Search

TheCopaifera oleoresins are widely used in folk medicine to treat various diseases. The goal of this study was to develop a validated reverse-phase high-performance liquid chromatography method with photodiode array detection (RP-HPLC-PDA) to quantify eight terpenes: ent-hardwickiic acid, ent-copalic acid, ent-7α-acetoxy hardwickiic acid, ent-16-hydroxy-3,13-clerodadiene-15,18-dioic acid, ent-5,13-labdadiene-15-oic acid, junenol, ent-kaurenoic acid, and 13E-ent-labda-7,13-dien-15-oic acid in the oleoresins of Copaifera pubiflora L. (OCP), Copaifera trapezifolia L. (OCT) and Copaifera langsdorffii L. (OCL). The linearity of the method was confirmed in the range of 20.00–500 µg.mL−1 (r2 > 0.999). The limit of quantification was between 1,05 and 16.89 µg.mL−1. Precision and accuracy ranges were found to be %RSD <0.2 and 96% to 110%, respectively. Based on the obtained results, the developed analytical method is rapid, precise, accurate, and sensitive for quantifying these terpenes in Copaifera's oleoresins. [ABSTRACT FROM AUTHOR]

Lignan dinitrohinokinin displays important biological activities, which led to the preparation of its poly-ε-caprolactone nanoparticles. Kinetics analysis revealed initially slow drug release followed by a prolonged, moderate release 6 h later due to DNHK diffusion through the polymeric matrix. Molecular dynamics simulations show that DNHK molecules that interact stronger with other DNHK molecules near the PCL/DNHK surface are more difficult to dissociate from the nanoparticle. The smaller diameter nanocapsules with negative surface charge conferred good colloidal stability. The formulations showed a size distribution with monodisperse systems formation. In vivo evaluation of schistosomicidal activity against Schistosoma mansoni showed that DNHK, when incorporated into nanoparticles, caused egg number reduction of 4.2% and 28.1% at 40 mg/kg and 94.2% and 84.4% at 400 mg/kg in the liver and the spleen, respectively. The PCL nanoparticles were stable in aqueous dispersion and could be optimized to be used as a promising lignan release agent. [ABSTRACT FROM AUTHOR]

Context:(−)-6,6′-Dinitrohinokinin (DNHK) display remarkable antiparasitic activity and was, therefore, incorporated into a nanoparticle formulation. Objective:Incorporation of DNHK in poly lactic-co-glycolic acid (PLGA) nanoparticles aiming to improve its biological activities. Materials and methods:Synthesis, characterization and incorporation of DNHK into glycolic acid (PLGA) nanoparticles by nanoprecipitation method. The nanoparticles were characterized by ultraviolet-visible spectroscopy, X-ray diffraction, field emission electron microscopic scanningmansoni(FESEM), and dynamic light scattering (DLS). For thein vitrotest withSchistosoma mansoni, the DNHK-loaded PLGA was diluted into the medium, and added at concentrations 10–200 µM to the culture medium containing one adult worm pair. The parasites were kept for 120 h and monitored every 24 h to evaluate their general condition, including: pairing, alterations in motor activity and mortality. Results:The loaded PLGA nanoparticles gave an encapsulation efficiency of 42.2% and showed spherical characteristics in monodisperse polymeric matrix. The adult worm pairs were separated after 120 h of incubation for concentrations higher than 50 µM of DNHK-loaded PLGA. The groups incubated with 150 and 200 µM of DNHK-loaded PLGA for 24 and 120 h killed 100% of adult worms, afforded LC50values of 137.0 ± 2.12 µM and 79.01 ± 1.90 µM, respectively, which was similar to the effect displayed by 10 µM of praziquantel. Discussion and conclusions:The incorporation of DNHK-loaded showed schistosomicidal activity and allowed its sustained release. The loaded PLGA system can be administered intravenously, as well as it may be internalized by endocytosis by the target organisms. [ABSTRACT FROM PUBLISHER]

