This document provides an overview of prostaglandins, leukotrienes, and thromboxanes. It discusses their introduction, classification, chemical structures, biosynthesis, regulation, mechanisms of action, functions, and applications. Specifically, it notes that prostaglandins are derived from arachidonic acid and have diverse hormone-like effects. Leukotrienes are inflammatory mediators produced from arachidonic acid oxidation. They are involved in inflammation and hypersensitivity reactions. Thromboxanes are involved in blood clotting and are derived from arachidonic acid through a biosynthetic pathway involving thromboxane-A-synthase.
Chemistry of Prostaglandins, leukotrienes and thromboxanes(Advance medicinal ...Rohit kaushiK.
1st discovered in human serum in 1930, were found to be stimulate uterine contraction and reduce pressure.
Presumed to be synthesized by prostate gland hence the name.
Later found that synthesized in all tissue except erythrocytes.
It have a cyclopentane ring (formed from 8 to 12 carbon atoms) and two side chains, with carboxyl group on one side.
They differ In their structure due to substituent group double bond on cyclopentane ring.
Prostaglandins are structurally resemble with prostanoic acid, 20-carbon fatty acid.
Abbreviated as PG, with the class designated by a capital letter A,B,D,E,F,G,H and I, followed by a number.
PGE and PGF; 1st isolated from the biological fluids.
The letters refer to the different ring structure, except in PGG and PGH: same ring structure (cyclo endohydroperoxide).
In the same series, depending upon double bonds on the side chains designated as PGE1, PGE2, PGE3..etc
The number of double bonds varies from 1-3.
PROSTAGLANDINS RECEPTORS
They function close to the site of synthesis and are deactivated to inactive metabolites before moving into the circuation.
Act locally in very low concentration, and acts on GPCR receptors.
INHIBITION OF PROSTAGLANDINS
Corticosteroids (e.g. cortisol) prevent the formation of arachidonic acid by inhibiting the enzyme phospholipase A2.
Anti inflammatory drugs inhibits the synthesis of prostaglandins.
They block the action of cyclooxygenase.
Aspirin irreversibly inhibits cyclooxygenase.
DEGRADATION OF PROSTAGLANDINS
All eicosanoids are metabolized rapidly.
Degradation mainly occurs in liver and lung.
Two enzymes, namely 15-α-hydroxy PG dehydrogenase & 13-PG reductase, convert hydroxyl group at C15 to keto group & then to C13 and C14 dihydroderivative.
BIOCHEMICAL ACTION OF PROSTAGLANDINS
The Prostaglandins (PGE, PGA, & PGI2) are vasodilator in nature. So they decreases blood pressure.
PGE1 & PGE2 induce the symptoms of inflammation (redness, swelling, edema etc.) due to arteriolar vasodilator, and cause rheumatoid arthritis, psoriasis etc. so Corticosteroids are used to treat these conditions.
PGE2 & PGF2 are used for the medical termination of pregnancy and induction of labor.
Pyrogens (fever causing) promote PG synthesis leading to the formation of PGE2.
Migraine is also due to PGE2.
PGE2 along with histamine and bradykinin causes pain.
PGI2 inhibit platelet aggregation.
They are used in the treatment of gastric ulcers, hyoertention, thrombosis, asthma etc.
Prostaglandins are also employed in the medical termination of pregnancy, prevention of conception, induction of labor etc.
Leukotrienes are synthesized by leucocytes, mast cells, lung, heart, spleen etc. by lipoxygenase pathway of arachidonic acid.
Leukotrienes are 20- Carbon polyenoic fatty acids having a number of substituents.
Depending upon the substitutions, they are divided into LTA, LTB, LTD, and LTE.
Each type is divided into sub-groups depending upon the number of double bonds which vary from 3-5.
Leukotrienes possess
Chemistry of Prostaglandins, leukotrienes and thromboxanes(Advance medicinal ...Rohit kaushiK.
1st discovered in human serum in 1930, were found to be stimulate uterine contraction and reduce pressure.
Presumed to be synthesized by prostate gland hence the name.
Later found that synthesized in all tissue except erythrocytes.
It have a cyclopentane ring (formed from 8 to 12 carbon atoms) and two side chains, with carboxyl group on one side.
They differ In their structure due to substituent group double bond on cyclopentane ring.
Prostaglandins are structurally resemble with prostanoic acid, 20-carbon fatty acid.
Abbreviated as PG, with the class designated by a capital letter A,B,D,E,F,G,H and I, followed by a number.
