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Nimmy.A.Shibu
Group:4
• The prostaglandins (PG) are a group of physiologically
active lipid compounds having diverse hormone-like
effects in animals.
• They are derived enzymatically from fatty acids. Every
prostaglandin contains 20 carbon atoms, including a 5-
carbon ring.
• They are a subclass of eicosanoids and of the
prostanoid class of fatty acid derivatives.
• they are not secreted from a gland, but rather are created
at the time they are needed directly where the problem
exists.
• Structures of the more common prostaglandins
A, E, and F are structurally related to prosranoic
acid.
• Specific prostaglandins are named with a letter
(which indicates the type of ring structure)
followed by a number (which indicates the
number of double bonds in the hydrocarbon
structure). For example, prostaglandin E1 is
abbreviated PGE1 or PGE1, and prostaglandin
I2 is abbreviated PGI2 or PGI2.
• PGE2 contains a carboxyl group, a beta-hydroxy-ketone
ring, a secondary alkylic alcohol and two carbon-carbon
double bonds.
• A series are alpha and beta-unsarurated ketones.
• cause constriction or dilation in vascular smooth muscle
cells
• cause aggregation or disaggregation of platelets
• sensitize spinal neurons to pain
• induce labor
• decrease intraocular pressure
• regulate inflammation
• regulate calcium movement
• regulate hormones
• control cell growth
• acts on thermoregulatory center of hypothalamus to
produce fever
• Synthesized aerobically from polyunsaturated fatty acids.
• Multienzyme comples called Prostaglandin H Synthase
(PGHS).
• PGHS is present as two component– Cyclo-oxygenasesystem
and peroxidase system.
• PGHS is present as two isozymes PGHS1 & PGHS2.
• Phospholipase A2 released from cell membrane hydrolysis
phospholipids into lysophospholipids and arachidonic acid.
• Arachidonic acid converted to PG by oxidative cyclization with
cyclo-oxygenase of PGHS.
• This system forms the first unstable cyclic endoperoxide PG-
G2.
• PG-G2 is converted to PG-H2 by glutathionine dependent
peroxidase component of PGHS system.
• PG-H2 is the precursor of Prostanoids.
1. Inflammation:
-PGs are natural mediators of
inflammation.
-PGE2 & PGE1 induce signs of inflammation,
edness , heat, swelling, edema.
2. Pain & Fever:
-PGE2 can enhance the intensity & duration of
pain caused by bradykinin & histamin.
3.Reproduction:
-PGE2 & PGF2 have been used to induce
parturition as well as terminate pregnancy.
-PGE series of PG play role male infertility.
4. Peptic Ulcers:
- synthetic PGs have been useful in
inhibiting gastric secretions in patients with gastric
ulcers.
5. Regulation of Blood Pressure:
-PGE, PGA & PGI2 being vasodilators
lower the systemic arterial pressure , increase
local blood flow .
- help in treating hypertension.
6.PGI2 inhibit platelet aggregation.
7. PGE2 & TXA2 promote clotting process.
• NSAIDs--inhibit cyclooxygenase:
Eg: aspirin, indomethacin, phenylbutazone.
• Corticosteroids--inhibit phospholipase A2 production:
Eg: hydrocortisone, prednisone, beta-
mathasone.
• COX-2 selective inhibitors or coxibs:
Eg: anexins.
• Cyclopentenone prostaglandins may play a role in
inhibiting inflammation.
• The most important dietary precursor of prostaglandins is
linoleic acid, an essential fatty acid. About I0g of linoleic
acid is ingested daily in adults. A small part of this intake
is converted by elongation and desaturation in liver to
arachidonic acid (eicosatetraenoicacid) and to some
extent to dihomo-y-linoleic acid. Since the total daily
excretion of prostaglandins and their metabolites is only
about I mg.
• Rapidly removed from circulation.
• Upto 90% of PGs are destroyed in liver.
