FLAVONIODS ARE
UBIQUITOUS IN
FLOWERING
PLANTS
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orgachemweb@gmail.com
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The above ring systems
were reported
to display a wide variety of biochemical and pharmacological activities
as reported in various research journals during the period 1990-2000.
Recent Advances
(1991-2000)
--- Potent and Specific
inhibition
of cAMP phosphodiesterase.
--- Protein Kinase C
activity.
--- Antineoplastic agents
(many
flavones reported to have this
activity)
activity against pancreatic cancer.
---- to treat inflammation
(anti-inflammatory
activity) and arthiritic
conditions.
---- Antiallergic and
antiasthmatic
agents (several chromones were
reported to have this activity)
--- 5 – Lipoxygenase
inhibitors.
--- Cyclooxygenase
inhibitors.
--- Agents for the
treatment of
osteoporosis.
--- Potent antithrombotic
agents.
--- Potent, selective,
non-cytotoxic
inhibitor of
phosphatidylinositol-3-Kinase.
--- Immunomodulator agent.
--- Potent bone resorption
inhibitor
that activates protein kinase C
activity.
--- Potent uroselective
alpha-1-adrenoceptor
antagonist with additional
5-HTIA
receptor – antagonist activity.
--- Platelet
antiaggregatory agents.
--- Antiestrogenic,
antineoplastic
agents (with topoisomerase-
I inhibitory activity).
--- Antibacterial agents.
--- Antiproliferative
agents.
--- Antitumor and
antimetastic
agents.
--- Cardioprotective agents
with
potent antiplatelet activity.
--- Disodium chromoglycate
(chromone
derivative) is a commercial drug
as
an
antiallergic agent to treat asthma.
--- Symptomatic
antidiabetic agents,
aldose reductase inhibitor.
--- Dopamine autoreceptor
agonist.
--- Leukotriene
B4-antagonist.
--- Cardioprotective agents.
--- Antipsychotic and
neuroprotective
agents.
--- Antidepressant agents.
--- Anticonvulsant and
neuroprotective
agents.
--- Antidementia agents
(coumarins
especially)
--- Agents to treat
atherosclerosis.
--- to treat AIDS,
Anti-HIV
agents. Some natural coumarins are potent
and
selective
non-nucleoside HIV – 1 reverse transcriptase inhibitors.
---Coronary vasodilating
and antihypertensive
agents (coumarins
especially)
--- Antiviral agents.
--- Selective dopomine
autoreceptor
agonist.
--- Thromboxane A2 (TxA2)
synthatase
– inhibitory activity.
--- Antimalarial agent that
inhibits
that inhibits the growth of both
chloroquine-sensitive
(D6) and multidrug-resistant (W2) strains of
Plasmodium faclciparum in vitro (xanthones especially)
--- Agents to treat
atherosclerosis
and mycocardial ischemia (coumarins
especially)
--- Anticonvulsant and
neuroprotective
agents (Coumarins especially)
--- Agents to treat
cerebrovascular
disorders.
--- Antidepressants.
--- Potentially useful for
improving
circulatory system, kidney functions
and
treating
stress.
--- Hypotensive induced
Ulcers.
--- To treat psoriasis and
Vitilago.
--- Urinary disorders ( A
commercial
drug, flavoxate, for example).
--- Antioxidants ( A number
of
flavones which have ortho-dihydro
system,
for example quercetin, (-) -epi-catechin,
procyanidin
isomers,anthocyanins,red
wine,green tea extract,grape seed extract
and pine
bark extract which contain flavonoids,catechins and
procyanidin
are excellent antioxidants. These are available
Commercially).
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--- Phytoestrogens
(Isoflavones
like genistein, daidzein found in soy
beans.
These isoflavones have antioxidant activity also. Coumestans
also have
phytoestrogenic activity).
---Flavonoids found in
plants involve
protection of plants against pests
,virus,bacteria
and fungi, attraction of pollination , promotes
fertility
and
germinination
and as oviposition stimulants .Infact flavonoids act
as
defensive
agents--phytoalexins, alleopathic and insect-antifeedant
agents--
to
protect the plants.
--- The role of
natural
flavonoids as antiviral , antifungal ,in human
medicine
is well recorded.
--- Recent studies revealed
that
food beverages (wine,beer,green tea)
fruits
and vegetables
and honey are known to have antioxidant
activity
---In general plant
phenolics including
catechins and procyanidins are
antioxidants
, known to possess anicarcinogenic,antiallergic and
anti-inflammatory
properties.
---Centochroman (chroman
derivative,
contraceptive agent),silibyn
(natural
flavonoid,hepato
protective agent), flavoxate hydrochloride
(flavone
derivative,diuretic
agent),rotenone (natural isoflavanone
derivative,insecticidal),Disodium
chromoglycate
(chromone derivative,antiallergic
agent to treat
asthma),psoralen,trimethylpsoralen
and
methoxalen
(furanocoumarins,to treat vitiligo ,leucoderma and
psoriasis),dicoumarol(coumarin
derivative, blood anticoagulating
agent)
are commercially
available.
---Several
chromones,flavones and
coumarins are in various stages of
clinical
trials
as drugs.
The Literature Survey is
based on
reports from:
--- Annual drug data report.
--- Drug data report.
--- Drugs for future.
--- Journal of medicinal
chemistry
and other journals and patent search.
--- Annual reports in
medicinal
chemistry.
---Monographs on
natural
products
Based on the study,
the Synthesis
and biological screening of chromones, flavonoids,
coumarins,isoflavones
and chalkones etc.with subsituents at various positions will be
rewarding.A
new range of products included in our synthetic programme are several
substituted
derivatives of these oxygen heterocycles .
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