PGE and PGF; 1st isolated from the biological fluids.
The letters refer to the different ring structure, except in PGG and PGH: same ring structure (cyclo endohydroperoxide).
In the same series, depending upon double bonds on the side chains designated as PGE1, PGE2, PGE3..etc
The number of double bonds varies from 1-3.
PROSTAGLANDINS RECEPTORS
They function close to the site of synthesis and are deactivated to inactive metabolites before moving into the circuation.
Act locally in very low concentration, and acts on GPCR receptors.
INHIBITION OF PROSTAGLANDINS
Corticosteroids (e.g. cortisol) prevent the formation of arachidonic acid by inhibiting the enzyme phospholipase A2.
Anti inflammatory drugs inhibits the synthesis of prostaglandins.
They block the action of cyclooxygenase.
Aspirin irreversibly inhibits cyclooxygenase.
DEGRADATION OF PROSTAGLANDINS
All eicosanoids are metabolized rapidly.
Degradation mainly occurs in liver and lung.
Two enzymes, namely 15-α-hydroxy PG dehydrogenase & 13-PG reductase, convert hydroxyl group at C15 to keto group & then to C13 and C14 dihydroderivative.
BIOCHEMICAL ACTION OF PROSTAGLANDINS
The Prostaglandins (PGE, PGA, & PGI2) are vasodilator in nature. So they decreases blood pressure.
PGE1 & PGE2 induce the symptoms of inflammation (redness, swelling, edema etc.) due to arteriolar vasodilator, and cause rheumatoid arthritis, psoriasis etc. so Corticosteroids are used to treat these conditions.
PGE2 & PGF2 are used for the medical termination of pregnancy and induction of labor.
Pyrogens (fever causing) promote PG synthesis leading to the formation of PGE2.
Migraine is also due to PGE2.
PGE2 along with histamine and bradykinin causes pain.
PGI2 inhibit platelet aggregation.
They are used in the treatment of gastric ulcers, hyoertention, thrombosis, asthma etc.
Prostaglandins are also employed in the medical termination of pregnancy, prevention of conception, induction of labor etc.
Leukotrienes are synthesized by leucocytes, mast cells, lung, heart, spleen etc. by lipoxygenase pathway of arachidonic acid.
Leukotrienes are 20- Carbon polyenoic fatty acids having a number of substituents.
Depending upon the substitutions, they are divided into LTA, LTB, LTD, and LTE.
Each type is divided into sub-groups depending upon the number of double bonds which vary from 3-5.
Leukotrienes possess
Introduction
Classification
Therapeutic values of peptidomimetics
Design of peptidomimetics by manipulation of amino acids
Modification of peptide backbone
Chemistry of prostaglandins, leukotrienes and thromboxanes
Presented by Shikha Popali and Harshpal singh Wahi students from Gurunanak college of pharmacy, Nagpur in Department of pharmaceutical Chemistry. The explained topic is seful for every chemistry student and for others too
synthesis of hetero-cyclic drugs which act as anti-malarial drugs where you get all information about synthesis, preparation, properties, uses of drugs.
Active constituent of drugs used in diabetic therapyAkshay Kank
In this slide the active constituents which is isolated from herbal sources used for to treat the type 1 and type 2 diabetes is covered. 'Gymnema' and 'swerita chirata' herbal plant is also covered in the slide.This work help in to focus the herbal emphasis on diabetes.
ENZYME INHIBITION THE MOST IMPORTANT TOPIC FOR BIOLOGY AS WELL AS CHEMISTRY PEOPLES. WE HAVE HERE COVERED FOR THE PHARMA STUDENTS THIS WILL MAKE THEM EASY AS WE ARE COLLECTED ALL THE DATA A SINGLE PLACE WICH COVERS ALL THE COTENTS.
There are many ways that drug-resistant infections can be prevented: immunization, safe food preparation, handwashing, and using antibiotics as directed and only when necessary. In addition, preventing infections also prevents the spread of resistant bacteria.The main cause of antibiotic resistance is antibiotic use. When we use antibiotics, some bacteria die but resistant bacteria can survive and even multiply. The overuse of antibiotics makes resistant bacteria more common. The more we use antibiotics, the more chances bacteria have to become resistant to them.
Stereochemistry is the ‘chemistry of space’ , that is stereochemistry deals with the spatial arrangements of atoms and groups in a molecule.
Stereochemistry can trace its roots to the year 1842 when the French chemist Louis Pasteur made an observation that the salts of tartaric acid collected from a wine production vessel have the ability to rotate plane-polarized light, whereas the same salts from different sources did not have this ability.
