Pharmaceutical development of tablets containing a spray-dried optimized extract from Lippia origanoides H. B. K.: influence of excipients and toxicological assessment

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.

Volatile compounds and palynological analysis from pollen pots of stingless bees from the mid-north region of Brazil

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.

Teor de fenóis e flavonoides, atividades antioxidante e citotóxica dasfolhas, frutos, cascas dos frutos e sementes de Piptadenia moniliformisBenth (Leguminosae – Mimosoideae) / Phenols, flavonoids and antioxidant and cytotoxic activity of leaves, fruits, peel of fruits and seeds of Piptadenia moniliformis Benth (Leguminosae - Mimosoideae)

The total phenol and flavonoid content, in addition to the antioxidant and cytotoxic activities, of extracts and fractions of Piptadenia moniliformis was determined. This honey plant species is commonly known as "catanduba" or "angico de bezerro". The aqueous fraction derived from the peels of the fruits exhibited the highest antioxidant activity, remaining comparable to the standard value, and there was a general correlation between this activity and the phenol and flavonoid content. The antioxidant potential of this species provides a basis for future developments in herbal medicines and cosmetics. Only the hydro alcoholic extract, the dichloromethane fractions and the ethyl acetate fractions showed moderate cytotoxicity.

Foram determinados o teor de fenóis e flavonoides, as atividades antioxidante e citotóxica dos extratos e frações de Piptadenia moniliformis. Essa é uma espécie melitófila comumente conhecida como "catanduba" ou "angico de bezerro". Das frações testadas, a fração aquosa das cascas dos frutos apresentou a maior atividade antioxidante, com valor comparável ao padrão, e no geral houve correlação do teor de fenóis e flavonoides com essa atividade. Os resultados do potencial antioxidante para essa espécie fornecem subsídios para futuros trabalhos que visem o desenvolvimento de fitoterápicos e cosméticos. Quanto à atividade citotóxica apenas o extrato hidroalcoólico e as frações diclorometano e acetato de etila demonstraram moderada citotoxicidade.

Chemical composition and anxiolytic-like effects of the Bauhinia platypetala

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.

Evaluation of effects of dichloromethane fraction from Platonia insignis on pilocarpine-induced seizures

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 percent, 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.

Variabilidade sazonal dos constituintes da própolis vermelha e bioatividade em Artermia salina / Seasonal variability of red propolis constituents and brine shrimp bioassay

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.