| |
Estrogen acts by binding to its receptors, termed as ERs.
The binding brings two ERs together (homo- or heterodimerization
with cognate ER proteins) along with
coregulatory proteins
which suppress or activate gene transcription by the complex,
eventually leading to a physiological or sometimes pathological
response. By acting on this system, enterolactone may offer
a natural selective estrogen-receptor modulator (SERM) type
effect. Thus by binding the estrogen receptor in different
target tissues, enterolactone may bring about agonist or
antagonist type response, depending on the availability and
recruitment of tissue specific co-regulatory proteins to
the estrogen receptor signalling complex. Therefore, and
depending on the concentration of endogenous estradiol and
the distribution of estrogen receptors, enterolactone may
act as either an estrogen receptor (ER) agonist or as an
estrogen antagonist. When estrogen levels fall enterolactone
may exert a weak estrogen-like effect (mimicking the presence
of estrogen), when estrogen levels are high enterolactone
occupies and block estrogen receptors thus acting to smooth
the peaks and troughs.
Importantly, the estrogenic activity of enterolactone is
relatively weak and therefore the risk of unwanted effects
due to adverse estrogenicity is minimal. |