Isomers are compounds that contain exactly the same number of atoms, i.e., they have exactly the same empirical formula, but differ from each other by the way in which the atoms are arranged.
Constitutional isomers, also known as structural isomers, are specific types of isomers that share the same molecular formula but have different bonding atomic organization and bonding patterns.
Stereoisomers are molecules having the same molecular formula and the atomic arrangement, but differ in their spatial arrangement.
Geometric isomers are two or more coordination compounds which contain the same number and types of atoms, and bonds (i.e., the connectivity between atoms is the same), but which have different spatial arrangements of the atoms.
There are 2 types of geometric isomers, ‘cis’ and ‘trans’.-cis isomers: when similar groups are present on the same side of the double bonds, then they are termed as cis.- trans isomers: when similar groups are present on the opposite sides of the double bonds then they are called trans isomers.
cis-diethylstilbestrol has only 7% of the estrogenic activity of trans-diethylstilbesterol.
Cisplatin have anticancer activity where ae trans platin is an inactive compound.
In chemistry, a molecule or ion is called chiral if it cannot be superposed on its mirror image by any combination of rotations, translations, and some conformational changes.
Chirality is the property of being non identical to ones mirror image.
Chiral center is defined as the atom bearing 4 different atoms or group of atoms.
Molecules that form nonsuperimposable mirror images, and thus exist as enantiomers, are said to be chiral molecules.
For a molecule to be chiral, it cannot contain a plane of symmetry.
The term enantioselectivity refers to the efficiency with which the reaction produces one enantiomer.
Enantiomers are stereoisomers that are non-superimposable mirror images.
Have identical properties.
Similar shapes
Diastereomers are stereoisomers that are non superimposable and are not mirror images.
Have distinct physical properties.
Have different molecular shapes.
Enantiomers consist of a pair of molecules that are mirror images of each other and are not superimposable.
When a molecule contains only one chiral centre , the two stereoisomers are known as enantiomers.
These may be referred to or labelled using the configurational descriptors as either:
R(rectus meaning right handed) or S(sinister meaning left handed),
D(dextrorotatory)or L (laevorotatory)
E-Entgegen or Z- Zusamen
Analog design is usually defined as the modification of a drug molecule or of any bioactive compound in order to prepare a new molecule showing chemical and biological similarity with the original model compound
PEPTIDOMIMETICS , HERE WE HAVE INCLUDED THE INTRODUCTION, CLASSIFICATION, ADVANTAGES , DISADVANTAGES, ITS METHODS PREPARATION, PRINCIPLES OD DRUG DESIGN, ITS CHEMISTRY. STEREOCHEMISTRY, SYNTHESIS AND APPLICATIONS
Introduction
Classification
Therapeutic values of peptidomimetics
Design of peptidomimetics by manipulation of amino acids
Modification of peptide backbone
Chemistry of prostaglandins, leukotrienes and thromboxanes
Presented by Shikha Popali and Harshpal singh Wahi students from Gurunanak college of pharmacy, Nagpur in Department of pharmaceutical Chemistry. The explained topic is seful for every chemistry student and for others too
synthesis of hetero-cyclic drugs which act as anti-malarial drugs where you get all information about synthesis, preparation, properties, uses of drugs.
Active constituent of drugs used in diabetic therapyAkshay Kank
In this slide the active constituents which is isolated from herbal sources used for to treat the type 1 and type 2 diabetes is covered. 'Gymnema' and 'swerita chirata' herbal plant is also covered in the slide.This work help in to focus the herbal emphasis on diabetes.
ENZYME INHIBITION THE MOST IMPORTANT TOPIC FOR BIOLOGY AS WELL AS CHEMISTRY PEOPLES. WE HAVE HERE COVERED FOR THE PHARMA STUDENTS THIS WILL MAKE THEM EASY AS WE ARE COLLECTED ALL THE DATA A SINGLE PLACE WICH COVERS ALL THE COTENTS.
There are many ways that drug-resistant infections can be prevented: immunization, safe food preparation, handwashing, and using antibiotics as directed and only when necessary. In addition, preventing infections also prevents the spread of resistant bacteria.The main cause of antibiotic resistance is antibiotic use. When we use antibiotics, some bacteria die but resistant bacteria can survive and even multiply. The overuse of antibiotics makes resistant bacteria more common. The more we use antibiotics, the more chances bacteria have to become resistant to them.
