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Novel Marine Sources
(As per PCI Syllubus 2019-20)
a) Anticancer agents
b)Cardiovascular agents
By
Dr Sabeena Hussain Syed
Dept of Pharmacognosy
Genba Sopanrao Moze College of Pharmacy
INTRODUCTION
Eventhough 70% earth’s surface is covered by oceans and seas, rich in flora and fauna,
it has not been properly explored for the search of biomedicinals.
It is necessary to tap the marine sources for commercial utility of novel drugs in the
treatment of human ailments.
The marine source include sponges, coelenterates, tunicates, echinoderm and bryozoan
and a wide variety of microorganisms.
Currently, the potential for marine natural products as drug candidates has been recognized
all over the world, and the field is constantly growing and developing
For example, during this period, six out of nine currently used drugs of marine origin have
been approved by FDA. Focusing specifically on anti-cancer drugs, two more
antineoplastic agents, Plitidepsin and Polatuzumab vedotin, have been approved.
Hence, the full list of the marine-derived drugs used for cancer treatment at the end of 2019
included
Anti-Cancer (Cytotoxic) Agents
S.No Drug Name Source Use
1 Cytarabine
(Cytosine Arabinoside
Ara-C)
Caribbean Sponges Treatment of leukemia
2 Eribulin mesylate Synthetic analogue of halichondrin B, a substance derived
from a marine sponge
Metastatic breast cancer
3 Brentuximab vedotin Antibody-drug conjugate:
Antibody conjugated to the synthetic dolastatin 10(,
produced by cyanobacteria symbiotic to sea
hare Dolabella auricularia ) analog monomethylauristatin
A, via a protease-sensitive dipeptide linker
Treatment of Hodgkin’s
lymphoma
4 Trabectidine The tetrahydroisoquinoline alkaloid was extracted from
the sea squirt Ecteinascidia turbinata
Soft tissue sarcoma and
ovarian cancer
5 Plitidepsin Cyclic depsipeptide originally isolated from the tunicate
Aplidium albicans
Treatment of leukemia,
lymphoma, and multiple
myeloma
6 Polatuzumab vedotin antibody-drug conjugate
Polatuzumab vedotin is a CD79b specific antibody
conjugated to the antineoplastic agent monomethyl
auristatin E
Chronic lymphocytic
leukemia, B-cell
lymphomas, non-Hodgkin
lymphomas
Cardiovascular Agents
Cardiovascular disease (CVD) is a leading cause of death worldwide, which involves devastating dysfunctions of
the heart (cardiac) and the blood vessels (vascular). CVD includes atherosclerosis, hypertension, cardiac
hypertrophy, heart failure, arrhythmia, ischemic stroke, and coronary heart disease.
The residual cardiovascular risk remains very high despite the clinical use of anti-CVD drugs, such as lipid-
lowering statins. This scenario highlights the urgent need to identify novel therapeutic agents for treating CVD.
Numerous studies have indicated that marine natural products are one of the most important sources of lead
compounds in drug discovery for their natural origin, multiple bioactivities, and relatively high safety profile.
Studies in the past decade have indicated that several marine-derived natural products represent an underexplored
reservoir for the discovery of cardiovascular lead drugs with unique scaffolds and potential exploitation in the
pharmaceutical industry.
S.No Drug Name Source Use
1 Zeaxanthin
heneicosylate
Dunaliella salina
microalgae
Decreased age-associated cardiac
dysfunction in rats through the activation
of retinoid receptors.
2 Lepadiformines A
and B
Marine alkaloids from the
tunicate Clavelina
moluccensis
Cardiac inward rectifying K+ currentt
inhibition.
3 Zooxanthellamide
Cs
Marine dinoflagellate
Symbiodinium species
Vasoconstriction of rat blood vessels.
4 Fucoidan Brown algae and seaweed Improves the endothelial lining of blood
vessels.
