Hormones are chemical messengers that are secreted into the blood by endocrine glands and have profound effects on metabolic processes and cellular communication. They can be classified based on their chemical composition, location of receptors, or solubility. The major classes of hormones include steroids such as sex and adrenal hormones, peptides/proteins such as insulin and growth hormone, and amines such as epinephrine. Steroid hormones are derived from cholesterol and include estrogens, androgens, progesterone, corticosteroids, and aldosterone. Peptide hormones include insulin, glucagon, and somatostatin which are secreted by the pancreas, as well as hormones from the pituitary, parathyroid,
2. INTRODUCTION
Hormones are chemical messengers secreted into blood by
endocrine or ductless glands.
The term hormone was introduced by Satrling in 1905 and
comes from the Greek word “Hormacin” meaning “excite” or
“arouse”.
Hormones are substances synthesized in the body in small
quantities but have a profound biochemical effect in the control
and regulation of metabolic events and contribute in some
cases to intercellular and intracellular communication.
3. INTRODUCTION
A characteristic of hormones is that they are released, usually
by specialized secretory cells in endocrine glands, and are
carried by the circulation, to target cells where they have an
effect.
5. INTRODUCTION
Functions of hormones cover four major areas namely:
a. Reproduction,
b. Growth and development,
c. Maintenance of internal environment, and
d. Energy production, utilization and storage.
7. CLASSIFICATION OF
HORMONES
1. Classification on the Basis of their Chemical
Composition
Hormones can be classified chemically into three major groups.
i. Steroids Hormones: These hormones are fat soluble
compounds like adrenal cortical hormone and sex hormones
(androgens and estrogens).
ii. Amines: these hormones are small, water-soluble
compounds containing amino groups like epinephrine,
thyroxine and several derivatives of tyrosine.
iii. Peptides/Protein Hormones: these are either large protein
or small or medium size peptides e.g., insulin, glucagon and
pituitary hormones.
8. CLASSIFICATION OF
HORMONES
2. Classification on the Basis of their Mechanism
On this basis, hormones can be classified into two categories.
i. Hormones that bind to Intracellular Receptors: These
include androgens, calcitrol, estrogens, glucocorticoids,
mineralocorticoids, progestins, reticnoic acid, and thyroid
hormones (T3 and T4).
ii. Hormones that bind to Cell Surface Receptors: These
can be further classified on the basis of secondary
messengers. It can be cAMP, cGMP, DAG, InsP3 and
9. CLASSIFICATION OF
HORMONES
3. Classification on the Basis of Solubility
On the basis of solubility, hormones can be classified as:
i. Lipid-Soluble Hormones: The lipid soluble hormones
include steroid and thyroid hormones.
ii. Water-Soluble Hormones: The water soluble hormones
include amines, peptide hormones, and the eicosanoid
hormones.
11. STEROID HORMONES
These include the sex hormones and the hormones from adrenal
cortex.
These are synthesized in mammals by the ovary (or testis), adrenal
cortex, corpus luteum and the placenta.
Sex Hormones
Three types of sex hormones are recognized :
a. Estrogens (female or ovarian or follicular hormones)
b. Androgens (male or testicular hormones)
c. Progestins (corpus luteal hormones).
12. STEROID HORMONES
1. Ovarian Hormones
Mammalian ovary contains
ovarian follicles and corpus
lutea.
Hormones produced mainly
the follicles are known as
estrogens.
Chemically, the estrogens
derivatives of a C18
hydrocarbon, estrane.
13. STEROID HORMONES
The three compounds of this
group with hormonal activity are :
1. β-estradiol
2. Estriol
3. Estrone
15. STEROID HORMONES
All these are characterized by the absence of a CH3 group at carbon
10 and by the aromatic nature of ring A, making the OH group
phenolic in character.
Of all these, b-estradiol is most potent physiologically, estrone less
potent and estriol is least active.
Their relative potencies are 50 : 5 : 1 respectively.
Although ovary is the chief source of estrogens, they are in smaller
amounts also produced by the testis and the adrenal cortex.
16. STEROID HORMONES
2. Testicular
Hormones
These hormones are secreted
mainly by the testes, the male
reproductive organs and are
called as androgens.
Chemically, these are
of a C19 hydrocarbon,
androstane.
They have no side chain on
17-carbon of steroid skeleton.
