Revision Study Material Unit - X: Anti-Viral & HIV Drugs

REVISION STUDY MATERIAL
UNIT - X
Anti-Viral & HIV Drugs

1. Gossypol
• Gossypol is a natural phenol derived from the
seeds of cotton plant (genus Gossypium)..
• Cotton plants produce gossypol in order to slow
down the reproduction of the insects that eat cotton
bolls and seeds.
• The compound also affects reproduction in
mammals. The oil of Gossypium seed affected male
fertility due to the presence of contraceptive
compound gossypol.
• Gossypol is a phenolic aldehyde that permeates
cells and acts as an inhibitor for several
dehydrogenase enzymes.
• It is a yellow pigment.
USES:-
•It inhibits replication of the HIV-1 virus.
•It also causes low potassium levels, and thus
causes temporary paralysis.
•Gossypol is antimalarial being the selective
inhibitor of Plasmodium falciparum (pfLDH over
hLDHs), an essential enzyme for energy generation
within malarial parasite.
.
2. Hypericin
• Hypericin is a napthodianthrone isolated from
Hypericum perforatum (St John's Wort)
• It occurs as a red dye and forms hypercinate salts
with sodium and potassium. .
• Hypericin is a natural photosensitizer
• It is a potent antiretroviral agent.
• Hypericin a prime candidate for clinical application
in the treatment of human glioma tumors.
• Hypericin is reported to interact with DNA in vitro
and in intact cells.
• Hypericin accumulates preferentially in cancerous
tissues, it is also used as an indicator of cancerous
cells.
Biological Activity
• Photosensitive antiviral, anticancer and
antidepressant agent derived from
Hypericum perforatum.
• Inactivates enveloped viruses (including
HIV), inhibits tyrosine kinases and is
preferentially cytotoxic to tumor cells upon
stimulation by visible light.
3. Inophyllum (Calophyllum inophyllum)
• Inophyllums B and A inhibited HIVreverse

transcriptase, which was isolated from
Tamanu (Calophyllum inophyllum).
• The root bark contains and antibacterial
principle .
• The plant is also reported to have novel
inhibitors of HIV-1reverse transcriptase.
• The plant contains 4- phenylcoumarins that
have antitumour activity
Uses
• Anti viral
•Active ingredients in the oil are believed to
regenerate tissue, used in skin creams.
•The gum resin is said to be good for old sores and
wounds.
• The resin may be useful for chronic catarrh.
•It is used in decoction for internal haemorrhages
and as a wash for indolent ulcers.
4. Calanolide A & B
• Calanolide A & B are the new non-nucleoside

reverse transcriptase inhibitor (NNRTI) first
acquired from Calophyllum lanigerum trees in
Malaysia.
• The U.S. National Cancer Institute tested
calanolide as a possible cancer treatment
• It was later found to have potent anti-HIV
activity.
• Calanolide A is unique among NNRTIs in that it
may bind two distinct sites in reverse
transcriptase
Calanolide A
Botany
• Calanolide A is a compound isolated from the latex of
the tree, Calophyllum lanigerum var. austrocoriaceum
• Grows in the rain forest of the Malaysian state of
Sarawak on the island of Borneo.
Chemistry
• Contain xanthones, steroids, triterpenes, coumarins,
and benzopyrans.
• Calanolide A falls into the category of a
dipyranocoumarin.
• It is classified as a nonnucleoside HIV-1 specific reverse
transcriptase (RT) inhibitor.
Uses
• Initial studies show promise for treating HIV-1
HIV
• Calanolide A has been found to inhibit a wide variety of HIV-
1 strains, drug-resistant strains, and HIV disease in various
stages.
• It is in a category of HIV medicines called non-nucleoside
reverse transcriptase inhibitors (NNRTIs).
• Calanolide A prevents HIV from entering the nucleus of
healthy T-cells.
• This prevents the cells from producing new virus and
decreases the amount of virus in the body.
Calanolide B
• Calanolide B - a novel and naturally-occurring non-
nucleoside reverse transcriptase inhibitor of HIV-1. (NNRTI)
• Obtain from the latex of Calophyllum teysmannii var.
5.Vidarabine
• A nucleoside antibiotic isolated from Streptomyces
antibioticus.
• It has some antineoplastic properties and has broad
spectrum activity against DNA viruses in cell cultures
and significant antiviral activity against infections
caused by a variety of viruses such as the herpes
viruses, the vaccinia VIRUS and varicella zoster
virus.
The Mechanism of Action of Vidarabine
• Vidarabine works by interfering with the synthesis of
viral DNA.
USES
• Vidarabine is an antiviral used in treating eye
infections caused by herpes simplex virus
• It is also used to treat herpes encephalitis,
although the drug acyclovir has proven more
effective as a therapy for this disease.
• Vidarabine's brand name is Vira A.
Ophthalmic Ointment
• Vidarabine is indicated for the treatment of acute
keratoconjunctivitis and recurrent epithelial
keratitis due to Herpes simplex virus
6. Glycyrrhizin
• Glycyrrhizin is the main sweet-tasting compound
from Glychyrrhiza glabra (licorice root).
• Glycyrrhizin is a triterpenoid saponin glycoside of
glycyrrhizic (or glycyrrhizinic) acid.
• On hydrolysis, the glycoside loses its sweet taste
and is converted to the aglycone glycyrrhetinic
acid plus two molecules of glucuronic acid.
• Chemically, glycyrrhizin is sulphated
polysaccharide
Anti-viral activity & Anti HIV activity
• It has been proven to have antiviral activity against DNA
and RNA virus (VZV, HIV, Influenza A and B, types 1 and 2
herpes simplex and hepatitis B and C) in vitro an in vivo
ANTI VIRAL & ANTI HIV
• Tethya crypta –Ara-A – Anti viral
• Tridi demnum – diademnis – Antiviral
• Budistoma olivaceum – Eudistomin A – Inhibit
immuno deficiency virus – AIDS
• Distea avara (sponge) – Evarol, Evarone –Anti
HIV –AIDS
• Ascidian lissocilium – Patellazole –B –Simplex
virus
• Laminaria Brown algae – Inhibit DNA, RNA
development, HIV, Simplex
Ara –A Didemins
 Semisynthetic anti viral agent Cyclic depsi peptides
 Arabinosyl nuclioside isolated Didemnin anti tumor agent
from marine sponge Tethya
crypta Isolated from Tridi demnum
Eudistomins & B- Avarol & avarone
Carbolin Sesquiterpene benzenoids
o Isolated from sponge Derived from Disidea avara
o Eudistoma olivaceum
Anti HIV
Polycitoridae
Inhibit immuno deficiency virus
Patellazole B
Laurenterol
 Ophioderma variegata Complex derivative isolated
 Antibacterial activity from Lissoclinum pattela
Active against simplex

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REVISION STUDY MATERIAL

Anti-Viral & HIV Drugs

• Inophyllums B and A inhibited HIVreverse

• Calanolide A & B are the new non-nucleoside

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