ABSTRACT
The physiological responses to estrogen hormones are mediated within specific tissues by at least two distinct receptors, ER and ER. Several natural and synthetic molecules show activity by interacting with these proteins. In particular, a number of vegetal compounds known as phytoestrogens shows estrogenic or anti-estrogenic activity. The majority of these compounds belongs to the isoflavones family and the most representative one, genistein, shows anti-proliferative effects on various hormone-sensitive cancer cells, including breast, ovarian and prostate cancer. In this work we describe the identification of structurally related homoisoflavones isolated from Leopoldia comosa (L.) Parl. (L. comosa), a perennial bulbous plant, potentially useful as hormonal substitutes or complements in cancer treatments. Two of these compounds have been selected as potential ligands of estrogen receptors (ERs) and the interaction with both isoforms of estrogen receptors have been investigated through molecular docking on their crystallographic structures. The results provide evidence of the binding of these compounds to the target receptors and their interactions with key residues of the active sites of the two proteins, and thus they could represent suitable leads for the development of novel tools for the dissection of ER signaling and the development of new pharmacological treatments in hormone-sensitive cancers.
Subject(s)
Hyacinthus/chemistry , Isoflavones/chemistry , Receptors, Estrogen/metabolism , Catalytic Domain/drug effects , Isoflavones/pharmacology , Models, Molecular , Molecular Docking Simulation , Molecular Structure , Plant Extracts/chemistry , Plant Extracts/pharmacology , Receptors, Estrogen/chemistryABSTRACT
The aims of this work are to assess the persistence of rotenone in oil and drupes of olive plants of cultivars Nocellara del Belice (NB) and Cassanese (CA), and to compare the quality of oils from rotenone-treated and untreated plants. Samples of drupes and oil were analyzed at 2, 12, 22 and 30 days after treatment. Rotenone levels in drupes of treated plants declined by about 50% after 22 days from treatment (0.037 mg kg(-1) in NB and 0.039 mg kg(-1) in CA), whereas the respective values in the oil were higher (0.209 mg kg(-1) in NB and 0.229 mg kg(-1) in CA) and had a lower decay half-life (4.02 days in NB and 4.71 days in CA). For both cultivars, no significant differences in oil physicochemical and nutritional parameters were found between the two treatments. The panel test of oils extracted after 22 days did not reveal significant differences in unpleasant aromatic notes nor defects between the two treatments. Our results confirm that serious doubts remain about the safety and healthiness of oils extracted from drupes treated with rotenone. This information could assess the real risk in the use of this product for plant protection in olive growing.