Stereochemistry is the ‘chemistry of space’ , that is stereochemistry deals with the spatial arrangements of atoms and groups in a molecule.
Stereochemistry can trace its roots to the year 1842 when the French chemist Louis Pasteur made an observation that the salts of tartaric acid collected from a wine production vessel have the ability to rotate plane-polarized light, whereas the same salts from different sources did not have this ability.
Isomers are compounds that contain exactly the same number of atoms, i.e., they have exactly the same empirical formula, but differ from each other by the way in which the atoms are arranged.
Constitutional isomers, also known as structural isomers, are specific types of isomers that share the same molecular formula but have different bonding atomic organization and bonding patterns.
Stereoisomers are molecules having the same molecular formula and the atomic arrangement, but differ in their spatial arrangement.
Geometric isomers are two or more coordination compounds which contain the same number and types of atoms, and bonds (i.e., the connectivity between atoms is the same), but which have different spatial arrangements of the atoms.
There are 2 types of geometric isomers, ‘cis’ and ‘trans’.-cis isomers: when similar groups are present on the same side of the double bonds, then they are termed as cis.- trans isomers: when similar groups are present on the opposite sides of the double bonds then they are called trans isomers.
cis-diethylstilbestrol has only 7% of the estrogenic activity of trans-diethylstilbesterol.
Cisplatin have anticancer activity where ae trans platin is an inactive compound.
In chemistry, a molecule or ion is called chiral if it cannot be superposed on its mirror image by any combination of rotations, translations, and some conformational changes.
Chirality is the property of being non identical to ones mirror image.
Chiral center is defined as the atom bearing 4 different atoms or group of atoms.
Molecules that form nonsuperimposable mirror images, and thus exist as enantiomers, are said to be chiral molecules.
For a molecule to be chiral, it cannot contain a plane of symmetry.
The term enantioselectivity refers to the efficiency with which the reaction produces one enantiomer.
Enantiomers are stereoisomers that are non-superimposable mirror images.
Have identical properties.
Similar shapes
Diastereomers are stereoisomers that are non superimposable and are not mirror images.
Have distinct physical properties.
Have different molecular shapes.
Enantiomers consist of a pair of molecules that are mirror images of each other and are not superimposable.
When a molecule contains only one chiral centre , the two stereoisomers are known as enantiomers.
These may be referred to or labelled using the configurational descriptors as either:
R(rectus meaning right handed) or S(sinister meaning left handed),
D(dextrorotatory)or L (laevorotatory)
E-Entgegen or Z- Zusamen
Analog design is usually defined as the modification of a drug molecule or of any bioactive compound in order to prepare a new molecule showing chemical and biological similarity with the original model compound
PEPTIDOMIMETICS , HERE WE HAVE INCLUDED THE INTRODUCTION, CLASSIFICATION, ADVANTAGES , DISADVANTAGES, ITS METHODS PREPARATION, PRINCIPLES OD DRUG DESIGN, ITS CHEMISTRY. STEREOCHEMISTRY, SYNTHESIS AND APPLICATIONS
The principal eicosanoids of biological significance to humans are a group of molecules derived from the 20:4 (20 carbons: 4 sites of unsaturation) fatty acid, arachidonic acid.
Eicosanoids is the class of lipids derived from arachidonic acid. Eicosanoids play an important role in the growth and development, cellular signalling, drug response, platelet action and maintenance of body homeostasis.
Dr. Jibachha Sah,M.V.Sc( Veterinary pharmacology, TU,Nepal),posted lecturer notes on AUTONOMIC AND SYSTEMIC PHARMACOLOGY for B.V.Sc & A.H. 6 th semester veterinary students of College of veterinary science,Nepal Polytechnique Institute, Bharatpur, Bhojard, Chitwan, Nepal.I hope this lecture notes may be beneficial for other Nepalese veterinary students. Please send your comment and suggestion .Email:jibachhashah@gmail.com,moble,00977-9845024121
e-content of Stereochemistry for Pharmacy and Chemistry students.
contents includes Isomerism, Chirality, Stereoisomers, Enantiomer, Diastereomer, Cis And Trans Configuration ,L And D Configuration ,R And S Configuration and Importance of the chirality in drugs ,Intravenous anaesthetics , etc.
Ethnobotany and Ethnopharmacology:
Ethnobotany in herbal drug evaluation,
Impact of Ethnobotany in traditional medicine,
New development in herbals,
Bio-prospecting tools for drug discovery,
Role of Ethnopharmacology in drug evaluation,
Reverse Pharmacology.
