| Until 2002, hormone replacement therapy (HRT) was the gold standard for treatment of menopausal symptoms; however, HRT is an unacceptable treatment for many women due to significant concerns about its safety. As a consequence, many women are actively seeking alternative treatments for menopausal symptoms, particularly botanical dietary supplements. However, convincing evidence of the safety and efficacy of the currently available botanicals for the treatment of menopausal symptoms is lacking, thus investigation of new botanical alternatives to HRT is necessary. This study focuses on herbs used traditionally in Costa Rica for the treatment of menopausal symptoms in order to identify herbs that may be developed into such alternative therapies. Through literature searches and visiting herb markets in Costa Rica seventeen plant species were identified as having traditional use for the treatment of menopausal symptoms in Costa Rica. These plants were collected in Costa Rica, and extracts were prepared and tested for activity in the estrogen receptor competitive binding assay, the ERbeta-CALUX reporter gene assay, and gene expression assays measuring the effect on expression of endogenous estrogen responsive genes in MCF-7 cells. Of the seventeen extracts, 6 extracts demonstrated estrogenic activity in these in vitro bioassays. One of these plants, Pimenta dioica (L.) Merr. (Myrtaceae), was selected for follow up study in order to isolate and identify active constituents through bioassay guided fractionation. This resulted in the isolation of quercitrin as well as 2-(p-hydroxyphenoxy)-6,8-dimethyl-5,7-dihydroxychromone, a new 2-phenoxychromone. The results of this study demonstrate that plants with traditional use in the treatment of menopausal symptoms have estrogenic activity, and that the compounds isolated in this study may be used in the development of standardized extracts of P. dioica for future studies in animal models and eventually in humans. |
