Академический Документы
Профессиональный Документы
Культура Документы
DNA TECHNOLOGY
August 13, 2013
DNA is a long chain nucleotide having million or billion
nucleotide. It contains hereditary information which is
transferred from one generation to another.
Gene is a small part of DNA. It contains thousands of
nucleotides. It is responsible for hereditary characters.
DNA of different species is different: both quantitatively
and qualitatively. From the information present in DNA,
protein is synthesized. Protein synthesis is regulated and
monitored by information present in DNA. Any mutation/
modification/ change in DNA results in synthesis of
abnormal protein. This is main cause of cancer.
In the synthesis of protein following steps are involved:
Transcription- information is transferred from DNA to
RNA
Translation- information is used to synthesize protein/
information in DNA is decoded to form protein.
Replication- DNA divides to give two daughter cells and
each cell should contain exact information
CLASSICAL
METHOD/
GENOMICCLONING/
FINGERPRINTING OF GENETIC MATERIAL BY USING
PROBE:
DNA has numerous genes. It is fragmented by enzyme
endonucleases. Probes are used to get required
information. Probes are known sequence of nucleotides
and these are radiolabeled or fluorescent. It is easy to
detect/ identify the nucleotides by using probes. Probes
are used to identify unknown sequence of nucleotide.
In the synthesis of protein, certain specific characteristics
are found. As the universal rule, genetic information
always flow unidirectionally i.e. from DNA to RNA and
then to protein. This law is called Central Dogma of
Molecular Genetics. There are some exceptions to this
law. In case of retrovirus (RNA virus), this law is violated.
Information is transferred from RNA to DNA and then to
RNA and protein is synthesized. Enzyme responsible for
this is reverse transcriptase.
It
is
making/synthesi
zing the genome
by
adding
different types of
genes.
INITIATORS:
Initiators are also
added to initiate
the
process.
Genes
responsible for
methionine
synthesis
are
used for this
purpose.
Polymerase
starts
the
process
by
unwinding the
SOMATOSTATIN:
Page 2 of 8
Surface of
cell
contain
insulin
receptors
and these
contain
and
chains
linked by
disulphide linkage.
When resistance is developed even if insulin is present it
will not regulate sugar level.
Resistance may develop due to infection or inflammatory
condition.
Increasing dose of insulin may help to maintain the
glucose level.
SULFONYLUREA:
August 21, 2013
INSULIN:
Gene responsible for the synthesis for insulin has 22
exons and 21 introns. These are responsible for encoding.
Insulin receptor also has two chains, which are linked by
disulphide linkage.
In humans, it is product of single polypeptide which
breakdown in two chains. In bacteria, two chains are
formed separately and then joined together.
Insulin regulates number of metabolic processes mainly
maintains blood sugar level. Its deficiency leads to
diabetes. Diabetes is of two types. Type I is due to
absence of insulin and type II is due to insulin receptor
resistance,
In type II, oral hypoglycemic agents can be given but in
type I only insulin is given. Hypoglycemic agents reduce
blood sugar level even when blood sugar level is normal.
Hypoglycemic agents reduce blood sugar level even when
blood sugar is normal. Antihyperglycemic agents only
reduce blood sugar level when t is high. These agents are
safer than hypoglycemic agents.
Insulin receptors are present at the surface of the cell.
Insulin is synthesized by human beings (endogenous
substance).
It is responsible for monitoring or regulating number of
metabolic processes.
Insulin increases membrane transfer of glucose, amino
acid and potassium.
In case of mutation of gene abnormal molecules of insulin
are produced, which lead to deficiency of insulin or may
be absence.
BIGUANIDES:
These are Antihyperglycemic agents. Insulin release is not
affected. These agents increase absorption of glucose in
the peripheral tissues, decrease hepatic output, inhibit
gluconeogenesis and decrease absorption of glucose.
Metformin and phenformin are its example.
Meglitinide is a substituted benzoic acid derivative and its
action is like sulfonylurea i.e. increases pancreatic release
of insulin.
THIAZOLIDINEDIONE DERIVATIVE:
It increases insulin receptor sensitivity and reduces the
resistance. It affect circulatory lipids i.e. disturbs lipid
profile and change pattern of LDL and HDL. It also affects
LFT. Compounds introduced initially were pioglitazone,
rosiglitazone and troglitazone. These agents were
withdrawn from the market.
Pioglitazone has favorable effect on HDL i.e. increases its
level, but it also increases the level of LDL. Sometimes
effect of LDL is more sever and it is not desirable.
August 23, 2013
SULFONYLUREA:
SAR:
Sulfanilamide is a
chemotherapeutic
agent.
It
has
Page 3 of 8
THIAZOLIDINEDIONE:
PROSTAGLANDINS
September 13, 2013
Prostaglandins are inflammatory mediators. 1st time it
was found in prostate gland thats why termed as
prostaglandins. It was thought that only these glands
produce it but later it was found that each and every cell
can form it.
The precursor is prostanoic acid and arachidonic acid.
Eicosanoic acid/ ethanoic acid is composed of 20 carbons.
These have 2 chains with cyclopentane ring. At 1st position
carboxylic group is present and at 20th position methyl
group is present.
Different types of prostaglandins are found and difference
is in the position of the double bonds and number or
position of the functional groups. Two types of functional
groups
are
present
i.e.
ketonic
and
hydroxyl.
Prostaglandin
A: ketonic group is present at 9th position and the double
bond is between 10th and 11th position.