Prostaglandin

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Prostaglandin

  • 2. • The prostaglandins (PG) are a group of physiologically active lipid compounds having diverse hormone-like effects in animals. • They are derived enzymatically from fatty acids. Every prostaglandin contains 20 carbon atoms, including a 5- carbon ring. • They are a subclass of eicosanoids and of the prostanoid class of fatty acid derivatives. • they are not secreted from a gland, but rather are created at the time they are needed directly where the problem exists.
  • 3. • Structures of the more common prostaglandins A, E, and F are structurally related to prosranoic acid. • Specific prostaglandins are named with a letter (which indicates the type of ring structure) followed by a number (which indicates the number of double bonds in the hydrocarbon structure). For example, prostaglandin E1 is abbreviated PGE1 or PGE1, and prostaglandin I2 is abbreviated PGI2 or PGI2.
  • 4.
  • 5. • PGE2 contains a carboxyl group, a beta-hydroxy-ketone ring, a secondary alkylic alcohol and two carbon-carbon double bonds.
  • 6. • A series are alpha and beta-unsarurated ketones.
  • 7.
  • 8.
  • 9. • cause constriction or dilation in vascular smooth muscle cells • cause aggregation or disaggregation of platelets • sensitize spinal neurons to pain • induce labor • decrease intraocular pressure • regulate inflammation • regulate calcium movement • regulate hormones • control cell growth • acts on thermoregulatory center of hypothalamus to produce fever
  • 10.
  • 11. • Synthesized aerobically from polyunsaturated fatty acids. • Multienzyme comples called Prostaglandin H Synthase (PGHS). • PGHS is present as two component– Cyclo-oxygenasesystem and peroxidase system. • PGHS is present as two isozymes PGHS1 & PGHS2. • Phospholipase A2 released from cell membrane hydrolysis phospholipids into lysophospholipids and arachidonic acid. • Arachidonic acid converted to PG by oxidative cyclization with cyclo-oxygenase of PGHS. • This system forms the first unstable cyclic endoperoxide PG- G2. • PG-G2 is converted to PG-H2 by glutathionine dependent peroxidase component of PGHS system. • PG-H2 is the precursor of Prostanoids.
  • 12.
  • 13. 1. Inflammation: -PGs are natural mediators of inflammation. -PGE2 & PGE1 induce signs of inflammation, edness , heat, swelling, edema. 2. Pain & Fever: -PGE2 can enhance the intensity & duration of pain caused by bradykinin & histamin. 3.Reproduction: -PGE2 & PGF2 have been used to induce parturition as well as terminate pregnancy. -PGE series of PG play role male infertility.
  • 14. 4. Peptic Ulcers: - synthetic PGs have been useful in inhibiting gastric secretions in patients with gastric ulcers. 5. Regulation of Blood Pressure: -PGE, PGA & PGI2 being vasodilators lower the systemic arterial pressure , increase local blood flow . - help in treating hypertension. 6.PGI2 inhibit platelet aggregation. 7. PGE2 & TXA2 promote clotting process.
  • 15.
  • 16. • NSAIDs--inhibit cyclooxygenase: Eg: aspirin, indomethacin, phenylbutazone. • Corticosteroids--inhibit phospholipase A2 production: Eg: hydrocortisone, prednisone, beta- mathasone. • COX-2 selective inhibitors or coxibs: Eg: anexins. • Cyclopentenone prostaglandins may play a role in inhibiting inflammation.
  • 17. • The most important dietary precursor of prostaglandins is linoleic acid, an essential fatty acid. About I0g of linoleic acid is ingested daily in adults. A small part of this intake is converted by elongation and desaturation in liver to arachidonic acid (eicosatetraenoicacid) and to some extent to dihomo-y-linoleic acid. Since the total daily excretion of prostaglandins and their metabolites is only about I mg. • Rapidly removed from circulation. • Upto 90% of PGs are destroyed in liver.