17. STEROID HORMONES
There are many hormones
secreted from testes with
androgenic activity.
The three important ones are :
1. Testosterone
2. Androsterone
3. Dehydroepiandrosterone
18. STEROID HORMONES
Testosterone is most potent of all
these and
dehydroepiandrosterone is least
active.
The relative potency ratio of
these three forms is 20 : 7 : 1.
A few testicular hormones are
also produced by the adrenal
gland.
19. STEROID HORMONES
3. Corpus Luteal
Hormones
The hormones secreted by the
ovarian bed, corpus luteum are
collectively called as gestagens
progestins.
The principal gestogen is
progesterone.
Progesterone is a C21 steroid
secreted by the corpus luteum
during the second half of the
menstrual cycle.
20. STEROID HORMONES
4. Adrenal Cortical Hormones
Adrenal cortex secretes some 40-50 closely related C21
collectively called as corticosteroids.
The corticosteroids may be grouped under two categories :
A. Mineralocorticoids. — concerned primarily with the
electrolytes and the distribution of water in tissues, e.g.,
aldosterone and deoxycorticosterone.
B. Glucocorticoids. — concerned primarily with the
carbohydrates, proteins and fats, e.g., cortisone, cortisol
corticosterone.
23. STEROID HORMONES
The estimated 24-hour production of major compounds of human
adrenal gland is :
Corticosteroids
Cortisol 8-24 mg
Corticosterone 1.5−4 mg
Aldosterone 0.04−0.2 mg
24. STEROID HORMONES
Aldosterone is 30 times more active than deoxycorticosterone.
Deoxycorticosterone, in its turn, is 4 times more potent than cortisone
and cortisol in maintenance of life.
Corticosterone is least active in this regard.
25. STEROID HORMONES
Classes of Steroid Hormones
Steroid Class Principal Active
Steroid in Humans
No. of Carbon
Atoms
Parent Ring
Structure
Estrogens Estradiol 18 Estrane
Androgens Testosterone 19 Androstane
Progestins Progesterone 21 Pregnane
Glucocorticoids Cortisol 21 Pregnane
Mineralocorticoi
ds
Aldosterone 21 Pregnane
27. Biosynthesis of Androgens and Estrogens
The androgens are synthesized from cholesterol by the
tissues, chiefly from testes.
In the testes, cholesterol is converted to pregnenolone,
and 17a-hydroxyprogesterone.
17a-hydroxyprogesterone is then converted to
which is then converted to testosterone and androsterone.
Testosterone can be converted to estradiol by the action of
aromatase.
Testosterone can also be converted to dihydrotestosterone by
reductase.
28. Biosynthesis of Progesterone
In the corpus luteum, placenta and adrenal cortex,
synthesized from pregnenolone by 3b-hydroxysteroid
Progesterone is an intermediate common to the biosynthesis
steroid hormone from cholesterol.
29. STEROID HORMONES
Biosynthesis of Glucocorticoids
Progesterone is converted to either 17a-hydroxyprogesterone
17a-hydroxylase or to 11-deoxycorticosterone by 21a-
17a-Hydroxyprogesterone is then converted to 11-
21a-hydroxylase.
11-deoxycortisol is then converted by 11b-hydroxylase to
11-deoxycorticosterone is converted to corticosterone by 11b-
hydroxylase.
30. STEROID HORMONES
Synthesis of Mineralocorticoids
Corticosterone is converted to aldosterone by 18-hydroxylase.
This reaction is stimulated by angiotensin II, a hormone
angiotensin by angiotensin-converting enzyme.
31. PEPTIDE HORMONES
Peptide hormones are most prevalent and consist of chains of amino
acids.
Larger peptides are usually referred to as proteins, while complex
protein hormones with carbohydrate side chains are called
glycoprotein hormones.
Peptide Hormones are classified as:
1. Hormones of the pancreas
2. Hormones of the Hypophysis
3. Hormones of the Parathyroid
4. Hormones of the Gastrointestinal Tract
5. Hormones of the Corpus Luteum
32. PEPTIDE HORMONES
1. Hormones of the Pancreas
Each pancreas has about 1,00,000 islets of Langerhans, which
clusters of various types of cells.
These islets in mammals contain at least 4 major types of cells:
a. α cells
b. β cells
c. δ cells
d. F cells
33. PEPTIDE HORMONES
The β cells contain granules which manufacture a hormone insulin,
store it and eventually release it directly into the bloodstream at the
appropriate times.
