ABSTRACT Lippia origanoides is a honey shrub which has showed hypotensive potential assessed by in vivo studies. The aim of this work is the development of a pharmaceutical formulation composed by an optimized extract obtained from aerial parts of L. origanoides. The quantification of the naringenin marker in the dry extract and tablets developed was performed, as well as the assessment of the oral acute toxicity in rats. The hydroalcoholic extract of L. origanoides was spray-dried with the addition of colloidal silicon dioxide (Lo-HAE/CSD), and then applied in the preparation of eight different lots of tablets. The influence of the diluent (cellulose or babassu mesocarp), the presence of binder, and the percentage of lubricant, as well as organoleptic and physicochemical characteristics were screened. For the quantification of the marker content both in Lo-HAE/CSD and in the tablets, an analytical curve of the naringenin standard was fitted, and the samples were then analyzed in UFLC. The toxicological assessment was performed in female Wistar rats according to the Acute Toxic Class Method from OECD. The developed tablets produced meet acceptable macroscopic characteristics, and the presence of babassu as diluent provided improved physicochemical properties. The best content of Lo-HAE/CSD in the tablet (100.27%) was identified for the lot containing babassu, composed by 1.0% magnesium stearate, without PVP binder in its formulation. Moreover, Lo-HAE/CSD showed no signs of toxicity. Therefore, the babassu mesocarp powder is a promising pharmaceutical excipient for the development of herbal tablets containing the Lippia origanoides extract.

ABSTRACT Samburá is the botanical pollen nectar agglutinated by salivary secretions of bees. Stingless bee pollen samples were collected in three periods of the year in Monsenhor Gil town, PI, Brazil, for extraction of volatile constituents by different techniques, analyzed by gas chromatography-mass spectrometry (GC-MS) and the palynological analysis used to identify the dominant pollen. Among the volatile compounds identified, kaur-16-ene, methyl and ethyl hexadecanoate, methyl linoleate and heneicosane were identified more frequently in the studied parameters: period of sample collection and extraction techniques used. The palynological analysis identified the pollen of Mimosa caesalpiniifolia Benth. as the dominant pollen in all samples studied.

RESUMOCasearia sylvestris Swartz é uma planta medicinal amplamente distribuída no Brasil. Ela possui atividade anti-inflamatória, antiulcerogênica e antitumoral e é popularmente utilizada para tratar envenenamentos ofídicos, ferimentos, diarreia, gripes e resfriados. Suas folhas são ricas em diterpenos clerodânicos tricíclicos oxigenados, particularmente casearinas. Aqui, nós avaliamos as atividades antioxidantes de um fração com casearinas (FC) isolada de C. sylvestrise as alterações histológicas no sistema nervoso central e fígados de camundongos Mus musculus. Primeiramente, estudos in vitro(0,9, 1,8, 3,6, 5,4 e 7,2 μg/mL) revelaram valores de CE50 de 3,7, 6,4 e 0,16 µg/mL para nitrito, radical hidroxila e níveis de TBARS, respectivamente. Em seguida, a FC (2,5, 5, 10 e 25 mg/kg/dia) foi administrada intraperitonealmente por 7 dias consecutivos em camundongos Swiss. Os níveis de nitrito no hipocampo (26,2, 27,3, 30,2 e 26,6 µM) e no corpo estriado (26,3, 25,4, 34,3 e 27,5 µM) aumentaram em todos os animais tratados com a FC (P < 0.05). As menores doses reduziram os níveis de glutationa reduzida, de catalase e de TBARS no hipocampo e no corpo estriado. Com exceção da redução na formação de TBARS, a FC demonstrou atividade antioxidante apenas in vitro. Os animais exibiram alterações histológicas que sugerem neurotoxicidade e hepatotoxicidade, indicando a necessidade de cuidados em relação ao consumo de preparações medicinais à base de Casearia sylvestris.