The Indian economy is classified into different sectors to simplify the analysis and understanding of economic activities. For Class 10, it's essential to grasp the sectors of the Indian economy, understand their characteristics, and recognize their importance. This guide will provide detailed notes on the Sectors of the Indian Economy Class 10, using specific long-tail keywords to enhance comprehension.
For more information, visit-www.vavaclasses.com
The Roman Empire A Historical Colossus.pdfkaushalkr1407
The Roman Empire, a vast and enduring power, stands as one of history's most remarkable civilizations, leaving an indelible imprint on the world. It emerged from the Roman Republic, transitioning into an imperial powerhouse under the leadership of Augustus Caesar in 27 BCE. This transformation marked the beginning of an era defined by unprecedented territorial expansion, architectural marvels, and profound cultural influence.
The empire's roots lie in the city of Rome, founded, according to legend, by Romulus in 753 BCE. Over centuries, Rome evolved from a small settlement to a formidable republic, characterized by a complex political system with elected officials and checks on power. However, internal strife, class conflicts, and military ambitions paved the way for the end of the Republic. Julius Caesar’s dictatorship and subsequent assassination in 44 BCE created a power vacuum, leading to a civil war. Octavian, later Augustus, emerged victorious, heralding the Roman Empire’s birth.
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Roman architecture and engineering achievements were monumental. They perfected the arch, vault, and dome, constructing enduring structures like the Colosseum, Pantheon, and aqueducts. These engineering marvels not only showcased Roman ingenuity but also served practical purposes, from public entertainment to water supply.
How to Make a Field invisible in Odoo 17Celine George
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Students, digital devices and success - Andreas Schleicher - 27 May 2024..pptxEduSkills OECD
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How to Split Bills in the Odoo 17 POS ModuleCeline George
Bills have a main role in point of sale procedure. It will help to track sales, handling payments and giving receipts to customers. Bill splitting also has an important role in POS. For example, If some friends come together for dinner and if they want to divide the bill then it is possible by POS bill splitting. This slide will show how to split bills in odoo 17 POS.
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Read| The latest issue of The Challenger is here! We are thrilled to announce that our school paper has qualified for the NATIONAL SCHOOLS PRESS CONFERENCE (NSPC) 2024. Thank you for your unwavering support and trust. Dive into the stories that made us stand out!
We all have good and bad thoughts from time to time and situation to situation. We are bombarded daily with spiraling thoughts(both negative and positive) creating all-consuming feel , making us difficult to manage with associated suffering. Good thoughts are like our Mob Signal (Positive thought) amidst noise(negative thought) in the atmosphere. Negative thoughts like noise outweigh positive thoughts. These thoughts often create unwanted confusion, trouble, stress and frustration in our mind as well as chaos in our physical world. Negative thoughts are also known as “distorted thinking”.
2. CONTENTS :-
Eicosanoids
1. Prostaglandins
Introduction
Classification
Chemical structure
Biosynthesis of Prostaglandin
Regulation of Prostaglandin
Mechanism of action
Theraupeutic uses
2. Leukotrienes
Introduction
Biosynthesis of Leukotrienes
Mechanism of action
Function of Leukotrienes
3. Thromboxanes
Introduction
Biosynthesis of Thromboxanes
Function of Thromboxanes
Application
3. Eicosanoids
INTRODUCTION
Eicosanoids are oxidised derivatives of 20-carbon
polyunsaturated fatty acids (PUFAs) formed by the
cyclooxygenase (COX), lipoxygenase (LOX) and cytochrome .
Eicosanoids are Classified as
1. Prostanoids
• Prostaglandins
• Prostacyclins
• Thromboxanes
2. Leukotrienes
• Leukotrienes A4
• Leukotrienes B4
• Leukotrienes C4
• LeukotrienesD4
• Leukotrienes E4
4. 3. Lipoxins
• Lipoxins A4
• Lipoxins B4
All Eicosanoids contain 20 carbon atom
Eicosanoids are considred as Locally acting hormone with wide
range of biochemical Function
And also Arachidonic acid is Precursor of eicosanoids in human
beings.
6. The prostaglandins (PG) are a group
of physiologically active lipid compounds
called eicosanoids having diverse hormone-like effects in
animals. Prostaglandins have been found in almost every tissue in
humans and other animals. They are derived enzymatically from
the fatty acid that is arachidonic acid
Prostaglandin are derivative from hypothetical 20 carbon fatty
acid which is called as prostanoic acid and hence the name is
prostanoid.
