RESUMO
Phytoestrogens, a class of plant-derived compounds that are structural mimics of estrogen, can bind to estrogen receptors, acting as either agonists or antagonists. They have been implicated in estrogen-mediated physiology, which makes them interesting targets of study, especially for biomedical applications in woman's health. The 1998 Women's Health Initiative sparked considerable interest in natural alternatives to hormone replacement therapy, thereby triggering many additional studies on phytoestrogens. In this review, key advancements in dietary phytoestrogens are addressed, emphasizing their relation to breast pathophysiology. Recent developments such as clinical trials, precise bioassays for screening and selection of potential phytoestrogens, drug delivery systems to enhance bioavailability of therapeutically favorable phytoestrogens, regulatory guidelines on phytoestrogen-based supplements, and avenues that need further improvement are also discussed.
Assuntos
Mama/fisiopatologia , Fitoestrógenos/farmacologia , Receptores de Estrogênio , Animais , Neoplasias da Mama , Dieta , Suplementos Nutricionais , Sistemas de Liberação de Medicamentos , Feminino , Humanos , Preparações de Plantas , Ensaios Clínicos Controlados Aleatórios como AssuntoRESUMO
A number of Garcinia species accumulate benzophenone derivatives that may be useful for the treatment of breast cancer. The dereplication of new benzophenone derivatives from Garcinia species is challenging due to the occurrence of multiple isomers and the known compounds found in their extracts. In the current study, a strategy is described using the UPLC-QTOFMS(E) technique to identify tentatively the known and uncharacterized benzophenones of interest based upon the characteristic fragmentation ions. Several UPLC-QTOFMS peaks (a-ee) appeared to contain benzophenone derivatives, and 12 of these peaks contained compounds with MS ionization profiles not consistent with previously identified compounds from the seeds of Garcinia paucinervis, an endangered Chinese species. The targeted isolation of unidentified compounds of interest afforded five new benzophenones, paucinones E-I (1-5), which were determined by MS and NMR analysis and ECD spectroscopy. These compounds were evaluated for cytotoxicity against three breast cancer cell lines inclusive of MDA-MB-231, SKBR3, and MCF-7. These results indicate that the UPLC-QTOFMS(E)-guided isolation procedure is an efficient strategy for isolating new benzophenones from Garcinia species.