RESUMEN
Cancer has become the leading cause of death in developing countries due to increased life expectancy of the population and changes in lifestyle. Studies on active principles of plant have motivated researchers to develop new antitumor agents that are specific and effective for treatment of neoplasms. Kaurane diterpenes are considered important compounds in the development of new and highly effective anticancer chemotherapeutic agents due to their cytotoxic properties in the induction of apoptosis. We evaluated the cytotoxic and apoptotic activity of the epimer of kaurenoic acid (EKA) isolated from the medicinal plant Croton antisyphiliticus (Euphorbiaceae) toward tumor cell lines HeLa and B-16 and normal fibroblasts 3T3. Based on analyses with the MTT test, EKA showed cytotoxic activity, with half maximal inhibitory concentration values of 59.41, 68.18 and 60.30 µg/mL for the B-16, HeLa and 3T3 cell lines, respectively. The assay for necrotic or apoptotic cells by differential staining showed induction of apoptosis in all three cell lines. We conclude that EKA is not selective between tumor and normal cell lines; the mechanism of action of EKA is induction of apoptosis, which is part of the innate mechanism of cell defense against neoplasia.
Asunto(s)
Antineoplásicos/toxicidad , Apoptosis/efectos de los fármacos , Croton/química , Diterpenos/toxicidad , Extractos Vegetales/toxicidad , Animales , Antineoplásicos/química , Línea Celular Tumoral , Diterpenos/química , Células HeLa , Humanos , Concentración 50 Inhibidora , Melanoma Experimental , Ratones , Células 3T3 NIH , Extractos Vegetales/químicaRESUMEN
Despite the overall progress of sheep farming in Brazil, infections with the gastrointestinal parasite Haemonchus contortus represent one the most important problems in sheep production, aggravated by the increasing resistance of nematodes to traditional anthelmintic drugs caused by inadequate sheep flock management by breeders. Ethnopharmacological data indicate Annona muricata as a promising alternative for the control of gastrointestinal nematodes because of its general anthelmintic properties. The aim of this work was to evaluate the in vitro anthelmintic effects of A. muricata aqueous leaf extract against eggs, infective larvae and adult forms of parasitic nematode H. contortus. At higher doses, A. muricata extract showed 84.91% and 89.08% of efficacy in egg hatch test (EHT) and larval motility test (LMT), respectively. In the adult worm motility test, worms were completely immobilized within the first 6-8h of nematode exposition to different dilutions of extract. Phytochemical analysis indicated the presence of phenolic compounds in A. muricata aqueous leaf extract that may be responsible for the anthelmintic effects observed. Moreover those results validate the traditional use of A. muricata as a natural anthelmintic and then the pharmacological potential of its compounds for future in vivo investigations.
Asunto(s)
Annona/química , Antihelmínticos/farmacología , Hemoncosis/veterinaria , Haemonchus/efectos de los fármacos , Extractos Vegetales/farmacología , Enfermedades de las Ovejas/parasitología , Animales , Antihelmínticos/uso terapéutico , Heces/parasitología , Hemoncosis/tratamiento farmacológico , Hemoncosis/parasitología , Haemonchus/crecimiento & desarrollo , Haemonchus/fisiología , Larva/efectos de los fármacos , Larva/fisiología , Levamisol/farmacología , Masculino , Movimiento/efectos de los fármacos , Óvulo/efectos de los fármacos , Óvulo/fisiología , Fenoles/química , Fenoles/farmacología , Fenoles/uso terapéutico , Extractos Vegetales/uso terapéutico , Hojas de la Planta/química , Ovinos , Enfermedades de las Ovejas/tratamiento farmacológicoRESUMEN
Random amplified polymorphic DNA (RAPD) was used to detect polymorphisms among Zaprionus indianus fly populations collected from six municipalities in the States of São Paulo and Minas Gerais, Brazil. This species is an important, recently introduced fruit fly pest of figs and other fruit. Among 21 primers, 16 produced 73 reproducible polymorphic fragments; primer AM-9 produced the greatest number of polymorphic bands (nine), with 52% genetic variability among populations. Genetic divergence analysis of the Z. indianus populations demonstrated two major groups, named Western and Eastern groups. There was greater gene flow within than between groups. The correlation coefficient for genetic and geographic distances (Mantel test) was significant, demonstrating isolation by distance.