Context: Despite several pharmacological applications of Rosmarinus officinalis L. (Lamiaceae), studies on its analgesic and anti-inflammatory properties have been scarce. Objective: The aim of this work was to use in vivo models to evaluate the analgesic and anti-inflammatory activities of the aqueous extracts obtained from leaves (AEL) and stems (AES) of Rosmarinus officinalis, as well as its isolated compound - rosmarinic acid (RA). We also prepared and assessed the acetyl ester derivative of RA. Materials and methods: The analgesic activity was evaluated using abdominal constriction and formalin tests. For the evaluation of the anti-inflammatory effects, carrageenin-induced paw edema in rats were used. The extracts were used at doses of 100, 200 and 400 mg kg−1 compounds were tested at 10, 20 and 40 mg kg−1. Results: Orally administered AEL, AES and RA were not significantly active at any of the doses tested during the abdominal constriction test; the acetyl ester derivative of RA displayed significant analgesic activity. In the carrageenin-induced paw edema assay, the acetyl derivative of RA at all the tested doses produced significant anti-inflammatory effects and reduced the number of paw licks in the second phase of the formalin test. Discussion and conclusion: The results suggest that the analgesic effects of the acetyl derivative of RA operate via a peripheral-mediated mechanism. The acetyl ester derivative of RA is potentially applicable as a new lead compound for the management of pain and inflammation. [ABSTRACT FROM AUTHOR]

In this study we report the screening of the in vitro trypanocidal activity of 20 extracts obtained from 10 different plant species growing in the Brazilian Cerrado: Aspidosperma macrocarpum Mart. (Apocynaceae), Aegiphila sellowiana Cham. (Verbenaceae), Byrsonima intermedia Juss. (Malpighiaceae), Cyperus rotundus L. (Cyperaceae), Leandra lacunosa Cogn. (Melastomataceae), Miconia ligustroides (DC.) Naudin. (Melastomataceae), Miconia sellowiana Naudin. (Melastomataceae), Myrcia variabilis Mart. ex DC. (Myrtaceae), Solanum lycocarpum St. Hil. (Solanaceae), and Tibouchina stenocarpa Cogn. (Melastomataceae). The most active extracts were submitted to phytochemical analyses. High-resolution gas chromatography analysis of the n-hexane extract of T. stenocarpa (IC50 = 23.6 μg/mL), the most active extract amongst all the tested samples, allowed the identification of β-amyrin, α-amyrin, lupeol, friedelin, β-friedelanol, campesterol, stigmasterol, and β-sitosterol. Oleanolic and ursolic acids were isolated from the methylene chloride extract of T. stenocarpa (IC50 = 51.5 μg/mL), while ursolic acid was isolated from the methylene chloride extract of M. variabilis (IC50 = 38.4 μg/mL). Solasonine and solamargine were identified as major compounds by mass spectrometry analysis in the hydroalcoholic extract of the fruits of S. lycocarpum (IC50 = 57.1 μg/mL). The results showed that the trypanocidal activity may be related to the major compounds identified in the crude active extracts. [ABSTRACT FROM AUTHOR]

Initially, the seeds of Baccharis dracunculifolia were collected from populations of 10 different regions, and the cultivation experiment was carried out in an experimental area of 1,800 m² by cultivating 100 individuals of each population. The essential oil analyses were performed on both GC-FID and GC/MS, which allowed the identification of 14 compounds. The oil yield varied from 0.31% to 0.70% among populations and season. The major oxygenated sesquiterpenes in the cultivated experiment were (E)-nerolidol (32%) and spathulenol (17%). The mean concentration in the plant of (E)-nerolidol was five times higher in March (136.53 mg/100 g of plant) than it was in July (25.03 mg/100 g of plant). The mean concentration of spathulenol increased about three fold from July (16.25 mg/100 g of plant) to April (47.50 mg/100 g of plant). [ABSTRACT FROM AUTHOR]

This study aimed to evaluate the chemical composition of Baccharis dracunculifolia essential oil and the water soluble oil obtained by steam distillation that were analyzed by GC and GC/MS. In the first hour of distillation, B. dracunculifolia aerial parts yielded 0.08% oil and in the second hour, 0.27%. The oil recovered from the distillate water yielded 0.18 g/L in the first hour and 0.44 g/L in the second hour of distillation. The main volatile compounds identified in the distillate water were aromatic compounds and sesquiterpene alcohols. [ABSTRACT FROM AUTHOR]