Hormone menubar
Estrogens - The Female Hormones
Estrogens - Activity / Concentration in Tissues
Estrogen
concentration/activity in tissues Many factors
determine
estrogen
concentration/activity in a particular tissue
Estrogen's
affinity
(binding strength)
for components of
that tissue, relative to its affinity for the blood
Sex hormone-binding carriers
Potency of
different
estrogenic
compounds
Comparative strengths of ESTRADIOL
/ESTRONE/ESTRIOL
Activation/inactivation of
estrogen
receptors. Estrogens
(like all steroid hormones) readily diffuse across cell membranes, where they
bind with
estrogens receptors. This leads to the production of specific
proteins that express the effect of estrogen
upon the target cell.
Estrogen Receptors
(1)
Inactivated
by
PROGESTERONE
(2)
Activated
by many physical and chemical conditions
xenoestrogens -"Endocrine Disruptors"
Plasma, total, or free
Estrogen
concentrations .
Circulating Levels of estrogen
External
estrogen
dose
Estrogen HRT is NOT necessary
Tissue activity of
enzymes which convert
androgens
to
estrogens ;
- Aromatase,
the main enzyme that
converts
androgens
to estrogens
can be found in all parts of
the body:
• Fat
and skin. Major sources of
estrogen , especially in older people, since
aromatase
activity increases with aging;
•
Also fibroblasts, smooth muscle cells,
breast and endometrium (uterine lining),
pancreas, liver, brain, bone, more.
- Aromatase
activity
(and
therefore
estrogen
production)
is
affected by many factors:
• Aromatase
activity is increased ▲
by aging, and under the influence of
PROLACTIN,
CORTISOL,
prostaglandin, and the pituitary hormones FOLLICLE STIMULATING HORMONE and
GROWTH HORMONE.
• Aromatase activity is
inhibited
▼
by:
PROGESTERONE ,
thyroid hormones, aspirin, and high altitude.
- Aromatase
activity is
involved in breast cancer, endometriosis, uterine cancer, lupus, gynecomastia.
Also many
other diseases
• Aromatase in
mammary tissue appears to increase
estrogen
receptors and cause breast neoplasia. Independently of ovarian
estrogen
Tekmal, et al., 1999
Enzymes affecting
Steroid Production /Activity
Metabolic clearance of
estrogen. A healthy liver combines
estrogen
with glucuronic acid ("sugar
acid") to make it water-soluble for elimination. In the 1940's, the Biskindsdemonstrated some causes of liver impairment that decrease its ability to
excrete estrogen, including:
-
A dietary protein deficiency
-
Hypothyroidism.
Prevents the liver
from attaching glucuronic acid to estrogen ,
and so increases the body's retention of estrogen ,
which in turn impairs the thyroid gland's ability to secrete thyroid hormone.
Hypothyroidism often results from nutritional protein deficiency.
Estrogen Elimination
Activity of beta-glucuronidase, sulfatase
and other enzymes determine whether
estrogen
is in water-soluble
(inactive)
or oil-soluble (active)
form.
Water- soluble
estrogen
must be made oil-soluble to be able to enter cells and exert its effects
through their lipid membranes.
-
Sulfatase
•
Sulfatase. Attaches sulfuric acid, and also several other enzymes modify the activity
/solubility of
estrogens .
•
Sulfatase activity is inhibited ▼
by: antiestrogenic hormones. (E.g.
PROGESTERONE )
•
Sulfatase also releases estrogen
in tissues
-
Beta-glucuronidase
( found in inflamed tissue). Normally, the healthy liver combines
estrogen with glucuronic acid to make it
water-soluble for elimination. However, if it passes through inflamed tissue,
the large amounts of beta-glucuronidase there remove glucuronic acid, converting
inactive estrogen -glucuronides into active
estrogen ,
which accumulates in tissue
•
Beta-glucuronidase activity is increased
▲
by:
Inflammation.
•
Beta-glucuronidase activity is inhibited
▼
by PROGESTERONE (in some
tissues), and maybe more so with aging
Cristofalo VJ &
Kabakjian J
(1975) Mech.
Ageing Dev. 4, 19-28.
•
Breast cancer treatment uses glucaric acid - which
inhibits
estrogen
by beta-glucuronidase.
•
Glucuronidase -
converts
water-soluble
estrogen glucuronides into oil-soluble forms by attaching
glucuronic acid.
Estrogen
Transport and Availability
PROGESTERONE prevents tissue
from concentrating
estrogen
- PROGESTERONE antagonizes
the effect of
estrogen . By
reducing
estrogen receptor levels.
PROGESTERONE also acts indirectly, by its
antagonizing action against PROLACTIN, it
prevents PROLACTIN
from stimulating the formation of estrogen
receptors
-
Tissue/plasma
ESTRADIOL
( E2 )
ratio
varies with
PROGESTERONE presence -ranging from 20.36 in early follicular phase to 1.45
in mid-luteal phase when PROGESTERONE level is high.
-
During pregnancy, tissue
estrogen
decreases as blood
PROGESTERONE increases;
-
PROGESTERONE production sharply decreases in
aging allowing tissues to concentrate
estrogen
even with low serum
estrogen - similar to follicular phase of menstrual cycle.
-
In
postmenopausal women ,
the tissue E2
concentration is not significantly
lower than in menstruating women
in
follicular phase
Akerlund, et
al., 1981
-
An excessive
estrogen
presence is
causing an hormonal imbalance
(referred to as
Estrogen
Dominance ),
especially with
PROGESTERONE. One must consider not
only the absolute level of a hormone but also its relative ratios with other
hormones, including
ESTRADIOL ,
PROGESTERONE ,
TESTOSTERONE ,
CORTISOL and thyroid hormones. A "sea"of
estrogen "look-alikes"have infiltrated our lives today, having an
estrogen ic effect that is manifesting as a
wide range of health problems by causing hormonal imbalance, especially with
PROGESTERONE . E.g.
infertility/miscarriage, menopausal symptoms, PMS, fibrocystic breasts , ovarian cysts,
hirsutism, uterine fibroids, reproductive organ cancers in men and women , enlarged prostate, osteoporosis,
depression/anxiety, water retention, inflammation, and much more
Healthy women
without breast cancer have saliva-tested
PROGESTERONE levels routinely 200-300 times greater than saliva
ESTRADIOL level. Compare this to
women with breast cancer, who have a saliva
PROGESTERONE /
ESTRADIOL
ratio considerably less than 200 to 1.
When you consider the
many functions of
PROGESTERONE .
which are being suppressed by excess
estrogen ,
you can understand why just about every aspect of health is affected. A so-called
estrogen
dominance problem is addressed by first reducing
estrogen
exposure, attending to other important factors involved with hormone
imbalance* and then possibly, by supplementing
PROGESTERONE .
xenoestrogens -"Endocrine Disruptors"
ESTROGEN DOMINANCE
Reduce Body's
Estrogen levels
Estrogen dominance treatment 1-2-3
PROGESTERONE Functions
