ABSTRACT
Benzodiazepines are the standard drugs for the treatment of anxiety, but their undesirable side effects make it necessary to develop new anxiolytic drugs. The objective of this study was to evaluate the possible anxiolytic-simile effect of synthetic chalcone N-{(4'-[(E)-3-(4-fluorophenyl)-1-(phenyl) prop-2-en-1-one]} acetamide (PAAPFBA) on adult zebrafish (Danio rerio). PAAPFBA was synthesized with an 88.21% yield and its chemical structure was determined by 1H and 13C NMR. Initially, animals (n = 6/group) were treated (4 or 12 or 40 mg/kg, intraperitoneal) with PAAPFBA and were submitted to acute toxicity and open field tests. Then, other groups (n = 6/each) received PAAPFBA for the analysis of its effect on the Light & Dark Test. The participation of the GABAergic system was also assessed using the GABAA antagonist flumazenil. Molecular docking was performed using the GABAA receptor. The effect of PAAPFBA on anxiety induced by alcohol withdrawal was analyzed. PAAPFBA was non-toxic, reduced the locomotor activity, and showed an anxiolytic-like effect in both models. This effect was reduced by pre-treatment with the flumazenil. In agreement with in vivo studies, molecular docking indicated an interaction between chalcone and the GABAA receptor. The results suggest that PAAPFBA is an anxiolytic agent mediated via the GABAergic system.
Subject(s)
Anxiety/drug therapy , Chalcones/pharmacology , Acetamides/pharmacology , Animals , Anti-Anxiety Agents/pharmacology , Anxiety/metabolism , Behavior, Animal/drug effects , Female , GABA Agents/pharmacology , GABA Antagonists/pharmacology , GABAergic Neurons/drug effects , Male , Molecular Docking Simulation , Motor Activity/drug effects , Receptors, GABA-A/drug effects , Receptors, GABA-A/metabolism , ZebrafishABSTRACT
Vitex gardneriana Schauer (Lamiaceae) popularly known as "jaramataia", is a shrub commonly found in caatinga biome located in Northeast Brazil. In folk medicine, its leaves have been used as analgesic and anti-inflammatory agents. The chemical composition of the essential oil from leaves obtained by hydrodistillation was analyzed and identified by GC-MS and GC-FID and showing a total of 26 constituents (95.9%) being 2 monoterpenes (0.4%) and 24 sesquiterpenes (95.4%). The main constituents identified were cis-calamenene (29.7%), 6,9-guaiadiene (14.5%) and caryophyllene oxide (14.0%). The essential oil has been demonstrated high larvicidal activity against Aedes aegypti (LC50 = 28.0 µg/mL). In the evaluation of the bioassay with Artemia salina the essential oil showed LC50 = 98.11 µg/mL. In addition, the essential oil did not show cytotoxicity (IC50 > 2.50 mg/mL) by the hemolysis assay.
Vitex gardneriana Schauer (Lamiaceae) popularmente conocido como "jaramataia", es un arbusto que se encuentra comuÌnmente en el bioma de caatinga ubicado en el noreste de Brasil. En medicina popular, sus hojas se han utilizado como analgeÌsicos y agentes antiinflamatorios. La composicioÌn quiÌmica de los aceites esenciales de las hojas obtenidas por hidrodestilacioÌn fue analizada e identificada por GC-MS y GC-FID y mostrando un total de 26 constituyentes (95.9%) siendo 2 monoterpenos (0.4%) y 24 sesquiterpenos (95.4%). Los componentes principales fueron cis-calamenene (29.7%), 6,9-guaiadiene (14.5%) y caryophyllene oxide (14.0%). El aceite esencial ha demostrado una alta actividad larvicida contra Aedes aegypti (CL50 = 28.0 µg/mL). En la evaluacioÌn del bioensayo con Artemia salina, el aceite esencial demostroÌ CL50 = 98.11 µg/mL. AdemaÌs, el aceite esencial no mostroÌ citotoxicidad (IC50 > 2.5 mg / mL) mediante el ensayo de hemoÌlisis.
Subject(s)
Oils, Volatile/pharmacology , Plant Extracts/pharmacology , Plant Leaves/chemistry , Aedes/drug effects , Vitex/chemistry , Terpenes/analysis , Oils, Volatile/chemistry , Plant Extracts/chemistry , Chromatography, Gas , Larvicides , LarvaABSTRACT
The chemical composition of essential oils from leaves, stalks and inflorescences of Croton jacobinensis obtained by hydrodistillation were analyzed by GC-MS. E-caryophyllene, 1,8-cineole, alpha-pinene, viridiflorene, 8-cadinene were the main components in essential oils from plant parts. Essential oils of leaves, stalks, and inflorescences were tested at different concentrations against instar III larvae of Aedes aegypti and showed LC50 of 79.3, 117.2, 65.8 ug/ml, respectively.
La composición química de los aceites esenciales de las hojas, los tallos y las inflorescencias de Croton jacobinensis obtenidos por hidrodestilación se analizaron mediante GC-MS. E-cariofileno, alfa-pineno, 1,8-cineol, viridifloreno, 8-cadineno fueron los principales componentes de los aceites esenciales de partes de la planta. Los aceites esenciales de las hojas, tallos e inflorescencias fueron probados en diferentes concentraciones en contra de instar III de las larvas de Aedes aegypti y mostraron LC50 de 79,3; 117,2; 65,8 ug/ml, respectively.
