| The onset of menopause is associated with symptoms such as insomnia, loss of libido, vaginal atrophy, depression, and hot flashes. Menopause can also increase the risk of certain health problems such as heart disease, osteoporosis, and Alzheimer's disease. The lack of ideal therapies to treat menopausal symptoms necessitates investigations into alternatives. In this study, eight botanicals were studied for their estrogenic activity. Angelica sinensis (Oliv.) Diels (dong quai), Cimicifuga racemosa L. Nutt. (black cohosh), Glycyrrhiza glabra L. (licorice), Humulus lupulus L. var Nugget (hops), Panax ginseng C. A. Mey. (ginseng), Panax quinquefolium L. (American ginseng), Trifolium pratense L. (red clover), and Vitex agnus-castus L. (chaste berry) were all selected for evaluation based on literature, popular use, and traditional knowledge.; In order to investigate their potential usefulness in treating menopausal symptoms, each plant was evaluated for its ability to bind to purified estrogen receptors (ER) alpha and beta. Competitive binding experiments indicated that hops, red clover, and chaste berry all contained estrogen receptor ligands. Red clover contained four isoflavones, genistein, daidzein, biochanin A, and formononetin, that all bound to the ER, upregulated alkaline phosphatase (AP), and stimulated PR (progesterone receptor), and trefoil factor 1 protein (pS2). Hops was fractionated and four compounds were identified that bound to the estrogen receptor. 8-Prenylnaringenin, isoxanthohumol, and 6-prenylnaringenin all acted as estrogen receptor agonists, while xanthohumol bound to the ER but was also toxic in cells. Linoleic acid was identified as an estrogen receptor ligand in chaste berry.; Serotonin receptors were investigated as a potential alternative biological target for black cohosh. The extract contained a compound that acted as a mixed competitive ligand and agonist of the 5-HT7 receptor. Finally, all of the botanicals were studied for free radical scavenging properties. Bioassay guided fractionation of black cohosh resulted in the discovery of 10 compounds with antioxidant behavior. Those compounds were then studied for the ability to protect cellular DNA from oxidative damage induced by menadione. The crude extract and three compounds significantly reduced menadione-induced DNA damage. |
