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MALE SEX

HORMONES

Dihydrotestosterone

Active form of testosterone


Prostate gland, genitalia and some parts of

the skin

Plasma content ~1/10 that of


testosterone (400 g)
50 g are produced by testes; the rest are

produced peripherally

Other metabolites of
testosterone

Testosterone can undergo aromatization


producing the Estrogens
Accounts for presence of estrogen in males

Sex-Hormone binding
globulin

-globulins plasma proteins that


bind to testosterone and other sex
hormones
Highly specific, high affinity and limited

capacity for testosterone

Produced in the liver


Increased by estrogens, liver diseases,

hyperthyroidism
Decreased by androgens, advancing age,
hypothy

Function:

Regulation of androgen secretion

ACTH regulates androgen secretion in the


adrenals
Luteinizing hormone regulates androgen
secretion in the testes
Further regulated by the gonadotropin releasing

hormone (GRH)

Testosterone are inactivated by:


Glucuronide conjugation - major
Sulfate conjugation

Testosterone Metabolism

2 pathways:
Oxidation at C-17 position less active

compound
Reduction at C-5 position produces DHT

Functions of
testosterone

Accounts for masculinization male


primary and secondary sexual
characteristics
Increased protein formation and muscle
development
Increased bone matrix and Ca+2 deposition
Increased basal metabolic rate
Together with FSH, promotes
spermatogenesis

FEMALE SEX
HORMONES

SYNTHESIS OF
PROGESTERONE

Secreted by the corpus luteum


Major hormone of the luteal phase of the
menstrual cycle

SYNTHESIS OF
ESTROGEN

Estrone is the 1st known member of the sex


hormones.
Isolated from the urine of pregnants.
All these are characterized by the absence of a
CH3 group at C10 and by the aromatic ring A,
making the OH group phenolic in character.
-estradiol is the most potent estrogens.
Estrone is less potent and estriol is least active.
Their relative potencies are 50:5:1.
Although ovary is the chief source of estrogens,
they are in smaller amts also produced by the
testis& A.cortex.

BIOSYNTHESIS OF
ESTROGEN

Estrogen production is highest when a woman is


young & slows down with age.
Biosynthesis:In non-pregnant females, estrogen is mainly
synthesized in the ovary.
The estrogen(as well as androgen) transported by
binding to a specific plasma protein called sex
steroid binding protein.
The amt of SBT increases in pregnancy or estrogen
therapy which results in reduced androgenic action.
Testosterone, an androgen is the precursor of
estrogens.

SYNTHESIS OF
ESTROGEN

Acetate cholesterol pregnenolon


progesteron testosterone estrogen
Regulation of Secretion of Estrogen:The secretion of estrogen is regulated by
FSH released from anterior pituitary.
The release of FSH is caused by the
gonadotropic releasing hormone secreted
from hypothalamus.

Biosynthesis of Estrogens
Cholesterol

Pregnenolone

Progesterone
aromatase

Estrone (E1)
16-hydroxylase

Estriol

DHEA

Androstenedione
Testosterone
aromatase

17-Estradiol
(E2)

Aromatase
A mixed-function oxidase
Requires O2 and NADPH

Theca cells (ovary) source of testosterone and


androstenedione

Granulosa cells site of conversion to estradiol and


estrone by aromatase respectively

Peripheral aromatization

Aromatase activity is present in adipose tissue, liver,


skin and other tissues.

Reason for estrogenization that characterizes such


diseases as cirrhosis of the liver, hyperthyroidism,
aging and obesity.

Peripheral aromatization accounts for 80% of formation


estradiol from testosterone in males.

50% of the E2 produced during pregnancy comes from


aromatization of adrenal androgens

Transport in the blood


Transport proteins:
1. Sex hormone binding globulin (SHBG) - binds
estrogens.
2. Corticosteroid binding globulin (CBG)
progesterone

binds

Note: Binding proteins provide a circulating reservoir


of hormone & buffer against sudden changes in
the plasma level.

Metabolism in the liver


A. Estrogens
- conjugated with glucuronic acid or sulfated
- less active in primates compared to rodents;
- oral estrogens are more effective in humans
- conjugated derivatives are water-soluble
- excreted in bile, feces and urine

B. Progesterone
- sodium pregnanediol-2-glucuronide is the
progestin found in urine
- synthetic steroids, e.g. derivatives of 17hydroxyprogesterone avoid hepatic
widely used as contraceptives

major

metabolism;

General functions
Hormones prepare female reproductive system for
reproduction by:
1. Maturing the primordial germ cells
2. Developing the tissues that will allow for implantation of
the blastocyst
3. Providing the hormonal timing for ovulation
4. Establishing the environment required for maintenance of
pregnancy
5. Providing the hormonal influences for parturition and
lactation