7. The prostanoid has a 5 carbon cyclopentane ring which is form by
carbon 8 to carbon 12 and it has 2 side chain 1 chain of 7 carbons
these lied above plane of ring and other chain has below the ring.
Each of the biological active prostaglandin it has a hydroxyl
group at carbon number 15.
8. Classification of Prostaglandins
There is 9 classes of Prostaglandins that are
Prostaglandin A, Prostaglandin B, Prostaglandin C, Prostaglandin
D, Prostaglandin E, Prostaglandin F, Prostaglandin G,
Prostaglandin H, Prostaglandin I
Prostaglandin are classified into three series.
1 series which consist 1 double bond from linoleic acid
Prostaglandin E1.
2 series which consist 2 double bond from Arachidonic acid
Prostaglandin E2.
3 series which consist 3 double bond from Eicosapentaenoic acid
Prostaglandin E3.
9. OH
CH3
O
O
H
O OH
Prostaglandin E2
And double bond between carbon 13 and 14 various
substituent at the cyclopentane ring.
And also these structure has keto group at carbon 9 and
hydroxyl group at carbon 11.
Chemical structures
10. OH
CH3
O
H
O OH
O
H
Prostaglandin F2
These is the structure of Prostaglandine F2.
It has hydroxyl group at carbon number 9 and 11.
As other biologically active prostaglandin it has hydroxyl
group at carbon number 15.
double bond between 13 and 14.
11. Chemical structure of prostacyclins
Prostacyclins contain additional ring formed by cyclization of
side chain by linkage of carbon 6 to carbon 9 through oxygen
atom on that why it is called as Prostacyclins.
13. Thromboxane had derivatives of oxane ring and it is a six memebered
ring intrepted by oxygen atom. these is interupted by oxygen ring and
also they are synthesized from arachidonic acid.
And also it synthesize in human body and it has additional oxygen
atom joined with carbon 9 and 11.
Prostaglandin are derivative of prostanoic acid which is 20 carbon
fatty acid and they are most potent biologically substances.
It produced in almost tissue except erythrocytes.
Thromboxane
14. Prostaglandin are different from true hormone in human body
Prostaglandins are thought to be local hormone secrete by prostate
hormone.
And also prostaglandin were first isolated from prostate gland
secreation hence it named as prostaglandin.
15. Sweedish scientist Ulf van euler got nobel prize in 1970 for
discovery of prostaglandin.
Prostaglandin actually derived from fatty acid called as Arachidonic
acid which is 20 Carbon fatty acid.
16. Biosynthesis of Prostaglandin
At cellular level where are the prostaglandins produced and also
prostaglandin are very unstable compound and there half life
around 30 seconds.
Prostaglandin synthesis is take place from the membrane
phospholipids.
From the memebrane phospholipid it is cleaved by phospholipid
A2 It release precurser for prostaglandin synthesis which is
arachidonic acid.
From that arachidonic acid in sequential enzymatic step
prostaglandin would be produced.
17. This crucial step whenever it is required synthesize phospholipid
A2 releases arachidonic acid from membrane phospholipid there
by prostaglandin synthesis takes place.
Now key enzyme for prostaglandin synthesis pathway is
Prostaglandin H synthase.
Prostaglandin H synthase has 2 kind of activity one
cyclooxygenase activity and peroxidase activity.
Cyclooxygenase activity forms prostaglandin G2 from
arachidonic acid.
And also peroxidase activity that reduces prostaglandin G2 to
prostaglandin H2.
18.
19.
20. Regulation of Prostaglandin production
The prostaglandin the key raw material of prostaglandin
production is arachidonic acid derived from cell membrane.
And it is triggered by a enzyme which is phospholipase A2.
Now modulating phospholipase A2 activity the prostaglandin
production from arachidonic acid derived from cell membrane.
And it is triggered by a enzyme which is phospholipase A2
activity the prostaglandin production can be regulated.
It turns out epinephrine Thrombin, Angiotensin ll , Bradykinin,
vasopressin are positively regulate phospholiphase A2 and that
leads to production of prostaglandin.
21. Steroid kind of inhibit prostaglandin A2 activity and there by
prevent production of prostaglandin.
Prostaglandin H synthase its activity triggered by cathecolamines.
Where as it inhibit by compound like methyl salysilate and similar
compound like aspirin and others.
22.
23. Mechanism of Action
Prostaglandin found to be working G protein couple receptor
signalling pathway.