The α cells contain granules which produce another hormone,
glucagon.
The δ cells secrete a hormone, somatostatin.
The F cells secrete pancreatic polypeptide.
The α and β cells make up 20% and 75% of the total, respectively.
34. PEPTIDE HORMONES
Insulin
Human insulin is a molecule of 5,734 Da which falls on the
between a large polypeptide and a small protein.
It is composed of two separate peptide chains, designated the
and the B chain.
These two chains are joined together by two disulfide bridges.
The human insulin A chain consists of 21 amino acid residues
B chain of 30 amino acid residues.
A third disulfide exists in the A-chain between the cysteine 6
36. Biosynthesis of Insulin
Insulin is synthesized as a pre-prohormone, that is a pre-
proinsulin.
The initial portion of 23 amino acids is called the leader
sequence and directs the synthesis of pro-insulin. The leader
sequence is cleaved off.
The pro-insulin which is synthesized has the conformation
necessary for forming the proper disulphide bridges between
A- and B-chains.
It undergoes a series of site-specific cleavages forming the
mature insulin and an equimolecular amount of connecting
37. PEPTIDE HORMONES
Glucagon
Glucagon has a molecular weight of 3,485 Da and is comprised
of a single amino acid chain of 29 amino acids that is devoid of
disulfide linkages.
Histidine is the N-terminal amino acid and threonine, the C-
terminal amino acid.
38. PEPTIDE HORMONES
Glucagon’s N-terminal histidine at position #1 is essential for its
biological activity.
The adjacent residues, #2 (serine) and #5 (threonine), are involved in
implementing the adenylyl cyclase activity which is key to the
initiation of glucagon-mediated biological responses.
Residues #19–#26 (blue color) have an equal potential to stabilize the
structure either as β sheets, or as α-helices.
The C-terminal two residues, asparagine (#28) and threonine (#29),
increase glucagon’s tight binding to its receptor.
Unlike insulin, it contains no cystine, proline or isoleucine, but
possesses methionine and tryptophan in appreciable amounts.
40. PEPTIDE HORMONES
Somatostatin
Two forms of somatostatin exists; S14 and S28, which are
single chain polypeptides of 14 and 28 amino acids,
respectively.
Somatostatin-14 has one disulfide bond.
It is produced by the δ-cells of the endocrine pancreas and
dispersed cells in the gastrointestinal tract.
41. PEPTIDE HORMONES
Other Pancreatic Hormones
A. Pancreatic Polypeptide (PP)
Pancreatic polypeptide (PP) is a 36-amino-acid peptide that is
known to stimulate the gastric secretion of HCl and pepsin.
Most of the PP is expressed and then secreted by the F cells of
the pancreas.
PP circulates in the plasma as a dimer with a half-life of 6–7
minutes.
42. PEPTIDE HORMONES
B. Amylin
The pancreatic β-cell islets produce the peptide hormone
amylin.
It has also been formerly known as islet amyloid polypeptide
(IAPP).
Amylin is a 37-amino-acid peptide.
Amylin and insulin are co-secreted from the pancreatic beta
cells at the time of food intake.
43. PEPTIDE HORMONES
Constituent Hormones of Endocrine Pancreas
Cell Type Hormone Structure
a Glucagon 29 amino acids
b
Insulin
Amylin
Two chains:
a= 21 amino acids
b = 30 amino acids
37 amino acids
d
Somatostatin Two forms:
S-14 = 14 amino
acids
S-28 = 28 amino
acids
F Pancreatic Polypeptide 36 amino acids
44. PEPTIDE HORMONES
2. Hormones of the Hypophysis or Pituitary
Gland
Hypophysis or pituitary gland consists of 3 lobes:
a) An anterior lobe or adenohypophysis
b) An intermediate lobe
c) A posterior lobe or neurohypophysis
All the three lobes secrete substances having hormonal activity.
45. PEPTIDE HORMONES
The secretion of pituitary hormones is controlled by the hormones (or factors)
released from hypothalamus, a region of the brain immediately proximal to the
pituitary.
These hormones are called as hypothalamo-releasing hormones or
hypothalamic factors.
