Is coumestrol a natural beneficial compound or a hazardous agent?
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1
Aristotle University of Thessaloniki, Department of Pharmacology, Greece
Background: Coumestrol is a non-steroidal estrogen-like compound which belongs in the class of coumestan phytoestrogens. It is found in clover and alfalfa sprouts, sunflower seeds, lima and pinto been seeds and round split peas. As it is one of the constituents of soy products which are widely consumed by Western population, the investigation of its neuroendocrine effects as a weak estrogen agonist/antagonist is a compelling need.
Genotoxicity: Coumestrol induces DNA strand breaks, micronuclei and mutations in the Hypoxanthine phorsporibosyl transferase (HPRT) gene of Chinese hamster overy cells. In human lymphoblastoid cells, coumestrol has been found to induce micronuclei on day two after exposure, followed by an increase in apoptotic activity. These findings may be explained by mutations caused in the Thymidine Kinase (TK) gene, inhibition of topoisomerase-II (topo-II) function or modulation of the p53 signaling pathways.
Estrogen agonism/antagonism: Dietary exposure to coumestrol has been found to increase ER-β mRNA expression in the paraventricular nucleus of hypothalamus in Sprague–Dawley rats. In fact, coumestrol has the opposite action to estradiol and therefore disrupts the ER-β dependent processes, acting as an anti-estrogen. This antiestrogenic effect may be tissue specific.Competitive binding assays have exhibited that coumestrol binds to ER-β with a higher affinity than does estradiol. The Coumestrol Relative Binding Affinity (%RBA) for ER-α is 94, while for ER-β is 185, compared to 17-beta-estradiol. Other studies have demonstrated that coumestrol has anti-estrogenic effects on sexual differentiation when administered to neonatal rats through lactation. Coumestrol has been found to decrease ovarian weight and increase apoptotic cell death in ovaries of adult rats exposed during lactation. In addition, another study has shown that oral administration of coumestrol induces testis alterations on dogs.
Conclusion: Despite the beneficial actions of phytoestrogens, including a reduction in the risk of breast and prostate cancer, soothing of the menopausal symptoms and reduced cardiovascular disease risk, more studies are necessary to investigate their potential anti-estrogenic and genotoxic effects which may prove to be to detrimental to human neuroendocrine function.
Keywords:
Coumestrol,
Phytoestrogens,
herbal medicines
Conference:
8th Southeast European Congress on Xenobiotic Metabolism and Toxicity - XEMET 2010, Thessaloniki, Greece, 1 Oct - 5 Oct, 2010.
Presentation Type:
Poster
Topic:
Xenobiotic toxicity
Citation:
Kara
E,
Tsanakalis
F and
Papaioannidou
P
(2010). Is coumestrol a natural beneficial compound or a hazardous agent?.
Front. Pharmacol.
Conference Abstract:
8th Southeast European Congress on Xenobiotic Metabolism and Toxicity - XEMET 2010.
doi: 10.3389/conf.fphar.2010.60.00136
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Received:
28 Oct 2010;
Published Online:
04 Nov 2010.
*
Correspondence:
Dr. Paraskevi Papaioannidou, Aristotle University of Thessaloniki, Department of Pharmacology, Thessaloniki, Greece, ppap@auth.gr