Cardiovascular Agents from Marine Sources
Other cardiovascular drugs
S.No Drug Name Source Use
5 Eledosin Salivary gland of Cephalopod Vascodilator effect
6 Holothruin Sea cucumber Cardiotonic

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Novel Marine Drugs

  • 1. Novel Marine Sources (As per PCI Syllubus 2019-20) a) Anticancer agents b)Cardiovascular agents By Dr Sabeena Hussain Syed Dept of Pharmacognosy Genba Sopanrao Moze College of Pharmacy
  • 2. INTRODUCTION Eventhough 70% earth’s surface is covered by oceans and seas, rich in flora and fauna, it has not been properly explored for the search of biomedicinals. It is necessary to tap the marine sources for commercial utility of novel drugs in the treatment of human ailments. The marine source include sponges, coelenterates, tunicates, echinoderm and bryozoan and a wide variety of microorganisms.
  • 3. Currently, the potential for marine natural products as drug candidates has been recognized all over the world, and the field is constantly growing and developing For example, during this period, six out of nine currently used drugs of marine origin have been approved by FDA. Focusing specifically on anti-cancer drugs, two more antineoplastic agents, Plitidepsin and Polatuzumab vedotin, have been approved. Hence, the full list of the marine-derived drugs used for cancer treatment at the end of 2019 included
  • 4. Anti-Cancer (Cytotoxic) Agents S.No Drug Name Source Use 1 Cytarabine (Cytosine Arabinoside Ara-C) Caribbean Sponges Treatment of leukemia 2 Eribulin mesylate Synthetic analogue of halichondrin B, a substance derived from a marine sponge Metastatic breast cancer 3 Brentuximab vedotin Antibody-drug conjugate: Antibody conjugated to the synthetic dolastatin 10(, produced by cyanobacteria symbiotic to sea hare Dolabella auricularia ) analog monomethylauristatin A, via a protease-sensitive dipeptide linker Treatment of Hodgkin’s lymphoma 4 Trabectidine The tetrahydroisoquinoline alkaloid was extracted from the sea squirt Ecteinascidia turbinata Soft tissue sarcoma and ovarian cancer 5 Plitidepsin Cyclic depsipeptide originally isolated from the tunicate Aplidium albicans Treatment of leukemia, lymphoma, and multiple myeloma 6 Polatuzumab vedotin antibody-drug conjugate Polatuzumab vedotin is a CD79b specific antibody conjugated to the antineoplastic agent monomethyl auristatin E Chronic lymphocytic leukemia, B-cell lymphomas, non-Hodgkin lymphomas
  • 5. Cardiovascular Agents Cardiovascular disease (CVD) is a leading cause of death worldwide, which involves devastating dysfunctions of the heart (cardiac) and the blood vessels (vascular). CVD includes atherosclerosis, hypertension, cardiac hypertrophy, heart failure, arrhythmia, ischemic stroke, and coronary heart disease. The residual cardiovascular risk remains very high despite the clinical use of anti-CVD drugs, such as lipid- lowering statins. This scenario highlights the urgent need to identify novel therapeutic agents for treating CVD. Numerous studies have indicated that marine natural products are one of the most important sources of lead compounds in drug discovery for their natural origin, multiple bioactivities, and relatively high safety profile. Studies in the past decade have indicated that several marine-derived natural products represent an underexplored reservoir for the discovery of cardiovascular lead drugs with unique scaffolds and potential exploitation in the pharmaceutical industry.
  • 6. S.No Drug Name Source Use 1 Zeaxanthin heneicosylate Dunaliella salina microalgae Decreased age-associated cardiac dysfunction in rats through the activation of retinoid receptors. 2 Lepadiformines A and B Marine alkaloids from the tunicate Clavelina moluccensis Cardiac inward rectifying K+ currentt inhibition. 3 Zooxanthellamide Cs Marine dinoflagellate Symbiodinium species Vasoconstriction of rat blood vessels. 4 Fucoidan Brown algae and seaweed Improves the endothelial lining of blood vessels. Cardiovascular Agents from Marine Sources Other cardiovascular drugs S.No Drug Name Source Use 5 Eledosin Salivary gland of Cephalopod Vascodilator effect 6 Holothruin Sea cucumber Cardiotonic