Menopause-associated degenerative diseases such as osteoporosis, remain an increasingly significant problem affecting women in particular. Nowadays, numerous traditional herbal medicines are used worldwide for the treatment of osteoporosis and plant derived supplements are increasingly considered as a “natural” alternative to drugs in preventing post-menopausal disorders [1]. In this study, we exploited traditional medicine knowledge of ancient Greek doctors (e.g. Dioscorides) and Greek flora’s diversity for the detection of novel plant-derived selective estrogen receptor modulators (SERMs). To achieve this goal, 36 plant species were selected, based on traditional medicine sources and current literature [2] and 74 extracts were prepared and screened using well-validated cellular models of menopause-related diseases. Preliminary evaluation revealed 9 extracts (mainly obtained from plant species belonging to Leguminosae family) between the most promising osteoprotective candidates and were selected for isolation of their major constituents using several chromatographic techniques. In total, 62 compounds (terpenes, isoflavones, phenolic acids, flavonols, flavones, coumestans, furanocoumarins, anthraquinones) were isolated and identified using NMR spectroscopy, whereas 5 of which were isolated for the first time. All these compounds were in vitro evaluated using a cell–based screening concerning: a) the differentiation of MC3T3-E1 cells to osteoblasts b) the inhibition of differentiation of RAW264.7 macrophages to osteoclasts c) their estrogenic properties using MCF-7 and Ishikawa cell lines. According to the combined results, phenolic acids (vanillic acid, gallic acid) terpenes (β-amyrin, lupeol, stigmastenone), coumestans (coumestrol, 2-α,α-dimethylallylcoumestrol, isotrifoliol), coumarin and isoflavone derrivatives exhibited potential osteoprotective properties.
References
[1] Wang ZQ, Li JL, Sun YL, Yao M, Gao J, Yang Z, Shi Q, Cui XJ, Wang YJ. Evid Based Complement Alternat Med 2013; 356260;
[2] Dontas I, Lelovas P, Kourkoulis S, Aligiannis N, Paliogianni A, Mitakou S, Galanos A, Lyritis G. Menopause 2011; 18(8): 915-922;