Medicinally important marine organisms, Sponges, Corals, ALgae, Sea cucumbers

1. Novel Medicinal Agents from Marine
Sources
By
Dr Gana Manjusha Kondepudi
Associate Professor
Vignan Institute of Pharmaceutical Technology

2. The ocean contains more than
200,000 described species of
invertebrates and algae.
Marine plants, animals, and
microbes produce compounds
that have potential as
pharmaceuticals.
These "secondary
metabolites," chemicals that are
not needed by the organism for
basic or primary metabolic
processes, are believed to confer
some evolutionary advantage.

3. Many of these
plants and animals
•live in densely
populated habitats
•are non-motile and
•have only primitive
immune systems,
they have evolved
chemical compounds
•to help defend against predators,
•to attract or inhibit other
organisms from settling or
growing on them, and
•to provide chemical cues to
synchronize reproduction among
organisms that expel their eggs
and sperm into the water.

4. For example, many natural products have been identified
that inhibit cell division, the process that is the primary target
of many anti-cancer drugs.
The marine environment became a focus of natural products
drug discovery research because of its relatively unexplored
biodiversity compared to terrestrial environments.

5. The potential of marine natural products as pharmaceuticals was
introduced by the pioneering work of Bergmann in the 1950s ,
which led to the only two marine-derived pharmaceuticals that
are clinically available today.
The anticancer drug, Ara-
C, is used to treat acute
myelocytic leukemia and
non-Hodgkin's lymphoma.
The antiviral drug, Ara-A,
is used for the treatment
of herpes infections
Both are derived from nucleosides isolated from
a shallow-water marine sponge collected off the
coast of Florida.

6. Marine sponges are among the most prolific sources of
diverse chemical compounds with therapeutic potential .
Of the more than 5000 chemical compounds derived from
marine organisms, more than 30% have been isolated from
sponges.

7. Other marine sources of
bioactive molecules with
therapeutic potential are
bryozoans
ascidians
molluscs
cnidarians,
algae

8. These bioactive molecules possess
Antibiotic
Anti Inflammatory
Neuropsychological and
cardiovascular
Anti Viral
Anti Cancer
activities

9. CARDIOVASCULAR ACTIVE SUBSTANCES
i) Anthopluerins: These are the
group of peptides obtained
from coelenterates viz.
Anthopleura xanthogrammica
giving type A and type B (AP-A
and AP-B) and Anthopleura
elegantissima giving type C
(AP-C). AP-A shows positive
inotropic action without an
effect on Na+ K+ ATPase pump.

10. CARDIOVASCULAR ACTIVE SUBSTANCES
ii) Eptatretin: It is found in
the aneural bronchial hearts
of Pacific hogfish Viz
Eptatretus stoutii.
It is a potent cardiac
stimulant with direct
stimulant action on
mammalian myocardium
which is compatible to
adrenaline.

11. iii) Laminine: A marine algae
Laminaria angustata Gives this
basic amino acid compound with
hypotensive effects.
iv) D (-) Octopamine: It
produces adrenergic and
cardiovascular response and is
found in Octopus macropus,
O.vulgaris, Eledone moschata.

12. v) Saxitoxin : It shows a hypotensive
effect and is found in butter clam i.e.
Saxidomus giganteus, California mussel,
Mytilus Californianus.

13. vi) Autonomium: This compound has
Isosteric structure of adrenaline and
acetylcholine and is found in Verongia
fistularis. It produces both alpha and
beta adrenergic effects and also
exhibits cholinergic activity. This
compound shows CNS stimulant
effects in mice exhibited by significant
increase in spontaneous motor
activity. Due to both adrenergic and
cholinergic effects, this compound
may proven to be useful in regulating
the behaviour of heart.

14. ATX- II: this is one of the polypeptides
found in sea anemones.
Like anthopluerins, it also shows
portent and dose-dependent
cardiotonic response in mammalian
heart preparations.
It is suggested that the cardiotonic
effect is due to indirect action on the
pump activity e induced by increased
sodium transport as a result of a
delayed inactivation of fast sodium
current.

15. Besides ATX- II and anthopluerins, various polypeptides have
been obtained from different sea anemones like Condylactis
gigantea with 195 amino acid residue peptide and hemolytic
action in rabbits, Parasicyonis actionstoloides with a neurotoxic
peptide and very less number of amino acids and Actinia
equina with 147 amino acids exhibiting bradycardia rapid
hypertension and respiratory arrest in the intact rat,

16. Holothurins and asterosaponins: these are marine saponins
holothurins contain triterpenoid moiety as aglycone and
asterosaponins have steroidal aglycone.
Holothurins are present in sea cucumbers, belonging to the
family Holothuridae.
Holothurins have cardiotonic action.
They show hemolytic activity. Holoxins like holotoxin A, B and
C are desulphated holothurins nad possess antifungal activity.