Sr. no. Pituitary Hormones Hypothalmic Releasing Hormone
1 Thyroid Stimulating Hormone, TSH Thyrotrophin Releasing Hormone, TRH
2 Adrenocorticotrophic Hormone,
ACTH
Corticotrophin releasing Hormone, CRH
3 Follicle Stimulating Hormone, FSH
Luteinizing Hormone, LH
Gonadotrophin releasing Hormone, GnRH
4 Growth Hormone, GH Growth Hormone Releasing Hormone,
GHRH
5 Prolactin, PL Prolactin releasing Hormone, PLRH
46. PEPTIDE HORMONES
a) Hormones of Anterior Pituitary (Adenohypophysis)
Anterior pituitary gland (Adenohypophysis) secrete a number of
hormones of vital importance and all of them are protein in nature, and
these nourish the secretory activities of other glands.
These hormones are called as tropins or trophic hormones.
47. PEPTIDE HORMONES
A. Thyrotropin or Thyroid-Stimulating Hormone, TSH.
The molecule of TSH is a dimer made up of a and b subunits.
It is a glycoprotein with molecular weight about 30,000.
Each molecule has 8-9 cystine residues and the disulfide
present as intrachain linkages rather than interchain linkages.
48. PEPTIDE HORMONES
B. Corticotropin or Adrenocorticotrophic Hormone, ACTH.
Corticotropin is a straight chain polypeptide with a molecular
about 4,500 and consists of 39 amino acid residues.
The most potent segment of activity is from residue 15 to 18
(Lys.Lys.Arg. Arg).
The release of ACTH is controlled by CRH.
49. PEPTIDE HORMONES
C. Gonadotropins or Gonadotrophic Hormones, GTH.
Gonadotropins include:
i. Follicle Stimulating Hormone, FSH
ii. Luteinizing hormone, LH
iii. Prolactin, PRL
The gonadotropins, FSH and LH, are both regulated by the
hypothalamic gonadotrophin releasing hormone, GnRH.
50. PEPTIDE HORMONES
i. Follicle-stimulating hormone, FSH
It is a glycoprotein that contains galactose, mannose,
galactosamine, glucosamine, sialic acid, fucose and uronic acid.
It has a molecular weight of about 30,000 in man.
ii. Luteinizing hormone, LH
It is a peptide hormone with molecular weight of about 26,000 (in
man).
It lacks tryptophan but has a high content of cystine and proline.
Each molecule contains 10 glucosamine and 3 galactosamine
residues.
51. PEPTIDE HORMONES
iii. Prolactin PRL, Luteotrophic Hormone, LTH
This is also a peptide hormone with 198 amino acid residues and a
molecular weight of about 23,500.
It has 3 disulfide bonds between cysteine residues at 4-11, 58-173
and 190-198.
It differs from FSH and LH in that it contains no carbohydrate.
53. PEPTIDE HORMONES
D. Somatotropin or Somatotrophic hormone, STH or Growth
Hormone, GH.
Somatotropin obtained from human hypophysis is a protein
with molecular weight 27,000.
It has 191 amino acids and consists of 2 disulfide bridges
between adjacent cysteine residues.
The N-terminal and C-terminal residues are both
phenylalanine.
54. PEPTIDE HORMONES
Constituent Hormones of Anterior Pituitary (Adenohypophysis)
Cell Type Hormone Structure
Basophils or β cells
Thyrotropin, TSH Two Protein Subunits:
a = 96 amino acids
b = 112 amino acids
Neutrophils or
chromophobe cells
Corticotropin,
ACTH
Polypeptide = 39 amino
acids
Basophils or β cells
FSH Two Protein Subunits:
a = 96 amino acids
b = 111 amino acids
Basophils or β cells
LH Two Protein Subunits:
a = 96 amino acids
b = 121 amino acids
55. PEPTIDE HORMONES
Constituent Hormones of Anterior Pituitary (Adenohypophysis)
Cell Type Hormone Structure
Acidophils or α cells
Prolactin, PRL Protein of 198 amino
acids
Acidophils or α cells
Growth Hormone, GH
or Somatotropin, STH
Protein of 191amino
acids
56. PEPTIDE HORMONES
b) Hormones of Posterior Pituitary or Neurohypophysis
Two important hormones are secreted from the posterior
pituitary in both males and females.
These are:
a. Oxytocin (OT)
b. Vasopressin (VP), the antidiuretic hormone,
The two hormones are structurally closely related nonapeptides
that are derived from a common ancestral gene.