ABSTRACTCasearia sylvestris Swartz is a medicinal plant widely distributed in Brazil. It has anti-inflammatory, antiulcer and antitumor activities and is popularly used to treat snakebites, wounds, diarrhea, flu and chest colds. Its leaves are rich in oxygenated tricyclic cis-clerodane diterpenes, particulary casearins. Herein, we evaluated the antioxidant activities of a fraction with casearins (FC) isolated from C. sylvestrisand histological changes on the central nervous system and livers of Mus musculus mice. Firstly, in vitro studies (0.9, 1.8, 3.6, 5.4 and 7.2 μg/mL) revealed EC50 values of 3.7, 6.4 and 0.16 µg/mL for nitrite, hydroxyl radical and TBARS levels, respectively. Secondly, FC (2.5, 5, 10 and 25 mg/kg/day) was intraperitoneally administered to Swiss mice for 7 consecutive days. Nitrite levels in the hippocampus (26.2, 27.3, 30.2 and 26.6 µM) and striatum (26.3, 25.4, 34.3 and 27.5 µM) increased in all treated animals (P < 0.05). Lower doses dropped reduced glutathione, catalase and TBARS levels in the hippocampus and striatum. With the exception of this reduction in TBARS formation, FC displayed only in vitro antioxidant activity. Animals exhibited histological alterations suggestive of neurotoxicity and hepatotoxicity, indicating the need for precaution regarding the consumption of medicinal formulations based on Casearia sylvestris.

The pantropical genus Bauhinia, Fabaceae, known popularly as cow's foot, is widely used in folk medicine as antidiabetic. Behavioral effects of the ethanolic extract and ethereal, aqueous and ethyl acetate fractions from B. platypetala Benth. ex Hemsl. leaves were studied in male Swiss mice. The ethanolic extract and fractions were administered intraperitoneally and its effects on spontaneous motor activity (total motility, locomotion, rearing and grooming behavior) were monitored. Anxiolytic-like properties were studied in the elevated plus-maze test and the possible antidepressant-like actions were evaluated in the forced swimming test. The results revealed that only the highest dose of the ethereal fraction (50 mg/kg, i.p.) caused a significant decrease in total motility, locomotion and rearing. Sole dose injected (50 mg/kg) of ethanolic extract and ethereal fractions increased the exploration of the elevated plus-maze open arms in a similar way to that of diazepam (2 mg/kg, i.p.). In the forced swimming test, the ethanolic extract and their fractions (12.5, 25 or 50 mg/kg) was not as effective as paroxetine (10 or 20 mg/kg, i.p.) and imipramine (25 or 50 mg/kg, i.p.) in reducing immobility. These results suggest that some of the components of the ethanolic extract and of the ethereal fraction from B. platypetala, such as p-cymene, phytol, D-lactic acid, hexadecanoic acid, among others, may have anxiolytic-like properties, which deserve further investigation. Furthermore, the results obtained indicate that ethanolic extract from B. platypetala and their fractions do not present antidepressive properties. However, these properties cannot be related to the chemical constituents identified in this specie.

The objective of present study was to evaluate the antioxidant and anticonvulsant activities of dichloromethane fraction (DMF) from Platonia insignis Mart., Clusiaceae. The DMF from P. insignis (2 mg/kg) was tested by intraperitoneal (i.p.) to evaluate effects on lipid peroxidation level, nitrite formation, as well as on locomotor and anticonvulsant activities. Wistar rats were treated with, (saline/Tween 80 0.5%, i.p., control group), DMF (2 mg/kg, i.p., DMF group), pilocarpine (400 mg/kg, i.p., P400 group), or the combination of DMF (2 mg/kg, i.p.) and pilocarpine (400 mg/kg, i.p., DMF plus P400). After the treatments all groups were observed for 24 h. In P400 group rats there was a decrease in the motor activity when compared with control group. In DMF plus P400 co-administered rats was observed an increase in motor activity when compared with P400 group. In P400 group rats there was a significant increase in lipid peroxidation and nitrite levels. In DMF plus P400 co-administered rats, antioxidant treatment significantly reduced the lipid peroxidation level and nitrite content after seizures. Previous findings strongly support the hypothesis that oxidative stress occurs in rat striatum during pilocarpine-induced seizures, and our results imply that strong neuprotective effect on this brain region could be achieved using DMF from P. insignis.

A própolis é uma substância resinosa coletada pelas abelhas de diversas partes das plantas. Sua composição depende da época, vegetação e local de coleta. Apresenta diversas atividades biológicas como antimicrobiana, antioxidante, antitumoral, dentre outras. Foi realizado estudo da variabilidade sazonal, nos meses de fevereiro, junho e outubro de 2006, dos constituintes voláteis da própolis vermelha de Pernambuco através da extração por headspace dinâmico e identificação por cromatografia gasosa acoplada com espectrometria de massas (CG-EM). Foram identificados 34 constituintes voláteis, sendo monoterpenos e monoterpenóides, sesquiterpenos e sesquiterpenóides, fenilpropanóides, aldeídos, cetonas e η-alcanos. Os constituintes majoritários foram o trans-anetol, α-copaeno e o metil cis-isoeugenol. Também foi realizado o perfil fitoquímico por cromatografia em camada delgada (CCD), através da qual os constituintes fenólicos foram identificados como majoritários. Com o extrato bruto metanólico da própolis, realizou-se o ensaio de letalidade em Artemia salina, que demonstrou DL50 de 18,9 µg/mL, sugerindo uma possível atividade antitumoral.