An often prostaglandin stimulation leads to increase in cyclic
Amp and protein kinase.
A activation followed by several nuclear changes in terms of
chin expression.
Several Prostaglandin has several effect on different level
example prostaglandin I2 leads to vascular dilation.
24. Whereas thromboxanes which is secreated or prevently present in
thrombocyte they induce vasoconstriction.
And also these two has opposite function.
Now prostaglandin I2 which is known as prostacyclin prevent
platelet aggregation.
Where as thromboxanes promote platelet aggregation.
In which prostaglandin F2 are stimulates uterine muscle
contraction sometimes used to terminate pregnancy.
Now Prostaglandin E and Prostaglandin F has opposing role in
terms of broncho constriction and broncho dilation.
25. Prostaglandin F leads bronchial smooth muscle constriction
where PGE leads to dilation of the bronchials.
Prostaglandin E2 and Prostaglandin D2 increase capillary
permeability enabling neutrophill and other imune cell to be
extravated from particular blood capillary near by the tissue and
it also implicate in terms of inflamation.
So that Prostaglandin E2 and prostaglandin D2 are involved in
inflammatory responses.
Now overall prostaglandin prevent are decrease gastric
secreation and increase intestinal mobility.
26. THERAUPEUTIC USES
Abortion : PGs have a place in midterm abortion, missed
abortion. Methotrexate alongwith misoprostol is also highly
successful for inducing abortion in the first few weeks of
pregnancy. Pretreatment with mifepristone improves the efficacy
of PGE2 as abortifacient.
Cervical priming : Applied Intravaginally or in the cervical
canal, low doses of PGE2 which do not affect uterine motility,
make the cervix soft and compliant.
27. Glaucoma : Topical PGF2a analogues like lanatoprost, bimatoprost
that are receptor agonists are the first choice drugs in wide angle
glaucoma.
Peptic ulcer : PGEI (misoprostol) is occasionally used for healing
peptic ulcer.
Avoid Platelet damage : PGI2 (Epoprostenol) can be used to
prevent platelet aggregation and damage during haemodialysis.
28. Leukotrienes
INTRODUCTION
Leukotrienes is kind of similar leukocytes. It kind of
associated with Leukocytes.
Trienes are tell us some features of chemical.
There are 3 consecutive double bond.
Now we understand leukotrienes as kind of chemical
molecules which might have chemical features 3
consecutive double bond found in leukocytes.
So these leukotrienes are actually a family of eicosanoids
(arachidonic acid derivatives).
29. Leukotrienes are inflammatory mediators just like other
arachidonic derivative such as prostaglandin.
Leukotrienes are a family of eicosanoid inflammatory
mediators produced in leukocytes by the oxidation of arachidonic
acid (AA) and the essential fatty acid eicosapentaenoic acid (EPA)
by the enzyme arachidonate 5-lipoxygenase.
Leukotrienes use lipid signaling to convey information to either the
cell producing them (autocrine signaling) or neighboring cells
(paracrine signaling) in order to regulate immune responses.
The production of leukotrienes is usually accompanied by the
production of histamine and prostaglandins, which also act as
inflammatory mediators.
30.
31. 5-lip-oxygenase act on arachidonic acid to form 5-
hydroperoxyeicosatetraenoic acid .
Acts and associate with 5-lox activating protein.
The 5HPETE later converted into leukotriene A4 also it is unstable
and rapidly hydrolyse by the action of enzyme by leukotriene A4
hydrolase to form leukotriene B4 in neutrophils and monocytes.
The LTB4 is one of the most potent inflammation mediating lipids.
And LTA4 (Leukotriene A4) which forms leukotriene C4 which
incorporate with glutathion and with action of LTC4 synthase it
forms leukotrienes C4.
Biosynthesis of Leukotrienes
32. This forms in mast cells and eosinophills.
Later Leukotriene C4 release glutamate to forms leukotriene D4.
Later leukotriene D4 release glycine it forms leukotriene E4.
33.
34.
35. MECHANISM OF ACTION
Which is usually accompanied with the production of
prostaglandins and histamines which are inflamattory
mediators from arachidonic acid there could be production of
leukotrienes and also in otherside which form prostaglandin
derivatives which also take part in inflammatory response.
Leukotrienes receptors are class of G-Protein couple receptor
so generally work by elevation of cyclic Amp in the cell and
leads to several inflammatory cytokinin genes.
But few leukotrienes receptor also nuclear receptor type.
36. And these receptor generally found in easinophil, endothelial
cells, mast cells.
