This document discusses mineralocorticoids, which are steroid hormones that regulate electrolyte and water balance. The key mineralocorticoid is aldosterone, which is synthesized in and secreted by the adrenal cortex. It acts in the kidneys to increase sodium reabsorption and potassium excretion, maintaining fluid volume and osmolarity. Aldosterone binds to mineralocorticoid receptors in the cytoplasm and nucleus of kidney cells, activating proteins like sodium-potassium ATPase that transport ions. Structural features that increase its mineralocorticoid effects include an 11β-OH group and 18-aldehyde. Marketed drugs for conditions like Addison's disease include fludrocortisone acetate and deoxy
3. Introduction
They are part of the Feedback mechanism in the immune system that
turns immune activity(inflammation) down. MCs cause their effect by
binding to the mineralocorticoid receptors (MRs) which almost exist in
all organisms tissues.
The most important and studying mineralocorticoid hormone is
ALDOSTERONE
Steroids hormone involve in Carbohydrate regulation and mineral
balance. Two classes of this hormone are synthesized in the cortex of
adrenal gland. One of them is the MINERALOCORTICOID, which
control the reabsorption of inorganic ions by the kidney.
4. Definition
Mineralocorticoid are the acute life-saving portion of the adrenocortical
hormone.
The main site of action is kidney. However ,it acts also on the salivary
glands, sweat glands & intestinal epithelial cells
Secreted by Zona glomerulosa of adrenal cortex.
ALDOSTERONE
The naturally occurring hormone that has an 11 beta OH and 18 CHO that naturally
bridge to form a hemiacetal, causes significant salt retention
7. It acts through the messenger RNA(mRNA)
mechanism.
Being lipid soluble , aldosterone it diffuses readily
into the cytoplasm of the tubular epithelial cells
through the lipid layer of the cell membrane.
In the cytoplasm, it binds with the specific receptor
protein.
Aldosterone –receptor complex diffuses into the
nucleus where it binds to deoxyribonucleic acid (DNA)
and causes formation of mRNA.
8. The mRNA diffuses back into the cytoplasm and causes protein
synthesis along with ribosomes.
Theses synthesized proteins are in the form of enzymes.
One of such enzymes is sodium potassium ATPase, which helps
in the transport of sodium and potassium.
9. Structural Activity Relationship(SAR)
Mineralocorticoids are adrenal cortex steroids and analogs with high
salt-retaining activity.They are used mainly for treatment of Addision
disease
The naturally occuring hormone aldosterone has an 11β-OH and an 18-
CHO.
10.
11. Double bonds at C1 increases anti-inflammatory
activity & decreases mineralocorticoid effect.
Hydroxyl group at C21 on ring increases
mineralocorticoid activity.
Introduction of 6-a-F and 9-a-F increases both
glucocorticoid and mineralocorticoid activity
12. corticosterone Aldosterone
Aldosterone is structurally same as cortisol, but it has an aldehyde at the 18- methyl
& don’t contain 17 alpha hydroxyl group, but aldosterone has 200 times higher
mineralocorticoid activity than corticosterone.
13. Funtion
On intestine: It increases sodium absorption from the intestine ,
especially from colon and prevents loss sodium through faces.
It also has a small effect on metabolism of fats, carbohydrate &
protein
It maintains the osmolarity and volume of ECF.
It increases sodium absorption from the intestine and prevents
loss of sodium through stool.
It is usually called life- saving hormone because , its absence
causes death within 3 days to 2 weeks.
14. Marketed Products
Fludrocorticosterone Acetate
Dose: Adult: oral: 0.2-2 mg per day
Biological half life: varies between 18 -36
hours
Brand Names: Fludrocortisone Acetate,
Florinef acetate , Alflorone, Cortineff,
Fluoricort
Uses:- For the treatment of Addison disease
and for inhibition of endogenous
adrenocortical secretions
15. Deoxycorticosterone
Dose: Adult: IM : 10 to 20 mg
(once/twice per week)
Chemical Names: Deoxycorticosterone
acetate ; Deoxycortone acetate;
Percorten; Dorcostrin; Syncotry;
Cortexone
Uses:-used via intramascular injections
in the replacement therapy of the
adrenocortical steroid
16. Reference
https://www.slideshare.net/mobile/taimooratif/mineralocorticoids-52963417
20th october 2019, 9:50 pm
Wilson and Gisvold's Textbook of “ORGANIC MEDICINALAND
PHARMACEUTICAL CHEMISTRY”John H. Block, Ph.D., R.Ph.,
11th edition, lipPINCOTT WILLIAMS & WILKINS page no 789-801
Foye’s principle of Medicinal Chemistry, by Thomas l. Lemke; david A.
Williams; Victoria f. Rachi; S. William Zito ; sixth edition;
page no.913-926