57. PEPTIDE HORMONES
a. Oxytocin
It is a nonapeptide amide.
A disulfide bond is present to link the two cysteine residues present in
the molecule.
b. Vasopressin
It is also a cyclic nonapeptide amide and resembles oxytocin except
that isoleucine is replaced by phenylalanine and leucine by arginine.
59. PEPTIDE HORMONES
Constituent Hormones of Posterior Pituitary (Neurohypophysis)
Hormone Structure
Oxytocin Polypeptide of 9 amino acids
(CYIQNCPLG)
C’s are disulfide bonded
Vasopressin or Antidiuretic Hormone Polypeptide of 9 amino acids
(CYFQNCPRG)
C’s are disulfide bonded
60. PEPTIDE HORMONES
3. Hormones of the Parathyroid
Parathyroids secrete a hormone called parathyroid hormone
(parathormone, PTH) or Collip’s hormone.
It is a linear polypeptide consisting of 84 amino acids
weight=9300) with no cysteine residues and hence no disulfide
bridges.
A fragment of the intact hormone consisting of the first 34
at the N-terminal region of the molecule is sufficient for the
exert its entire spectrum of characteristic biological effects.
61. PEPTIDE HORMONES
4. Hormones of the Gastrointestinal Tract
The gastrointestinal hormones are a family of polypeptides
by specialized endocrine cells present in the stomach, intestine,
colon which function both as traditional hormonal messengers
neurotransmitters.
Of the many regulatory gastrointestinal peptides, following are
understood are considered to be the authentic hormones:
A.Gastrin
B. Secretin
C.Cholecystokinin (CCK)
62. PEPTIDE HORMONES
A. Gastrin
It is produced G cells in the pyloric mucosa, which is apparently
stimulated by the proteins present in food or possibly by HCl.
The main form of gastrin obtained from G cells is a heptadecapeptide.
At the N-terminal end of the heptadecapeptide, there is a pyroglutamyl
residue, and at the c-terminal end, there is a phenylalaninamide
residue.
63. PEPTIDE HORMONES
Two forms of heptadecapeptide exist:
I. One in which the tyrosyl residue at postion 12 is free (Gastrin 1)
II. The other in which it is sulphated.
64. PEPTIDE HORMONES
B. Secretin
Secretin has only 27 amino acids with molecular weight of 3,056.
The entire molecule of 27 amino acids is required for full biological
activity.
Secretin is localized to the upper duodenal and jejunal S cells.
65. PEPTIDE HORMONES
C. Cholycystokinin, CCK
It is also secreted by the upper part of the small intestine.
Cholecystokinin is a polypeptide with 33 amino acid residues and a
molecular weight of 3,883.
It is, however, noteworthy that the last 5 amino acids towards the C-
terminal in the gastrin and cholecystokinin are exactly the same.
It is in this terminal portion of these hormones that the principal
activity resides.
67. AMINO ACID DERIVATIVES
1. Thyroidal Hormones
The mammalian thyroid gland biosynthesizes, stores, and
secretes two molecular species of thyroid hormone:
I. Thyroxine (T4; 3,5,3′,5′-tetraiodothyronine)
II. Triiodothyronine (T3; 3,5,3′-triiodothyronine)
69. AMINO ACID DERIVATIVES
Thyroid hormones are poorly soluble in water, and more than 99% of
the T3 and T4 circulating in the blood is bound to a carrier proteins.
The principle carrier of thyroid hormones is thyroxin-binding globulin.
70. AMINO ACID DERIVATIVES
[Calcitonin (CT) is a small polypeptide hormone secreted by the
specialized C cells that are found primarily in the thyroid gland.
It consisting of a straight chain peptide of 32 amino acids, with
a seven-membered disulfide ring at the N-terminus and a
prolinamide residue at the C-terminus. ]
71. AMINO ACID DERIVATIVES
2. Hormones of Adrenal Medulla
The adrenal medulla produces two hormones:
a. Epinephrine or Adrenaline
b. Norepinephrine or Noradrenaline
Chemically, these two hormones are catecholamines
(dihydroxyphenylamines) and are closely related to tyrosine and
phenylalanine.
Norepinephrine, however, differs from epinephrine structurally
in having a hydrogen atom in place of the methyl group.