RESUMEN
Vaccinium uliginosum L. (commonly known as bog bilberry) and Vaccinium myrtillus L. (commonly known as bilberry) are species of the genus Vaccinium (family Ericaceae). The red-purple-blue coloration of blueberries is attributed largely to the anthocyanins found in bilberries. Anthocyanins, known for their potent biological activity as antioxidants, have a significant involvement in the prophylaxis of cancer or other diseases, including those of metabolic origin. Bilberry is the most important economically wild berry in Northern Europe, and it is also extensively used in juice and food production. A review of the latest literature was performed to assess the composition and biological activity of V. uliginosum and V. myrtillus. Clinical studies confirm the benefits of V. uliginosum and V. myrtillus supplementation as part of a healthy diet. Because of their antioxidant, anti-inflammatory, anti-cancer, and apoptosis-reducing activity, both bog bilberries and bilberries can be used interchangeably as a dietary supplement with anti-free radical actions in the prevention of cancer diseases and cataracts, or as a component of sunscreen preparations.
Asunto(s)
Arándanos Azules (Planta) , Vaccinium myrtillus , Antocianinas/farmacología , Alimentos Funcionales , Frutas , Antioxidantes/farmacología , Extractos Vegetales/farmacologíaRESUMEN
One of the key stages in the development of new therapies in the treatment of toxoplasmosis is the identification of new non-toxic small molecules with high specificity to Toxoplasma gondii. In the search for such structures, thiosemicarbazide-based compounds have emerged as a novel and promising leads. Here, a series of imidazole-thiosemicarbazides with suitable properties for CNS penetration was evaluated to determine the structural requirements needed for potent anti-Toxoplasma gondii activity. The best 4-arylthiosemicarbazides 3 and 4 showed much higher potency when compared to sulfadiazine at concentrations that are non-toxic to the host cells, indicating a high selectivity of their anti-toxoplasma activity.
Asunto(s)
Antiparasitarios/farmacología , Evaluación Preclínica de Medicamentos , Semicarbacidas/farmacología , Toxoplasma/efectos de los fármacos , Animales , Antiparasitarios/química , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos/métodos , Humanos , Concentración 50 Inhibidora , Modelos Moleculares , Conformación Molecular , Estructura Molecular , Pruebas de Sensibilidad Parasitaria , Semicarbacidas/química , Relación Estructura-Actividad , Toxoplasmosis/tratamiento farmacológico , Toxoplasmosis/parasitologíaRESUMEN
Two thiosemicarbazide derivatives 1 and 2, three 2-amino-1,3,4-thiadiazole derivatives 3-5, and three N1- substituted-4-methyl-1,2,4-triazole-5-thione derivatives 6-8 were synthesized and evaluated for their central nervous system effects using rodent behavioral models. With the exception of 6, all compounds were devoid of neurotoxicity and they did not affect the body temperature of mice. New lead structures 1-4 with potential analgesic activity were identified.