uso terapéutico , Dolor/tratamiento farmacológico , Vitex/química , Analgésicos/síntesis química , Animales , Ciclización , Lactonas/síntesis química , Estructura Molecular , EstereoisomerismoRESUMEN
The polyisoprenylated benzophenones machuone and clusiachromene A have been isolated from the fruits of Clusia columnaris. The hexane extract of the young branches with leaves afforded a new euphane derivative, whose structure was elucidated by spectroscopic methods. On the contrary, the most polar EtOAc and ButOH extracts were constituted of flavonoid C-glucosides (isovitexin, vitexin and vitexin-2"-xyloside) and seven biflavonoids of the so-called Garcinia group.
Dos frutos de Clusia columnaris foram isoladas as benzofenonas poliisopreniladas machuona e clusiacromeno A. Do extrato em hexano obtido de galhos e folhas novas, um novo triterpeno do tipo eufano foi isolado. Sua estrutura foi elucidada através de métodos espectroscópicos. Por outro lado, dos extratos mais polares - em acetato de etila e em butanol, foram isolados os flavonóides C-glicosilados isovitexina, vitexina e vitexina-2"-xilosídeo, além de sete bisflavonóides conhecidos como bisflavonóides do grupo da Garcinia.
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Benzofenonas/aislamiento & purificación , Benzofenonas/química , Clusia/química , Clusiaceae/química , Flavonoides/aislamiento & purificación , Flavonoides/químicaRESUMEN
The objective of this study was to investigate spinal and supraspinal antinociceptive effects of a new synthetic compound, (+/-)-cis-(6-ethyl-tetrahydropyran-2-yl)-formic acid (tetrahydropyran derivative). Its activity was compared with those from morphine. In peripheral models of inflammation and hyperalgesia, tetrahydropyran derivative significantly reduced nociceptive effect induced by acetic acid or formalin in mice. Tetrahydropyran derivative developed antinociceptive effect on the tail-flick and hot-plate tests with a long-acting curve maintaining the effect for 4 h longer than morphine. The opioid receptor antagonist naloxone totally reverted tetrahydropyran derivative effects on both models. Morphine as well as tetrahydropyran derivative induced tolerance and sedation in mice. However, tetrahydropyran derivative-induced tolerance had its onset retarded and the sedative activity was lower when compared to that induced by morphine. These results indicate that this new substance develops an antinociceptive activity and may be used in the future as a substitute for traditional opioids.