Asunto(s)
Cordia/química , Naftoquinonas/química , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Brasil , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Espectroscopía de Resonancia Magnética , Estructura Molecular , Extractos Vegetales/química , Raíces de Plantas/química , Espectroscopía Infrarroja por Transformada de FourierRESUMEN
The new glucosyl sarpagan alkaloid designated as 21(R*)-(O-ß-glucosyl)-hydroxy-sarpagan-17-oic acid, along with eleven known alkaloids were isolated from a soluble alkaloidal fraction from the ethanol extract of Rauvolfia ligustrina. Their structures were elucidated by interpretation of spectroscopic data (1D and 2D NMR), HRESIMS experiment, GIAO 13C NMR calculations, and comparison with literature data. All the isolated alkaloids were screened by their neuroinhibitory effects using the electrically stimulated mice vas deferens bioassay. Compounds 1, 2 and 9 presented a potent inhibitory effect in the neurotransmission while 3 and 11 showed an acute neuroexcitatory effect. Compound 10 exhibited a very effective post-synaptic inhibitory activity.
Asunto(s)
Alcaloides Indólicos/farmacología , Raíces de Plantas/química , Rauwolfia/química , Transmisión Sináptica/efectos de los fármacos , Animales , Brasil , Estimulación Eléctrica , Técnicas In Vitro , Alcaloides Indólicos/química , Espectroscopía de Resonancia Magnética , Masculino , Ratones , Estructura Molecular , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Extractos Vegetales/química , Conducto Deferente/efectos de los fármacosRESUMEN
Six previously undescribed tropane alkaloids, designated as erythrobezerrines A-F, were isolated from the EtOH extract from the stem bark of Erythroxylum bezerrae Plowman. Their structures were elucidated based on the interpretation of the NMR and MS data and in some instances, confirmed by X-ray diffraction analysis. The cytotoxicity of the isolated compounds was evaluated against the cancer cell lines L929, PC-3, HCT-116, SNB-19 and NCI-H460, but only erythrobezerrine C showed moderate activity with IC50 values of 3.38 and 5.43⯵M for HCT-116 and NCI-H460, respectively.