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Abstract
Selective estrogen receptor modulators (SERMs) have been used in hormone related disorders, and their role in clinical medicine is evolving. Tamoxifen and raloxifen are the most commonly used synthetic SERMs, and their long-term use are known to create side effects. Hence, efforts have been directed to identify molecules which could retain the beneficial effects of estrogen, at the same time produce minimal side effects. Urolithins, the products of colon microbiota from ellagitannin rich foodstuff, have immense health benefits and have been demonstrated to bind to estrogen receptors. This class of compounds holds promise as therapeutic and nutritional supplement in cardiovascular disorders, osteoporosis, muscle health, neurological disorders, and cancers of breast, endometrium, and prostate, or, in essence, most of the hormone/endocrine-dependent diseases. One of our findings from the past decade of research on SERMs and estrogen modulators, showed that pomegranate, one of the indirect but major sources of urolithins, can act as SERM. The prospect of urolithins to act as agonist, antagonist, or SERM will depend on its structure; the estrogen receptor conformational change, availability and abundance of co-activators/co-repressors in the target tissues, and also the presence of other estrogen receptor ligands. Given that, urolithins need to be carefully studied for its SERM activity considering the pleotropic action of estrogen receptors and its numerous roles in physiological systems. In this review, we unveil the possibility of urolithins as a potent SERM, which we are currently investigating, in the hormone dependent tissues.
Highlights
Selective estrogen receptor modulators (SERMs) are non-steroidal compounds that bind to estrogen receptors and can act like estrogen or be a partial agonist or antagonist with mixed activity depending on the tissue it acts
Its relevance seems more pronounced in the hormonedependent tissues, which connote its potential in hormone or endocrine-related pathogenesis
It is known that estrogen receptors exhibit a complex and dynamic activity depending on the different conformation it attains according to the ligand structure and binding
Summary
Selective estrogen receptor modulators (SERMs) are non-steroidal compounds that bind to estrogen receptors and can act like estrogen or be a partial agonist or antagonist with mixed activity depending on the tissue it acts. The following sections unfold the benefits of urolithins in tissues where estrogen has a remarkable role This includes its anti-inflammatory potential, cardiovascular benefits, breast, endometrial and prostate cancer protection, bone, muscle, and cognitive health where estrogen receptors are abundant and play a pivotal role. Urolithins are found to inhibit human endometrial cancer cells in an in vitro study [20] It modulated the expression of ERα-dependent genes like ERβ, PGR, pS2, and GREB1. It is interesting to note that urolithin metabolites can exert a mild anti-SARS-CoV-2 Mpro inhibition [113] at physiological relevant concentrations (2–50 μM), detectable in human colon tissues after consumption of hydrolyzable tannin-rich foods, as per clinical studies [114]. It has been understood that SARS-Cov-2 can activate pro-inflammatory chemokines in the early stage, and this can lead to the development of either a protective immune response or an exacerbated inflammatory response
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