Asunto(s)
Drosophilidae/genética , Variación Genética/genética , Polimorfismo Genético/genética , Animales , Brasil , Drosophilidae/clasificación , Técnica del ADN Polimorfo Amplificado AleatorioRESUMEN
In this work, the analgesic and anti-inflammatory activities of Zeyheria montana Mart. ethanol leaf extract were investigated at doses of 75, 150 and 300 mg/kg body weight. In the analgesic assay, against a chemical stimulus in mice, acetic acid-induced writhes were significantly inhibited by the extract at doses of 75 mg/kg (67.27 percent), 150 mg/kg (49.38 percent) and 300 mg/kg (82.87 percent). Also, a vigorous decrease in hyperalgesia was observed when measured after 2 h and 6 h of lipopolysaccharide stimulation of rats for all doses of extract tested. Z. montana extract, at doses of 75 and 300 mg/kg, caused very slight central analgesia in rats submitted to thermal stimulus, particularly noticeable at 30 min following treatment. The anti-inflammatory activity of Z. montana extract on carrageenan-induced oedema in rats was evaluated. The oedema development, measured at 180 min following carrageenan intraplantar injection, was significantly reduced by all tested doses: 75 mg/kg (33.30 percent), 150 mg/kg (45.80 percent) and 300 mg/kg (75.00 percent). The LD50 value was greater than 2000 mg/kg. These results demonstrated that the ethanol extract from Z. montana leaf possesses anti-nociceptive and anti-inflammatory activities, which could be of relevance for the pharmacological control of pain and inflammatory processes.
Asunto(s)
Animales , Masculino , Ratones , Ratas , Analgésicos/uso terapéutico , Antiinflamatorios/uso terapéutico , Bignoniaceae/química , Hiperalgesia/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Analgésicos/aislamiento & purificación , Antiinflamatorios/aislamiento & purificación , Cromatografía Líquida de Alta Presión , Evaluación Preclínica de Medicamentos , Etanol/aislamiento & purificación , Etanol/farmacología , Fitoterapia , Dimensión del Dolor/efectos de los fármacos , Hojas de la Planta/química , Ratas WistarRESUMEN
In this work, the analgesic and anti-inflammatory activities of Zeyheria montana Mart. ethanol leaf extract were investigated at doses of 75, 150 and 300 mg/kg body weight. In the analgesic assay, against a chemical stimulus in mice, acetic acid-induced writhes were significantly inhibited by the extract at doses of 75 mg/kg (67.27%), 150 mg/kg (49.38%) and 300 mg/kg (82.87%). Also, a vigorous decrease in hyperalgesia was observed when measured after 2 h and 6 h of lipopolysaccharide stimulation of rats for all doses of extract tested. Z. montana extract, at doses of 75 and 300 mg/kg, caused very slight central analgesia in rats submitted to thermal stimulus, particularly noticeable at 30 min following treatment. The anti-inflammatory activity of Z. montana extract on carrageenan-induced oedema in rats was evaluated. The oedema development, measured at 180 min following carrageenan intraplantar injection, was significantly reduced by all tested doses: 75 mg/kg (33.30%), 150 mg/kg (45.80%) and 300 mg/kg (75.00%). The LD50 value was greater than 2000 mg/kg. These results demonstrated that the ethanol extract from Z. montana leaf possesses anti-nociceptive and anti-inflammatory activities, which could be of relevance for the pharmacological control of pain and inflammatory processes.