17. Asterosaponins which are obtained from Star fishes of
family asteroidae are toxic to various Marine organisms they
exert different pharmacological actions like hemolytic anti
inflammatory hypertensive and analgesic effects and also
cytolytic action due to interference in protein metabolism
and neuromuscular blocking effects.
They are inhibitors of ATPase , but holothurins are potent
in this comparison.

18. Spongosine: chemically it is a nucleoside (methoxy derivative of
adenosine) it is found in the extract of Caribbean sponge
Crypotethia crypts. It reduces both the rate and the force of
contractions of heart.
Like spongosine many nucleotides have been reported from
Marine sources like doridosine (hypertensive and hypothermic)
from Anisodoris nobilis,5-deoxy-5 iodotubericidin( muscle
relaxant, hypothermic and potent inhibitor of adenosine kinase)
from red algae Hypnea valentine.
Eledosin: it is a powerful hypertensive compound obtained from
posterior salivary glands of cephalopod Eledone moschata. It
shows strong vasodilator effects.

19. Laminine Spongosine

20. Cytotoxic anticancer compounds
Ara -C
It is a 1-alpha-D-arabinofuranosyl cytosine or cytosine
arabinoside.
It is obtained as a synthetic compound based on the knowledge
of naturally occurring moieties present in Caribbean sponges viz
spongosine, spongouridine.
Ara-C is used in the treatment of acute myelogenous leukaemia
and human acute leukaemia.
It is Active against Erlich carcinoma, sarcoma-180 and L-1210
leukaemia in mice.

21. Ara -C Crassin Acetate
Sinularin

22. Crassin acetate:
It is a member of cembranoids which are cyclic diterpenes
obtain from soft corals.
Crassin acetate is obtained from Carribbean gorgonian
Pseudoplexaura porosa, which is cytotoxic to human leukemic
and Hela cells in vitro.
Among the various cembranoids, a soft coral Sinularia flexibilis
gives sinularin, dihydrosinularin and sinulariolide.

23. Many compounds with antitumor and immunosuppressant
compounds have been reported Ex: geranyl hydroquinone
(Cytotoxic to leukemia and mammary carcinoma) from
chloroform extract of Aplidium speices,
Aplysistatin (Anti leukemic) from sea hare Aplysia angasi;
halitoxin (Anti tumor) from a sponge Haliclona virdis; didemnins
A, B and C (Potent inhibitors of leukemic cells in vitro) from
Caribbean tunicate Trididemnum species.

24. Geranyl
hydroquinone
Aplysistatin

25. Anti Microbial Compounds
A large number of antimicrobial compounds have been detected
from marine organisms like sea cucumbers, marine algae, sea
hare, gorgonian corals and red algae.

27. Antibiotic Compounds

28. Anti-inflammatory and antispasmodic agents:
1. Manoalide:
It is obtained from the Luffariella variables. It is act by direct
inactivation of phospholipase A2, which is present in some
neurotoxins and also has a role in synthesis of PGs in humans.
Also has analgesic and selective anti-inflammatory activity.
2. Flaxibilide:
It is a diterpenoid obtained from the Sinularia flexibilis.

29. 3. Flustramine A and B:
It is obtained from the Flustra foliaceal (Swedish marine moss
animal). It is used as muscle relaxant.
4. Tetradoxin:
It is obtained from the puffer fishes Spherides rubripes, (liver and
ovaries). It is used as strong antispasmodic.
5. Dendalone-3-hydroxy butyrate:
It is obtained from the Phyllospongia dendyi. It is used as anti-
inflammatory agent.

30. Antiviral compounds:
1. Ara-A:
It is obtained from the sponge, Tethya crypta.
2. Avarol and Avarone:
It is obtained from the sponge, Disidea avara. These
compounds inhibit the immuno-deficient virus, have high
therapeutic indicates and the ability to cross blood brain
barrier. The compounds have potential use in the treatment of
AIDS.

31. 3. Eudostomin-A:
It obtained from the Eudostoma olivaceum.
4. Patellazole-B:
It obtained from the ascidian lissocilium patella.
5. Oppositol:
It is obtained from laurencia suboppostia.

33. Antiparasitic compounds:
1. Domoic acid:
It is obtained from the red algae, chondria armata. It is used as
anthelmintic.
2. α-kainic acid:
It is obtained from the red algae, digenia simplex. It is used
broad spectrum anthelmintic. It is effective against parasitic
roundworm, whip worm and tape worm.
3. Cucummechinoside-F:
It is obtained from the sea cucumber. It is used as antiprotozoal
activity.

34. 4. Bengamide-F:
It is obtained from the sponges, nudibranch and a zoanthid.
5. Laminine:
It is obtained from Laminaria angustata. It is use as an
anthelmintic as well as smooth muscle relaxant.

35. Anticoagulant agents:
1. Carrageenan:
It is obtained from the Chondrus, Euchauma and Gigrtina. It is
reported anticoagulant activity.
2. Galaxtan sulphuric acid:
It is obtained from the Iridaea laminariodes.
3. Fucoidan:
It is obtained from the Fucus vesiculosus, polyides rotundus.

36. MARINE TOXINS

38. THANK YOU