In endothelial cells and also found in smooth muscles cells
important role in smooth muscle contraction and they form
physiological role incase of disease.
37. Function of Leukotrienes
Major role of leukotrienes (specially, leukotrienes D4) is to trigger
contraction in the smooth muscle lining the bronchioles.
Contraction of branchioles is triggered by leukotriene and these is
the key underline feature rhinitis or asthma like diseases.
Leukotrienes contribute to the pathophysiology of asthma,
especially in patients with aspirin. Exacerbated respiratory disease
whose symptoms are
Airflow obstruction, Increased secretion of mucus, Mucosal
accumulation, Broncho constriction, Infiltration of inflammatory
cells in the airway wall.
39. Excess of leukotriene leads to anaphylactic shock
And also leukotrienes inhibitors could be useful for patients with later
stages of alzheimer disease.
And also improve memory loss
And also Leukotrienes classified as
Leukotrienes A4
Leukotrienes B4
Leukotrienes C4
Leukotrienes D4
Leukotrienes E4
Leukotrienes designated as 4 because 4 double bond in their structures
are
40. Leukotrienes are involved in the inflammation and immediate
hypersensitivity reaction.
Leukotriene B4
Increased chemotaxis of polymorphonuclear leukocytes.
Chemotaxis are directed migration of cell in response to
chemical stimulus such as growth factor.
Release of lysosomal enzymes, adesion of white blood cells.
41. Leukotriene C4 , Leukotriene D4, Leukotriene E4
• Involved in contraction of smooth muscle.
• They cause Bronchoconstriction, and Vasoconstriction.
• They also called as slow reacting substance of anaphylaxis.
• Anaphylaxis is seveir potentially life threatening allergic reaction.
• And this reaction occur within seconds or minutes of exposure to
allergens.
42. Thromboxanes
INTRODUCTION
Thromboxane is named for its role in clot formation.
Thromboxane is a member of the family of lipids known as
eicosanoids and also it is derived from arachidonic acid.
Arachidonic acid get converted into thromboxane A2 and
thromboxane B2.
Key enzyme help in these process is known as
thromboxane-A-synthase.
Both thromboxanes are characterized as 6-membered ether
containing cyclic ring.
43.
44. Biosynthesis of Thromboxanes
o Thromboxanes is synthesized in platelet.
o On the platelet membrane they would be phospholiphase and these
would generate arachidonic acid.
o The arachidonic acid converted initially prostaglandin H2 with the
help of cyclo oxygenase.
o Later prostaglandin H2 is converted into either prostacyclin with the
help of prostacyclin synthase or it can converted into thromboxane
A2 with the help of Thromboxane A synthase.
o These Thromboxane A Synthase enzyme exclusively present in the
platelet membrane. Platelet is the site of thromboxane production.
45. Thromboxane once generated can bind to thromboxane receptor
present in wide variety of cell for example blood vessel.
Thromboxane ultimately leads to G-protein mediating signalling
which elevates calcium level in cytoplasm.
Once calcium level elevated it helps in clot formation or
eventually in vasoconstriction.
46.
47. Function of Thromboxanes
One of the major function of the thromboxane is to perform
vasoconstriction.
Thromboxane and prostacyclin has opposite role.
Prostacyclin has vasodilatory role where as thromboxanes has
vasoconstriction role.
And also vasoconstriction caused by thromboxanes play a role in
prinz metal ’s angina and blocked coronary artery.
Any kind of cardiac inflammatory disease one of the leading role
could be played by thromboxanes.
In immune diet if human body has sufficient omega 3 fatty acid
thromboxane A3 has generated instead of thromboxane A2.
48. While thromboxane A2 is potent vasoconstrictor and thromboxane
A3 is less potent vasoconstrictor.
Vasoconstriction mediated effect is less if diet contain omega 3
fatty acid
In this synthesis of thromboxane by blocking cycloxygenase
specific substance such has aspirin can block production of
thromboxane.
Other than thromboxane synthase inhibitor inhibit thromboxane
A-synthase.
49. APPLICATION OF THROMBOXANES
Thromboxanes exert hormone-like Application.
They interact with G-protein-linked receptors on the cell surface
to activate signal transduction pathways inside the cell.
TXs modify inflammatory responses but are most well-known for
their role in platelet aggregation, vasoconstriction, and smooth
muscle proliferation – they are an essential part of the wound
repair mechanism.
Thromboxane synthesis and thus platelet aggregation is inhibited
by non-steroidal anti-inflammatory drugs like aspirin.