Page 4 of 8
EXAMPLE:
Misoprostol is used as an anti-ulcerative agent
Fenprostalene is used to cause abortion
Alprostadil is used to treat erectile dysfunction
Bimatoprost is used to treat ocular hypertension
Lipoxygenase
ANTIVIRAL AGENTS
August 23, 2013
VIRUS:
Virus is a cellular parasite. It contains one type of nucleic
acid either RNA or DNA, which is surrounded by core of
protein. This core of protein may be surrounded by
another protein called envelope or capsule. It is a cellular
parasite and can survive on host. It uses substrate and
enzymatic pathways of host cells for protein synthesis and
replication.
MECHANISM OF ACTIONS:
Antiviral agents act by following mechanisms:
Inhibition of process
o
Fusion with the host cell
o
Transcription
o
Translation
o
Replication
PROBLEMS:
RIBAVIRIN (VIRAZOLE):
Brad spectrum
AMANTADINE/ RIMANTADINE:
Rimantadine is derivative of amantadine. These inhibit
uncoating and penetration of virus. These are mainly
effective against influenza A virus. They have preventive
action and can be used prophylactically. If virus has
already penetrated or infection is there then these are
not effective.
ZIDOVUDINE(RETROVIR):
It is active against retrovirus/ reverse
transcriptase. It is used in the case of AIDS,
herpes and some types of leukemia. It is an
analogue of thymidine.
TRIFLURIDINE/ 2-DEOXY-5-IODOXIDINE:
MISCELLANEOUS COMPOUNDS:
ACYCLOVIR (ZOVIRAX):
It is active against number of viruses like Herpes simplex
virus, zoster virus and is choice of treatment in the case of
These
agents
are
classified
accordin
g
to
chemical
structure
into
following
classes:
Page 6 of 8
Aminoquinoline derivatives
Quinidine derivative
4-aminoquinoline derivative
8-aminoquinoline derivative
Biguanide derivative
9-aminoacridine derivative
Few extracted compounds/ isolated
4-AMINOQUINOLINE:
Compounds have quinolone nucleus with
substituted amino group. Derivatives have side
chain in which one hydrogen of amino group is
replaced by the side chain. Side chain has butyl
and diethyl amino group. It is diethylaminobutyl
side chain; its first carbon can be substituted with
methyl and then will be called 1-methyl butyl
diethylamino group. All compounds of 4 and 8aminoquinoline have same side chains.
SAR:
First compound of the series if santoquin. It was
synthesized by Germans. At that time it was considered as
best derivative of 4-aminoquionoline. It has methyl group
at 3rd position. Later, it was found that substitution of
methyl group has decreased the activity.
One of the most important and commonly used derivative
is chloroquine, in which chlorine group is substituted at
7th position of 4-aminochloroquine.
In hydroxychloroquine, OH group is attached with the
chlorine group, and it is more active than chloroquine.
In amodiaquine, cyclic compound is attached
Mefloquine also contain cyclic compound and CF3 group
is also present.
September 24, 2013
PYRIMIDINE:
If we consider structural activity, chlorine group at para
position will increase the activity. If chlorine group is
replaced by methyl group, then activity will be decreased.
Pyrimidine derivatives are effective in exoerythrocytic
stage while, biguanides and proguanine are effective in
pre-erythrocytic stage.
Proguanine is used with atovaquone against the resistant
strain.
HALOFANTRINE:
Halofantrine is recently introduced compound and is used
in combination with biguanides and pyrimidine
derivatives against the resistant strains.
ARTEMISININ:
It is used in diverse traditional medicine. Now, it is
available as one of the important compound and drug of
choice. Two derivatives are available. One is water soluble
and other is lipid soluble. This compound has lactone ring
and oxygen ring. Oxygen ring is cleaved or broken to give
Page 7 of 8
LIFE CYCLE:
It is divided into two phases
ASEXUAL PHASE:
It occurs in host, vertebrate or human being. Female
mosquito (anopheles)when bite unaffected person then
plasmodium is transferred through saliva into the blood of
the host. It is then accumulated in the liver and then
transferred to the blood. This stage is known as
erythrocytic stage. When it is in liver it is called
hepatocytic stage. In erythrocytic stage, hemoglobin is
degraded. 30% hemoglobin is degraded. It is used by
parasite for synthesis of their protein. After 3-4 days
symptoms appear like chill, fever, etc.
SEXUAL PHASE:
When a mosquito bites a person protozoid enters the
salivary gland of mosquito and then moves to the
stomach. Gametocytes are oozed and then the cycle
continues
Two derivatives of chloroquine act at extraintestinal
stage. Amebiasis is a stage when protozoa are in intestine.
When it moves and come to liver then these drugs act
here.
We havent got any specific molecule acting
prophylactically.
Halofantrine if mixed with table salt can act
prophylactically.
Attenuated sporozoids or radiated attenuated sporozoids
are also available for prophylactic use.
Pyrimethamine is used in combination to inhibit synthesis
of folic acid.
Atovaquone interferes with electron transport chain. It is
selective inhibitor of electron transport chain in
plasmodium. Superoxide radical is formed and damages
the plasmodium. It is used in combination with
cycloguanil or proguanine against resistant strains. It is
obtained from Chinese plant. Some are water soluble and
some are oil soluble.
Decoding of plasmodium is also done and it is used
experimentally.
October 1, 2013
Page 8 of 8