Propolis is a resinous hive product collected by honeybees from plant sources. The composition of the propolis depends on the season, the vegetation, and the area of collection. It presents a diverse biological activities such as antimicrobial, antioxidant and antitumoral. The seasonal variability of the red propolis constituents from Pernambuco State were accomplished in the months of February, June and October of 2006. The volatile red propolis constituients were captured by the dynamic headspace technique and analyzed by GC-MS. In the analysis of the samples, 34 constituents were identified as the mono and sesquiterpens, phenylpropanoids, aldehydes, cetons and n-alcanes, presenting as majority constituents the trans-anethol, α-copaene and methyl cis-isoeugenol. The phytochemistry profile was performed by thin layer chromatography (TLC). Through this technique the majority constituents were identified as phenols. The Brine shrimp bioassay was used to evaluate of the red propolis methanolic extract, which demonstrated a DL50 of 18.9 µg/mL and an activity antitumoral was possibly suggested.

The synthesis of chiral acetylenic regioisomers was described by using an appropriate intermediate such as isopropylidene glycerol, a synthon widely used in the enantioselective syntheses. This intermediate was prepared from D-mannitol. The nine obtained compounds have been characterized by their respective spectral data. The mixture of chiral acetylenic alcohols showed activity against Escherichia coli when tested through the monitoring of CO2 released during microbial respiration by using a conductimetric system.

The essential oils of five samples obtained in different regions of the state of Piaui were analyzed by GC-MS. Ninety-one volatile constituents were tentatively identified and eight were positively identified. The principal components obtained from each sample were: 1,8-cineole, exo-fenchol, terpin-4-ol and fenchone (Teresina), a-pinene, caryophyllene oxide, b-pinene and a-copaene (Pio IX), (E)-caryophyllene, a-copaene, a-pinene, caryophyllene oxide and d-cadinene (Campo Maior), (E)-caryophyllene, a-gurjunene and b-selinene (Pedro II) and (E)-caryophyllene, a-gurjunene, d-cadinene and a-copaene (Lagoa de Sao Francisco). The five samples presented differences in the chemical composition of volatile fractions. The studies pointed out the need of characterizing propolis from Piaui by geographic regions and by seasons (drought and rainy periods).

The chemical composition of the ethanolic extract of the leaves and roots from Philodendron imbe Schott was investigated. The main constituents isolated the leaves were beta-sitosterol one polyprenoid hexaprenol, and 6beta-hydroxy-stigmast-4-en-3-one, a steroid, not yet reported in the Philodendron gender. A mixture of constituents, namely, ethyl myristoleate, alpha-bisabolol, ethyl isopalmitate, 3-octadecenyl-phenol and the major component ethyl palmitate, were isolated from the roots. Structure elucidation of these secondary metabolites was accomplished by spectrometric analysis, including 1D and 2D NMR experiments such as ¹H, ¹H and ¹H,13C-COSY.

Phytochemical investigation of the bark of Cenostigma macrophyllum (Leguminosae-Caesapinioideae) resulted in the isolation and identification of valoneic acid dilactone, ellagic acid, lupeol, alkyl ferulate, four free sterols (cholesterol, campesterol, stigmasterol and sitosterol), a mixture of sitosteryl ester derivatives of fatty acids, sitosterol-3-O-beta-D-glucopyranoside, stigmasterol-3-O-beta-D-glucopyranoside and saturated and unsaturated fatty acids. The structures of the isolated compounds were identified by ¹H and 13C NMR spectral analysis and comparison with literature data. The mixtures of 3-beta-hydroxysterols and fatty acids were analysed by GC/MS.

The chemical study of the propolis produced in Teresina city, state of Piaui, resulted in the identification of six cycloartane triterpenoids: isomangiferolic acid, 24-methylenecycloartane-3beta,26-diol, mangiferolic acid, mangiferonic acid, ambonic acid and ambolic acid. The substances were characterized by one and two-dimensional ¹H and 13C NMR analysis.